Inhibition of α-glucosidase and α-amylase by flavonoid glycosides from Lu'an GuaPian tea: molecular docking and interaction mechanism,Food & Function

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Inhibition of α-glucosidase and α-amylase by flavonoid glycosides from Lu'an GuaPian tea: molecular docking and interaction mechanism
Food & Function ( IF 5.1 ) Pub Date : 2018-06-26 , DOI: 10.1039/c8fo00562a
Fang Hua _{1,

2,

3,

4,

5} , Peng Zhou _{6,

7,

8,

9,

10} , Hao-Yue Wu _{1,

2,

3,

4,

5} , Gang-Xiu Chu _{1,

2,

3,

4,

5} , Zhong-Wen Xie _{1,

2,

3,

4,

5} , Guan-Hu Bao _{1,

2,

3,

4,

5}

Affiliation

Green tea may favorably modulate blood glucose homeostasis, and regular consumption of green tea can prevent the development of type 2 diabetes mellitus. In this study, α-glucosidase and α-amylase inhibitory effects of the novel acylated flavonol tetraglycoside (camellikaempferoside C, 1) and 14 other flavone and flavone glycosides (FGs) isolated from Lu'an GuaPian (Camellia sinensis L.O. Kuntze) were evaluated. The kaempferol monoglycoside (15) showed inhibitory activity against α-glucosidase with IC₅₀ at 40.02 ± 4.61 μM, and kaempferol diglycoside (13) showed α-amylase inhibition with IC₅₀ at 0.09 ± 0.02 μM. Further, inhibitory mechanisms of FGs 15 and 13 were studied by molecular docking analysis and fluorescence spectrometry. Molecular docking suggested that FG 15 interacted with α-glucosidase mainly by hydrogen bonding, which was the same interaction force between FG 13 and α-amylase. Intrinsic fluorescence of α-glucosidase and α-amylase was quenched by 15 and 13, respectively, through a static quenching mechanism. The spontaneous formation of 15-α-glucosidase and 13-α-amylase complexes was driven by van der Waals forces and hydrogen bonding. The present study provides new insight into the potential application of Lu'an GuaPian green tea as a functional food ingredient to regulate postprandial hyperglycemia through inhibition of α-glucosidase/α-amylase by FGs, particularly the mono⁻ and di⁻ glycosides of kaempferol.

中文翻译：

六安瓜片茶中黄酮苷对α-葡萄糖苷酶和α-淀粉酶的抑制作用：分子对接和相互作用机理

绿茶可以有利地调节血糖的动态平衡，经常食用绿茶可以预防2型糖尿病的发生。在这项研究中，评估了从Lu安瓜片（Camellia sinensis LO Kuntze）分离的新型酰化黄酮醇四糖苷（camellikaempferoside C，1）和14种其他黄酮和黄酮苷（FGs）的α-葡萄糖苷酶和α-淀粉酶抑制作用。山奈黄素的单糖苷（15）显示针对α葡糖苷酶带IC抑制活性₅₀在40.02±4.61μM，山奈酚二糖苷（13）显示出α淀粉酶与抑制IC ₅₀ 0.09±0.02μM。此外，FG 15和FG的抑制机制通过分子对接分析和荧光光谱法研究了13种。分子对接表明FG 15主要通过氢键与α-葡萄糖苷酶相互作用，这与FG 13与α-淀粉酶之间的相互作用力相同。通过静态猝灭机制，α-葡萄糖苷酶和α-淀粉酶的固有荧光分别被15和13猝灭。15 -α-葡萄糖苷酶和13-的自发形成α-淀粉酶复合物是由范德华力和氢键驱动的。本研究提供新的见解六安瓜片绿茶的潜在应用程序作为功能性食品组分通过的FG，特别是单以调节通过抑制α葡糖苷酶/α淀粉酶的餐后高血糖^-和二^-山奈酚苷。

更新日期：2018-08-15

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