School of Food Science and Engineering, South China University of Technology, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, Guangzhou, PR China.
Sino-Singapore International Joint Research Institute, Guangzhou, China.
Crit Rev Food Sci Nutr. 2020;60(4):695-708. doi: 10.1080/10408398.2018.1548428. Epub 2019 Jan 13.
The objective of this review is to summarize knowledge on the inhibitory effects (IEs) of flavonoids on α-amylase (αA) and α-glucosidase (αG) relevant to the search of substitutes of acarbose (Aca). Flavonoids reported to be more effective at inhibiting αG than Aca have been summarized. The concept of "relative coefficient to Aca (RC)" has been proposed to integrate data from various reports. Correlations between hydrogen bond donors (H-donors), hydrogen bond acceptors (H-acceptors), partition coefficient values (XLog P3), and RC are discussed. Two kinds of binding modes between flavonoids and enzymes have been observed: (i) flavonoids directly bind to amino acid residues (AARs) in the active sites of enzymes and exclude the binding of substrate; (ii) flavonoids interact with AARs near the active site and close the channel to the active center. Some groups are correlated with stronger IEs: (i) substitutions of caffeoyl, galloyl, and prenyl groups in flavonoids enhance IEs; (ii) steric hindrance attenuates IEs, and linear molecules tend to be stronger inhibitors of porcine pancreatic αA (PPA). Whilst many achievements have been made, our understanding of the combined effects of different flavonoids, and flavonoids and Aca, remain ambiguous, and the effects of food matrices and stomach digestion on IEs of flavonoids are poorly understood. This review provides a comprehensive understanding on the use of flavonoids as αA and αG inhibitors for controlling diabetes.
本综述旨在总结黄酮类化合物对α-淀粉酶（αA）和α-葡萄糖苷酶（αG）的抑制作用（IEs）的知识，以寻找阿卡波糖（Aca）的替代品。总结了报道中对αG 的抑制作用比 Aca 更强的黄酮类化合物。提出了“相对阿卡波糖系数（RC）”的概念，以整合来自不同报告的数据。讨论了氢键供体（H-供体）、氢键受体（H-受体）、分配系数值（XLog P3）与 RC 之间的相关性。观察到黄酮类化合物与酶之间存在两种结合模式：（i）黄酮类化合物直接与酶的活性位点中的氨基酸残基（AARs）结合，从而阻止底物的结合；（ii）黄酮类化合物与活性位点附近的 AARs 相互作用，关闭通往活性中心的通道。一些基团与更强的 IEs 相关：（i）黄酮类化合物中咖啡酰基、没食子酰基和香叶基取代物增强 IEs；（ii）空间位阻减弱 IEs，线性分子往往是猪胰αA（PPA）的更强抑制剂。尽管已经取得了许多成就，但我们对不同黄酮类化合物以及黄酮类化合物和 Aca 的综合作用的理解仍然不清楚，并且食物基质和胃消化对黄酮类化合物 IEs 的影响也知之甚少。本综述提供了对黄酮类化合物作为αA 和 αG 抑制剂用于控制糖尿病的综合理解。
