New class of antifungal agents: jasplakinolide, a cyclodepsipeptide from the marine sponge, Jaspis species.
Jasplakinolide is a cyclodepsipeptide which represents a new class of antifungal agents with potent activity against Candida albicans. Jasplakinolide is fungicidal against C. albicans with both a MIC and a minimum lethal concentration of 25 micrograms/ml in a broth dilution assay. This activity compares to that of the imidazole miconazole nitrate, which had a MIC of 6.2 micrograms/ml and a minimum lethal concentration of 50 micrograms/ml in the same assay. Topical administration of 2% jasplakinolide cream against a murine vaginal C. albicans infection was equivalent in efficacy to administration of miconazole nitrate at 2%. Subcutaneous administration of jasplakinolide was not effective against a systemic murine C. albicans infection.
Scott
V R
VR
Department of Antimicrobial Chemotherapy, Syntex Research, Palo Alto, California 94304.
Boehme
R
R
Matthews
T R
TR
D000818:Animals; D000935:Antifungal Agents / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D002175:Candida / Q000187:drug effects* / Q000378:metabolism; D002177:Candidiasis / Q000188:drug therapy*; D002181:Candidiasis, Vulvovaginal / Q000188:drug therapy; D055598:Chemical Phenomena; D002621:Chemistry; D047630:Depsipeptides; D005260:Female; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests; D010456:Peptides, Cyclic / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity
D000935:Antifungal Agents; D047630:Depsipeptides; D010456:Peptides, Cyclic; C057531:jasplakinolide