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  • Title: Inhibition of α-glucosidase and α-amylase by herbal compounds for the treatment of type 2 diabetes: A validation of in silico reverse docking with in vitro enzyme assays.
    Author: Tolmie M, Bester MJ, Apostolides Z.
    Journal: J Diabetes; 2021 Oct; 13(10):779-791. PubMed ID: 33550683.
    Abstract:
    BACKGROUND: α-Amylase and α-glucosidase are important therapeutic targets for the management of type 2 diabetes mellitus. The inhibition of these enzymes decreases postprandial hyperglycemia. In the present study, compounds found in commercially available herbs and spices were tested for their ability to inhibit α-amylase and α-glucosidase. These compounds were acetyleugenol, apigenin, cinnamic acid, eriodictyol, myrcene, piperine, and rosmarinic acid. METHODS: The enzyme inhibitory nature of the compounds was evaluated using in silico docking analysis with Maestro software and was further confirmed by in vitro α-amylase and α-glucosidase biochemical assays. RESULTS: The relationships between the in silico and in vitro results were well correlated; a more negative docking score was associated with a higher in vitro inhibitory activity. There was no significant (P > .05) difference between the inhibition constant (Ki ) value of acarbose, a widely prescribed α-glucosidase and α-amylase inhibitor, and those of apigenin, eriodictyol, and piperine. For α-amylase, there was no significant (P > .05) difference between the Ki value of acarbose and those of apigenin, cinnamic acid, and rosmarinic acid. The effect of the herbal compounds on cell viability was assessed with the sulforhodamine B (SRB) assay in C2C12 and HepG2 cells. Acetyleugenol, cinnamic acid, myrcene, piperine, and rosmarinic acid had similar (P > .05) IC50 values to acarbose. CONCLUSIONS: Several of the herbal compounds studied could regulate postprandial hyperglycemia. Using herbal plants has several advantages including low cost, natural origin, and easy cultivation. These compounds can easily be consumed as teas or as herbs and spices to flavor food. 背景: α-淀粉酶和α-葡萄糖苷酶是2型糖尿病治疗的重要靶点。抑制这些酶可以降低餐后高血糖。在本研究中, 测试了在市售草药和香料中发现的化合物对α-淀粉酶和α-葡萄糖苷酶的抑制能力。这些化合物是乙酰亮酚、芹菜素、肉桂酸、芥子醇、月桂烯、胡椒碱和迷迭香酸。 方法: 用Maestro软件进行电子对接分析, 并通过体外α-淀粉酶和α-葡萄糖苷酶生化测定进一步证实化合物的抑酶活性。 结果: 体内和体外结果之间有很好的相关性；对接得分越低, 体外抑制活性越高。广泛应用的α-葡萄糖苷酶和α-淀粉酶抑制剂阿卡波糖与芹菜素、芥子醇和胡椒碱的抑制常数(Ki)值无显著性差异(P>0.05)。对于α-淀粉酶, 阿卡波糖的Ki值与芹菜素、肉桂酸、迷迭香酸无显著差异(P>0.05)。另外采用了硫代罗丹明B(SRB)比色法检测中药复方对C2C12和HepG2细胞活力的影响。乙酰亮酚、肉桂酸、月桂烯、胡椒碱和迷迭香酸的IC50值与阿卡波糖相似(P>0.05)。 结论: 所研究的几种中草药化合物具有调节餐后高血糖的作用。使用中草药植物具有成本低、来源天然、易于栽培等优点。这些化合物可以很容易地作为茶或草药和香料食用并为食物调味。.
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