Twenty-carbon compounds derived from MEVALONIC ACID or deoxyxylulose phosphate.
A group of DITERPENES cyclized into 3-ring PHENANTHRENES.
A group of DITERPENES cyclized into 2-rings with a side-chain.
A group of DITERPENES cyclized into four rings.
A large plant genus of the family EUPHORBIACEAE, order Euphorbiales, subclass Rosidae. They have a milky sap and a female flower consisting of a single pistil, surrounded by numerous male flowers of one stamen each. Euphorbia hirta is rarely called milkweed but that name is normally used for ASCLEPIAS.
A plant genus of the family FABACEAE. The common name of "Bird-Of-Paradise" is also used for other plants such as Heliconia (HELICONIACEAE) and Strelitzia (STRELITZIACEAE) and some birds. The common name of "Cat's-Claw" is more often used with UNCARIA. The common name of "Pernambuco" also refers to a state in Brazil. Furanoditerpenoid lactones and caesalpin are produced by members of this genus.
A genus in the mint family (LAMIACEAE).
A plant family of the order Lamiales, subclass Asteridae, class Magnoliopsida. The leaves are opposite or whorled. The flowers are aggregated in spikes, clusters, or racemes.
A plant genus of the family CUPRESSACEAE which should not be confused with other cedar and cypress trees of THUJA or CUPRESSUS genera.
A plant genus of the family CISTACEAE. The common name of rock rose is also sometimes used with the closely related Helianthemum genus (CISTACEAE).
A plant family of the order Pinales, class Pinopsida, division Coniferophyta (conifers). They are mainly resinous, aromatic evergreen trees.
The outer layer of the woody parts of plants.
A plant genus of the family LAMIACEAE that contains pimarane-type diterpenes. Several species of Orthosiphon are also called Java tea.
A plant genus of the family ANNONACEAE. Members contain 8-oxopolyalthiaine.
A plant family of the order Myrtales, subclass Rosidae, class Magnoliopsida. They are mainly trees and shrubs. Many members contain mucilage and COUMARINS.
A plant genus of the family ASTERACEAE. Members contain scandenolide (a sesquiterpene lactone) and germacranolides.
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.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
The above-ground plant without the roots.
A plant genus of the family CUPRESSACEAE.
A class in the phylum CNIDARIA, comprised mostly of corals and anemones. All members occur only as polyps; the medusa stage is completely absent.
A plant genus of the family TAXODIACEAE. Its POLLEN is one of the major ALLERGENS.
A plant genus in the family CAPRIFOLIACEAE. The common name derives from its traditional use for menstrual cramps. It is a source of viburnine, valerianic acid, vibsanin, and ursolic acid. Note that true cranberry is VACCINIUM MACROCARPON.
SESQUITERPENES cyclized into two adjoining rings, one being 7-carbons and the other is 5-carbons.
A plant genus of the family FLACOURTIACEAE. Members contain casearins which are clerodane type DITERPENES.
A plant genus of the family Plantaginaceae. Members contain thyrsiflorin and other scopadulane (labdane) type DITERPENES.
A class of compounds composed of repeating 5-carbon units of HEMITERPENES.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
A plant species of the Salvia genus known as a spice and medicinal plant.
A plant family of the order Ranunculales, subclass Magnoliidae, class Magnoliopsida. Members are mostly vines and shrubs and they contain isoquinoline alkaloids, some of which have been used as arrow poisons.
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.
Flammable, amorphous, vegetable products of secretion or disintegration, usually formed in special cavities of plants. They are generally insoluble in water and soluble in alcohol, carbon tetrachloride, ether, or volatile oils. They are fusible and have a conchoidal fracture. They are the oxidation or polymerization products of the terpenes, and are mixtures of aromatic acids and esters. Most are soft and sticky, but harden after exposure to cold. (From Grant & Hackh's Chemical Dictionary, 5th ed & Dorland, 28th ed)
The figwort plant family of the order Lamiales. The family is characterized by bisexual flowers with tubular corollas (fused petals) that are bilaterally symmetrical (two-lips) and have four stamens in most, two of which are usually shorter.
A division of predominantly marine EUKARYOTA, commonly known as brown algae, having CHROMATOPHORES containing carotenoid PIGMENTS, BIOLOGICAL. ALGINATES and phlorotannins occur widely in all major orders. They are considered the most highly evolved algae because of their well-developed multicellular organization and structural complexity.
A plant genus of the family LILIACEAE. Members of this genus produce imperialine, a steroidal alkaloid which acts at muscarinic receptors.
A genus of trees in the Lamiaceae family containing assorted flavonoids with possible analgesic and antineoplastic properties. The fruit of these trees is used in herbal preparations.
A plant division. They are simple plants that lack vascular tissue and possess rudimentary rootlike organs (rhizoids). Like MOSSES, liverworts have alternation of generations between haploid gamete-bearing forms (gametophytes) and diploid spore-bearing forms (sporophytes).
A plant genus in the family PINACEAE, order Pinales, class Pinopsida, division Coniferophyta.
A plant genus of the family ARISTOLOCHIACEAE. Species of this genus have been used in traditional medicine but they contain aristolochic acid which is associated with nephropathy. These are sometimes called 'snakeroot' but that name is also used with a number of other plants such as POLYGALA; SANICULA; ASARUM; ARISTOLOCHIA; AGERATINA; and others.
The characteristic three-dimensional shape of a molecule.
A plant genus of the LAMIACEAE family. It is known as a spice and medicinal plant.
A large plant family of the order Asterales, subclass Asteridae, class Magnoliopsida. The family is also known as Compositae. Flower petals are joined near the base and stamens alternate with the corolla lobes. The common name of "daisy" refers to several genera of this family including Aster; CHRYSANTHEMUM; RUDBECKIA; TANACETUM.
A mass spectrometric technique that is used for the analysis of a wide range of biomolecules, such as glycoalkaloids, glycoproteins, polysaccharides, and peptides. Positive and negative fast atom bombardment spectra are recorded on a mass spectrometer fitted with an atom gun with xenon as the customary beam. The mass spectra obtained contain molecular weight recognition as well as sequence information.
A plant genus of the family EUPHORBIACEAE. The common name of dragon's blood is also used for DRACAENA and Daemonorops (ARECACEAE). Croton tiglium is the source of CROTON OIL.
A beverage made from ground COFFEA beans (SEEDS) infused in hot water. It generally contains CAFFEINE and THEOPHYLLINE unless it is decaffeinated.
Spectrophotometry in the infrared region, usually for the purpose of chemical analysis through measurement of absorption spectra associated with rotational and vibrational energy levels of molecules. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A product of hard secondary xylem composed of CELLULOSE, hemicellulose, and LIGNANS, that is under the bark of trees and shrubs. It is used in construction and as a source of CHARCOAL and many other products.
Expanded structures, usually green, of vascular plants, characteristically consisting of a bladelike expansion attached to a stem, and functioning as the principal organ of photosynthesis and transpiration. (American Heritage Dictionary, 2d ed)
A republic stretching from the Indian Ocean east to New Guinea, comprising six main islands: Java, Sumatra, Bali, Kalimantan (the Indonesian portion of the island of Borneo), Sulawesi (formerly known as the Celebes) and Irian Jaya (the western part of New Guinea). Its capital is Djakarta. The ethnic groups living there are largely Chinese, Arab, Eurasian, Indian, and Pakistani; 85% of the peoples are of the Islamic faith.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Parts of plants that usually grow vertically upwards towards the light and support the leaves, buds, and reproductive structures. (From Concise Dictionary of Biology, 1990)
Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.
Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Any compound that contains a constituent sugar, in which the hydroxyl group attached to the first carbon is substituted by an alcoholic, phenolic, or other group. They are named specifically for the sugar contained, such as glucoside (glucose), pentoside (pentose), fructoside (fructose), etc. Upon hydrolysis, a sugar and nonsugar component (aglycone) are formed. (From Dorland, 28th ed; From Miall's Dictionary of Chemistry, 5th ed)
Substances that are destructive to protozoans.
Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
The usually underground portions of a plant that serve as support, store food, and through which water and mineral nutrients enter the plant. (From American Heritage Dictionary, 1982; Concise Dictionary of Biology, 1990)
A somewhat heterogeneous class of enzymes that catalyze the transfer of alkyl or related groups (excluding methyl groups). EC 2.5.

Antagonistic effects of extract from leaves of ginkgo biloba on glutamate neurotoxicity. (1/2175)

AIM: To determine whether the extract of leaves of Ginkgo biloba L (EGb) and several active constituents of EGb have protective effects against glutamate (Glu)-induced neuronal damage. METHODS: Microscopy and image analysis of nucleus areas in the arcuate nuclei (AN) of mice were made. The neuronal viability in primary cultures from mouse cerebral cortex was assessed using MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] staining and the intracellular free calcium concentration ([Ca2+]i) of single neuron was measured using Fura-2. RESULTS: EGb (2.5 mg.L-1) and its constituent ginkgolide B (Gin B, 2 mg.L-1) protected the neuronal viability against Glu-induced injury, and prevented the Glu-induced elevation in [Ca2+]i. EGb (3-10 mg.kg-1) attenuated the decrease of nucleus areas in arcuate nuclei induced by Glu (1 g.kg-1, s.c.). CONCLUSION: EGb and Gin B prevent neurons from Glu neurotoxicity through reduction of the rise in [Ca2+]i.  (+info)

A common pharmacophore for cytotoxic natural products that stabilize microtubules. (2/2175)

Taxol (paclitaxel), a complex diterpene obtained from the Pacific yew, Taxus brevifolia, is arguably the most important new drug in cancer chemotherapy. The mechanism of cytotoxic action for paclitaxel-i.e., the stabilization of microtubules leading to mitotic arrest-is now shared by four recently identified natural products, eleutherobin, epothilones A and B, and discodermolide. Their ability to competitively inhibit [3H]paclitaxel binding to microtubules strongly suggests the existence of a common binding site. Recently, we have developed nonaromatic analogues of paclitaxel that maintain high cytotoxicity and tubulin binding (e.g., nonataxel). We now propose a common pharmacophore that unites paclitaxel, nonataxel, the epothilones, eleutherobin, and discodermolide, and rationalizes the extensive structure-activity relationship data pertinent to these compounds. Insights from the common pharmacophore have enabled the development of a hybrid construct with demonstrated cytotoxic and tubulin-binding activity.  (+info)

On the complexities of ceramide changes in cells undergoing apoptosis: lack of evidence for a second messenger function in apoptotic induction. (3/2175)

The generation of cellular ceramides as a second messenger has been implicated as a regulatory and required step for the induction of apoptosis. In this study, we have applied a recently developed mass spectrometric technique to the determination of changes in physiological ceramide levels during apoptosis induced by tumor necrosis factor plus cycloheximide in U937 cells and the chemical agents anisomycin or geranylgeraniol in HL-60 cells. The mass spectrometric method has significant advantages over traditional methods for ceramide quantitation in that it determines the relative abundance of all ceramide species present in complex biological lipid mixtures individually and simultaneously. We quantitiated ceramides ranging from C14 to C26, finding that their basal levels and relative distribution varied significantly, both within and between different cell types. However, we were not able to detect any significant changes in either total ceramide content or species distribution until 1 h or more post-stimulation with any of these treatments, by which time the cells were in an advanced stage of apoptosis. Differences were also seen between all three treatments in the ceramide species distribution observed in these late stages of apoptosis. These data indicate that in vivo ceramide generation occurs as a consequence of apoptosis rather than as an essential second messenger involved in its induction. They also pose new questions about the potential roles that certain ceramide species may play in the late stages of apoptosis, and demonstrate a clear need to utilize the resolving power of mass spectrometry-based assays in any future investigations into the biological function of ceramides.  (+info)

Inhibition of GABA-gated chloride channels by 12,14-dichlorodehydroabietic acid in mammalian brain. (4/2175)

1. 12,14-dichlorodehydroabietic acid (12,14-Cl2DHA) reduced GABA-stimulated uptake of 36Cl- into mouse brain synaptoneurosomes suggesting inhibition of mammalian GABA(A) receptor function. 2. 12,14-Cl2DHA did not affect the binding of [3H]-muscimol to brain membranes but displaced specifically bound [3H]-EBOB. The inhibitory effect on [3H]-EBOB binding was not reversible. 12,14-Cl2DHA reduced the availability of [3H]-EBOB binding sites (Bmax) without changing the KD of the radioligand for remaining sites. 12,14-Cl2DHA did not affect the rate of association of [3H]-EBOB with its chloride channel receptor, but increased the initial rate of [3H]-EBOB dissociation. 3. 12,14-Cl2DHA enhanced the incidence of EPSCs when rapidly applied to cultured rat cortical neurones. Longer exposures produced block of IPSCs with marked increases in the frequency of EPSCs and min EPSCs. 12,14-Cl2DHA also irreversibly suppressed chloride currents evoked by pulses of exogenous GABA in these cells. 4. Ultimately, 12,14-Cl2DHA inhibited all synaptic traffic and action currents in current clamped cells indicating that, in contrast to picrotoxinin (which causes paroxysmal bursting), it is not fully selective for the GABA(A) receptor-chloride channel complex. 5. The depolarizing block seen with 12,14-Cl2DHA in amphotericin-perforated preparations implicates loss of Ca2+ buffering in the polarity change and this may account for inhibition of spontaneous action potentials. 6. Our investigation demonstrates that 12,14-Cl2DHA blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive insurmountable GABA(A) antagonist. The mechanism likely involves either irreversible binding of 12,14-Cl2DHA to the trioxabicyclooctane recognition site or a site that is allosterically coupled to it. We cannot exclude, however, the possibility that 12,14-Cl2DHA causes localized proteolysis or more extensive conformational change within a critical subunit of the chloride channel.  (+info)

A non-pungent triprenyl phenol of fungal origin, scutigeral, stimulates rat dorsal root ganglion neurons via interaction at vanilloid receptors. (5/2175)

1. A [3H]-resiniferatoxin (RTX) binding assay utilizing rat spinal cord membranes was employed to identify novel vanilloids in a collection of natural products of fungal origin. Of the five active compounds found (scutigeral, acetyl-scutigeral, ovinal, neogrifolin, and methyl-neogrifolin), scutigeral (Ki=19 microM), isolated from the edible mushroom Albatrellus ovinus, was selected for further characterization. 2. Scutigeral induced a dose-dependent 45Ca uptake by rat dorsal root ganglion neurons with an EC50 of 1.6 microM, which was fully inhibited by the competitive vanilloid receptor antagonist capsazepine (IC50=5.2 microM). 3. [3H]-RTX binding isotherms were shifted by scutigeral (10-80 microM) in a competitive manner. The Schild plot of the data had a slope of 0.8 and gave an apparent Kd estimate for scutigeral of 32 microM. 4. Although in the above assays scutigeral mimicked capsaicin, it was not pungent on the human tongue up to a dose of 100 nmol per tongue, nor did it provoke protective wiping movements in the rat (up to 100 microM) upon intraocular instillation. 5. In accord with being non-pungent, scutigeral (5 microM) did not elicit a measurable inward current in isolated rat dorsal root ganglion neurons under voltage-clamp conditions. It did, however, reduce the proportion of neurons (from 61 to 15%) that responded to a subsequent capsaicin (1 microM) challenge. In these neurons, scutigeral both delayed (from 27 to 72 s) and diminished (from 5.0 to 1.9 nA) the maximal current evoked by capsaicin. 6. In conclusion, scutigeral and its congeners form a new chemical class of vanilloids, the triprenyl phenols. Scutigeral promises to be a novel chemical lead for the development of orally active, non-pungent vanilloids.  (+info)

A novel aromatic-ring-hydroxylating dioxygenase from the diterpenoid-degrading bacterium Pseudomonas abietaniphila BKME-9. (6/2175)

Pseudomonas abietaniphila BKME-9 is able to degrade dehydroabietic acid (DhA) via ring hydroxylation by a novel dioxygenase. The ditA1, ditA2, and ditA3 genes, which encode the alpha and beta subunits of the oxygenase and the ferredoxin of the diterpenoid dioxygenase, respectively, were isolated and sequenced. The ferredoxin gene is 9. 2 kb upstream of the oxygenase genes and 872 bp upstream of a putative meta ring cleavage dioxygenase gene, ditC. A Tn5 insertion in the alpha subunit gene, ditA1, resulted in the accumulation by the mutant strain BKME-941 of the pathway intermediate, 7-oxoDhA. Disruption of the ferredoxin gene, ditA3, in wild-type BKME-9 by mutant-allele exchange resulted in a strain (BKME-91) with a phenotype identical to that of the mutant strain BKME-941. Sequence analysis of the putative ferredoxin indicated that it is likely to be a [4Fe-4S]- or [3Fe-4S]-type ferredoxin and not a [2Fe-2S]-type ferredoxin, as found in all previously described ring-hydroxylating dioxygenases. Expression in Escherichia coli of ditA1A2A3, encoding the diterpenoid dioxygenase without its putative reductase component, resulted in a functional enzyme. The diterpenoid dioxygenase attacks 7-oxoDhA, and not DhA, at C-11 and C-12, producing 7-oxo-11, 12-dihydroxy-8,13-abietadien acid, which was identified by 1H nuclear magnetic resonance, UV-visible light, and high-resolution mass spectrometry. The organization of the genes encoding the various components of the diterpenoid dioxygenase, the phylogenetic distinctiveness of both the alpha subunit and the ferredoxin component, and the unusual Fe-S cluster of the ferredoxin all suggest that this enzyme belongs to a new class of aromatic ring-hydroxylating dioxygenases.  (+info)

Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-kappaB transcriptional activation. (7/2175)

PG490 (triptolide) is a diterpene triepoxide with potent immunosuppressive and antiinflammatory properties. PG490 inhibits interleukin(IL)-2 expression by normal human peripheral blood lymphocytes stimulated with phorbol 12-myristate 13-acetate (PMA) and antibody to CD3 (IC50 of 10 ng/ml), and with PMA and ionomycin (Iono, IC50 of 40 ng/ml). In Jurkat T-cells, PG490 inhibits PMA/Iono-stimulated IL-2 transcription. PG490 inhibits the induction of DNA binding activity at the purine-box/antigen receptor response element (ARRE)/nuclear factor of activated T-cells (NF-AT) target sequence but not at the NF-kappaB site. PG490 can completely inhibit transcriptional activation at the purine-box/ARRE/NF-AT and NF-kappaB target DNA sequences triggered by all stimuli examined (PMA, PMA/Iono, tumor necrosis factor-alpha). PG490 also inhibits PMA-stimulated activation of a chimeric transcription factor in which the C-terminal TA1 transactivation domain of NF-kappaB p65 is fused to the DNA binding domain of GAL4. In 16HBE human bronchial epithelial cells, IL-8 expression is regulated predominantly by NF-kappaB, and PG490 but not cyclosporin A can completely inhibit expression of IL-8. The mechanism of PG490 inhibition of cytokine gene expression differs from cyclosporin A and involves nuclear inhibition of transcriptional activation of NF-kappaB and the purine-box regulator operating at the ARRE/NF-AT site at a step after specific DNA binding.  (+info)

PG490 (triptolide) cooperates with tumor necrosis factor-alpha to induce apoptosis in tumor cells. (8/2175)

Progress in the treatment of solid tumors has been slow and sporadic. The efficacy of conventional chemotherapy in solid tumors is limited because tumors frequently have mutations in the p53 gene. Also, chemotherapy only kills rapidly dividing cells. Members of the tumor necrosis factor (TNF) family, however, induce apoptosis regardless of the p53 phenotype. Unfortunately, the cytotoxicity of TNF-alpha is limited by its activation of NF-kappaB and activation of NF-kappaB is proinflammatory. We have identified a compound called PG490, that is composed of purified triptolide, which induces apoptosis in tumor cells and sensitizes tumor cells to TNF-alpha-induced apoptosis. PG490 potently inhibited TNF-alpha-induced activation of NF-kappaB. PG490 also blocked TNF-alpha-mediated induction of c-IAP2 (hiap-1) and c-IAP1 (hiap-2), members of the inhibitor of apoptosis (IAP) family. Interestingly, PG490 did not block DNA binding of NF-kappaB, but it blocked transactivation of NF-kappaB. Our identification of a compound that blocks TNF-alpha-induced activation of NF-kappaB may enhance the cytotoxicity of TNF-alpha on tumors in vivo and limit its proinflammatory effects.  (+info)

Two new briarane diterpenoids, briarenolides, F (1) and G (2), were isolated from an octocoral identified as Briareum sp. The structures of briaranes 1 and 2 were established by spectroscopic methods and by comparison of the spectroscopic data with those of known briarane analogues. Briarenolide F was proven to be the first 6-hydroperoxybriarane derivative and this compound displayed a significant inhibitory effect on the generation of superoxide anion by human neutrophils.
Two new eunicellin-based diterpenes, seco-briarellinone (1) and briarellin S (2), and a known seco-asbestinin (3) have been isolated from the methanolic extract of the common octocoral Briareum asbestinum collected in Bocas del Toro, Caribbean of Panama. The structures and relative stereochemistry of the compounds were defined using extensive spectroscopic analysis including 1D, 2D-nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). Compounds 1 and 2 displayed anti-inflammatory properties inhibiting nitric oxide (NO) production induced by lipopolisacharide (LPS) in macrophages with an Inhibitory concentration 50% (IC50) of 4.7 μM and 20.3 μM, respectively. This is the first report of briarellin diterpenes containing a ketone group at C-12.
Geranylgeranylacetone (GGA) derivatives induce HSP70 expression and reveal cardioprotective effects. a Western blot showing induction of HSP70 levels in HL-1 ca
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Topical application of marine briarane-type diterpenes effectively inhibits 12-O-tetradecanoylphorbol-13-acetate-induced inflammation and dermatitis in murine skin. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
A fresh prenyleudesmane type diterpene, sinupol (8), and a fresh capnosane type diterpenoid, sinulacetate (9), were isolated in the Xisha soft coral along with five known related diterpenes (4C7 and 10). uncovered the wealthy chemical diversity of the biological materials and resulted in the breakthrough of three unusual book diterpenes with unparalleled carbon skeletons (1C3) [3] exhibiting a fascinating dose-dependent promotion influence on ConA-induced T lymphocyte proliferation. Stimulated by this breakthrough, and and discover even more R1626 interesting and biologically energetic metabolites chemically, trace components especially, we recently completed Rabbit Polyclonal to Fibrillin-1 a further chemical substance investigation from the Et2O-soluble small percentage of the name animal. This analysis led to the isolation and characterization of a fresh prenyleudesmane diterpene, sinupol (8), and a fresh capnosane diterpene, sinulacetate (9), as well as five known related diterpenoids R1626 ...
This invention relates resiniferatoxin derivatives useful in a vanilloid receptor binding assay and methods for production thereof.
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Divergent synthesis and chemical reactivity of bicyclic lactone fragments of complex rearranged spongian diterpenes.: The synthesis and direct comparison of the
Abstract:. This review explores the mechanisms of cytotoxic and anti‑inflammatory properties of andrographolide and derivatives of andrographolide in various cell lines. In vitro and in vivo studies that shed light on the molecular mechanisms of cytotoxicity and anti‑inflammatory property of andrographolide and its derivatives are reviewed here. Cytotoxic effect of andrographolide on cancer cell lines are mainly due to the induction of reactive oxygen species, activation of c‑Jun N‑terminal kinase, inhibition of autophagy, and induction of apoptosis. Anti‑inflammatory effect of andrographolide is predominantly due to the covalent inhibition of nuclear factor kappa B transcription factor and thereby inhibition of various targets genes such as tumor necrosis factor‑alpha, interleukin‑6, macrophage inflammatory protein‑2, and nitric oxide synthase. Andrographolide is known to directly bind Ras protein; therefore, inhibition of growth factor‑activated downstream pathways such as ...
Picroliv (active principle from Picrorrhiza kurroa) with major chemical constituent of andrographolide (active constituent of Andrographis paniculata) was tested in HBsAg positive serum samples obtained from hepatitis B virus (HBV) associated acute and chronic liver diseases and healthy HBsAg paitnets, found that Picroliv also inhibited purified HBV antigens (HBsAg and HBsAg) prepared from healthy HBsAg carriers amd may be considered as a potential agent against HBV. In anti-hepatitis C virus (HCV) study of andrographolide, a diterpenoid lactone extracted from Andrographis paniculata, reseachers found that activated p38 MAPK phosphorylation, which stimulated nuclear factor erythroid 2-related factor 2 (Nrf2)-mediated HO-1 expression, and this was found to be associated with its anti-HCV activity. Other in the study of infective hepatitis, Kalmegh(Andrographis paniculata Nees)showed as a promised agent as on the total assessment 80% cases of this series were cured and 20% patients were relieved ...
Coral Symbiodiniaceae and bacteria maintain a symbiotic relationship that is essential for coral survival. The symbiotic communities component in the polyps host could affect coral resistance and the ability to recover from stress. In this study, we increased the cultured range temperature (26 ± 1 ℃) of Sarcophyton trocheliophorum and Euphyllia ancora at 32 ℃ for 12 hours, and then amplified the ITS2 sequence of Symbiodinium and the bacterial 16S rRNA sequence in the sample, respectively to compare Symbiodiniaceae and bacteria diversity and abundance with normal culture temperature. The results showed that there was no change in the dominant species of Symbiodinium in these two corals in the heat treatment group, but the diversity of Symbiodinium in the two corals was significantly different. On the other hand, after thermal treatment, the endophytic bacteria of S. trocheliophorum represented more aerobic bacteria Delfitia, while the E. ancora was infected with more pathogenic endosymbiotic
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A pilot study using drug-resistant cancer cells in cell cultures and in mice has found that the compounds kahweol acetate and cafestol in coffee may inhibit the growth of prostate cancer. The results were presented at the European Association of Urology congress in Barcelona and published in The Prostate.
Geranylgeranylacetone (GGA), an anti-ulcer drug widely used in Japan, has attracted interest because of its various therapeutic effects. Therefore, we investigated the effects of GGA on human hepatic stellate cells (HSCs) in vitro and in a mouse model of liver fibrosis. LX2, an immortalized human HSC line, was cultured and treated with GGA at concentrations up to 0.5 mM. After GGA treatment, changes in cellular morphology, apoptosis, and fibrosis-related gene expression were assessed. Male C57BL/6 J mouse model of carbon tetrachloride (CCl4)-induced liver fibrosis was treated with GGA. Liver fibrosis was evaluated using Sirius red staining and immunohistochemistry for α-smooth muscle actin (SMA). GGA decreased the density of LX2 and primary human hepatic stellate cells but not that of HepG2 cells (a human hepatoma cell line), which was employed as control. In addition, GGA decreased the expression of fibrogenic genes and increased that of C/EBP homologous protein (CHOP). It also induced endoplasmic
Sigma-Aldrich offers abstracts and full-text articles by [Yan Guan, Jiuyun Zhang, Changzhong Wang, Ning Wang, Zhifang Liu, Jingjin Shi].
We know that, Resiniferatoxin (RTX) is a naturally occurring, ultrapotent capsaicin analog that activates the vanilloid receptor in a subpopulation of primary afferent sensory neurons involved in nociception (the transmission of physiological pain). RTX causes an ion channel in the plasma membrane of sensory neurons - the transient receptor potential vanilloid 1 - to become permeable to cations, most particularly the calcium cation; this evokes a powerful irritant effect followed by desensitization and analgesia. Research is being conducted at the National Institutes of Health and the University of Pennsylvania to design a novel class of analgesics from the latex of resin spurge (Euphorbia resinifera), a cactus-like plant commonly found in Morocco that contains high concentrations of RTX. Resiniferatoxin has a rating of 16,000,000,000 on the Scoville Scale making it one of the highest rated substances known. ...
Pseudopterosin A is a diterpene glycoside isolated from the gorgian sea whip Pseudopterogorgia elisabethae, found in the Bahamas and Florida Keys. Pseudopterosins A-D, which differ in the degree of acetylation at the sugar ring, were first isolated and reported in 1986. There are at least 25 unique diterpenes isolated from this species of marine animal. Samples of P. elisabethae from the Bahamas are found to have higher concentrations of pseudopterosins than populations from the Florida Keys, which have a greater diversity in diterpene structures. Pseudopterosins have anti-inflammatory and analgesic activity, with a mechanism of action different from the common non-steroidal anti-inflammatory drugs, NSAIDs. Commercially, pseudopterosins are found in skin creams as topical anti-inflammatory agents. Elisabethatriene (2) has been identified as a key intermediate for the synthesis of the class of pseudopterosins and seco-pseudopterosins. A proposed mechanistic pathway for the synthesis of ...
Andrographolide and DDAG are biologically active compounds. Unlike andrographolide, DDAG are not cytotoxic to A549, BEAS-2B and RBL-2H3 cells. DDAG dose-dependently inhibited OVA-induced increases in total cell counts and eosinophil counts, IL-4, IL-5, and IL-13 levels in lavage fluid and serum OVA-specific IgE level in a mouse asthma model. Additionally, DDAG attenuated mucus production, mast cell degranulation, pro-inflammatory biomarker expression in lung tissues and AHR in mice. DDAG also blocked p65 nuclear translocation and DNA-binding activity in the OVA-challenged lung and in TNF-a -stimulated cells. Andrographolide suppressed cigarette smoke-induced increases in BAL fluid cell counts, levels of IL-1?, MCP-1, IP-10 and KC and levels of oxidative biomarkers but promoted GPx and GR activities. In BEAS-2B cells, andrographolide markedly increased nuclear Nrf2 accumulation, promoted binding to ARE and total cellular glutathione level in response to CSE. Andrographolide up-regulated GCLC, ...
Andrographolide, a chief component of the leaves of Andrographis paniculata has been found to be gastroprotective effects as its antioxidants and mucin levels were significantly maintained in the gastric tissue of drug-pretreated animals with toxic effects in normal rats. hydroalcoholic extract of Andrographis paniculata (HAEAP), another chemical compound of Andrographis, has also exerted its overprotective effect by regulating effect on H(+)K(+)ATPase activity and /or mucin preserving effects and flavonoids presence in maintaining the antioxidants and thiol status in the gastrointestinal tract ...
Andrographolide, a chief component of the leaves of Andrographis paniculata has been found to be gastroprotective effects as its antioxidants and mucin levels were significantly maintained in the gastric tissue of drug-pretreated animals with toxic effects in normal rats. hydroalcoholic extract of Andrographis paniculata (HAEAP), another chemical compound of Andrographis, has also exerted its overprotective effect by regulating effect on H(+)K(+)ATPase activity and /or mucin preserving effects and flavonoids presence in maintaining the antioxidants and thiol status in the gastrointestinal tract ...
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TY - JOUR. T1 - Structure-activity profiles of eleutherobin analogs and their cross- resistance in Taxol-resistant cell lines. AU - McDaid, Hayley M.. AU - Bhattacharya, Samit K.. AU - Chen, Xiao Tao. AU - He, Lifeng. AU - Shen, Heng Jia. AU - Gutteridge, Clare E.. AU - Horwitz, Susan Band. AU - Danishefsky, Samuel J.. N1 - Funding Information: This research was supported by grants from the National Institutes of Health (CA 39821 to S.B.H and CA 28824 to S.J.D.) H.M. McDaid á L. He á H.-J. Shen á S.B. Horwitz (&) Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, USA Tel. +1-718-430-2163; Fax +1-718-430-8922. PY - 1999. Y1 - 1999. N2 - Purpose: Eleutherobin, a natural product, is an antimitotic agent that promotes the polymerization of stable microtubules. Although its mechanism of action is similar to that of Taxol, its structure is distinct. A structure- activity profile of synthetic eleutherobin derivatives that have ...
Diterpenes are a class of chemical compounds composed of two terpene units with the molecular formula C20H32; they may also be thought of as consisting of four isoprene units. They are biosynthesized by plants, animals and fungi via the HMG-CoA reductase pathway, with geranylgeranyl pyrophosphate being a primary intermediate. Diterpenes form the basis for biologically important compounds such as retinol, retinal, and phytol. They are known to be antimicrobial and antiinflammatory. As with most terpenes a huge number of potential structures exists, which may be broadly divided according to the number of rings present. Diterpenes are formally defined as being hydrocarbons and thus contain no heteroatoms. Functionalized structures should instead be called diterpenoids[citation needed], although in scientific literature the two terms are often used interchangeably. Although a wide range of terpene structures exist few of them are biologically significant, by contrast diterpenoids possess a rich ...
Andrographolide (AGL) is a labdane diterpenoid that has been isolated from the stem and leaves of Andrographis paniculata. In Ayurvedic tradition, Andrographis, commonly known as Kalmegh or King of Bitters has long been used as a bitter tonic, to promote digestion and appetite. Recently, there are many reports that have findings on anti-inflammatory and cytotoxic activites of AGL. This motivated us to carry out this study, in which we aimed at investigating the anti-apoptotic potential of AGL with special emphasis on breast cancer. One of the major anti-apoptotic proteins that are found to be over-expressed in cancers is Bcl-2 (B-cell lymphoma 2). We performed molecular docking analysis of AGL against Bcl-2 followed by prediction of ADME/Tox analysis. The docking results showed that AGL interacts potentially with BcL-2 with a docking score of -4.675 Kcal/mol. It also has significant pharmacokinetics property evaluated using preADMET tools. Following that the docking results have been evaluated ...
Seki, S; Oda, T; and Ohashi, M, Differential effects of aphidicolin on replicative dna synthesis and unscheduled dna synthesis in permeable mouse sarcoma cells. (1980). Subject Strain Bibliography 1980. 284 ...
Tagalide A (1) and tagalol A (2), representing dolabrane-type diterpenes with unprecedented ring-A/B/C/D- and ring-A/B/C-fused cores (vii-viii), respectively, were isolated from the Chinese mangrove, Ceriops tagal. The relative and absolute configurations of these dolabranes were unambiguously established by HRESIM
The IUPHAR/BPS Guide to Pharmacology. ingenol mebutate ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Aliases : Solyc01g080900.3. Description : 17.6.1.4 hormone metabolism.gibberelin.synthesis-degradation.ent-kaurenoic acid hydroxylase/oxygenase ent-kaurenoic acid hydroxylase (KAO2) ent-kaurenoic acid hydroxylase 2 (KAO2). ...
Ingenol 3-angelate is one of the active ingredients in E. antiquorum and E. peplus, extracts of which have been used as traditional medicines in Thailand and Australia. In this paper, we report the initial characterization of ingenol 3-angelate as a PKC ligand. We find impressive potency of ingenol 3-angelate as a ligand for PKC, especially considering its relatively hydrophilic nature. Ingenol 3-angelate induces a different pattern of translocation of PKC-δ in the cell, compared with the pattern of PMA, the typical tumor-promoting phorbol ester. Ingenol 3-angelate induces a higher level of secretion of the inflammatory cytokine IL-6 compared with PMA and displays a marked biphasic dose-response curve for the induction. Finally, ingenol 3-angelate was unable to cause the same extent of association of the C1b domain of PKC-δ with lipids compared with PMA or the physiological regulator DAG and was able to partially block the association induced by these agents. The novel pattern of behavior of ...
Invertebrates / Devils Hand Colored Polyp / Lobophytum sp. on Scleractinia / Wild Corals Soft . Quality Marine offers a great variety of corals and invertebrates, and is very supportive of numerous aquaculture efforts around the globe from which we offer the retailer and the hobbyist an environmentally sensitive alternative to wild harvest.
Clinical trial for Intractable Cancer-related Pain | Intractable Cancer Pain , Study to Evaluate Safety and MTD of Epidural Resiniferatoxin Injection for Treatment of Intractable Cancer Pain
Since epidemiological studies had repeatedly revealed lower rates of colon and liver cancers in coffee drinkers we made potential protective mechanisms of coffee and its components a specific focus in our research activity. Our main interest is directzed towards the diterpenes kahweol and cafestol which are contained in the coffee bean and in several types of coffee. Indeed, we have observed more than one beneficial effect as a consequence of their intake. For instance, carcinogen-detoxfying enzymes are induced whereas carcinogen-activating enzymes are at the same time inhibited. There is also enhancement of an important system that repairs alkylated DNA and protection against oxidative stress is increased at several levels. Investigation of all of these systems of protection is presently being continued in order to achieve a more thorough characterization of the involved mechanisms and to find new approaches. In this context, we are particularly intertested in redox effects on thiols such as ...
Valnemulin hydrochloride is a pleuromutilin antibiotic which inhibits protein synthesis in bacteria by binding the peptidyl transferase enzyme in the 50s ribosomal subunit. - Mechanism of Action & Protocol.
Pleuromutilin antibiotics, meningococcal disease, tuberculosis, a new fluoroquinolone to treat acute bacterial skin and skin structure infections, and WHO’s position on HPV vaccine recommendations makes up this week’s Top 5 articles.
Naz, S., Kerr, R. G., & Ramaswamy, N. (2000). New anti-proliferative epoxy-sterols from Pseudopterogorgia Americana. Tetrahedron Letters, 41(32), 6035-6040 ...
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GHRP-2 stimulates the release of an endogenous growth hormone (GH) within the somatotropes of the anterior pituitary in the human body.
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Effect of andrographolide treatment on cancer cells. Cancer is a multifaceted disease with complex processes and requires a multi-target therapeutic approach to
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The precise mechanisms to explain the suggested association between coffee consumption and reduced overall mortality risk are currently unknown, and research is ongoing to understand this area in more detail. However, a number of hypotheses exist and have considered roles for specific coffee constituents, including caffeine, cafestol and kahweol, as well as some of the […]
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alloaromadendrene: isolated from the volatile oil of the soft corals Clavularia viridis and Sarcophyton acutangulum; structure in first source
grayanotoxin III: from leaves of Leucothoe grayana (Ericaceae); RN refers to (3beta,6beta,14R)-isomer; structure given in first source
Giloy contains diterpenes compound including tinosporone, tinosporic acid, cardifolisides A to E. ...

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