Compounds AT2433-A1 (Al), AT2433-A2 (A2), AT2433-B1 (Bl), and AT2433-B2 (B2) were isolated from the cultured broth of Actinomadura melliaura sp. nov. (SCC 1655). Structurally these materials are closely related to rebeccamycin (1), an indolocarbazole antitumor antibiotic. Al, A2, Bl, and B2 were active against Staphylococcus aureus A9537, Streptococcus faecalis A20688, Streptococcusfaecium (ATCC 9790), Micrococcus lutea (ATCC 9341), Bacillus subtilis (ATCC 6633). Al and Bl were active against P388 leukemia in mice.
Growing cells of Fusarium oxysporum f.sp. vasinfectum (ATCC 7808) formed 3-acetoxyscirpene-4,15-diol from anguidine (4,15-diacetoxyscirpene-3-ol) by way of the intermediates triacetoxyscirpene, 3,4-diacetoxyscirpene-15-ol and 3,15-diacetoxyscirpene-4-ol. The new 3-acetoxy analog was found to be less active than anguidine and the two other monoacetoxy derivatives when tested against a series of fungal strains and against HeLa cells in vitro.
Resting cells of Streptomyces griseus, Mucor mucedo, and a growing culture of Acinetobacter calcoaceticus when mixed with compounds related to 12,13epoxytrichothec-9-ene-4,8,15-diacetoxy-3a-ol(anguidine) produced a series of derivatives that were either partially hydrolyzed or selectively acylated. These derivatives showed marked differences in activities as assayed by antifungal and tissue culture cytotoxicity tests.
The in vivo antitumor activities, as measured by inhibition of transplanted P-388 and L-1210 leukemia in mice, have been determined for a series of analogs of anguidine including triacetoxyscirpenol, the three diacetoxyscirpenols, the three monoacetoxyscirpenols, and scirpenetriol. An acetoxy function at position 15 appears to be required for good activity.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.