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异嗜色菌素I和II,由杂色青霉FO-2338产生的新型抗gp120-CD4结合抑制剂。I.筛选、分类学、发酵、分离及生物活性。

Isochromophilones I and II, novel inhibitors against gp120-CD4 binding produced by Penicillium multicolor FO-2338. I. Screening, taxonomy, fermentation, isolation and biological activity.

作者信息

Matsuzaki K, Ikeda H, Masuma R, Tanaka H, Omura S

机构信息

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

出版信息

J Antibiot (Tokyo). 1995 Jul;48(7):703-7. doi: 10.7164/antibiotics.48.703.

Abstract

Isochromophilones I and II, the first novel gp120-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 C22H27O4Cl, respectively) have an azaphilone skeleton and a chlorine atom. Isochromophilones strongly inhibited gp120-CD4 binding (IC50: 6.6 and 3.9 microM, respectively), but the other related compounds did not. Isochromophilone II inhibited significantly HIV replication in peripheral human lymphocytes at 25 microM.

摘要

异嗜色菌素I和II是首批源自微生物的新型gp120-CD4结合抑制剂,它们是从一种名为多色青霉FO-2338的土壤真菌培养 broth中分离得到的。这些化合物与已知的相关化合物菌核盘菌素、赭色嗜色菌素和红嗜色菌素一起,从培养 broth中获得为黄色粉末。异嗜色菌素I和II(分别为C23H25O5Cl和C22H27O4Cl)具有氮杂蒽酮骨架和一个氯原子。异嗜色菌素强烈抑制gp120-CD4结合(IC50分别为6.6和3.9 microM),但其他相关化合物则没有。异嗜色菌素II在25 microM时显著抑制人外周血淋巴细胞中的HIV复制。

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