新木脂素的酶法糖基化及抗肿瘤活性
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。
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--D-glucopyranoside (1) and honokiol-4'-O--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 mol/L. Conclusion The glycoslated products show enhanced water solubility and drug sensitivity against SMMC7721 cells, suggesting their value as potential therapeutic drugs.
马涛、郭星、霍强、李静、李红梅、李楠、靳伟、吴成柱
肿瘤学药学生物科学研究方法、生物科学研究技术
新木脂素糖基转移酶抗肿瘤活性
马涛,郭星,霍强,李静,李红梅,李楠,靳伟,吴成柱.新木脂素的酶法糖基化及抗肿瘤活性[EB/OL].(2017-12-07)[2025-08-19].https://chinaxiv.org/abs/201712.00734.点此复制
评论