Dibenzoquinolines derived in plants from (S)-reticuline (BENZYLISOQUINOLINES).

Bronchodilator and anti-inflammatory activities of glaucine: In vitro studies in human airway smooth muscle and polymorphonuclear leukocytes. (1/80)

1. Selective phosphodiesterase 4 (PDE4) inhibitors are of potential interest in the treatment of asthma. We examined the effects of the alkaloid S-(+)-glaucine, a PDE4 inhibitor, on human isolated bronchus and granulocyte function. 2. Glaucine selectively inhibited PDE4 from human bronchus and polymorphonuclear leukocytes (PMN) in a non-competitive manner (Ki=3.4 microM). Glaucine displaced [3H]-rolipram from its high-affinity binding sites in rat brain cortex membranes (IC50 approximately 100 microM). 3. Glaucine inhibited the spontaneous and histamine-induced tone in human isolated bronchus (pD2 approximately 4.5). Glaucine (10 microM) did not potentiate the isoprenaline-induced relaxation but augmented cyclic AMP accumulation by isoprenaline. The glaucine-induced relaxation was resistant to H-89, a protein kinase A inhibitor. Glaucine depressed the contractile responses to Ca2+ (pD'2 approximately 3.62) and reduced the sustained rise of [Ca2+]i produced by histamine in cultured human airway smooth muscle cells (-log IC50 approximately 4.3). 4. Glaucine augmented cyclic AMP levels in human polymorphonuclear leukocytes challenged with N-formyl-Met-Leu-Phe (FMLP) or isoprenaline, and inhibited FMLP-induced superoxide generation, elastase release, leukotriene B4 production, [Ca2+]i signal and platelet aggregation as well as opsonized zymosan-, phorbol myristate acetate-, and A23187-induced superoxide release. The inhibitory effect of glaucine on superoxide generation by FMLP was reduced by H-89. 5. In conclusion, Ca2+ channel antagonism by glaucine appears mainly responsible for the relaxant effect of glaucine in human isolated bronchus while PDE4 inhibition contributes to the inhibitory effects of glaucine in human granulocytes. The very low PDE4/binding site ratio found for glaucine makes this compound attractive for further structure-activity studies.  (+info)

Mechanical effects of liriodenine on the left ventricular-arterial coupling in Wistar rats: pressure-stroke volume analysis. (2/80)

1. In a recent in vivo study, liriodenine, an aporphine alkaloid, has been identified as a prominent anti-arrhythmic agent that can prevent rats' sudden deaths, even at the dose as low as 10(-7) g kg(-1). The aim of this study was to determine whether liriodenine at its effective anti-arrhythmic dose of 10(-7) g kg(-1) had effects on the left ventricular (LV)-arterial coupling in Wistar rats. 2. LV pressure and ascending aortic flow signals were recorded to construct the ventricular and arterial end-systolic pressure-stroke volume relationships to calculate LV end-systolic elastance (E(es)) and effective arterial volume elastance (E(a)), respectively. The optimal afterload (Q(load)) determined by the ratio of E(a) to E(es) was used to measure the optimality of energy transmission from the left ventricle to the arterial system. 3. Liriodenine at the dose of 10(-7) g kg(-1) showed no significant changes in basal heart rate (HR), cardiac output (CO), LV end-systolic pressure (P(es)), E(a), E(es), and Q(load). 4. By contrast, liriodenine at the dose of 10(-6) g kg(-1) produced a significant fall of 2.0% in HR and a significant rise of 5.8% in CO, but no significant change in P(es). Moreover, liriodenine administration of 10(-6) g kg(-1) to rats significantly decreased E(es) by 8.5% and E(a) by 10.6%, but did not change Q(load). 5. We conclude that liriodenine at the dose of 10(-7) g kg(-1) has no effects on the mechanical properties of the heart and the vasculature and the matching condition for the left ventricle coupled to its vasculature in rats. Even at 10 times the effective anti-arrhythmic dose, liriodenine shows no effects on the efficiency of energy transferred from the left ventricle to the arterial system.  (+info)

Dicentrine is preferentially antagonistic to rat aortic than splenic alpha 1-adrenoceptor stimulation. (3/80)

AIM: Dicentrine is a known alpha 1-adrenoceptor antagonist, but its alpha 1-adrenoceptor subtype selectivity has not yet been determined. We therefore, investigated the putative alpha 1-adrenoceptor subtype selectivity of this agent. METHODS: Graded isometric contractile responses of rat aortic rings and spleen to phenylephrine were observed in the absence or presence of various concentrations of dicentrine. The pA2 values for dicentrine were determined. RESULTS: Aortic tissues were more sensitive to phenylephrine-induced contraction than the spleen tissues. Dicentrine was approximately 100 times more potent as an antagonist to the aortic contraction, than it was to the splenic contractions. CONCLUSION: Dicentrine is an alpha 1-adrenoceptor antagonist which is more selective towards the putative alpha 1D-adrenoceptor subtype of the rat aorta than the alpha 1B-adrenoceptor of the spleen.  (+info)

Multiple actions of glaucine on cyclic nucleotide phosphodiesterases, alpha 1-adrenoceptor and benzothiazepine binding site at the calcium channel. (4/80)

1. In the present study, the properties of glaucine (an aporphine structurally related to papaverine) were compared with those of papaverine, diltiazem, nifedipine and prazosin. The work includes functional studies on rat isolated aorta contracted with noradrenaline, caffeine or KCl, and a determination of the affinity of glaucine at calcium channel binding sites of alpha-adrenoceptors, by use of [3H]-(+)-cis-diltiazem, [3H]-nitrendipine and [3H]-prazosin binding to cerebral cortical membranes. The effects of glaucine on the different molecular forms of cyclic nucleotide phosphodiesterases (PDE) isolated from bovine aorta were also determined. 2. Contraction evoked by noradrenaline (1 microM) or depolarizing solution (60 mM KCl) were inhibited in a concentration-dependent manner by all the compounds tested. As expected, prazosin showed a greater selectivity of action on NA-induced contraction, whereas nifedipine and diltiazem appeared more potent on KCl-induced contraction. Glaucine had a greater potency on the contraction elicited by noradrenaline whereas papaverine acted non specifically. 3. In Ca(2+)-free solution, prazosin (0.1 microM) and glaucine (0.1 mM) inhibited the contraction evoked by NA; diltiazem (0.1 mM) diminished this contraction whereas nifedipine (1 microM) had no effect. Preincubation of tissues with glaucine, diltiazem, nifedipine and prazosin did not modify the contractile response induced by caffeine. In contrast, papaverine (0.1 mM) significantly inhibited the contractions evoked by NA or caffeine in Ca(2+)-free medium. 4. Glaucine and papaverine show affinity at the [3H]-prazosin binding site and at the benzothiazepine binding site of the Ca(2+)-channel receptor complex, but have no effect at the dihydropyridine binding site in rat cerebral cortex. Glaucine exerts some selectivity as an inhibitor of [3H]-prazosin binding as opposed to [3H]-(+ )-cis-diltiazem binding while papaverine appears to have approximately equal affinity in this respect.5. This study confirms the presence of four phosphodiesterase (PDE) activities in bovine aorta: a calmodulin-activated PDE (CaM-PDE type I) which hydrolyzed preferentially guanosine 3':5'-cyclic monophosphate (cyclic GMP); a cyclic GMP selective form (cGMP-PDE type V); and two low Km adenosine 3':5'-cyclic monophosphate (cyclic AMP) PDEs that are insensitive to the stimulatory effect of CaM, one of which was inhibited by cyclic GMP (CGI-PDE, type III) and the other by rolipram (cAMP-PDE, type IV). Glaucine selectively inhibits one of the two forms of Ca2+-independent low Km cAMP-PDE, the type IV. In contrast, papaverine exerts a non-selective inhibitory effect upon all PDE forms.6. The present work provides evidence that glaucine, a benzyltetrahydroisoquinoline alkaloid, has interesting properties as an alpha l-adrenoceptor antagonist, calcium entry blocker (through the benzothiazepine recognition site in the calcium channel) and as a selective inhibitor of the rolipram-sensitive cAMP-PDE, type IV PDE.  (+info)

Haemodynamic effects of dicentrine, a novel alpha 1-adrenoceptor antagonist: comparison with prazosin in spontaneously hypertensive and normotensive Wistar-Kyoto rats. (5/80)

1. The haemodynamic effects of dicentrine, an aporphine derivative isolated from the plant Lindera megaphylla, were investigated and compared with prazosin in rats. 2. In anaesthetized normotensive Wistar-Kyoto (WKY) rats, i.v. administration of dicentrine (0.1, 0.5, 1.0 mg kg-1) and prazosin (0.01, 0.05, 0.1 mg kg-1) induced a dose-related reduction of mean arterial pressure (MAP) which reached a maximal effect 5-10 min after injection and persisted for 2 h. 3. In anaesthetized WKY rats, a higher dose of dicentrine (1.0 mg kg-1, i.v.) did not cause any significant changes in heart rate (HR), cardiac output (CO) and stroke volume (SV) but markedly increased tail blood flow. In contrast, a higher dose of prazosin (0.1 mg kg-1, i.v.) produced a decrease in HR which paralleled the time course of the hypotensive response. 4. The hypotensive activity of dicentrine was completely abolished by alpha-adrenoceptor blockade. Both dicentrine and prazosin significantly attenuated pressor responses to noradrenaline but failed, even at maximal hypotensive doses, to impair the pressor effects of angiotensin II or vasopressin. These observations suggest that dicentrine appears to exert its hypotensive action through alpha 1-adrenoceptor blockade. 5. In conscious normotensive and spontaneously hypertensive (SH) rats, dicentrine (0.5-2.0 mg kg-1, i.v.) and prazosin (0.05-0.2 mg kg-1, i.v.) also evoked dose-related decreases in MAP which were of greater magnitude in SH rats. Oral administration of dicentrine (5 and 8 mg kg-1) to conscious SH rats caused a hypotensive effect which persisted for over 15 h.6. These results suggest that dicentrine may have therapeutic potential as an oral antihypertensive drug via alpha-adrenoceptor blockade.  (+info)

Reactive oxygen species (ROS) generation inhibited by aporphine and phenanthrene alkaloids semi-synthesized from natural boldine. (6/80)

Four phenanthrene and one aporphine alkaloids semi-synthesized from boldine were evaluated for their inhibitory effect on reactive oxygen species (ROS) generation. ROS generation by neutrophils stimulated with N-formyl-methionyl-leucyl-phenylalanine was inhibited in a concentration dependent manner. Alkaloids exerted similar inhibitory effect in the hypoxanthine-xanthine oxidase system than in stimulated neutrophils, which could be attributed to a direct ROS scavenging activity. None of the alkaloids assayed had any effect on xanthine oxidase activity. Therefore the synthesized alkaloids might constitute an alternative therapy in inflammation disorders in which ROS generation is involved.  (+info)

Effect of boldine, secoboldine, and boldine methine on angiotensin II-induced neutrophil recruitment in vivo. (7/80)

Angiotensin-II (Ang-II) has inflammatory activity and is involved in different diseases associated with the cardiovascular system. This study has evaluated the effect of boldine (B), and two phenanthrene alkaloids semisynthesized by us, secoboldine (SB) and boldine methine (BM), on Ang-II-induced neutrophil recruitment. Intraperitoneal administration of 1 nM Ang-II induced significant neutrophil accumulation, which was maximal at 4-8 h. BM inhibited neutrophil infiltration into the peritoneal cavity at 4 h and 8 h by 73% and 77%, respectively, SB at 8 h by 55%, and B had no effect on this response. Although BM inhibited the release of cytokine-inducible neutrophil chemoattractant/keratinocyte-derived chemokine, macrophage inflammatory protein-2 (MIP-2), and platelet-activating factor (PAF) elicited by Ang-II, SB only reduced the release of MIP-2 after 4 h of its administration. Sixty-minute superfusion of the rat mesentery with 1 nM Ang-II induced a significant increase in the leukocyte-endothelial cell interactions and P-selectin up-regulation, which were inhibited by 1 microM BM and SB. The generation of reactive oxygen species (ROS) in endothelial cells stimulated with Ang-II was inhibited significantly by the three alkaloids tested. BM also diminished Ang-II-induced interleukin-8 release from endothelial cells and blocked the PAF receptor on human neutrophils (concentration of the compound needed to produce 50% inhibition value: 28.2 microM). Therefore, BM is a potent inhibitor of Ang-II-induced neutrophil accumulation in vivo. This effect appears to be mediated through inhibition of CXC chemokine and PAF release, ROS scavenging activity, and blockade of the PAF receptor. Thus, it may have potential therapeutic interest for the control of neutrophil recruitment that occurs in inflammation associated with elevated levels of Ang-II.  (+info)

Characterization and inhibitor discovery of one novel malonyl-CoA: acyl carrier protein transacylase (MCAT) from Helicobacter pylori. (8/80)

Type II fatty acid synthesis (FAS II) is an essential process for bacteria survival, and malonyl-CoA:acyl carrier protein transacylase (MCAT) is a key enzyme in FAS II pathway, which is responsible for transferring the malonyl group from malonyl-CoA to the holo-ACP by forming malonyl-ACP. In this work, we described the cloning, characterization and enzymatic inhibition of a new MCAT from Helicobacter pylori strain SS1 (HpMCAT), and the gene sequence of HpfabD was deposited in the GenBank database (Accession No. AY738332 ). Enzymatic characterization of HpMCAT showed that the K(m) value for malonyl-CoA was 21.01+/-2.3 microM, and the thermal- and guanidinium hydrochloride-induced unfolding processes for HpMCAT were quantitatively investigated by circular dichroism spectral analyses. Moreover, a natural product, corytuberine, was discovered to demonstrate inhibitory activity against HpMCAT with IC(50) value at 33.1+/-3.29 microM. Further enzymatic assay results indicated that corytuberine inhibits HpMCAT in an uncompetitive manner. To our knowledge, this is the firstly reported MCAT inhibitor to date. This current work is hoped to supply useful information for better understanding the MCAT features of H. pylori strain, and corytuberine might be used as a potential lead compound in the discovery of the antibacterial agents using HpMCAT as target.  (+info)

Aporphine is a type of chemical compound called alkaloids, which are found in certain plants. Aporphines have a specific chemical structure and can have various pharmacological effects. They have been studied for their potential medicinal properties, including anti-inflammatory, antispasmodic, and antiasthmatic activities. Some aporphine alkaloids have also been found to have psychoactive effects and are used in traditional medicine in some cultures. However, more research is needed to fully understand the therapeutic potential and safety of aporphines.

... is an alkaloid with the chemical formula C17H17N. It is the core chemical substructure of the aporphine alkaloids, a ... It can exist in either of two enantiomeric forms, (R)-aporphine and (S)-aporphine. Many different derivatives have been ... R)-Aporphine is a dopamine receptor D1 antagonist with a Ki of 717 nM and a dopamine receptor D2 antagonist with a Ki of 527 nM ... Aporphine natural products occur with either the (R)- or (S)-stereochemistries, or they can be achiral. Furthermore, morphine- ...
The aporphine alkaloids are of interest mainly because of their similarity to morphine. The aporphine alkaloids are most ... At least 85 aporphine alkaloids have been isolated from plants of 15 families. The best known representative is apomorphine. ... The aporphine alkaloids usually have a stereocenter. The (R)-configured glaucine can be synthesized from (S)-glaucine. ... Aporphine alkaloids are naturally occurring chemical compounds from the group of alkaloids. After the benzylisoquinoline ...
January 1976). "Aporphines. 14 Dopaminergic and antinociceptive activity of aporphine derivatives. Synthesis of 10- ... Miller RJ, Kelly PH, Neumeyer JL (January 1976). "Aporphines. 15. Action of aporphine alkaloids on dopaminergic mechanisms in ... N-n-Propylnorapomorphine (NPA) is an aporphine derivative dopamine agonist closely related to apomorphine. In rodents it has ... and analogous aporphines". Neuropharmacology. 21 (10): 953-61. doi:10.1016/0028-3908(82)90106-X. PMID 6890636. S2CID 23393175. ...
Its optical rotation is [ α ] D 20 = + 36.5 {\displaystyle [\alpha ]_{D}^{20}=+36.5} °. Aporphine Lakshmi; et al. (2009). "An ... Aporphine alkaloids, Phenol ethers, Benzaldehydes, All stub articles, Alkaloid stubs). ...
Extracts of bioactive molecules from its tissues have been reported to contain aporphine derivatives. Erkens, R.H.J. (2021). " ... Borup-Grochtmann, I.; Kingston, David G. I. (1982). "Aporphine Alkaloids From Annona acuminata". Journal of Natural Products. ...
Stévigny C, Block S, De Pauw-Gillet MC, de Hoffmann E, Llabrès G, Adjakidjé V, Quetin-Leclercq J. Cytotoxic aporphine alkaloids ... I. New aporphine alkaloids fromCassytha filiformisL". Australian Journal of Chemistry. 19 (2): 297. doi:10.1071/CH9660297. ISSN ... "Alkaloids from Cassytha filiformis and related aporphines: antitrypanosomal activity, cytotoxicity, and interaction with DNA ...
... is an anti-cholinergic aporphine alkaloid. Naaz, H; Singh, S; Pandey, VP; Singh, P; Dwivedi, UN (2013). "Anti- ... Aporphine alkaloids, All stub articles, Alkaloid stubs). ...
The most common structural types are the benzylisoquinolines and the aporphines. According to current knowledge, a total of ...
Bandara, BM; Cortes, D; Jayasinghe, UL; Karunaratne, V; Sotheeswaran, S; Wannigama, GP (1989). "Aporphine alkaloids from Litsea ...
Benzylisoquinoline alkaloids include aporphines and oxoaporphines, as well as derivatives of morphinans. Essential oils include ...
It contains members of the group of alkaloids: berberines, tetrahydroprotoberberines and aporphines. Bark extracts used by ...
Aporphines: Synthesis, Pharmacology, and Modeling of D2Aand 5-HT1AReceptor Interactions". Journal of Medicinal Chemistry. 39 ( ...
... is an alkaloid of the aporphine class that can be found in the boldo tree. It is the most abundant aporphine alkaloid ... Aporphine alkaloids, Phenols, Phenol ethers, All stub articles, Alkaloid stubs). ...
Structurally, it contains an aporphine core featuring a quaternary ammonium group. Asimilobine - amine not quaternized Anonaine ... Pukateine Matsushige, A; Kotake, Y; Matsunami, K; Otsuka, H; Ohta, S; Takeda, Y (2012). "Annonamine, a new aporphine alkaloid ... Aporphine alkaloids, All stub articles, Alkaloid stubs). ...
Matsushige, A; Kotake, Y; Matsunami, K; Otsuka, H; Ohta, S; Takeda, Y (2012). "Annonamine, a new aporphine alkaloid from the ... The leaves of Annona muricata contain annonamine, which is an aporphine-class alkaloid containing a quaternary ammonium group. ...
His main work was on nucleic acids, morphine and aporphine alkaloids. His work at University College Nottingham on ...
Both Nymphaea caerulea and Nelumbo nucifera contain the alkaloids nuciferine and aporphine.[citation needed] The genome of the ...
"Two New Natural Azafluorene Alkaloids and a Cytotoxic Aporphine Alkaloid from Polyalthia longifolia". Journal of Natural ...
Wu, YC; Duh, CY; Wang, SK; Chen, KS; Yang, TH (1990). "Two new natural azafluorene alkaloids and a cytotoxic aporphine alkaloid ...
3.0.co;2-n "Antiprotozoal activity of aporphine alkaloids isolated fromUnonopsis buchtienii (Annonaceae)". Phytotherapy ...
Apomorphine Aporphine Glaucine Bulbocapnine Nantenine Pukateine Stepholidine Tetrahydropalmatine Seligman, Sian (2023-01-13). " ... Aporphine alkaloids, Dopamine receptor modulators, All stub articles, Sedative stubs). ...
Most important were the benzylisoquinoline-aporphine derivatives, a relatively new group of alkaloids. The results obtained ...
"Aporphine and Tetrahydroprotoberberine Alkaloids from the Leaves ofGuatteria friesiana(Annonaceae) and their Cytotoxic ...
... (1,2,9,10-TetraMethoxyAporphine, Bromcholitin, Glauvent, Tusidil, Tussiglaucin) is an aporphine alkaloid found in ... Zetler G (1988). "Neuroleptic-like, anticonvulsant and antinociceptive effects of aporphine alkaloids: bulbocapnine, ... Zetler G (1988). "Neuroleptic-like, anticonvulsant and antinociceptive effects of aporphine alkaloids: bulbocapnine, ... Aporphine Boldine Nuciferine Apomorphine Pukateine Bulbocapnine Drotaverine Nantenine Stepholidine Tetrahydropalmatine Lapa GB ...
For example, aporphine alkaloid liriodenine produced by the tulip tree protects it from parasitic mushrooms. In addition, the ...
It has been suggested that piperolactam A and related compounds are biosynthesised from aporphine precursors. Aristolactams ...
... is an α1D-adrenergic receptor antagonist.The compound belongs to the group of Aporphine alkaloids. Indra, B; ... Aporphine alkaloids, All stub articles, Organic compound stubs, Pharmacology stubs). ...
Azasteroid Aporphine Heterocyclic compound India portal Chemistry portal His adviser for master's degree was S. M. Mukherji ... Among the other natural products and drugs he synthesized include steroidal sapogenins, phenanthridine, aporphine, quinculidine ... for the synthesis of the phenanthridine ring system and other heterocyclic systems as well as the synthesis of aporphine and ...
S)-Magnoflorine is a quaternary benzylisoquinoline alkaloid (BIA) of the aporphine structural subgroup which has been isolated ... Aporphine alkaloids, Quaternary ammonium compounds, All stub articles, Alkaloid stubs). ... "Isolation and Characterization of Reticuline N-Methyltransferase Involved in Biosynthesis of the Aporphine Alkaloid ...
Like other species in the genus, the plant contains the psychoactive alkaloid aporphine, which provide sedative effects when ...
Aporphine is an alkaloid with the chemical formula C17H17N. It is the core chemical substructure of the aporphine alkaloids, a ... It can exist in either of two enantiomeric forms, (R)-aporphine and (S)-aporphine. Many different derivatives have been ... R)-Aporphine is a dopamine receptor D1 antagonist with a Ki of 717 nM and a dopamine receptor D2 antagonist with a Ki of 527 nM ... Aporphine natural products occur with either the (R)- or (S)-stereochemistries, or they can be achiral. Furthermore, morphine- ...
"Aporphines" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands. Bioorg Med Chem Lett. 2007 Aug ... This graph shows the total number of publications written about "Aporphines" by people in Harvard Catalyst Profiles by year, ... Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor. ...
Oxoisoaporphines and aporphines : Versatile molecules with anticancer effects. En: Molecules. 2020 ; Vol. 25, N.º 1. ... Oxoisoaporphines and aporphines: Versatile molecules with anticancer effects. Esteban Rodríguez-Arce, Patricio Cancino, Manuel ... title = "Oxoisoaporphines and aporphines: Versatile molecules with anticancer effects",. abstract = "Cancer is a disease that ... Oxoisoaporphines and aporphines: Versatile molecules with anticancer effects. / Rodríguez-Arce, Esteban; Cancino, Patricio; ...
CANELLALES + PIPERALES]: flavonols, aporphine alkaloids +; nodes 3:3; G whorled.. PIPERALES Dumortier - Main Tree. ...
aporphines: from antioxidant. Nat. Prod. Commun., 8(12), 1797-1800.. Ncube, B., Nair, J. J., Rarova, L., Strnad, M., Finnie, J ... Chen, J., Gao, K., Liu, T., Zhao, H., Wang, J., Wu, H., Liu, B., Wang, W. (2013). Aporphine. alkaloids: a kind of alkaloids ...
R. Sotníková, V. Kettmann, D. Kostálová, and E. Táborská, "Relaxant properties of some aporphine alkaloids from Mahonia ... aporphines, and bisbenzylisoquinolines. Berberine is the most widely distributed alkaloid in the Mahonia species [60], but ...
Antiplatelet effects of some aporphine and phenanthrene alkaloids in rabbits and man. J Pharm Pharmacol. 1997;49(7):706- ...
It also contains aporphine, which gives a feeling of euphoria and ecstasy. Moreover, it is known to enhance memory, increase ...
Dereplication of Aporphine Alkaloids by UHPLC-HR-ESI-MS/MS and NMR from Duguetia lanceolata St. -Hil (Annonaceae) and ... Additionally, it was also demonstrated the potential of aporphine alkaloids from Duguetia lanceolata St. -Hil (Annonaceae) in ... that were shown to be composed of aporphine alkaloids. 1H NMR analysis and UHPLC-HR-ESI-MS/MS based dereplication allowed the ...
Nuciferine, a major aporphine alkaloid constituent of lotus leaves, is a raw material for obesity treatment. Extensive studies ... Nuciferine, a major aporphine alkaloid constituent of lotus leaves, is a raw material for obesity treatment. Extensive studies ...
... and one aporphine alkaloid (magnoflorine) of Rhizoma coptidis as research goals (Fig. 1). ...
... dehydro derivatives of such simple aporphines, oxidative derivatives of such simple aporphines, aporphines with an aromatic ... Aporphine and oxoaporphine compounds and pharmaceutical use thereof US20050074510A1 (en) * 2003-10-04. 2005-04-07. Bobrowski ... Aporphine and oxoaporphine compounds and pharmaceutical use thereof US7057044B2 (en) * 2003-04-04. 2006-06-06. Lotus ... Aporphine and oxoaporphine compounds and pharmaceutical use thereof US20050074510A1 (en) * 2003-10-04. 2005-04-07. Bobrowski ...
... and a new aporphine-type alkaloid, hernovine were isolated. Hernovine, m.p. 143∼145° (sint. 130°), C18H15O4N, was proved to ...
Antioxidant and anticancer aporphine alkaloids from the leaves of Nelumbo nucifera Gaertn. cv. Rosa-plena. Molecules. 2014;19: ... Ma C, Wang J, Chu H, Zhang X, Wang Z, Wang H, Li G. Purification and Characterization of Aporphine Alkaloids from Leaves of ... Recent studies have revealed that the major constituents of AELL are aporphine alkaloids [49]. Nuciferine, a vital constituent ... of aporphine alkaloids, had a pharmacologic profile of action associated with arterial relaxation via suppressing extracellular ...
Aporphines. 48. Enantioselectivity of (R)-(-)- and (S)-(+)-N-n-propylnorapomorphine on dopamine receptors. J Med Chem. 1983 Apr ... Binding of [3H]apomorphine to an aporphine binding site as well as to dopamine sites in tissue from bovine caudate nucleus. ... Aporphines. 39. Synthesis, dopamine receptor binding, and pharmacological activity of (R)-(-)- and (S)-(+)-2-hydroxyapomorphine ... Aporphines, 36. Dopamine receptor interactions of trihydroxyaporphines. Synthesis, radioreceptor binding, and striatal ...
Our Blue Lotus 25x extract has a high concentration of aporphine and nuciferine content present. Blue Lotus has been used in ...
Dictionarypedia has 1,261 entries pertaining to words where the second letter is p and fourth letter is r. Find all 1,261 results here.
Kwan, T.K.; Shipton, F.; Nor Azman, N.S.; Hossan, S.; Jin, K.T.; Wiart, C. Cytotoxic aporphines from Artabotrys crassifolius. ...
Boldine and Related Aporphines: From Antioxidant to Antiproliferative Properties Darina Muthna, Jana Cmielova, Pavel Tomsik and ...
Inhibition of intestinal glucose uptake by aporphines and secoaporphines. CHUN-JUNG LIN ; Chen C.-H.; Liu F.-W.; Kang J.-J.; ...
The Aporphine alkaloid vaporizes at 125 degrees Celsius. When vaped the Blue lily It is sometimes combined with Damiana ... The other alkaloid is Aporphine which is more common in plants and is a non-selective dopamine agonist. ...
The aporphine alkaloid evaporates at 125 degrees Celsius.. Additional information. Gram. 500 G, 1000 G ...
Magnoflorine is an important aporphine alkaloid in Coptidis Rhizoma. As reported previously, coexisting components in Coptidis ...
Aporphine is an understudied alkaloid that is said to be psychoactive. Aporphine converts into apomorphine which then acts like ... On the other hand, blue Lotus contains Aporphine & Nuciferine. These alkaloids also account for the hypnotic and sedative ...
A set of dimeric aporphines with an aryloxy group at C8, C9, and C11 have been isolated from six genera and shown to elicit ... Aporphines, a major group of aporphinoid alkaloids, exhibit interesting and diverse pharmacological activities. ...
... and bisnorargemonine and the aporphine alkaloids corydine and isocorydine were isolated from the aerial part of the E. ...
It contains an anti-spasmotic called Nuciferin and contains aporphine. The history of this species says that is appears to a ...
His main work was on nucleic acids, morphine and aporphine alkaloids. His work at University College Nottingham on ...
Repurposing bioactive aporphine alkaloids as efflux pump inhibitors. Fitoterapia 2019, 139, 104371. [Google Scholar] [CrossRef ...
Anti-protozoal activity of aporphine and protoberberine alkaloids from Annickia kummeriae (Engl. & Diels) Setten & Maas ( ...
  • It is the core chemical substructure of the aporphine alkaloids, a subclass of quinoline alkaloids. (wikipedia.org)
  • For example, many water-lilies (Nymphaea species) produce aporphine alkaloids such as nymphaeine, nymphaline, nupharine, α- and β-nupharidine. (wikipedia.org)
  • Most aporphine alkaloids are toxic. (wikipedia.org)
  • We chose five isoquinoline alkaloids (berberine, coptisine, palmatine, jateorrhizine, epiberberine) and one aporphine alkaloid (magnoflorine) of Rhizoma coptidis as research goals (Fig. 1 ). (springer.com)
  • The pavinane alkaloids isonorargemonine, caryachine, norargemonine, and bisnorargemonine and the aporphine alkaloids corydine and isocorydine were isolated from the aerial part of the E. douglasii species for the first time. (cas.cz)
  • Anti-protozoal activity of aporphine and protoberberine alkaloids from Annickia kummeriae (Engl. (ac.ir)
  • As an aporphine alkaloid, it shares structural similarities with other alkaloids present in plants. (genominfo.org)
  • The psychoactive effects of the flower are attributed to two aporphine alkaloids, apomorphine and nuciferine. (lushiouslocsbyeuphoria.store)
  • Oregon grape contains isoquinoline alkaloids (including berberine, berbamine, and hydrastine) and other alkaloids of aporphine-type. (herbsandremedies.club)
  • The psychoactive effects of Blue Lotus can be attributed to the presence of alkaloids such as aporphine, and nuciferine. (lotus-factory.com)
  • They were interested in synthesising some of the aporphine alkaloids which are biosynthetic derivatives of isoquinoline alkaloids and can be found in several families of plants and have interesting and important pharmacological properties. (mickel.ch)
  • APORPHINE ALKALOIDS OF LITSEA ROTUNDIFOLIA AND L. The download Grundkurs Geschäftsprozess Management: Methoden und Werkzeuge für die IT of this link sent to find the discriminatory Prophecy of educational sentiments and Zimbabwean patients basic as fawn on the prosthetic and image, tool information, chemical and research injustice site parallel events of many event Reviews. (marvelit.com)
  • The relaxation impacts of Blue Lotus are famous and is highly recommended before sleep thanks to aporphine, nuciferine and natural alkaloids contained within. (hibiscusteahouse.com)
  • blue lotus oil contains the two primary alkaloids nuciferine and aporphine, which are believed to have relaxing and mood-enhancing effects. (purebluelotusoil.com)
  • The alkaloids found in the oil, particularly nuciferine and aporphine, are believed to interact with the brain's dopamine and serotonin receptors, which can help to elevate mood and reduce negative feelings. (purebluelotusoil.com)
  • Other bioactive compounds from Magnolia Bark are the alkaloids benzyl-tetrahydroisoquinoline and aporphine which are found in the leaves, branches and bark. (nootropicsexpert.com)
  • Furthermore, morphine-based natural products can be heated in acid to give aporphine degradation products, like the FDA-approved Parkinson's drug apomorphine, which was first discovered by the Finnish chemist Arppe in 1845. (wikipedia.org)
  • A specific type of aporphine is apomorphine. (wikipedia.org)
  • These include apomorphine by Neumeyer and Raminelli, Pukateine by Happel, Isocorydine by Di, Nuciferine and Oliveroline by Cuny, Glaucine by Meyers, Dicentrine by Cava, and Lysicamine by Raminelli, and an overview of some of the synthetic approaches toward the aporphine ring system is outlined in the figure at the right. (wikipedia.org)
  • Aporphine converts into apomorphine which then acts like dopamine in the body. (redstormscientific.com)
  • Nuciferine and Aporphine, which work on the dopamine system to engender feelings of pleasure and possibility. (awepothecary.com)
  • Aporphine is a dopamine receptor agonist, specifically D1 and D2. (wikipedia.org)
  • In vitro tests of some aporphine derivatives isolated from Cassytha filiformis, namely actinodaphnine, cassythine, and dicentrine, showed antiparasitic activity against Trypanosoma brucei. (wikipedia.org)
  • Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT2C receptor. (harvard.edu)
  • Aporphine can be synthesized in a seven-step reaction. (wikipedia.org)
  • Aporphine natural products occur with either the (R)- or (S)-stereochemistries, or they can be achiral. (wikipedia.org)
  • A number of natural products semisynthetic analogs belonging to the aporphine class have been synthesized. (wikipedia.org)
  • These include apomorphine by Neumeyer and Raminelli, Pukateine by Happel, Isocorydine by Di, Nuciferine and Oliveroline by Cuny, Glaucine by Meyers, Dicentrine by Cava, and Lysicamine by Raminelli, and an overview of some of the synthetic approaches toward the aporphine ring system is outlined in the figure at the right. (wikipedia.org)
  • Nuciferine and Aporphine, which work on the dopamine system to engender feelings of pleasure and possibility. (awepothecary.com)
  • Aporphine is a dopamine receptor agonist, specifically D1 and D2. (wikipedia.org)
  • In the past few decades, aporphine has attracted continuing interest to be widely used to develop selective or multitarget directed ligands (MTDLs) targeting the CNS (e.g., dopamine D1/2/5, serotonin 5-HT1A/2A/2C and 5-HT7, adrenergic α/ß receptors, and cholinesterase enzymes), thereby serving as valuable pharmacological probes for mechanism studies or as potential leads for CNS drug discovery. (bvsalud.org)
  • They found that two of these compounds - an isoquinoline derivative called A5 and an aporphine derivative called C1 - reduced the viability of glioblastoma cells, suppressed the formation of new tumor stem cells and boosted the effectiveness of temozolomide. (fapesp.br)
  • Discovery of Aporphine Analogues as Potential Antiplatelet and Antioxidant Agents: Design, Synthesis, Structure-Activity Relationships, Biological Evaluations, and in silico Molecular Docking Studies. (nih.gov)
  • Aporphine is a privileged scaffold in the field of organic synthesis and medicinal chemistry for the discovery of new therapeutic agents for central nervous system (CNS) diseases, cancer, metabolic syndrome, and other diseases. (bvsalud.org)
  • Aporphine natural products occur with either the (R)- or (S)-stereochemistries, or they can be achiral. (wikipedia.org)
  • A number of natural products semisynthetic analogs belonging to the aporphine class have been synthesized. (wikipedia.org)
  • In continued efforts to understand the impacts of structural modification of the 1,2,9,10-tetraoxygenated aporphine template on affinity, selectivity, and activity at 5-HT2R subtypes, we used (+)-boldine (8) as a semisynthetic feedstock in the preparation of C-2-alkoxylated (+)-predicentrine analogues. (bvsalud.org)