KMID : 0545120160260010056
|
|
Journal of Microbiology and Biotechnology 2016 Volume.26 No. 1 p.56 ~ p.60
|
|
Biosynthesis of Novel Glucosides Geldanamycin Analogs by Enzymatic Synthesis
|
|
Huo Qiang
Li Hong Mei Lee Jae-Kyoung Li Jing Ma Tao Zhang Xin Yu Dai Yi Qun Hong Young-Soo Wu Cheng Zhu
|
|
Abstract
|
|
|
Two new glucosides (1 and 2) of geldanamycin (GA) analogs were obtained from in vitro glycosylation by UDP-glycosyltransferase (YjiC). Based on spectroscopic (HR-ESI-MS, 1D, and 2D-NMR) analyses, the glucosides were elucidated as 4,5-dihydro-7-O-descarbamoyl-7- hydroxyl GA-7-O-¥â-D-glucoside (1) and ACDL3172-18-O-¥â-D-glucoside (2). Furthermore, the water solubility of compounds 1 and 2 was about 215.2 and 90.7 times higher respectively, than that of the substrates. Among compounds 1-4, only 3 showed weak antiproliferative activity against four human tumor cell lines: MDA-MB-231, SMMC7721, HepG2, and SW480 (IC50: 13.6, 15.1, 31.8, and 22.7 ¥ìM, respectively).
|
|
KEYWORD
|
|
Geldanamycin analogs, glycosyltransferase, water-solubility, cytotoxicity
|
|
FullTexts / Linksout information
|
|
|
|
Listed journal information
|
|
|
|