【摘要】：采用超濾親和結(jié)合液相色譜-質(zhì)譜聯(lián)用(UF-LC-MS)和分子對接技術(shù)篩選毛菊苣種子中高親和α-葡萄糖苷酶抑制劑。以4-硝基苯-α-D-吡喃葡萄糖苷(PNPG)為底物,阿卡波糖為陽性對照,評價毛菊苣種子提取物對α-葡萄糖苷酶的抑制活性,其中阿卡波糖IC_(50)為0.003 mg/m L,毛菊苣種子IC_(50)為0.447 mg/m L。利用UF-LC-MS技術(shù)對毛菊苣種子提取物進(jìn)行篩選鑒定,獲得4種化合物;通過Autodock軟件篩選出2種與α-葡萄糖苷酶有較高親和力的化合物,分別是綠原酸和異綠原酸A。結(jié)合體外酶活實(shí)驗(yàn),驗(yàn)證了綠原酸、異綠原酸A對α-葡萄糖苷酶的抑制活性。結(jié)果表明,各化合物對α-葡萄糖苷酶的抑制活性由大到小依次是:阿卡波糖異綠原酸A綠原酸,其中異綠原酸A與阿卡波糖抑制率相近。
[Abstract]:The high affinity 偽 -glucosidase inhibitor was screened by UF-LC-MS and molecular docking technique. The inhibitory activity of seed extract of Cichory on 偽 -glucosidase was evaluated by using 4-nitrobenzen- 偽 -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 偽 -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 偽-glucosidase was confirmed by in vitro enzyme activity test. The results showed that the inhibitory activity of each compound on 偽 -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.
【作者單位】： 石河子大學(xué)藥學(xué)院;石河子大學(xué)化學(xué)化工學(xué)院;
【基金】：石河子大學(xué)杰出青年科技人才培育計劃(No.2015ZRKXJQ08) 國家自然科學(xué)基金(No.81560680)資助項(xiàng)目~~
【分類號】：O657.63;TQ464

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