KMID : 0043320150380122208
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Archives of Pharmacal Research 2015 Volume.38 No. 12 p.2208 ~ p.2215
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Enzymatic synthesis of novel isobavachalcone glucosides via a UDP-glycosyltransferase
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Li Hong Mei
Lee Jae-Kyoung Nie Li Juan Huo Qiang Ma Tao Sohng Jae-Kyung Hong Young-Soo Wu Cheng Zhu
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Abstract
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Glycosylation is often used to improve a natural product¡¯s properties such as water solubility, chemical stability, pharmacological potency, and structure diversification. In this study, we studied the enzymatic synthesis of novel isobavachalcone glucosides using a UDP-glycosyltransferase (YjiC) from Bacillus licheniformis DSM-13. The chemical structures of compounds 1 and 2 were elucidated by spectroscopic techniques, including LC?MS, MS, and NMR. Meanwhile, the parameters of glycosylation reaction such as incubation time, UDP-glucose concentration, and pH of buffer were also optimized during this study. Furthermore, the compounds 1 and 2 exhibited weak anti-proliferative activities against five human cancer cell lines, with IC50 values ranging from 58.6 to 86.6 ¥ìM.
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KEYWORD
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Isobavachalcone, Glycosylation, YjiC, Diversification, Cytotoxicity
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