Biosynthesis of novel glucosides geldanamycin analogs by enzymatic synthesis.
JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY(2016)
摘要
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-beta-D-glucoside (1) and ACDL3172-18-O-beta-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 mu M, respectively).
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关键词
Geldanamycin analogs,glycosyltransferase,water solubility,cytotoxicity
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