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 ...

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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

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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

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For the first time Alcyonacea from Tanzania are recorded, including two new species: Cladiella daphnae and Sinularia platylobata. Both these species are described and figured, while descriptions are also given of specimens of Lobophytum crassum von Marenzeller, 1886, L. rotundum Tixier-Durivault, 1957, and L. venustum, Tixier-Durivault, 1957. In addition, Sinularia compactum Tixier-Durivault, 1970 and Sinularia conferta (Dana, 1846) are discussed ...

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 ...

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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 ...

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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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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