| 1. |
- Appendino, G, et al.
(författare)
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SERCA-inhibiting activity of C-19 terpenolides from Thapsia garganica and their possible biogenesis
- 2005
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Ingår i: Journal of Natural Products. - : American Chemical Society (ACS). - 0163-3864 .- 1520-6025. ; 68:8, s. 1213-1217
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Tidskriftsartikel (refereegranskat)abstract
- An investigation of Thapsia garganica afforded a series of tetracyclic C-19 dilactones, whose production was dependent on the time and location of the collection. These unusual tetrahomosesquiterpenoids are presumably biosynthesized via a carbon dioxide-triggered electrophilic polyolefin cyclization. Despite the structural differences with thapsigargin, these compounds showed SERCA-inhibiting properties.
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| 2. |
- Aqueveque, P, et al.
(författare)
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Favolon B, a new triterpenoid isolated from the Chilean Mycena sp strain 96180
- 2005
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Ingår i: Journal of Antibiotics. - 0021-8820. ; 58:1, s. 61-64
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Tidskriftsartikel (refereegranskat)abstract
- A new biologically active triterpenoid, favolon B (1), was isolated from fermentation broths of Mycena sp. strain 96180. Favolon B showed antifungal activities towards Botrytis cinerea, Mucor miehei, Paecilomyces variotii and Penicillium notatum. No activities were observed against bacteria and yeasts. The structure of favolon B was elucidated by spectroscopic techniques.
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| 3. |
- Aujard, Isabelle, et al.
(författare)
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Tridemethylisovelleral, a potent cytotoxic agent
- 2005
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Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896. ; 13:22, s. 6145-6150
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Tidskriftsartikel (refereegranskat)abstract
- The synthesis and in vitro cytotoxicity toward various tumor cell lines of (+/-)-tridemethylisovelleral, an analogue of the bioactive fungal sesquiterpene (+)-isovelleral retaining the bicyclo[4,1,0]hept-2-en-1,2-dicarbaidehyde system but lacking the three methyl groups, is reported. The cytotoxicity of tridemethylisovelleral toward several tumor cell lines was found to be comparable with those of established antitumor drugs, and significantly higher than that of isovelleral. (c) 2005 Elsevier Ltd. All rights reserved.
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| 4. |
- Bautista, D M, et al.
(författare)
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Pungent products from garlic activate the sensory ion channel TRPA1
- 2005
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Ingår i: Proceedings of the National Academy of Sciences. - : Proceedings of the National Academy of Sciences. - 1091-6490 .- 0027-8424. ; 102:34, s. 12248-12252
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Tidskriftsartikel (refereegranskat)abstract
- Garlic belongs to the Allium family of plants that produce organosulfur compounds, such as allicin and diallyl disulfide (DADS), which account for their pungency and spicy aroma. Many health benefits have been ascribed to Allium extracts, including hypotensive and vasorelaxant activities. However, the molecular mechanisms underlying these effects remain unknown. Intriguingly, allicin and DADS share structural similarities with allyl isothiocyanate, the pungent ingredient in wasabi and other mustard plants that induces pain and inflammation by activating TRPA1, an excitatory ion channel on primary sensory neurons of the pain pathway. Here we show that allicin and DADS excite an allyl isothiocyanate-sensitive subpopulation of sensory neurons and induce vasodilation by activating capsaicin-sensitive perivascular sensory nerve endings. Moreover, allicin and DADS activate the cloned TRPA1 channel when expressed in heterologous systems. These and other results suggest that garlic excites sensory neurons primarily through activation of TRPA1. Thus different plant genera, including Allium and Brassica, have developed evolutionary convergent strategies that target TRPA1 channels on sensory nerve endings to achieve chemical deterrence.
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| 5. |
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| 6. |
- Johansson, Martin H, et al.
(författare)
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Synthesis of decaline analogues of isovelleral
- 2005
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Ingår i: Zeitschrift fuer Naturforschung. Section B: A Journal of Chemical Sciences. - 0932-0776. ; 60:9, s. 984-989
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Tidskriftsartikel (refereegranskat)abstract
- Decaline analogues of the bioactive fungal sesquiterpene (+)-isovelleral (1a), retaining the bicyclo[4,1,0]hept-2-en-1,2-dicarbaldehyde system, were prepared, and their cytotoxic and antimicrobial activities were compared with those of the natural product. While the two isomers (+/-)-2 and (+/-)-3 were as active as isovelleral (1a), the isomer (+/-)-4 was approximately 10 times less potent.
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| 7. |
- Kettering, M, et al.
(författare)
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Heptemerones A-G, seven novel diterpenoids from Coprinus heptemerus: Producing organism, fermentation, isolation and biological activities
- 2005
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Ingår i: Journal of Antibiotics. - 0021-8820. ; 58:6, s. 390-396
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Tidskriftsartikel (refereegranskat)abstract
- Seven novel diterpenoids, named heptemerones A-G, were isolated from the broth of submerged cultures of Coprinus heptemerus, a basidiomycete which previously had not been known to produce secondary metabolites. The compounds were purified by solid phase extraction and silica gel chromatography followed by preparative HPLC. Among the biological activities the inhibition of fungal germination was the most potent, and depended highly on the composition of the assay medium. In water, inhibition occurred at 5 similar to 10 fold lower concentrations as compared to complex media. Heptemerone G was the most active compound with MICs starting at 1 mu g/ml. Four of the antifungal compounds exhibited plant protective activity in a leaf segment assay using Magnaporthe grisea as the pathogen. Growth of yeasts and bacteria was hardly affected. Cytotoxic activities were moderate and only heptemerone D was phytotoxic.
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| 8. |
- Movahed Rad, Pouya, et al.
(författare)
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Endogenous unsaturated C18 N-acylethanolamines are vanilloid receptor (TRPV1) agonists.
- 2005
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Ingår i: Journal of Biological Chemistry. - 1083-351X .- 0021-9258. ; 280:46, s. 38496-38504
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Tidskriftsartikel (refereegranskat)abstract
- The endogenous C18 N-acylethanolamines (NAEs) N-linolenoylethanolamine (18:3 NAE), N-linoleoylethanolamine (18:2 NAE), N-oleoylethanolamine (18:1 NAE), and N-stearoylethanolamine (18:0 NAE) are structurally related to the endocannabinoid anandamide (20:4 NAE), but these lipids are poor ligands at cannabinoid CB1 receptors. Anandamide is also an activator of the transient receptor potential (TRP) vanilloid 1 (TRPV1) on primary sensory neurons. Here we show that C18 NAEs are present in rat sensory ganglia and vascular tissue. With the exception of 18:3 NAE in rat sensory ganglia, the levels of C18 NAEs are equal to or substantially exceed those of anandamide. At submicromolar concentrations, 18:3 NAE, 18:2 NAE, and 18:1 NAE, but not 18:0 NAE and oleic acid, activate native rTRPV1 on perivascular sensory nerves. 18:1 NAE does not activate these nerves in TRPV1 gene knock-out mice. Only the unsaturated C18 NAEs elicit whole cell currents and fluorometric calcium responses in HEK293 cells expressing hTRPV1. Molecular modeling revealed a low energy cluster of U-shaped unsaturated NAE conformers, sharing several pharmacophoric elements with capsaicin. Furthermore, one of the two major low energy conformational families of anandamide also overlaps with the cannabinoid CB1 receptor ligand HU210, which is in line with anandamide being a dual activator of TRPV1 and the cannabinoid CB1 receptor. This study shows that several endogenous non-cannabinoid NAEs, many of which are more abundant than anandamide in rat tissues, activate TRPV1 and thus may play a role as endogenous TRPV1 modulators.
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| 9. |
- Rether, J, et al.
(författare)
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Inhibition of TNF-alpha promoter activity and synthesis by A11-99-1, a new cyclopentenone from the ascomycete Mollisia melaleuca
- 2005
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Ingår i: Zeitschrift fuer Naturforschung. Section C: A Journal of Biosciences. - 0939-5075. ; 60c:5-6, s. 478-484
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Tidskriftsartikel (refereegranskat)abstract
- In a search for inhibitors of the inducible tumor necrosis factor-alpha (TNF-alpha) promoter activity and synthesis, a new chlorinated cyclopentenone was isolated from fermentations of the ascomycete Mollisia melaleuca. The structure was determined by a combination of spectroscopic techniques. The compound blocked the inducible human TNF-alpha promoter activity and synthesis with IC50-values of 2.5-5 mu g/ml (8.1-16.1 mu M). Studies on the mode of action of the compound revealed that the inhibition of TNF-alpha promoter activity is caused by an inhibition of the phosphorylation of the I kappa B protein which prevents the activation of the transcription factor NF-kappa B. No cytotoxic, antibacterial and antifungal activities could be observed up to 100 mu g/ml (323 mu m) of the compound.
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| 10. |
- Valdivia, Carola, et al.
(författare)
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Diterpenoids from Coprinus heptemerus
- 2005
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Ingår i: Tetrahedron. - : Elsevier BV. - 0040-4020. ; 61:40, s. 9527-9532
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Tidskriftsartikel (refereegranskat)abstract
- Seven diterpenoids, isolated due to their ability to inhibit spore germination in the plant pathogenic fungus Magnaporthe grisea, were obtained from cultures of the basidiomycete Coprinus heptenlerus. The structures of the compounds, named heptemerones A-G, were determined with spectroscopic techniques. (c) 2005 Elsevier Ltd. All rights reserved.
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