A key strategy to mitigate postprandial hyperglycemia involves inhibiting α-amylases, which commence the starch digestion process in the gut. This study examined the inhibitory effects of resveratrol and stilbenoid tetramers, vaticanol B, (−)-hopeaphenol, and vatalbinoside A on human salivary and pancreatic α-amylases experimentally and through molecular docking studies. Vaticanol B demonstrated the most potent inhibition with IC₅₀ values of 5.3 ± 0.3 μM for salivary and 6.1 ± 0.5 μM for pancreatic α-amylase (compared to acarbose with IC₅₀ values of 1.2 ± 0.1 μM and 0.5 ± 0.0 μM, respectively). Kinetic analysis suggested a competitive inhibition mode for vaticanol B. Resveratrol and vatalbinoside A were poor inhibitors of human α-amylases, while (−)-hopeaphenol exhibited moderate inhibition. Molecular docking supported the inhibition data, and several aspects of the structural configurations explained the stronger inhibition exerted by vaticanol B. Overall, vaticanol B shows promise as a natural alternative to acarbose for inhibiting α-amylase.

中文翻译：

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白藜芦醇寡聚物对人唾液和胰腺 α-淀粉酶的抑制


缓解餐后高血糖的一个关键策略包括抑制 α-淀粉酶，它开始了肠道中的淀粉消化过程。本研究通过实验和分子对接研究检查了白藜芦醇和二苯乙烯类四聚体、梵蒂甘醇 B、（-）-hopeaphenol 和伐他比诺苷 A 对人唾液和胰腺 α-淀粉酶的抑制作用。梵蒂佳醇 B 表现出最有效的抑制作用，唾液的 IC 50 值为 5.3 ± 0.3 μM，胰腺 α-淀粉酶的 IC₅₀ 值为 6.1 ± 0.5 μM（与阿卡波糖的 IC₅₀ 值为 1.2 ± 0.1 μM 和 0.5 ± 0.0 μM 相比）。动力学分析表明梵蒂佳醇 B 的竞争性抑制模式。白藜芦醇和瓦他比诺苷 A 是人 α-淀粉酶的不良抑制剂，而 （-）-hopeaphenol 表现出中度抑制。分子对接支持抑制数据，结构配置的几个方面解释了梵蒂佳醇 B 施加的更强抑制作用。总体而言，梵蒂佳醇 B 有望成为阿卡波糖抑制 α-淀粉酶的天然替代品。