分类： 医学、药学 >> 基础医学 提交时间： 2018-01-25 合作期刊: 《南方医科大学学报》
摘要： 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.
分类： 医学、药学 >> 基础医学 提交时间： 2017-12-07 合作期刊: 《南方医科大学学报》
摘要： 目的 以厚朴酚与和厚朴酚为底物，进行酶法糖基化修饰以及检测其抗肿瘤活性，提高新木脂素类化合物（厚朴酚与和厚朴酚）的水溶性和生物活性。方法 利用来源于Bacillus的糖基转移酶（YjiC），通过酶法糖基化制备厚朴酚与和厚朴酚糖基化产物；经高效液相色谱（HPLC）、液相串联质谱（LC-MS）、核磁共振（NMR）检测分析鉴定其结构；通过MTT法检测药物对多种肿瘤细胞的增殖抑制效应。结果 利用酶法糖基化反应制备了2个新木脂素（厚朴酚与和厚朴酚）糖基化产物，并显著提高了其水溶性；糖基化产物分别鉴定为magnolol-2-O- β-D-glucopyranoside（1）和 honokiol-4'-O-β-D-glucopyranoside（2）；MTT结果显示，厚朴酚与和厚朴酚及其糖基化产物对4种肿瘤细胞均表现出较强的抑制细胞增殖的作用，且呈现浓度依赖性，其IC 50 范围为9.41~111.21 µmol/L。结论 厚朴酚与和厚朴酚糖基化产物显著提高水溶性以及增加了药物对SMMC7721细胞的敏感性，并具有良好的应用前景。
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