新木脂素的酶法糖基化及抗肿瘤活性

Subjects: Medicine, Pharmacy >> Preclinical Medicine submitted time 2017-12-07 Cooperative journals: 《南方医科大学学报》

李红梅 李静 靳伟 郭星 李楠 马涛 霍强 吴成柱

Abstract： Objective To improve the water solubility and biological activity of neoligans (magnolol and honokiol) and test the antitumor activity of the modified compounds. Methods The glycosylated products of magnolol and honokiol were obtained by enzymatic synthesis using a UDP-glycosyltransferase (YjiC) from Bacillus. The products were characterized by high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometry (LC-MS), and nuclear magnetic resonance (NMR) analysis. MTT assay was used to detect the growth inhibition of 4 human cancer cell lines induced by the compounds. Results We obtained two glucosides of neolignans (magnolol and honokiol) for the first time by enzymatic synthesis using a UDP-glycosyltransferase. Based on the spectroscopic data, the glucosides were identified as magnolol-2- O-β-D-glucopyranoside (1) and honokiol-4'-O-β-D-glucopyranoside (2). Compounds 1-4 exhibited moderate anti-proliferative activities against the 4 human cancer cell lines, with IC 50 values ranging from 9.41 to 111.21 µmol/L. Conclusion The glycoslated products show enhanced water solubility and drug sensitivity against SMMC7721 cells, suggesting their value as potential therapeutic drugs.

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