Mode of action of epoxyphomalins A and B and characterization of related metabolites from the marine-derived fungus Paraconiothyrium sp.
In: Journal of natural products, Jg. 73 (2010-12-27), Heft 12, S. 2053-6
academicJournal
Zugriff:
Epoxyphomalins A (1) and B (2) are highly potent cytotoxic fungal metabolites. During the course of purifying larger quantities of 1 and 2 from Paraconiothyrium sp. fermentation extracts, three new epoxyphomalins (3-5) were isolated and characterized, showing modifications to the oxidation pattern of the cyclohexene moiety or of C-9 of the decalin system. IC(50) values for cytotoxicity against a panel of 36 human tumor cell lines were determined for all new compounds. Compound 4 was found to be cytotoxic particularly toward prostate PC3M (IC(50) = 0.72 μM) and bladder BXF 1218 L (IC(50) = 1.43 μM) cancer cell lines. In addition, inhibition of chymotrypsin-, caspase-, and trypsin-like activity of purified 20S proteasomes was determined for epoxyphomalins A (1) and B (2). The results indicate that compounds 1 and 2 exert their cytotoxic effect through potent inhibition of the 20S proteasome.
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Mode of action of epoxyphomalins A and B and characterization of related metabolites from the marine-derived fungus Paraconiothyrium sp.
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Autor/in / Beteiligte Person: | Mohamed, IE ; Kehraus, S ; Krick, A ; König, GM ; Kelter, G ; Maier, A ; Fiebig, HH ; Kalesse, M ; Malek, NP ; Gross, H |
Zeitschrift: | Journal of natural products, Jg. 73 (2010-12-27), Heft 12, S. 2053-6 |
Veröffentlichung: | Cincinnati, American Society of Pharmacognosy., 2010 |
Medientyp: | academicJournal |
ISSN: | 1520-6025 (electronic) |
DOI: | 10.1021/np100310k |
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