Inhibitory effects against α-glucosidase and α-amylase of the flavonoids-rich extract from Scutellaria baicalensis shoots and interpretation of structure-activity relationship of its eight flavonoids by a refined assign-score method.
Ke Li, Fan Yao, Qiang Xue, Hang Fan, Lingguang Yang, Xiang Li, Liwei Sun, Yujun Liu
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引用次数: 84
Abstract
A flavonoids-rich extract of Scutellaria baicalensis shoots and its eight high content flavonoids were investigated for their inhibitory effects against α-glucosidase and α-amylase. Results show that abilities of the extract in inhibiting the two enzymes were obviously higher than those of acarbose. Moreover, inhibitory abilities of all the eight individual flavonoids against the two enzymes show exactly a same order (i.e., apigenin > baicalein > scutellarin > chrysin > apigenin-7-O-glucuronide > baicalin > chrysin-7-O-glucuronide > isocarthamidin-7-O-glucuronide), and their structure-activity relationship could be well-interpretated by the refined assign-score method. Furthermore, based on the inhibitory abilities and their contents in the extract, it was found that the eight flavonoids made predominant contributions, among which baicalein and scutellarin played roles as preliminary contributors, to overall inhibitory effects of the extract against the two enzymes. Beyond these, contributions of the eight flavonoids to the overall enzyme inhibitory activity were compared with those to the overall antioxidant activity characterized in our recent study, and it could be inferred that within the basic flavonoid structure the hydroxyl on C-4' of ring B was more effective than that on C-6 of ring A in enzyme inhibitory activities while they behaved inversely in antioxidant activities; scutellarin and apigenin contributed more to the overall enzyme inhibitory activity, and baicalin and scutellarin, to the overall antioxidant activity of the extract; and flavonoids of the extract, apart from directly inhibiting enzymes, might also be conducive to curing type 2 diabetes via scavenging various free radicals caused by increased oxidative stresses.
研究了黄芩芽富含黄酮类化合物的提取物及其8种高含量黄酮类化合物对α-葡萄糖苷酶和α-淀粉酶的抑制作用。结果表明,该提取物对这两种酶的抑制能力明显高于阿卡波糖。8种黄酮类化合物对这两种酶的抑制能力顺序为:芹菜素>黄芩素>黄芩素>菊花素>芹菜素-7- o -葡萄糖醛酸苷>黄芩苷>菊花素-7- o -葡萄糖醛酸苷>异胡萝卜素-7- o -葡萄糖醛酸苷),其构效关系可以用精细分配评分法很好地解释。此外,根据提取物对两种酶的抑制能力及其含量,发现8种黄酮类化合物对提取物对两种酶的总体抑制作用起主导作用,其中黄芩苷和黄芩苷起初步作用。此外,我们还比较了8种黄酮类化合物对总酶抑制活性的贡献与我们最近研究的总抗氧化活性的贡献,可以推断,在黄酮类化合物的基本结构中,B环C-4′上的羟基比A环C-6′上的羟基对酶抑制活性更有效,而抗氧化活性则相反;黄芩苷和黄芩苷对总酶抑制活性的贡献更大,黄芩苷和黄芩苷对总抗氧化活性的贡献更大;提取物中的黄酮类化合物,除了直接抑制酶外,还可能通过清除氧化应激增加引起的各种自由基,有助于治疗2型糖尿病。
期刊介绍:
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