Compounds of four rings containing a nitrogen. They are biosynthesized from reticuline via rearrangement of scoulerine. They are similar to BENZYLISOQUINOLINES. Members include chelerythrine and sanguinarine.
A major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cerebrovascular disorders.
Tetracyclic spiro-BENZAZEPINES isolated from the seeds of CEPHALOTAXUS. They are esters of the alkaloid cephalotaxine and may be effective as antineoplastic agents.
Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
A halogen with the atomic symbol Br, atomic number 36, and atomic weight 79.904. It is a volatile reddish-brown liquid that gives off suffocating vapors, is corrosive to the skin, and may cause severe gastroenteritis if ingested.
Alkaloids originally isolated from the ergot fungus Claviceps purpurea (Hypocreaceae). They include compounds that are structurally related to ergoline (ERGOLINES) and ergotamine (ERGOTAMINES). Many of the ergot alkaloids act as alpha-adrenergic antagonists.
A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
Long-lasting voltage-gated CALCIUM CHANNELS found in both excitable and nonexcitable tissue. They are responsible for normal myocardial and vascular smooth muscle contractility. Five subunits (alpha-1, alpha-2, beta, gamma, and delta) make up the L-type channel. The alpha-1 subunit is the binding site for calcium-based antagonists. Dihydropyridine-based calcium antagonists are used as markers for these binding sites.
Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.
Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.
Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture.
The poppy plant family of the order Papaverales, subclass Magnoliidae, class Magnoliopsida. These have bisexual, regular, cup-shaped flowers with one superior pistil and many stamens; 2 or 3 conspicuous, separate sepals and a number of separate petals. The fruit is a capsule. Leaves are usually deeply cut or divided into leaflets.
Tumors or cancer of the MOUTH.
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)
A cell line derived from cultured tumor cells.
The planning of the furnishings and decorations of an architectural interior.
The surface of a structure upon which one stands or walks.
Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS).
Exclusive legal rights or privileges applied to inventions, plants, etc.
A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.
Supplies used in building.
Group of alkaloids containing a benzylpyrrole group (derived from TRYPTOPHAN)
A group of ALKALOIDS, characterized by a nitrogen-containing necine, occurring mainly in plants of the BORAGINACEAE; COMPOSITAE; and LEGUMINOSAE plant families. They can be activated in the liver by hydrolysis of the ester and desaturation of the necine base to reactive electrophilic pyrrolic CYTOTOXINS.
Alkaloids extracted from various species of Cinchona.
A group of related plant alkaloids that contain the BERBERINE heterocyclic ring structure.
Compounds that contain a BENZENE ring fused to a furan ring.
A by-product of the destructive distillation of coal used as a topical antieczematic. It is an antipruritic and keratoplastic agent used also in the treatment of psoriasis and other skin conditions. Occupational exposure to soots, tars, and certain mineral oils is known to be carcinogenic according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985) (Merck Index, 11th ed).
Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.
Compounds of the general formula R-O-R arranged in a ring or crown formation.
A vasodilator that also has bronchodilatory action. It has been employed in the treatment of angina pectoris, in the treatment of asthma, and in conjunction with ultraviolet light A, has been tried in the treatment of vitiligo. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1024)
A plant genus of the family FABACEAE that is a source of psoralen (FICUSIN).
Complex pharmaceutical substances, preparations, or matter derived from organisms usually obtained by biological methods or assay.
The process of finding chemicals for potential therapeutic use.
Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.
Plants whose roots, leaves, seeds, bark, or other constituent parts possess therapeutic, tonic, purgative, curative or other pharmacologic attributes, when administered to man or animals.
Use of plants or herbs to treat diseases or to alleviate pain.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A plant genus of the family PAPAVERACEAE that contains benzo[c]phenanthridine alkaloids.
A genus of Eurasian herbaceous plants, the poppies (family PAPAVERACEAE of the dicotyledon class Magnoliopsida), that yield OPIUM from the latex of the unripe seed pods.
A method of separation of two or more substances by repeated distribution between two immiscible liquid phases that move past each other in opposite directions. It is a form of liquid-liquid chromatography. (Stedman, 25th ed)
An enzyme of the oxidoreductase class primarily found in PLANTS. It catalyzes reactions between linoleate and other fatty acids and oxygen to form hydroperoxy-fatty acid derivatives.
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Organic, monobasic acids derived from hydrocarbons by the equivalent of oxidation of a methyl group to an alcohol, aldehyde, and then acid. Fatty acids are saturated and unsaturated (FATTY ACIDS, UNSATURATED). (Grant & Hackh's Chemical Dictionary, 5th ed)
Eighteen-carbon cyclopentyl polyunsaturated fatty acids derived from ALPHA-LINOLENIC ACID via an oxidative pathway analogous to the EICOSANOIDS in animals. Biosynthesis is inhibited by SALICYLATES. A key member, jasmonic acid of PLANTS, plays a similar role to ARACHIDONIC ACID in animals.

Phosphatidylinositol 3-kinase and protein kinase C are required for the inhibition of caspase activity by epidermal growth factor. (1/443)

The mechanism by which growth factors exert an anti-apoptotic function on many cell types is not well understood. This issue is addressed in relation to epidermal growth factor (EGF) which inhibits apoptosis induced by staurosporine or wortmannin in an epithelial tumour cell line (CNE-2). The presence of EGF substantially reduced the in vitro Ac-DEVD-AMC hydrolytic activity and almost completely suppressed the intracellular cleavage of poly(ADP-ribose) polymerase in staurosporine- or wortmannin-treated cells. Staurosporine but not wortmannin caused the intracellular proteolytic processing of pro-caspase-3 and this event was transiently inhibited by EGF. Staurosporine-induced apoptosis was not inhibited by EGF in the presence of wortmannin or LY294002. Similarly, EGF failed to inhibit wortmannin-induced apoptosis in the presence of staurosporine, chelerythrine chloride or Go6850. These results suggest that phosphatidylinositol 3-kinase and protein kinase C play a role in the survival function of EGF but the reduction of cellular caspase activity cannot be satisfactorily explained by a lack of pro-caspase-3 activation.  (+info)

Effects of prostaglandin F2 alpha on intracellular pH, intracellular calcium, cell shortening and L-type calcium currents in rat myocytes. (2/443)

OBJECTIVE: We have studied the mechanisms underlying the positive inotropic action of prostaglandin F2 alpha (PGF2 alpha) by monitoring intracellular calcium transients, intracellular pH, L-type calcium currents and cell shortening in isolated ventricular myocytes. METHODS: Rat myocytes were loaded with fura-2AM for intracellular calcium measurements, or BCECF-AM for pH measurements. Cell shortening was recorded using an edge detection system, and L-type calcium currents measured using whole cell patch clamping. RESULTS: PGF2 alpha (3 nmol l-1-3 mumol l-1 increased single myocyte shortening and reduced resting cell length in a concentration-dependent manner. While myocyte shortening was increased by PGF2 alpha, this was not associated with any change in the amplitude of intracellular calcium transients, diastolic calcium, or L-type calcium currents. However, the same myocytes were capable of responding to catecholamines with increases in calcium transient amplitude and L-type calcium currents. PGF2 alpha (3 mumol l-1 caused a reversible rise in intracellular pH of 0.08 +/- 0.01 pH units (n = 5, p < 0.05). The Na(+)-H+ exchanger inhibitor, HOE 694 (10 mumol l-1, abolished the PGF2 alpha-induced rise in pH and the increase in cell shortening. PGF2 alpha-induced increases in cell shortening and intracellular pH were also attenuated by the protein kinase C (PKC) inhibitor, chelerythrine (2 mumol l-1. CONCLUSION: The positive inotropic action of PGF2 alpha appears to be mediated via activation of the Na(+)-H+ exchanger with the possible involvement of PKC. This suggests that PGF2 alpha-produces intracellular alkalosis, which then sensitizes cardiac myofilaments to calcium.  (+info)

Morphine preconditioning attenuates neutrophil activation in rat models of myocardial infarction. (3/443)

Previous results from our laboratory have suggested that morphine can attenuate neutrophil activation in patients with acute myocardial infarction. To elucidate if morphine preconditioning (PC) has the same effects via activation of neutrophil endopeptidase 24.11 (NEP), we measured serum levels of intercellular adhesion molecule-1 (ICAM-1), gp100MEL14 and NEP in adult Wistar rats subjected to ten different protocols (n = 10 for each) at baseline, immediately after and 2 h after morphine PC. All groups were subjected to 30 min of occlusion and 2 h of reperfusion. Similarly, morphine-induced PC was elicited by 3-min drug infusions (100 micrograms/kg) interspersed with 5-min drug-free periods before the prolonged 30-min occlusion. Infarct size (IS), as a percentage of the area at risk (AAR), was determined by triphenyltetrazolium staining. Pretreatment with morphine increased NEP activities (9.86 +/- 1.98 vs. 5.12 +/- 1.10 nmol/mg protein in control group; p < 0.001). Naloxone (mu-opioid receptor antagonist) (4.82 +/- 1.02 nmol/mg protein) and phosphoramidon (NEP inhibitor) (4.66 +/- 1.00 nmol/mg protein) inhibited morphine-activated NEP, whereas glibenclamide (ATP-sensitive potassium channel antagonist) and chelerythrine (protein kinase C inhibitor) had no effects. The ICAM-1 and gp100MEL14 of the third sampling were lowest for those with morphine PC (280 +/- 30 ng/ml and 2.2 +/- 0.7 micrograms/ml; p < 0.001), but naloxone (372 +/- 38 ng/ml and 3.8 +/- 0.9 micrograms/ml) and phosphoramidon (382 +/- 40 ng/ml and 4.2 +/- 1.1 micrograms/ml) abolished the above phenomenon. IS/AAR were definitely lowest for those with morphine PC (24 +/- 7%; p < 0.05). Morphine preconditioning increases NEP activities to attenuate shedding of gp100MEL14 and to ICAM-1 and, thus, provides myocardial protection.  (+info)

Isoform-selective activation of protein kinase C by nitric oxide in the heart of conscious rabbits: a signaling mechanism for both nitric oxide-induced and ischemia-induced preconditioning. (4/443)

Although isoform-selective translocation of protein kinase C (PKC) epsilon appears to play an important role in the late phase of ischemic preconditioning (PC), the mechanism(s) responsible for such translocation remains unclear. Furthermore, the signaling pathway that leads to the development of late PC after exogenous administration of NO in the absence of ischemia (NO donor-induced late PC) is unknown. In the present study we tested the hypothesis that NO activates PKC and that this is the mechanism for the development of both ischemia-induced and NO donor-induced late PC. A total of 95 chronically instrumented, conscious rabbits were used. In rabbits subjected to ischemic PC (six 4-minute occlusion/4-minute reperfusion cycles), administration of the NO synthase inhibitor Nomega-nitro-L-arginine (group III), at doses previously shown to block the development of late PC, completely blocked the ischemic PC-induced translocation of PKCepsilon but not of PKCeta, indicating that increased formation of NO is an essential mechanism whereby brief ischemia activates the epsilon isoform of PKC. Conversely, a translocation of PKCepsilon and -eta quantitatively similar to that induced by ischemic PC could be reproduced pharmacologically with the administration of 2 structurally unrelated NO donors, diethylenetriamine/NO (DETA/NO) and S-nitroso-N-acetylpenicillamine (SNAP), at doses previously shown to elicit a late PC effect. The particulate fraction of PKCepsilon increased from 35+/-2% of total in the control group (group I) to 60+/-1% after ischemic PC (group II) (P<0.05), to 54+/-2% after SNAP (group IV) (P<0.05) and to 52+/-2% after DETA/NO (group V) (P<0.05). The particulate fraction of PKCeta rose from 66+/-5% in the control group to 86+/-3% after ischemic PC (P<0.05), to 88+/-2% after SNAP (P<0.05) and to 85+/-1% after DETA/NO (P<0.05). Neither ischemic PC nor NO donors had any appreciable effect on the subcellular distribution of PKCalpha, -beta1, -beta2, -gamma, -delta, - micro, or -iota/lambda; on total PKC activity; or on the subcellular distribution of total PKC activity. Thus, the effects of SNAP and DETA/NO on PKC closely resembled those of ischemic PC. The DETA/NO-induced translocation of PKCepsilon (but not that of PKCeta) was completely prevented by the administration of the PKC inhibitor chelerythrine at a dose of 5 mg/kg (group VI) (particulate fraction of PKCepsilon, 38+/-4% of total, P<0.05 versus group V; particulate fraction of PKCeta, 79+/-2% of total). The same dose of chelerythrine completely prevented the DETA/NO-induced late PC effect against both myocardial stunning (groups VII through X) and myocardial infarction (groups XI through XV), indicating that NO donors induce late PC by activating PKC and that among the 10 isozymes of PKC expressed in the rabbit heart, the epsilon isotype is specifically involved in the development of this form of pharmacological PC. In all groups examined (groups I through VI), the changes in the subcellular distribution of PKCepsilon protein were associated with parallel changes in PKCepsilon isoform-selective activity, whereas total PKC activity was not significantly altered. Taken together, the results provide direct evidence that isoform-selective activation of PKCepsilon is a critical step in the signaling pathway whereby NO initiates the development of a late PC effect both after an ischemic stimulus (endogenous NO) and after treatment with NO-releasing agents (exogenous NO). To our knowledge, this is also the first report that NO can activate PKC in the heart. The finding that NO can promote isoform-specific activation of PKC identifies a new biological function of this radical and a new mechanism in the signaling cascade of ischemic PC and may also have important implications for other pathophysiological conditions in which NO is involved and for nitrate therapy.  (+info)

c-myc intron element-binding proteins are required for 1, 25-dihydroxyvitamin D3 regulation of c-myc during HL-60 cell differentiation and the involvement of HOXB4. (5/443)

1,25-Dihydroxyvitamin D3 (1,25-(OH)2D3) suppresses c-myc expression during differentiation of HL-60 cells along the monocytic pathway by blocking transcriptional elongation at the first exon/intron border of the c-myc gene. In the present study, the physiological relevance of three putative regulatory protein binding sites found within a 280-base pair region in intron 1 of the c-myc gene was explored. HL-60 promyelocytic leukemia cells were transiently transfected with three different c-myc promoter constructs cloned upstream of a chloramphenicol acetyltransferase (CAT) reporter gene. With the wild-type c-myc promoter construct (pMPCAT), which contains MIE1, MIE2, and MIE3 binding sites, 1,25-(OH)2D3 was able to decrease CAT activity by 45.4 +/- 7.9% (mean +/- S.E., n = 8). The ability of 1, 25-(OH)2D3 to inhibit CAT activity was significantly decreased to 18. 5 +/- 4.3% (59.3% reversal, p < 0.02) when examined with a MIE1 deletion construct (pMPCAT-MIE1). Moreover, 1,25-(OH)2D3 was completely ineffective at suppressing CAT activity in cells transfected with pMPCAT-287, a construct without MIE1, MIE2, and MIE3 binding sites (-6.5 +/- 10.9%, p < 0.002). MIE1- and MIE2-binding proteins induced by 1,25-(OH)2D3 had similar gel shift mobilities, while MIE3-binding proteins migrated differently. Furthermore, chelerythrine chloride, a selective protein kinase C (PKC) inhibitor, and a PKCbeta antisense oligonucleotide completely blocked the binding of nuclear proteins induced by 1,25-(OH)2D3 to MIE1, MIE2, and MIE3. A 1,25-(OH)2D3-inducible MIE1-binding protein was identified to be HOXB4. HOXB4 levels were significantly increased in response to 1,25-(OH)2D3. Taken together, these results indicate that HOXB4 is one of the nuclear phosphoproteins involved in c-myc transcription elongation block during HL-60 cell differentiation by 1,25-(OH)2D3.  (+info)

Importance of PKC and tyrosine kinase in single or multiple cycles of preconditioning in rat hearts. (6/443)

Both tyrosine kinase (TK) and protein kinase C (PKC) inhibitors have been shown individually to completely abolish the cardioprotective effects of ischemic preconditioning (IPC) in rabbits; however, blockade of both enzymes is necessary to totally abolish IPC in pigs. Recently, we have shown that TK inhibition partially attenuates the cardioprotective effect of IPC in intact rat hearts. Therefore, the present study was designed to test the hypothesis that inhibition of both TK and PKC is necessary to completely abolish IPC in the intact rat and that this effect is dependent on the intensity of the preconditioning stimulus. All animals were subjected to 30 min of coronary artery occlusion and 2 h of reperfusion. In series 1, multiple-cycle-induced IPC was produced via three 5-min occlusions interspersed with 5 min of reperfusion (3 x 5 IPC). Genistein (5 mg/kg), a TK inhibitor infused 30 min before IPC, and chelerythrine chloride (5 mg/kg), a PKC inhibitor infused 5 min before the prolonged ischemic insult, were administered alone or in combination in the absence or presence of 3 x 5 IPC. 3 x 5 IPC produced a marked reduction in infarct size as a percentage of area at risk compared with control (8.0 +/- 0.8 vs. 56.1 +/- 0.8%). The effects of 3 x 5 IPC were partially blocked by pretreatment with genistein (34.0 +/- 2.0%) or chelerythrine (26.4 +/- 2.8%) alone; however, combined administration of genistein and chelerythrine completely abolished the effects of 3 x 5 IPC (50.7 +/- 3.6%). In series 2, single-cycle IPC was elicited by one 5-min occlusion followed by 10 min of reperfusion (1 x 5 IPC). Compared with control, 1 x 5 IPC also significantly reduced infarct size (15.4 +/- 3.0%). Genistein or chelerythrine administered alone completely abolished 1 x 5 IPC-induced cardioprotection. These results suggest that the efficacy of TK and PKC inhibition to block IPC depends on the intensity of the preconditioning stimulus and that these kinases may work through parallel pathways.  (+info)

Chloride channel inhibition blocks the protection of ischemic preconditioning and hypo-osmotic stress in rabbit ventricular myocardium. (7/443)

The objective of this study was to examine the role of chloride (Cl-) channels in the myocardial protection of ischemic preconditioning (IP). Isolated rabbit ventricular myocytes were preconditioned with 10-minute simulated ischemia (SI) and 20-minute simulated reperfusion (SR) or not preconditioned (control). The myocytes then received 180-minute SI or 45-minute SI/120-minute SR. Indanyloxyacetic acid 94 (IAA-94, 10 micromol/L) or 5-nitro-2-(3-phenylpropylamino)benzoic acid (NPPB, 1 micromol/L) was administered before IP or before SI or SI/SR to inhibit Cl- channels. Electrophysiological studies indicate that these drugs, at the concentrations used, selectively abolished Cl- currents activated under hypo-osmotic conditions (215 versus 290 mOsm). IP significantly (P<0.001) reduced the percentage of dead myocytes after 60-minute (30.8+/-1.3%, mean+/-SEM), 90-minute (35.3+/-1.3%), and 120-minute (39.2+/-1.7%) SI compared with controls (44.7+/-1.6%, 54.5+/-1.3%, and 58.9+/-1.8%, respectively) and after 45-minute SI/120-minute SR (36.3+/-0.6%) compared with control (56.6+/-2.2%). Hypo-osmotic stress also produced protection similar to IP. IAA-94 or NPPB abolished the protection of both IP and hypo-osmotic stress. In buffer-perfused rabbit hearts preconditioned with three 5-minute ischemia/10-minute reperfusion cycles given before the 40-minute long ischemia and 60-minute reperfusion, IP significantly (P<0.0001) reduced infarct size (IP+vehicle, 4.7+/-0.9%, versus control+vehicle, 26.6+/-3.3%; mean+/-SEM). Again, IAA-94 or NPPB abolished the protection of IP. Our results implicate Cl- channels in the IP protection of the myocardium against ischemic/reperfusion injury and demonstrate that hypo-osmotic stress is capable of preconditioning cardiomyocytes.  (+info)

Nuclear factor-kappaB plays an essential role in the late phase of ischemic preconditioning in conscious rabbits. (8/443)

Although it is recognized that late preconditioning (PC) results from upregulation of cardioprotective genes, the specific transcription factor(s) that govern this genetic adaptation remains unknown. The aim of this study was to test the hypothesis that the development of late PC is mediated by nuclear factor-kappaB (NF-kappaB) and to elucidate the mechanisms that control the activation of NF-kappaB after an ischemic stimulus in vivo. A total of 152 chronically instrumented, conscious rabbits were used. A sequence of six 4-minute coronary occlusion/4-minute reperfusion cycles, which elicits late PC, induced rapid activation of NF-kappaB, as evidenced by a marked increase in p65 content (+164%; Western immunoblotting) and NF-kappaB DNA binding activity (+306%; electrophoretic mobility shift assay) in nuclear extracts isolated 30 minutes after the last reperfusion. These changes were attenuated 2 hours after ischemic PC and resolved by 4 hours. Competition and supershift assays confirmed the specificity of the NF-kappaB DNA complex signals. The mobility of the NF-kappaB DNA complex was shifted by anti-p65 and anti-p50 antibodies but not by anti-c-Rel antibodies, indicating that the subunits of NF-kappaB involved in gene activation after ischemic PC consist of p65-p50 heterodimers. Pretreatment with the NF-kappaB inhibitor diethyldithiocarbamate (DDTC; 150 mg/kg IP 15 minutes before ischemic PC) completely blocked the nuclear translocation and increased DNA binding activity of NF-kappaB. The same dose of DDTC completely blocked the cardioprotective effects of late PC against both myocardial stunning and myocardial infarction, indicating that NF-kappaB activation is essential for the development of this phenomenon in vivo. The ischemic PC-induced activation of NF-kappaB was also blocked by pretreatment with Nomega-nitro-L-arginine (L-NA), a nitric oxide synthase (NOS) inhibitor, N-2-mercaptopropionyl glycine (MPG), a reactive oxygen species (ROS) scavenger, chelerythrine, a protein kinase C (PKC) inhibitor, and lavendustin A, a tyrosine kinase inhibitor (all given at doses previously shown to block late PC), indicating that ischemic PC activates NF-kappaB via formation of NO and ROS and activation of PKC- and tyrosine kinase-dependent signaling pathways. A subcellular redistribution and increased DNA binding activity of NF-kappaB quantitatively similar to those induced by ischemic PC could be reproduced pharmacologically by giving the NO donor diethylenetriamine/NO (DETA/NO) (at a dose previously shown to elicit late PC), demonstrating that NO in itself can activate NF-kappaB in the heart. Taken together, these results provide direct evidence that activation of NF-kappaB is a critical step in the signal transduction pathway that underlies the development of the late phase of ischemic PC in conscious rabbits. The finding that four different pharmacological manipulations (L-NA, MPG, chelerythrine, and lavendustin A) produced similar inhibition of NF-kappaB suggests that this transcription factor is a common downstream pathway through which multiple signals elicited by ischemic stress (NO, ROS, PKC, tyrosine kinases) act to induce gene expression. To our knowledge, this is the first demonstration that NO can promote NF-kappaB activation in the heart, a finding that identifies a new biological function of NO and may have important implications for various pathophysiological conditions in which NO is involved and for nitrate therapy.  (+info)

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Title:The Anticancer Effect of Sanguinarine: A Review. VOLUME: 24 ISSUE: 24. Author(s):Chenxing Fu, Guiping Guan* and Hongbing Wang*. Affiliation:College of Bioscience and Biotechnology, College of Animal Science and Technology, Hunan Agricultural University, Changsha, Hunan 410128, College of Bioscience and Biotechnology, College of Animal Science and Technology, Hunan Agricultural University, Changsha, Hunan 410128, Hunan Institute of Animal and Veterinary Science, Changsha, Changsha 410131. Keywords:Sanguinarine, anti-tumor, apoptosis, pathways, anti-inflammatory, cancer.. Abstract:In vitro and in vivo studies have revealed that Sanguinarine has antioxidant, anti-inflammatory, proapoptotic, and growth inhibitory effects on tumor cells of a variety of cancers. Previous research showed that sanguinarine induced apoptosis (cell death) and/or antiproliferative while reducing tumor cell antiangiogenic and anti-invasive properties. This paper describes various sanguinarine anti-cancer mechanisms, ...
For decades, natural products represent a significant source of diverse and unique bioactive lead compounds in drug discovery field. In Clinical oncology, complete tumors remission is hampered by the development of drug-resistance. Therefore, development of cytotoxic agents that may overcome drug resistance is urgently needed. Here, the natural benzophenanthridine alkaloid sanguinarine has been studied for its cytotoxic activity against multidrug resistance (MDR) cancer cells. We investigated the role of the ATP-binding cassette (ABC) transporters BCRP/ABCG2, P-glycoprotein/ABCB1 and its close relative ABCB5 in drug resistance. Further drug resistance mechanisms analyzed in this study were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR). Multidrug resistant cells overexpressing BCRP, ABCB5 and mutated ∆EGFR were not cross-resistant towards sanguinarine. Interestingly, P-gp overexpressing cells were hypersensitive to sanguinarine. Doxorubicin uptake assay carried by flow
TY - JOUR. T1 - Molecular determinants of sensitivity or resistance of cancer cells toward sanguinarine. AU - Saeed, Mohamed E.M.. AU - Mahmoud, Nuha. AU - Sugimoto, Yoshikazu. AU - Efferth, Thomas. AU - Abdel-Aziz, Heba. PY - 2018/2/26. Y1 - 2018/2/26. N2 - For decades, natural products represented a significant source of diverse and unique bioactive lead compounds in drug discovery field. In Clinical oncology, complete tumors remission is hampered by the development of drug-resistance. Therefore, development of cytotoxic agents that may overcome drug resistance is urgently needed. Here, the natural benzophenanthridine alkaloid sanguinarine has been studied for its cytotoxic activity against multidrug resistance (MDR) cancer cells. We investigated the role of the ATP-binding cassette (ABC) transporters BCRP/ABCG2, P-glycoprotein/ABCB1 and its close relative ABCB5 in drug resistance. Further drug resistance mechanisms analyzed in this study were the tumor suppressor TP53 and the epidermal growth ...
Natural cell death is a well-known degenerative phenomenon occurring during development of the nervous system. The role of trophic molecules produced by target and afferent cells as well as by glial cells has been extensively demonstrated. Literature data demonstrate that cAMP can modulate the survival of neuronal cells. Cultures of mixed retinal cells were treated with forskolin (an activator of the enzyme adenylyl cyclase) for 48 h. The results show that 50 M forskolin induced a two-fold increase in the survival of retinal ganglion cells (RGCs) in the absence of exogenous trophic factors. This effect was dose dependent and abolished by 1 M H89 (an inhibitor of protein kinase A), 1.25 M chelerythrine chloride (an inhibitor of protein kinase C), 50 M PD 98059 (an inhibitor of MEK), 25 M Ly 294002 (an inhibitor of phosphatidylinositol-3 kinase), 30 nM brefeldin A (an inhibitor of polypeptide release), and 10 M genistein or 1 ng/ml herbimycin (inhibitors of tyrosine kinase enzymes). The inhibition ...
Background Microvascular endothelial inflammation and apoptosis are in charge of septic severe lung injury (ALI). by Traditional western blotting. Outcomes Ripasudil attenuated the LPS-induced swelling and apoptosis in PMVECs, that was reversed by L-NAME. Ripasudil suppressed Rock and roll2 activity and additional improved the eNOS activity. Ripasudil treatment improved the phosphorylation of eNOS, improved the expression degree of Bcl2, and reduced the expression degree of energetic caspase3 in LPS-treated PMVECs. Furthermore, the ripasudil treatment also inhibited the nuclear translocation of NF-B and additional suppressed the degrees of interleukin (IL) 6 and tumor necrosis element (TNF) . The co-treatment with L-NAME, nevertheless, impaired the anti-apoptotic and anti-inflammatory ramifications Chelerythrine Chloride IC50 of ripasudil on PMVECs without influencing Rock and roll2. Conclusions The book Rock and roll2 inhibitor ripasudil suppressed LPS-induced apoptosis and swelling in PMVECs ...
The effects of chelidonine on tubulin polymerisation, cell cycle progression and selected signal transmission pathways.. Panzer A, Joubert AM, Bianchi PC, Hamel E, Seegers JC.. Department of Physiology, University of Pretoria, South Africa.. Chelidonine is a tertiary benzophenanthridine alkaloid known to cause mitotic arrest and to interact weakly with tubulin. Our interest in chelidonine began when we found it to be a major contaminant of Ukrain, which is a compound reported to be selectively toxic to malignant cells. The effects of chelidonine in two normal (monkey kidney and Hs27), two transformed (Vero and Graham 293) and two malignant (WHCO5 and HeLa) cell lines, were examined. Chelidonine proved to be a weak inhibitor of cell growth, but no evidence for selective cytotoxicity was found in this study. It was confirmed that chelidonine inhibits tubulin polymerisation (IC50 = 24 microM), explaining its ability to disrupt microtubular structure in cells. A G2/M arrest results, which is ...
TY - JOUR. T1 - Antiplatelet effect of sanguinarine is correlated to calcium mobilization, thromboxane and cAMP production. AU - Jeng, Jiiang Huei. AU - Wu, Hui Lin. AU - Lin, Bor Ru. AU - Lan, Wan Hong. AU - Chang, Hsiao Hwa. AU - Ho, Yuan Soon. AU - Lee, Po Hsuen. AU - Wang, Ying Jan. AU - Wang, Juo Song. AU - Chen, Yi Jane. AU - Chang, Mei Chi. PY - 2007/4. Y1 - 2007/4. N2 - Sanguinarine is a plant alkaloid present in the root of Sanguinaria canadensis and Poppy fumaria species. Sanguinarine has been used as an antiseptic mouth rinse and a toothpaste additive to reduce dental plaque and gingival inflammation. In this study, we investigated the antiplatelet effects of sanguinarine, aiming to extend its potential pharmacological applications. Sanguinarine inhibited platelet aggregation induced by arachidonic acid (AA), collagen, U46619 and sub-threshold concentration of thrombin (0.05 U/ml) with IC50 concentrations of 8.3, 7.7, 8.6 and 4.4 μM, respectively. Sanguinarine (5-10 μM) inhibited ...
Dysregulation of apoptosis is a prime hallmark of leukemia. Therefore, drugs which restore the sensitivity of leukemic cells to apoptotic stimuli are promising candidates in the treatment of leukemia. The main objective of this dissertation was to examine the antileukemic effect of sanguinarine, in vitro, and to further examine the signaling mechanisms that may be involved. This study demonstrates that in human leukemic cells, sanguinarine activates a caspase-dependent apoptotic cell death pathway that is characterized by reactive oxygen species-dependent ceramide generation, and subsequent inhibition of Akt signaling pathway. In addition, sanguinarine also induces reactive oxygen species-dependent glutathione depletion and activation of extracellular signal-regulated kinase1/2. Moreover, inhibition of reactive oxygen species generation, using reactive oxygen species scavengers and antioxidants, significantly abrogates sanguinarine-induced ceramide generation, Akt dephosphorylation, extracellular signal
Pancreatic cancer is associated with low responsiveness to conventional chemotherapies and its incidence nearly equals its death rate. This warrants the development of novel mechanism-based approaches for the management of pancreatic cancer. This study was designed to determine the potential of sanguinarine, a plant alkaloid known to possess strong antimicrobial, anti-inflammatory, and antioxidant activities, against human pancreatic carcinoma cells. Employing human pancreatic carcinoma AsPC-1 and BxPC-3 cells, we specifically evaluated the pro-apoptotic and cell cycle deregulatory effects of sanguinarine and evaluated the involvement of Bcl-2 family proteins and p53 as the mechanism of the biological effects of sanguinarine. Our data demonstrated that sanguinarine (at low concentrations of 0.1-10 ?M; for 24 h) treatment to AsPC-1 and BxPC-3 cells resulted in a dose dependent (i) inhibition of viability and growth, (ii) colony formation ability, (iii) induction of apoptosis, and (iv) G0-G1 phase ...
Park SY, Jin ML, Kim YH, et al. Sanguinarine inhibits invasiveness and the MMP 9 and COX 2 expression in TPA-induced breast cancer cells by inducing HO-1 expression. Oncol Rep. 2014 Jan;31(1):497-504. PMID: 24220687.. Shao J, Liu D, Gong D, et al. Inhibitory effects of sanguinarine against the cyanobacterium Microcystis aeruginosa NIES-843 and possible mechanisms of action. Aquat Toxicol. 2013 Oct 15;142-143:257-63. PMID: 24060579.. Dong XZ, Zhang M, Wang K, et al. Sanguinarine inhibits vascular endothelial growth factor release by generation of reactive oxygen species in MCF-7 human mammary adenocarcinoma cells. Biomed Res Int. 2013;2013:517698. PMID: 23762849.. Niu X, Fan T, Li W, et al. Protective effect of sanguinarine against acetic acid-induced ulcerative colitis in mice. Toxicol Appl Pharmacol. 2013 Mar 15;267(3):256-65. PMID: 23352506.. Foss MH, Eun YJ, Grove CI, et al. Inhibitors of bacterial tubulin target bacterial membranes in vivo. Medchemcomm. 2013 Jan 1;4(1):112-119. PMID: ...
We have used a caged DAG compound to release the DAG analogue diC8 within cardiac myocytes in a controlled way using near-UV light.41 Photogenerated diC8 produced a positive inotropic effect, which was stereospecific and dose dependent, with an ≈4-fold enhancement of contractility under optimal conditions. This contractile response was modulated by the presence of cis-unsaturated fatty acids and blocked by the PKC inhibitor chelerythrine. This is the first direct demonstration, to our knowledge, of positive inotropy being initiated by a DAG analogue in mammalian adult ventricular muscle.. A few investigators have resolved smaller increases (12%22 and 116%28 ) in response to phorbol esters, but most investigators report dose-dependent negative ino-tropy after phorbol ester or DAG treatment.20 21 22 23 39 40 A strong case has been made that DAG mediates a physiologically important negative inotropy in ventricular tissues under some conditions.11 18 29 Our method of releasing diC8 from a caged ...
Activation of protein kinase C (PKC) via adenosine receptors is known to be involved in the cardioprotection of ischemic preconditioning (IPC). Specifically, activation of PKCε is critical for cardioprotection. There is ample evidence that PKCε resides in cardiac mitochondria. However, the signals that promote translocation of PKCε are largely unknown. The present study was designed to determine whether and how adenosine receptor activation induces translocation of PKCε to mitochondria. Freshly isolated adult rat cardiac myocytes and rat heart-derived H9c2 were used in the study. Immunofluorescence imaging of isolated mitochondria showed that PKCε but not PKCδ was localized in mitochondria and this mitochondrial localization of PKCε was significantly increased by adenosine treatment. The adenosine-induced increase in PKCε-positive mitochondria was largely prevented not only by PKC inhibitor chelerythrine, but also by the HSP90 inhibitor geldanamycin and by siRNA targeting HSP90. ...
STAT3 has been strongly implicated in human malignancies, and constitutive activation of STAT3 serves a crucial role in cell survival, angiogenesis, immune evasion, and inflammation. In this study, we showed that nitidine chloride, a natural phytochemical alkaloid derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through STAT3 signaling cascade. Nitidine chloride dose dependently suppressed VEGF-induced endothelial cell proliferation, migration, and tubular structure formation in vitro and dramatically reduced VEGF-triggered neovascularization in mouse cornea and Matrigel plugs in vivo. This angiogenesis inhibition mediated by nitidine chloride was well interpreted by the suppression of Janus kinase 2/STAT3 signaling and STAT3 DNA-binding activity in endothelial cells. Furthermore, nitidine chloride suppressed the constitutively activated STAT3 protein, its DNA-binding activity, and the expression of STAT3-dependent target genes, including cyclin D1, Bcl-xL, and VEGF ...
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While the effects of benzo[c]phenanthridine alkaloids (QBA), known mainly as sanguinarine and chelerythrine, on the inhibition of some kinds of cancer cell proliferation have been established, the effect on oral squamous cell is not known. Here, the antitumor activity of sanguinarine was demonstrated using in vitro assay systems in SAS, a human oral squamous cell carcinoma (OSCC) cell line. The anti-proliferative and -invasive effects were confirmed with IC?? values in the concentration range of 0.75-1.0 ?M by MTT assay and invasive assay, respectively. Sanguinarine was also able to suppress cell anchorage-independent growth, whereas it did not affect the cells adhering capabilities. Finally, sanguinarine induced apoptotic cell death by activating caspase and altering the Bcl-2/Bax ratio. Taken together, these results indicate that sanguinarine is a potential inhibitor of tumorigenesis and suggest that it may be valuable in the development of new anticancer drugs for the treatment of ...
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The N-methyl-D-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, which plays crucial roles in synaptic plasticity and development. We have recently shown that potentiation of NMDA receptor function by protein kinase C (PKC) appears to be mediated via activation of non-receptor tyrosine kinases. The aim of this study was to test whether this effect could be mediated by direct tyrosine phosphorylation of the NR2A or NR2B subunits of the receptor. Following treatment of rat hippocampal CA1 mini-slices with 500 nM phorbol 12-myristate 13-acetate (PMA) for 15 min, samples were homogenized, immunoprecipitated with anti-NR2A or NR2B antibodies and the resulting pellets subjected to Western blotting with antiphosphotyrosine antibody. An increase in tyrosine phosphorylation of both NR2A (76 +/- 11% above control) and NR2B (41 +/- 11%) was observed. This increase was blocked by pretreatment with the selective PKC inhibitor chelerythrine, with the tyrosine kinase inhibitor Lavendustin A or with the
The aim of the present study was to investigate the effect of chelidonine on mitotic slippage and apoptotic-like death in SGC-7901 human gastric cancer cells. The MTT assay was performed to detect the antiproliferative effect of chelidonine. Following treatment with chelidonine (10 µmol/l), the ultrastructure changes in SGC-7901, MCF-7 and HepG2 cells were observed by transmission electron microscopy. The effects of chelidonine on G2/M phase arrest and apoptosis of SGC-7901 cells were determined by flow cytometry. Indirect immunofluorescence assay and laser scanning confocal microscopy (LSCM) were used to detect the phosphorylation level of histone H3 (Ser10) and microtubule formation was detected using LSCM following immunofluorescent labeling. Subsequent to treatment with chelidonine (10 µmol/l), expression levels of mitotic slippage-associated proteins, including BUB1 mitotic checkpoint serine/threonine kinase B (BubR1), cyclin-dependent kinase 1 (Cdk1) and cyclin B1, and ...
Sugita M., Kuwata H., Kudo I., Hara S.. Protein kinase C (PKC) is a family of serine/threonine kinases involved in various signal transduction pathways. We investigated the roles of PKC in the regulation of group IIA secreted phospholipase A(2) (sPLA(2)-IIA) expression in cytokine-stimulated rat fibroblastic 3Y1 cells. Here we show that the induction of sPLA(2)-IIA by proinflammatory cytokines was under the control of both classical cPKCalpha and atypical aPKClambda/iota pathways by using PKC inhibitors, a PKC activator, and PKC knockdowns. Treatment of 3Y1 cells with PKC selective inhibitors having broad specificity, such as chelerythrine chloride and GF109203X, blocked IL-1beta/TNFalpha-dependent induction of sPLA(2)-IIA protein in a dose-dependent manner. Treatment with the PKC activator phorbol 12-myristate 13-acetate (PMA), which activates cPKC and novel nPKC isoforms, markedly attenuated the cytokine-dependent induction of sPLA(2)-IIA expression. In comparison, 24-h pretreatment with PMA, ...
Beck, Zoltán (2010) Erdős Lajos mesei világa és meséi. Iskolakultúra, 20 (1). pp. 150-152. ISSN 1215-5233 Kemény-Beke, Ádám and Aradi, János and Damjanovich, Judit and Beck, Zoltán and Facskó, Andrea and Berta, András and Bodnár, Andrea (2006) Apoptotic response of uveal melanoma cells upon treatment with chelidonine, sanguinarine and chelerythrine. Cancer Letters, 237 (1). pp. 67-75. ISSN 0304-3835 Beck, Zoltán (2003) Európai cigány irodalom. Iskolakultúra, 13 (12). pp. 128-130. ISSN 1215-5233 Tóth, Ferenc D. and Bácsi, Attila and Beck, Zoltán and Szabó, Judit (2001) Vertical transmission of human immunodeficiency virus (A review). Acta Microbiologica et Immunologica Hungarica, 48 (3-4). pp. 413-427. ISSN 1217-8950 Beck, Zoltán (2000) Cigány Tanulmányok. Iskolakultúra, 10 (12). pp. 103-104. ISSN 1215-5233 Beck, Zoltán (1998) Egy irodalom teremtődése. Az identitásképzés problematikája a magyar nyelvű cigány irodalomban. Iskolakultúra, 8 (9). pp. 55-66. ISSN ...
NK314 is a novel synthetic benzo[c]phenanthridine alkaloid that shows strong antitumor activity. It inhibited topoisomerase II activity and stabilized topoisomerase II-DNA cleavable complexes. The DNA breaks occurred within 1h after treatment with NK314 even without digestion of topoisomerase II by proteinase K, whereas etoposide required digestion of the enzyme protein in cleavable complex to detect DNA breaks. Pretreatment with topoisomerase II catalytic inhibitors, ICRF-193 and suramin, reduced both cleavable complex-mediated DNA breaks and proteinase K-independent DNA breaks, but protease inhibitors and nuclease inhibitors only decreased the latter.
Female A. domesticus exhibit variability in their phonotactic behavior. Some females respond to syllable periods (SPs) typical of the males calling song (CS; 50-70 ms), others respond additionally to CSs with shorter or longer SPs, outside the range of males calls. Other females are not selective to SP and respond to the full range of SPs. Nanoinjection of Juvenile Hormone III (JHIII) into the prothoracic ganglion increases phonotactic selectivity. Nanoinjection of chelerythrine chloride (a protein kinase C inhibitor) reduces the effect of JHIII. The L3 prothoracic interneuron responds selectively to the SP of the males CS and is proposed to be involved in controlling SP-selective phonotaxis. Prothoracic nanoinjection of JHIII increases selective responses of L3 which parallels its effects on phonotaxis. This increase in selectivity seems to result from a decrease in decrement, predominantly at the shorter and longer SPs. Such effects increase selectivity in response to the SPs that are most
PHENANTHRIDINE | C13H9N | CID 9189 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Phenanthridine N-oxide | C13H9NO | CID 26728 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
The hallmark of chromatin lies in its dynamic alteration of epigenetic marks, which regulates the gene expression and thereby, cellular homeostasis. Any small molecule compound that perturbs the chromatin structure could potentially alter the epigenetic s
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Objective: This study investigated signaling pathways that may contribute to the potent positive inotropic effect of human urotensin-II (hU-II) in human isolated right atrial trabeculae obtained from patients with coronary artery disease. Methods: Trabeculae were set up in tissue baths and stimulated to contract at 1 Hz. Tissues were incubated with 20 nM hU-II with or without phorbol 12-myristate 13-acetate (PMA, 10 μM) to desensitize PKC, the PKC inhibitor chelerythrine (10 μM), 10 μM 4α-phorbol that does not desensitize PKC, the myosin light chain kinase inhibitor wortmannin (50 nM, 10 μM), or the Rho kinase inhibitor Y-27632 (0.1-10 μM). Activated RhoA was determined by affinity immunoprecipitation, and phosphorylation of signaling proteins was determined by SDS-PAGE. Results: hU-II caused a potent positive inotropic response in atrial trabeculae, and this was concomitant with increased phosphorylation of regulatory myosin light chain (MLC-2, 1.8±0.4-fold, P less than 0.05, n=6) and PKCα/βII
The signalling mechanisms responsible for the hydrolysis of sphingomyelin mediated by 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] and interferon γ (IFN-γ) in HL-60 cells were investigated. IFN-γ was found to increase selectively the activity of cytosolic, Mg2+-independent, neutral sphingomyelinase. The treatment of HL-60 cells with the combination of 1,25(OH)2D3 and IFN-γ had an additive effect on sphingomyelin hydrolysis, ceramide release and the activity of cytosolic, Mg2+-independent, neutral sphingomyelinase. The pretreatment of HL-60 cells with staurosporine, chelerythrine chloride and bisindolylmaleimide abolished the activity of sphingomyelinase in response to 1,25(OH)2D3 and IFN-γ. Calphostin C, which acts on the regulatory site of protein kinase C (PKC), and Gö 6976, a selective inhibitor of Ca2+-dependent PKC isoforms, inhibited the effect of 1,25(OH)2D3 but had no effect on the IFN-γ-mediated increase in activity of sphingomyelinase. Isoform-specific antibodies were used to deplete ...
The N-terminal fragment of pro B-type natriuretic peptide (NT-proBNP) and proBNP are used as gold standard clinical markers of myocardial dysfunction such as cardiac hypertrophy and left ventricle heart failure. diffuse Western-immunostained bands order Chelerythrine Chloride on SDSCPAGE and each band collapsed to an obvious homogeneous band pursuing deglycosylation. Hence, glycosylated-proBNP could be one particular circulating form. Right here we provide comprehensive physiochemical characterization because of this O-linked proteins and evaluate these leads to various other defined circulating species, non-glycosylated-proBNP and NT-proBNP. Itll be proven that glycosylation does not have any impact on the secondary and quaternary framework of proBNP. Actually, at moderate focus in benign physiological neutral pH buffer, all three most likely circulating species are essentially without major secondary framework, i.electronic., are intrinsically unstructured proteins (IUPs). Furthermore, all ...
1,2-Dioctanoyl-sn-glycerol - CAS 60514-48-9 - Calbiochem CAS 60514-48-9 Cell-permeable activator of protein kinase C (PKC). - Find MSDS or SDS, a COA, data sheets and more information.
1,2-Dioctanoyl-sn-glycerol - CAS 60514-48-9 - Calbiochem Cell-permeable activator of protein kinase C (PKC). - Find MSDS or SDS, a COA, data sheets and more information.
Abstract. Caldesmon, an inhibitory actin binding protein, binds to actin and inhibits actin-myosin interactions, whereas caldesmon phosphorylation reverses the inhibitory effect of caldesmon on actin-myosin interactions, potentially leading to enhanced contraction. The goal of this study was to investigate the cellular signaling pathway responsible for caldesmon phosphorylation, which is involved in the regulation of the contraction induced by dexmedetomidine (DMT), an alpha-2 adrenoceptor agonist, in endothelium-denuded rat aortas. SP600125 (a c-Jun NH2-terminal kinase [JNK] inhibitor) dose-response curves were generated in aortas that were pre-contracted with DMT or phorbol 12,13-dibutyrate (PDBu), a protein kinase C (PKC) activator. Dose-response curves to the PKC inhibitor chelerythrine were generated in rat aortas pre-contracted with DMT. The effects of SP600125 and rauwolscine (an alpha-2 adrenoceptor inhibitor) on DMT-induced caldesmon phosphorylation in rat aortic vascular smooth muscle ...
Opium poppy (Papaver somniferum) produces a diverse array of bioactive benzylisoquinoline alkaloids and has emerged as a model system to study plant alkaloid metabolism. The plant is cultivated as the only commercial source of the narcotic analgesics morphine and codeine, but also produces many other alkaloids including the antimicrobial agent sanguinarine. Modulations in plant secondary metabolism as a result of environmental perturbations are often associated with the altered regulation of other metabolic pathways. As a key component of our functional genomics platform for opium poppy we have used proton nuclear magnetic resonance (1H NMR) metabolomics to investigate the interplay between primary and secondary metabolism in cultured opium poppy cells treated with a fungal elicitor. Metabolite fingerprinting and compound-specific profiling showed the extensive reprogramming of primary metabolic pathways in association with the induction of alkaloid biosynthesis in response to elicitor treatment. Using
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If patients could recognise themselves, or anyone else could recognise a patient from your description, please obtain the patients written consent to publication and send them to the editorial office before submitting your response [Patient consent forms] ...
Flow Free: Corydalis Flower Essence is an energetic cleanser; boldly moves through stagnation, creating improved flow and feelings of wellbeing.
A garden picture of Corydalis solida, Many thanks to Mr MB for his advice on growing this plant - I didnt even know which way up to plant the corms! Now its shooting up and even has a flower appearing.
Keltamo on myrkyllinen unikkokasvi. Sen biokemiaa ei tunneta vielä tarkasti, mutta se sisältää korkeintaan 2.3% alkaloideja: protopine, heleritiini, kelidoniini, jotka toimivat kuin morfiini. Aine vaikuttaa hermostoon, sekä voi aiheuttaa myös kehon halvaantumi- sen. Keltamo sisältää myöskin orgaanisia happoja, A ja C- vitamiineja, sitruuna-, omena- ja meripihka-happoja, flavonoideja ja tanniineja. Mitä vanhempi kasvi, sitä enemmän lääkinnällisiä ominaisuuksia siinä…
The United States FDA has approved the inclusion of sanguinarine in toothpastes as an antibacterial or anti-plaque agent.[4][5][6][7] Currently, it is believed that this use may cause leukoplakia, a premalignant oral lesion.[8] On 24 Nov 2003, the Colgate-Palmolive Company commented by memorandum (see: PDF file) to the United States Food and Drug Administration that then-proposed rules for levels of sanguinarine in mouthwash and dental wash products were lower than necessary. Professor George T. Gallagher also commented from his post at Boston University Goldman School of Dental Medicine, see his memorandum[1] of 23 June 2003.. Sangrovit® is an animal food additive sold and distributed in Europe. Sangrovit is manufactured by Germany-based Phytobiotics. Sangrovit contains sanguinarine and chelerythrine. On 14 May 2003, Cat Holmes reported in the Georgia Faces[9] that Jim Affolter and Selima Campbell, horticulturists at the University of Georgia College of Agricultural and Environmental Sciences, ...
Looking for online definition of Corydalis in the Medical Dictionary? Corydalis explanation free. What is Corydalis? Meaning of Corydalis medical term. What does Corydalis mean?
IC50: Selective protein kinase D (PKD) antagonist with the IC50 of 0.182, 0.280, 0.227, |10, 15.3, 20.3, 40.5 and |50 μM for PKD1, PKD2, PKD3, PKC, CAK, PLK1, CAMKIIα and Akt respectively.CID755673, benzoxoloazepinolone, is the first identified cell-activ
The intracellular signaling of human urotensin II (hU-II) and its interaction with other vasoconstrictors such as ANG II are poorly understood. In endothelium-denuded rat aorta, coadministration of hU-II (1 nM) and ANG II (2 nM) exerted a significant contractile effect that was associated with increased protein kinase C (PKC) activity and phosphorylation of PKC-α/βII and myosin light chain, whereas either hU-II or ANG II administered alone at these concentrations had no statistically significant effect. This synergistic effect was abrogated by the PKC inhibitor chelerythrine (10 and 30 μM), the selective PKC-α/βII inhibitor Gö-6976 (0.1 and 1 μM), the hU-II receptor ligand urantide (30 nM and 1 μM), or the ANG II antagonist losartan (1 μM). Moreover, in endothelium-intact rat aorta, the synergistic effect of hU-II and ANG II was not exerted any longer, and this synergistic effect was unmasked by pretreatment of the nitric oxide synthase inhibitor NG-nitro-L-arginine methyl ester. hU-II ...
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine: A specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.
When CD47 is ligated with a specific ligand, phosphatidylserine exposure is observed on the surface of the erythrocyte in a process known as eryptosis, which is similar to apoptosis. The aim of this study was to identify new proteins within the CD47 receptor mediated phosphatidylserine pathway and to elucidate the functions of any newly identified proteins. Previous research had suggested a link between protein 4.1R and CD47. Therefore, diseased protein 4.1R deficient erythrocytes were used as a molecular tool to help explore the role of protein 4.1R in the CD47 pathway. To achieve this aim, flow cytometry to measure phosphatidylserine exposure, 1D and 2D protein immunoblotting, 1D and 2D electrophoresis, RS100 ProteinChips coupled to SELDI-TOF, Q-TOF and MALDI-TOF, calcium influx, 2D serine/threonine phosphoblots and protein kinase A and protein kinase C inhibition were employed. Results showed increased phosphatidylserine exposure in 4.1R deficient erythrocytes and protein immunoblots ...
1. Baumann JC. Effect of Chelidonium, Curcuma, absinth and Carduus marianus on the bile and pancreatic secretion in liver diseases [in German]. Med Monatsschr. 1975;29:173-80. 2. Hiller KO, Ghorbani M, Schilcher H. Antispasmodic and relaxant activity of chelidonine, protopine, coptisine, and Chelidonium majus extracts on isolated guinea-pig ileum [letter]. Planta Med. 1998;64:758-60. 3. Hriscu A, Galesanu MR, Moisa L. Cholecystokinetic action of an alkaloid extract of Chelidonium majus. RevMed Chir Soc Med Nat Lasi. 1980;84:559-61. 4. Ritter R, Schatton WFH. Clinical trial on standardized celandine extract in patients with functional epigastric complaints: results of placebo-controlled double-blind trial. Comp Ther Med. 1993;1:189-93. 5. Kupke D, von Sanden H, Trinczek-Gartner H, et al. An evaluation of the choleretic activity of a plant-based cholagogue [in German]. Z Allgemeinmed. 1991;67:1046-1058. 6. Niederau C, Gopfert E. The effect of chelidonium- and turmeric root extract on upper ...
Citation: Schlapak, R. et al. (2009) Selective protein and DNA adsorption on PLL-PEG films modulated by ionic strength. Soft Matter, 5, pp.613-621. ...
Digestion is achieved by the GastroIntestinal Tract (GIT). The food supply must be matched to the GITs ability to process food.
Benzophenanthridines [82] Sanguinarine, oxynitidine, corynoloxine [95] Aporphines [82] Glaucine, coridine, liriodenine [96] ...
Dupont, C; Couillerot, E; Gillet, R; Caron, C; Zeches-Hanrot, M; Riou, JF; Trentesaux, C (2005). "The benzophenanthridine ... It also contains fagaronine, a benzophenanthridine alkaloid. A study by Williams, Soelberg and Jäger (2016) showed than ...
... is a benzophenanthridine alkaloid found in Zanthoxylum zanthoxyloides and other species in the genus Zanthoxylum. ... Dupont, C; Couillerot, E; Gillet, R; Caron, C; Zeches-Hanrot, M; Riou, JF; Trentesaux, C (2005). "The benzophenanthridine ...
This benzophenanthridine alkaloid can induce apoptosis in some transformed or malignant cell lines. D-Chelidonine, the main ... C. majus contains various isoquinoline alkaloids with protopine, protoberberine and benzophenanthridine structures. ...
... is a benzophenanthridine alkaloid present in the plant Chelidonium majus (greater celandine). It is a potent, ... "The actions of benzophenanthridine alkaloids, piperonyl butoxide and (S)-methoprene at the G-protein coupled cannabinoid CB₁ ...
Park SU, Yu M, Facchini PJ (2002). "Antisense RNA-mediated suppression of benzophenanthridine alkaloid biosynthesis in ... Dihydrobenzophenanthridine oxidase produces oxidized forms of benzophenanthridine alkaloids: In Sanguinaria canadensis ( ... cell suspensions and immobilized cultures for production of benzophenanthridine alkaloids". Appl. Microbiol. Biotechnol. 36 (5 ...
... the central enzyme in benzophenanthridine alkaloid biosynthesis". Phytochemistry. 29 (4): 1113-1122. doi:10.1016/0031-9422(90) ...
... is a benzophenanthridine alkaloid found in species of the genus Zanthoxylum , notably in Zanthoxylum nitidum. This ...
Benzophenanthridines [38] Sanguinarine, oxynitidine, corynoloxine [51] Aporphines [38] Glaucine, coridine, liriodenine [52] ...
... an enzyme essential to the formation of benzophenanthridine alkaloids in the response of plants to pathogenic attack". Proc. ... a covalently flavinylated oxidase of benzophenanthridine alkaloid biosynthesis in plants". J. Biol. Chem. 270 (41): 24475-81. ...
... a covalently flavinylated oxidase of benzophenanthridine alkaloid biosynthesis in plants". The Journal of Biological Chemistry ...
Maiti, M.; G. S. Kumar (27 September 2007). "Molecular aspects on the interaction of protoberberine, benzophenanthridine, and ...
"The actions of benzophenanthridine alkaloids, piperonyl butoxide and (S)-methoprene at the G-protein coupled cannabinoid CB₁ ...
... benzophenanthridines, pridophenanthridines, dibenzoquinolizines, terpenes, flavones and furocoumarins. Tylophorine from ...
The benzophenanthridine alkaloid chelerythrine is the major active natural product found in Z. clava-herculis, exhibiting anti- ...
The extract of bloodroot is called sanguinarine, a quaternary benzophenanthridine alkaloid which attacks and destroys living ...
Species identified in Nigeria contains several types of alkaloids including benzophenanthridines (nitidine, dihydronitidine, ...
A phenolic benzophenanthridine alkaloid from Fagara xanthoxyloides (1973) Alkaloids of Fagara macrophylla (1970) Photolysis of ... Comparative examination of two Zanthoxylum benzophenanthridine alkaloids for effects in rabbits (1989) Essential oils of Lippia ...
... benzophenanthridine, phthalide isoquinoline or rhoeadine metabolic pathways. Research on this matter is rare since it is very ...
They are derived from berberine, tetrahydroberberine, protopine and benzophenanthridine in Papaveroideae, and from ...
Benzophenanthridines, naturally occurring isoquinoline alkaloids with various biological activities, are known to exist in five ... Benzophenanthridines, naturally occurring isoquinoline alkaloids with various biological activities, are known to exist in five ...
... method was developed for the qualitative and quantitative determination of benzophenanthridine alkaloids from the methanol ... Benzophenanthridine alkaloids Hylomecon species Enantiomers Chiral separation HPLC This is a preview of subscription content, ... Mizuno, M., Kojima, H., Tanaka, T., Linuma, M., Zhi-Da, M., and Murata, H., Benzophenanthridine alkaloids from the seeds of ... Achiral and chiral determination of benzophenanthridine alkaloids from methanol extracts ofhylomecon species by high ...
Benzophenanthridines [82] Sanguinarine, oxynitidine, corynoloxine [95] Aporphines [82] Glaucine, coridine, liriodenine [96] ...
The Structures of Corynoline and Corynoloxine: Two Unusual Benzophenanthridine Alkaloids V. Syntheses of Benzophenanthridines ... The Benzophenanthridines. I. Introduction II. The Chemistry and Stereochemistry of Chelidonine III. The Chemistry of ... The C-6-Methoxylated Aromatic Benzophenanthridines IX. Bocconine X. Bocconoline and Corynolamine XI. The Characterization of a ... Dimeric Benzophenanthridine Alkaloid XII. Biosynthesis XIII. Pharmacology XIV. UV Spectroscopy References Chapter 18. The ...
Benzophenanthridines / pharmacology * Calcium Channels, L-Type / metabolism* * Cell Line * Gene Expression Regulation / drug ...
Benzophenanthridines * Biofilms / drug effects* * Complex Mixtures * Dental Plaque / prevention & control* * Dentifrices / ...
Evaluation of anticancer activities of benzo phenanthridine alkaloid sanguinarine in oral squamous cell carcinoma cell line.. ... Home » Evaluation of anticancer activities of benzo phenanthridine alkaloid sanguinarine in oral squamous cell carcinoma cell ...
Antitumor effects of the benzophenanthridine alkaloid sanguinarine in a rat syngeneic model of colorectal cancer.. Pica F, ... Antitumor effects of the benzophenanthridine alkaloid sanguinarine in a rat syngeneic model of colorectal cancer.. Primary tabs ... Home » Antitumor effects of the benzophenanthridine alkaloid sanguinarine in a rat syngeneic model of colorectal cancer. ...
Free amine benzophenanthridine alkaloid compositions. US5181903 *. Mar 25, 1988. Jan 26, 1993. Duke University. Method for ... Free amine benzophenanthridine alkaloid compositions. US5397307. Dec 7, 1993. Mar 14, 1995. Schneider (Usa) Inc.. Drug delivery ...
Chemical constituents of the roots of Macleaya microcarpa and activation efficacy of benzophenanthridine alkaloids for the ... eight compounds of derivatives of triterpenes and organic acids in addition to some previously identified benzophenanthridines ...
Benzophenanthridines [77]. Aporphines [77]. Proaporphines [77]. Homoaporphines [92]. Homoproaporphines [92]. Morphines[93] ...
Dupont, C; Couillerot, E; Gillet, R; Caron, C; Zeches-Hanrot, M; Riou, JF; Trentesaux, C (2005). "The benzophenanthridine ... It also contains fagaronine, a benzophenanthridine alkaloid. A study by Williams, Soelberg and Jäger (2016) showed than ...
Benzophenanthridines [38] Sanguinarine, oxynitidine, corynoloxine [51] Aporphines [38] Glaucine, coridine, liriodenine [52] ...
Metal-Catalyzed Domino Synthesis of Benzophenanthridines and 6 H-Naphtho[2,3- c]-chromenes. ...
Wolff J, Knipling L. Antimicrotubule properties of benzophenanthridine alkaloids. Biochemistry 1993;32(48):13334-9. ...
Fagaronine is a benzophenanthridine alkaloid found in Zanthoxylum zanthoxyloides and other species in the genus Zanthoxylum. ... Dupont, C; Couillerot, E; Gillet, R; Caron, C; Zeches-Hanrot, M; Riou, JF; Trentesaux, C (2005). "The benzophenanthridine ...
Vavreckova, C., Gawlik, I., and Muller, K. Benzophenanthridine alkaloids of Chelidonium majus; I. Inhibition of 5- and 12- ... Vavreckova, C., Gawlik, I., and Muller, K. Benzophenanthridine alkaloids of Chelidonium majus; II. Potent inhibitory action ...
Antibacterial benzofuran neolignans and benzophenanthridine alkaloids from the roots of Zanthoxylum capense.. Enhancing ...
Benzophenanthridine alkaloids from Zanthoxylum nitidum (Roxb.) DC, and their analgesic and anti-inflammatory activities. Chem ...
Antiinflammatory activity of quaternary benzophenanthridine alkaloids from Chelidonium majus. Planta Med. 43, 161-165. doi: ...
Shemon, A.N.; Sluyter, R.; Conigrave, A.D.; Wiley, J.S. Chelerythrine and other benzophenanthridine alkaloids block the human ... In 2004, Shemon observed that chelerythrine, a benzophenanthridine alkaloid, blocks the ATP- induced cation fluxes mediated by ...
A benzophenanthridine alkaloid isolated from the root of Zanthoxylum simulans, Chelidonium majus L., and other Papaveraceae.. ... chelerythrine (CHEBI:78373) is a benzophenanthridine alkaloid (CHEBI:38517) chelerythrine (CHEBI:78373) is a organic cation ( ...
This benzophenanthridine alkaloid has antimicrobial activity and plays a role in plant defence [2]. Besides its antimicrobial ...
This early-blooming poppy family member contains benzophenanthridine alkaloids, including sanguinarine.. Medicinal plant ...
Identification of metabolites of selected benzophenanthridine alkaloids and their toxicity evaluation. Journal of ...
Total Synthesis of Modified Benzophenanthridines - A Preliminary Anti-Cancer Study. PI: Dr. Prasanna Ramani. Sponsor: Heutrey ...
Shemon, A., Sluyter, R., Conigrave, A., Wiley, J. (2004). Chelerythrine And Other Benzophenanthridine Alkaloids Block The Human ... Shemon, A., Sluyter, R., Conigrave, A., Wiley, J. (2004). Chelerythrine And Other Benzophenanthridine Alkaloids Block The Human ...
Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C.. J Biol Chem 273:19829-33 (1998 ...
Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C. J. Biol. Chem. 273: 19829. ...
  • Antitumor effects of the benzophenanthridine alkaloid sanguinarine in a rat syngeneic model of colorectal cancer. (sureserver.com)
  • 1) are the benzophenanthridine alkaloids (sanguinarine, chelerythrine and chelidonine) and protoberberines (berberine, coptisine). (thefreedictionary.com)
  • Preparation of liposomes containing benzophenanthridine alkaloid sanguinarine and evaluation of its cytotoxic activity. (phys.org)
  • Here, the natural benzophenanthridine alkaloid sanguinarine has been studied for its cytotoxic activity against multidrug resistance (MDR) cancer cells. (frontiersin.org)
  • Sanguinarine is a benzophenanthridine alkaloid that exhibits a wide variety of beneficial properties, including anticancer, anti-inflammatory, and antibacterial activities. (lktlabs.com)
  • A methanolic extract of Sanguinaria canadensis rhizome contains a mixture of benzophenanthridine alkaloids with the major component sanguinarine. (scirp.org)
  • Sanguinarine is a toxic quaternary ammonium salt from the group of benzophenanthridine alkaloids. (bocsci.com)
  • To investigate the effects of microtubule-binding agents (paclitaxel, vinblastine, colchicine, podophyllotoxin), benzophenanthridine alkaloids (sanguinarine, chelerythrine, chelidonine) and other anti-tumor drugs (homoharringtonine, doxorubicin) on cell migration, we performed the in vitro wound healing assay. (biomedcentral.com)
  • The benzophenanthridine alkaloid sanguinarine, chelerythrine and chelidonine which affected microtubules in living cells, did not inhibit cell migration. (biomedcentral.com)
  • Sanguinarine (SNG), a benzophenanthridine alkaloid, has displayed various anticancer abilities in several vivo and studies. (edu.qa)
  • Nitidine chloride, a natural benzophenanthridine alkaloid, has been shown to inhibit cancer growth via induction of cell apoptosis and suppression of cancer angiogenesis. (adooq.com)
  • Dark incubation at 30ºC with chelerythrine HCl, a natural benzophenanthridine alkaloid, blocked the temperature-dependent migration as well as the light-induced abolishment of the pdc-pS73 spots. (arvojournals.org)
  • Ukrain (NSC-631570) is a semi-synthetic compound derived from the common weed, greater celandine ( Chelidonium majus L.). This plant contains a range of alkaloids, most notably chelidonine, also known as benzophenanthridine alkaloid. (biomedcentral.com)
  • A cytochrome P-450 (heme-thiolate) protein involved in benzophenanthridine alkaloid synthesis in higher plants. (brenda-enzymes.org)
  • Antiinflammatory activity of quaternary benzophenanthridine alkaloids from Chelidonium majus. (healthadverts.com)
  • Molecular cloning, expression, and induction of berberine bridge enzyme, an enzyme essential to the formation of benzophenanthridine alkaloids in the response of plants to pathogenic attack. (ebi.ac.uk)
  • It also contains fagaronine, a benzophenanthridine alkaloid. (wikipedia.org)
  • Fagaronine is a benzophenanthridine alkaloid found in Zanthoxylum zanthoxyloides and other species in the genus Zanthoxylum. (wikipedia.org)
  • The Benzophenanthridine Alkaloid Fagaronine Induces Erythroleukemic Cell Differentiation by Gene of GATA-1 gene by 3.2-fold. (diseasepdf.com)
  • A mutation within the GATA-1 bind-ing sites strongly decreased the promoter activation induced by Fagaronine, a benzophenanthridine alkaloid from Fagara zan- FAG. (diseasepdf.com)
  • Benzophenanthridines, naturally occurring isoquinoline alkaloids with various biological activities, are known to exist in five plant families, namely, the Fumariaceae (Genera Corydalis, Dicentra and Fumaria), the Papaveraceae, and the Rutaceae. (amrita.edu)
  • A benzophenanthridine alkaloid isolated from the root of Zanthoxylum simulans , Chelidonium majus L. , and other Papaveraceae . (ebi.ac.uk)
  • Antibacterial benzofuran neolignans and benzophenanthridine alkaloids from the roots of Zanthoxylum capense. (thefreedictionary.com)
  • A new benzophenanthridine alkaloid and other bioactive constituents from the stem bark of Zanthoxylum heitzii. (uio.no)
  • Protoberberine alkaloids (coralyne and its derivatives), which exhibit antileukemic activity in animal models, have been shown to be potent inducers of topoisomerase (topo) I-DNA clearable complexes using purified recombinant human DNA topo I. Different from the structurally similar benzophenanthridine alkaloid nitidine (a dual poison of both topos I and II), coralyne and its derivatives have marginal poisoning activity against DNA topo II. (elsevier.com)
  • The studied compounds related to bioisostere of benzophenanthridine alkaloid were synthesized and evaluated for antitumor cytotoxicity against human lung tumor cell (A 549). (elsevier.com)
  • Ongoing study on the chemical constituents of the roots of Macleaya microcarpa led to the isolation of eight compounds of derivatives of triterpenes and organic acids in addition to some previously identified benzophenanthridines . (bvsalud.org)
  • Angoline and chelerythrine, benzophenanthridine alkaloids that do not inhibit protein kinase C. (abcam.com)
  • A high performance liquid chromatographic (HPLC) method was developed for the qualitative and quantitative determination of benzophenanthridine alkaloids from the methanol extracts of Hylomecon hylomeconoides and H. vernale (Papaveraceae). (springer.com)
  • Greater celandine, similarly as other plants of the family Papaveraceae, produces benzylisoquinoline alkaloids, primarily benzophenanthridines. (saladgaffe.ml)