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Bisabosquals, novel squalene synthase inhibitors. I. Taxonomy, fermentation, isolation and biological activities.
- Source :
-
The Journal of antibiotics [J Antibiot (Tokyo)] 2001 Nov; Vol. 54 (11), pp. 890-5. - Publication Year :
- 2001
-
Abstract
- In the course of screening for yeast squalene synthase inhibitors, bisabosqual A was isolated from the culture broth of Stachybotrys sp. RF-7260. The related compounds bisabosquals B, C and D were also isolated from Stachybotrys ruwenzoriensis RF-6853. Bisabosquals inhibited squalene synthases. IC50 values of bisabosqual A against the microsomal squalene synthases from Saccharomyces cerevisiae, Candida albicans, HepG2 cell and rat liver were 0.43, 0.25, 0.95 and 2.5 microg/ml, respectively. Bisabosqual C exhibited inhibitory activities similar to bisabosqual A. Bisabosqual A showed broad spectrum antifungal activity in vitro.
- Subjects :
- Animals
Antifungal Agents pharmacology
Enzyme Inhibitors pharmacology
Fermentation
Hepatocytes
Humans
Inhibitory Concentration 50
Microbial Sensitivity Tests
Pyrans pharmacology
Rats
Stachybotrys chemistry
Stachybotrys classification
Antifungal Agents isolation & purification
Enzyme Inhibitors isolation & purification
Farnesyl-Diphosphate Farnesyltransferase antagonists & inhibitors
Pyrans isolation & purification
Stachybotrys metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0021-8820
- Volume :
- 54
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- The Journal of antibiotics
- Publication Type :
- Academic Journal
- Accession number :
- 11827030
- Full Text :
- https://doi.org/10.7164/antibiotics.54.890