超滤亲和结合液相色谱-质谱联用和分子对接技术筛选毛菊苣种子中高亲和性α-葡萄糖苷酶抑制剂

发布时间：2018-07-22 15:57

【摘要】：采用超滤亲和结合液相色谱-质谱联用(UF-LC-MS)和分子对接技术筛选毛菊苣种子中高亲和α-葡萄糖苷酶抑制剂。以4-硝基苯-α-D-吡喃葡萄糖苷(PNPG)为底物,阿卡波糖为阳性对照,评价毛菊苣种子提取物对α-葡萄糖苷酶的抑制活性,其中阿卡波糖IC_(50)为0.003 mg/m L,毛菊苣种子IC_(50)为0.447 mg/m L。利用UF-LC-MS技术对毛菊苣种子提取物进行筛选鉴定,获得4种化合物;通过Autodock软件筛选出2种与α-葡萄糖苷酶有较高亲和力的化合物,分别是绿原酸和异绿原酸A。结合体外酶活实验,验证了绿原酸、异绿原酸A对α-葡萄糖苷酶的抑制活性。结果表明,各化合物对α-葡萄糖苷酶的抑制活性由大到小依次是:阿卡波糖异绿原酸A绿原酸,其中异绿原酸A与阿卡波糖抑制率相近。
[Abstract]:The high affinity 伪 -glucosidase inhibitor was screened by UF-LC-MS and molecular docking technique. The inhibitory activity of seed extract of Cichory on 伪 -glucosidase was evaluated by using 4-nitrobenzen- 伪 -Dpyranoside (PNPG) as substrate and acarbose as positive control. The IC50 of acarbose was 0.003 mg/m / L and the IC50 of chicory seed was 0.447 mg/m / L. Four compounds were obtained by using UF-LC-MS, and two compounds with high affinity to 伪 -glucosidase, Lv Yuan acid and iso-Lv Yuan acid A, were screened by Autodock software. The inhibitory activity of Lv Yuan acid and Lv Yuan acid A on 伪-glucosidase was confirmed by in vitro enzyme activity test. The results showed that the inhibitory activity of each compound on 伪 -glucosidase was as follows: acarbose isoLv Yuan acid A Lv Yuan acid, in which the inhibition rate of isoLv Yuan acid A was similar to that of acarbose acid.
【作者单位】：石河子大学药学院;石河子大学化学化工学院;
【基金】：石河子大学杰出青年科技人才培育计划(No.2015ZRKXJQ08) 国家自然科学基金(No.81560680)资助项目~~
【分类号】：O657.63;TQ464

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