纤维素堆囊菌产生的新型大环内酯类化合物氧化磷酰乙酸：结构鉴定及其体外抗肿瘤生物活性

Phoxalone, a novel macrolide from Sorangium cellulosum: structure identification and its anti-tumor bioactivity in vitro.

作者信息

Guo Wen-Jie, Tao Wen-Yi

机构信息

Department of Pharmaceutical, School of Biotechnology, Southern Yangtze University, Wuxi, Jiangsu 214122, PR China.

出版信息

Biotechnol Lett. 2008 Feb;30(2):349-56. doi: 10.1007/s10529-007-9550-z. Epub 2007 Nov 8.

DOI:10.1007/s10529-007-9550-z

PMID:17989927

Abstract

A novel macrolide, isolated from the myxobacteria Sorangium cellulosum WXNXJ-C, was identified as 1,7,12,13-tetrahydroxy-14-methoxy-8,10-dimethyl-6-phenyl-5,15-dioxa-bicyclo[9.3.1]pentadecan-4-one, "Phoxalone". It had minimum IC(50) values of 0.24, 6.9, 10.3, 0.98 and 4 microg/ml, respectively, against tumour cell lines: B16, Bel7402, H446, MCF-7, and SGC7901. In addition, it had less cytotoxicity to normal human liver L02 cell lines (286 microg/ml, 24 h). A cytotoxic bioactivity study on H446 cell line in vitro suggested that Phoxalone arrested the mitosis in the G2/M phase.

摘要

从粘细菌纤维堆囊菌WXNXJ-C中分离出的一种新型大环内酯被鉴定为1,7,12,13-四羟基-14-甲氧基-8,10-二甲基-6-苯基-5,15-二氧杂-双环[9.3.1]十五烷-4-酮，即“磷唑酮”。它对肿瘤细胞系B16、Bel7402、H446、MCF-7和SGC7901的最低半数抑制浓度（IC50）值分别为0.24、6.9、10.3、0.98和4微克/毫升。此外，它对正常人肝脏L02细胞系的细胞毒性较小（286微克/毫升，24小时）。对H446细胞系进行的体外细胞毒性生物活性研究表明，磷唑酮使有丝分裂停滞在G2/M期。