中国食品学报

3种黄酮联合阿卡波糖抑制α-淀粉酶活性的机制

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王昆山 ¹ , 范金波 ¹ , 周素珍 ¹ , 于增辉 ¹ , 张璇 ¹ , 翟迎奥 ¹

中国食品学报 | 基础研究 2026,26(1): 83-95

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中国食品学报 | 基础研究 2026, 26(1): 83-95

3种黄酮联合阿卡波糖抑制α-淀粉酶活性的机制

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王昆山¹, 范金波¹, 周素珍¹, 于增辉¹, 张璇¹, 翟迎奥¹

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^1.渤海大学食品科学与工程学院辽宁锦州 121013

Mechanism of Three Flavonoids Combined with Acarbose in Inhibiting α-Amylase Activity

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出版时间: 2026-01-31 doi: 10.16429/j.1009-7848.2026.01.008

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摘要

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目的:探究3种黄酮【黄芩素(Bai)、金雀异黄酮(Gen)、异甘草素(Isl)】与阿卡波糖(Aca)联合抑制α-淀粉酶(AMY)的作用机制。方法:通过抑制率试验、联合指数(CI)分析、荧光光谱分析、紫外光谱分析、红外光谱分析及分子动力学模拟等方法，系统研究联合抑制对AMY的抑制效果及机制。结果:Bai/Gen/Isl与Aca在物质的量比为2 ∶ 1，3 ∶ 1，4 ∶ 1的条件下，均对AMY的抑制效果显著增强(P＜0.05)，其中Bai-Aca和Isl-Aca在物质的量比为3 ∶ 1时，表现出强协同效应(CI<1)，而Gen-Aca仅在物质的量比为3 ∶ 1时，且0.3

关键词

联合抑制 / 黄芩素 / 金雀异黄酮 / 异甘草素 / 阿卡波糖 / 分子动力学

Abstract

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Objective: To investigate the mechanism of synergistic inhibition of α-amylase (AMY) by three flavonoids [baicalein (Bai)， genistein (Gen)， isoliquiritigenin (Isl)] combined with acarbose (Aca). Through methods such as inhibition rate experiments， combination index (CI) analysis， fluorescence spectroscopy， ultraviolet spectroscopy， infrared spectroscopy， and molecular dynamics simulation， the inhibitory effects and action mechanisms of the combined inhibition on AMY were systematically studied. The results show that the inhibitory effects of Bai/Gen/Isl combined with Aca on AMY were significantly enhanced at molar ratios of 2∶1， 3∶1， and 4∶1. Among them， Bai-Aca and Isl-Aca exhibited a strong synergistic effect at a molar ratio of 3∶1(CI < 1)， while Gen-Aca showed synergism only at a molar ratio of 3∶1 and under the specific condition of 0.3 < Fa < 0.9(fraction affected). Fluorescence spectroscopy analysis showed that the combined inhibitors bind to AMY via a static quenching mechanism. Among them， Isl-Aca exhibits the highest binding constant (Ka) with AMY [K = (4.826±0.206)×105 L/mol at 298 K； Ka = (35.172±0.255)×105 L/mol at 300 K]， and its affinity is significantly enhanced with increasing temperature (P < 0.05)， indicating that the complex formed by Isl-Aca and AMY has the optimal stability. Thermodynamic parameters indicated that hydrophobic interactions were the main driving force for Bai-Aca and Isl-Aca， while Gen-Aca relied on hydrogen-bond binding. Synchronous fluorescence and ultraviolet spectroscopy showed that the combined inhibitors regulated the activity of AMY by changing the microenvironment of tryptophan (Trp) and tyrosine (Tyr) residues， with the inhibitory effect of Trp residues being dominant. Infrared spectroscopy and molecular dynamics simulation further revealed that Bai-Aca and Isl-Aca promoted the transformation of the secondary structure of AMY into a more stable β-turn， while Gen-Aca induced the formation of α-helix. However， the free-energy landscape of the latter complex presented a dispersed energy cluster， indicating weaker stability. In conclusion， the Bai-Aca and Isl-Aca combined inhibition systems significantly reduce the dosage of inhibitors through multi-target synergistic effects， while maintaining the high stability of the AMY complex. This provides a theoretical basis for the development of novel diabetes treatment strategies and functional foods based on flavonoids.

Key words

combined inhibition / baicalein / genistein / isoliquiritigenin / acarbose / molecular dynamics

引用本文

王昆山, 范金波, 周素珍, 于增辉, 张璇, 翟迎奥. 3种黄酮联合阿卡波糖抑制α-淀粉酶活性的机制. 中国食品学报, 2026 , 26 (1) : 83 -95 . DOI: 10.16429/j.1009-7848.2026.01.008

. Mechanism of Three Flavonoids Combined with Acarbose in Inhibiting α-Amylase Activity[J]. Journal of Chinese Institute of Food Science and Technology, 2026 , 26 (1) : 83 -95 . DOI: 10.16429/j.1009-7848.2026.01.008

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国家重点研发计划项目

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2026年第26卷第1期

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doi: 10.16429/j.1009-7848.2026.01.008

接收时间：2025-02-14
首发时间：2026-05-27
出版时间：2026-01-31

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收稿日期：2025-02-14

基金

国家重点研发计划项目

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^1.渤海大学食品科学与工程学院辽宁锦州 121013

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2种不同金属材料的力学参数

科 Family	属数 Number of genus	种数 Number of species	占总种数比例 Percentage of total species (%)	属 Genus	种数 Number of species	占总种数比例 Percentage of total species (%)
鹅膏菌科Amanitaceae	2	11	5.26	鹅膏菌属 Amanita	10	4.78
小菇科 Mycenaceae	2	12	5.74	丝盖伞属 Inocybe	5	2.39
多孔菌科 Polyporaceae	8	14	6.70	蜡蘑属 Laccaria	5	2.39
红菇科 Russulaceae	3	23	11.00	小皮伞属 Marasmius	6	2.87
				小菇属 Mycena	11	5.26
				光柄菇属 Pluteus	5	2.39
				红菇属 Russula	17	8.13
				栓菌属 Trametes	5	2.39