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1. chinaXiv:201801.00699 [pdf]

酶法糖基化合成一种新型补骨脂定葡萄糖苷

李静; 李楠; 赵玉茹; 戴轶群; 霍强; 马涛; 李红梅; 吴成柱
Subjects: Medicine, Pharmacy >> Preclinical Medicine

Objective To modify the structure of psoralidin using in vitro enzymatic glycosylation to improve its water solubilityand stability. Methods A new psoralidin glucoside (1) was obtained by enzymatic glycosylation using a UDP-glycosyltransferase. The chemical structure of compound 1 was elucidated by HR-ESI-MS and nuclear magnetic resonance(NMR) analysis. The high-performance liquid chromatography (HPLC) peaks were integrated and sample solution concentrations were calculated. MTT assay was used to detect the cytotoxicity of the compounds against 3 cancer cell lines in vitro. Results Based on the spectroscopic data, the new psoralidin glucoside was identified as psoralidin-6',7-di-O glucopyranoside (1), whose water solubility was 32.6-fold higher than that of the substrate. Analyses of pH and temperature stability demonstrated that compound 1 was more stable than psoralidin at pH 8.8 and at high temperatures. Only psoralidin exhibited a moderate cytotoxicity against 3 human cancer cell lines. Conclusion In vitro enzymatic glycosylation is a powerful approach for structural modification and improving water solubility and stability of compounds.

submitted time 2018-01-25 From cooperative journals:《南方医科大学学报》 Hits1495Downloads835 Comment 0

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