New cyclodepsipeptides, enniatins d, e and f produced by fusarium sp. fo-1305

Abstract

New cyclodepsipeptides named enniatins D, E and F were isolated from the culture broth of Fusarium sp. FO-1305 as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT). The respective structures of enniatins D, E and F were determined to be cyclo[d-α-hydroxyisovaleryl(d-Hiv)-l-N-methylleucinyl(l-Me-Leu)-d-Hiv-l-N-methylvalinyl(l-Me-Val)-d-Hiv-l-Me-Val], a mixture of cyclo-[d-Hiv-l-Me-Leu-d-Hiv-l-N-methylisoleucinyl(l-Me-Ile)-d-Hiv-l-Me-Val] and cyclo(d-Hiv-l-Me-Ile-d-Hiv-l-Me-Leu-d-Hiv-l-Me-Val), and cyclo(d-Hiv-l-Me-Leu-d-Hiv-l-Me-Ile-d-Hiv-l-Me-Ile) by spectral analyses and chemical degradation. The IC50 values of enniatins D, E and F for ACAT activity in an enzyme assay using rat liver microsomes were calculated to be 87, 57 and 40 μM, respectively. © 1992, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.