氯肽素，一种来自链霉菌属的新型抗HIV抗生素，可抑制gp120与CD4的结合。I. 分类学、发酵、分离、理化性质及生物活性。

Chloropeptins, new anti-HIV antibiotics inhibiting gp120-CD4 binding from Streptomyces sp. I. Taxonomy, fermentation, isolation, and physico-chemical properties and biological activities.

作者信息

Tanaka H, Matsuzaki K, Nakashima H, Ogino T, Matsumoto A, Ikeda H, Woodruff H B, Omura S

机构信息

School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 1997 Jan;50(1):58-65. doi: 10.7164/antibiotics.50.58.

DOI:10.7164/antibiotics.50.58

PMID:9066767

Abstract

Chloropeptins I and II, which are gp120-CD4 binding inhibitors, were isolated as pale yellow-brown powders from the mycelia of a soil actinomycete, Streptomyces sp, WK-3419. Their physico-chemical properties showed that they are chlorinated peptides. Chloropeptin I (C61H45N7O15Cl6) is a novel compound, but chloropeptin II was identified as complestatin. Both compounds inhibited gp120-CD4 binding (IC50: 1.3 and 2.0 microM, respectively), the cytopathic effect of HIV in MT-4 cells (EC50: 1.6 and 1.7 microM, respectively) and syncytium formation in co-cultured HIV-1-infected and uninfected MOLT-4 cells (IC50. 0.5 and 1.1 microM, respectively). Chloropeptin I was synergistic in the inhibition of the cytopathic effect when combined with other anti-HIV drugs such as zidovudine (AZT), didanosine (ddI), zalcitabine (ddC) and nevirapine.

摘要

氯肽素I和II是gp120-CD4结合抑制剂，它们是从土壤放线菌链霉菌属WK-3419的菌丝体中分离得到的浅黄棕色粉末。它们的物理化学性质表明它们是氯化肽。氯肽素I（C61H45N7O15Cl6）是一种新型化合物，但氯肽素II被鉴定为复合他汀。两种化合物均抑制gp120-CD4结合（IC50分别为1.3和2.0 microM）、HIV在MT-4细胞中的细胞病变效应（EC50分别为1.6和1.7 microM）以及在共培养的HIV-1感染和未感染的MOLT-4细胞中的合胞体形成（IC50分别为0.5和1.1 microM）。当与其他抗HIV药物如齐多夫定（AZT）、去羟肌苷（ddI）、扎西他滨（ddC）和奈韦拉平联合使用时，氯肽素I在抑制细胞病变效应方面具有协同作用。