Xu Tingting, Fan Ziyun, Lou Junqiao, Du Qi, Kong Yue, Lu Yujia, Wu Xueming
School of Medicine & Holistic Integrative Medicine, Nanjing University of Chinese Medicine Nanjing 210023 China.
State Key Laboratory Cultivation Base for TCM Quality and Efficacy, School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023 China
RSC Adv. 2022 Aug 23;12(37):23839-23844. doi: 10.1039/d2ra04408k. eCollection 2022 Aug 22.
Vitexin is an active component of many traditional chinese medicines, and is found in various plants. The low solubility of vitexin limits its pharmaceutical usage. In this study, solvent-stable β-fructosidase was used to glycosylate vitexin in organic solvents. The β-fructosidase showed high activity and stability in 30-80% (v/v) ethyl acetate with 90-99% yields of vitexin glycosides. Highly efficient synthesis of β-d-fructofuranosyl-(2→6)-vitexin (1.04 g L) and β-d-difructofuranosyl-(2→6)-vitexin (0.45 g L) was attained in 50% (v/v) ethyl acetate solvent system from 1.5 g L vitexin. Two novel vitexin glycosides showed higher anti-tumor activities compared to that of vitexin by employing a human breast cancer cytotoxicity assay.
牡荆素是许多传统中药的活性成分，存在于多种植物中。牡荆素的低溶解度限制了其药用价值。在本研究中，使用溶剂稳定的β-果糖苷酶在有机溶剂中对牡荆素进行糖基化。β-果糖苷酶在30 - 80%（v/v）乙酸乙酯中表现出高活性和稳定性，牡荆素糖苷的产率为90 - 99%。在50%（v/v）乙酸乙酯溶剂体系中，以1.5 g/L牡荆素高效合成了β-D-呋喃果糖基-(2→6)-牡荆素（1.04 g/L）和β-D-二呋喃果糖基-(2→6)-牡荆素（0.45 g/L）。通过人乳腺癌细胞毒性试验，两种新型牡荆素糖苷显示出比牡荆素更高的抗肿瘤活性。
