硫代亚磺酰化FK228的起源与生物活性
Origin and bioactivities of thiosulfinated FK228.
作者信息
Liu Xiangyang, Currens Grant C, Xue Liang, Cheng Yi-Qiang
机构信息
UNT System College of Pharmacy , University of North Texas Health Science Center , 3500 Camp Bowie Blvd , Fort Worth , TX 76107 , USA . Email:
Alcon NMR laboratory at Novartis , 6201 South Fwy , Fort Worth , TX 76134 , USA.
出版信息
Medchemcomm. 2019 Mar 25;10(4):538-542. doi: 10.1039/c9md00060g. eCollection 2019 Apr 1.
Abstract
During a large laboratory-scale purification of FK228 from the fermentation broth of MSMB43, a small amount of thiosulfinated FK228 (TS-FK228) was unexpectedly purified only after the broth was mixed with silica gel. Evidence supports the postulations that TS-FK228 was derived from FK228 through spontaneous chemical reaction with silica gel, and TS-FK228 existed as two isomers and . TS-FK228 demonstrated similar inhibitory activity and profile against human class I histone deacetylases but exhibited a much higher antiproliferative activity against representative human cancer cell lines when compared to FK228.
摘要
在大规模实验室规模从MSMB43发酵液中纯化FK228的过程中，仅在发酵液与硅胶混合后意外地纯化出少量硫代硫化FK228（TS-FK228）。有证据支持以下推测：TS-FK228是FK228与硅胶自发化学反应衍生而来，且TS-FK228以两种异构体形式存在。TS-FK228对人I类组蛋白去乙酰化酶表现出相似的抑制活性和作用模式，但与FK228相比，对代表性人类癌细胞系表现出更高的抗增殖活性。
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