Discovery, Production and Purification of the Na+, K+ Activated Atpase Inhibitor, L-681,110 from the Fermentation Broth of Streptomyces Sp. Ma-5038

Abstract

The maximum yield for the production of L-681,110 by Streptomycessp. MA-5038 (ATCC 31587) was observed after 5 days’ incubation at 28oC and pH about 8.3. L-681,110 was isolated from the fermentation broth by acetone extraction of the mycelia, absorption to Amberlite XAD-2 resin and two separations by thinlayer chromatography. The structure of L-681,110 was found to consist of a sixteen-membered lactone with a new type of substitution. The inhibition of ATPase, activity against Caenorhabditis elegans and stimulation of γ-amino-butyric acid release indicate that L-681,110 possesses some characteristics of both oligomycin and avermectin. L-681,110 was also active against tapeworm and ticks in an in vivo assay. © 1984, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.