从黄柄曲霉中分离并鉴定出FR198248（一种羟基化的1,3-二氢异苯并呋喃）作为肽脱甲酰基酶抑制剂。

Isolation and identification of FR198248, a hydroxylated 1,3-dihydroisobenzofuran, from Aspergillus flavipes as an inhibitor of peptide deformylase.

作者信息

Kwon Yun-Ju, Zheng Chang-Ji, Kim Won-Gon

机构信息

Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejon, Republic of Korea.

出版信息

Biosci Biotechnol Biochem. 2010;74(2):390-3. doi: 10.1271/bbb.90565. Epub 2010 Feb 7.

DOI:10.1271/bbb.90565

PMID:20139618

Abstract

Two highly hydroxylated 1,3-dihydroisobenzofurans, FR198248 (1) and FR202306 (2), were isolated as peptide deformylase (PDF) inhibitors from Aspergillus flavipes. Compounds 1 and 2 inhibited Staphylococus aureus PDF with IC(50) values of 3.6 and 2.5 microM, respectively, and also showed antibacterial activity with an MIC value of 25 microg/ml. In contrast, 6-O-methyl derivative 3 of compound 2 was inactive against both PDF and S. aureus.

摘要

从黄柄曲霉中分离出两种高度羟基化的1,3 - 二氢异苯并呋喃，FR198248（1）和FR202306（2），作为肽脱甲酰基酶（PDF）抑制剂。化合物1和2抑制金黄色葡萄球菌PDF的IC(50)值分别为3.6和2.5 microM，并且还显示出抗菌活性，MIC值为25 microg/ml。相比之下，化合物2的6 - O - 甲基衍生物3对PDF和金黄色葡萄球菌均无活性。