Isochromophilones I and II, Novel Inhibitors against gpl20-CD4 Binding Produced by Penicillium multicolor FO-2338: I. Screening, Taxonomy, Fermentation, Isolation and Biological Activity

Abstract

Isochromophilones I and II, the first novel gpl20-CD4 binding inhibitors of microbial origin, were isolated from a cultured broth of a soil fungus designated as Penicillium multicolor FO-2338. These compounds were obtained as yellow powders from the cultured broth together with the known related compounds sclerotiorin, ochrephilone and rubrorotiorin. Isochromophilones I and II (C23H25O5Cl and C22H27O4C1, respectively) have an azaphilone skeleton and a chlorine atom. Isochromophilones strongly inhibited gpl20-CD4 binding (IC50: 6.6 and 3.9 μm, respectively), but the other related compounds did not. Isochromophilone II inhibited significantly HIV replication in peripheral human lymphocytes at 25μM. © 1995, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.