R176502, a New Bafilolide Metabolite with Potent Antiproliferative Activity from a Novel Micromonospora Species

During the course of a screening program intended to identify new antiproliferative agents, a new bafilolide metabolite was discovered. R176502 (1) was isolated from the liquid fermentation cultures of a novel Micromonospora species found in African river bottom sediment. It was purified from ethyl...

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Bibliographic Details
Published in:Journal of antibiotics 2003/11/25, Vol.56(11), pp.909-916
Main Authors: LAAKSO, JODI A., MOCEK, URSULA M., DUN, JACKY VAN, WOUTERS, WALTER, JANICOT, MICHEL
Format: Article
Language:English
Subjects:
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - isolation & purification
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor - drug effects
Fermentation
Humans
Macrolides - chemistry
Macrolides - isolation & purification
Macrolides - pharmacology
Medical sciences
Micromonospora
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:During the course of a screening program intended to identify new antiproliferative agents, a new bafilolide metabolite was discovered. R176502 (1) was isolated from the liquid fermentation cultures of a novel Micromonospora species found in African river bottom sediment. It was purified from ethyl acetate extracts using a series of countercurrent chromatographic steps. The structure was determined using 1- and 2-D NMR experiments. Three previously described bafilomycins (bafilomycins A1 (2), B1 (3), and B2 (4)) were also isolated (from other microbial strains). R176502 exhibited potency for inhibition of tumor cell proliferation in the nM range of concentrations.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.56.909