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富含类黄酮和原花青素的 Eugenia dysenterica 果实和叶子部分能够抑制晚期糖基化终产物的形成以及α-淀粉酶和α-葡萄糖苷酶的活性。

Flavonoids and proanthocyanidins-rich fractions from Eugenia dysenterica fruits and leaves inhibit the formation of advanced glycation end-products and the activities of α-amylase and α-glucosidase.

机构信息

Institute of Biotechnology - Federal University of Uberlandia, Av. Pará, 1720, 38400-902, Uberlândia, MG, Brazil.

Institute of Biotechnology - Federal University of Uberlandia, Av. Pará, 1720, 38400-902, Uberlândia, MG, Brazil.

出版信息

J Ethnopharmacol. 2022 Mar 1;285:114902. doi: 10.1016/j.jep.2021.114902. Epub 2021 Dec 8.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Different parts of Eugenia dysenterica have been popularly used in Brazil for treating diabetes mellitus and its complications. The present study aimed to screen extracts from E. dysenterica fruit pulp, peel, seed and leaf for carbohydrate digestive enzymes inhibitors with antioxidant and anti-glycation capacities.

MATERIALS AND METHODS

Ethanol extracts of E. dysenterica were subjected to a liquid-liquid fractionation and the fractions were used to evaluate their antioxidant properties and inhibitory potential against the formation of advanced glycation end-products (AGEs) and α-amylase and α-glucosidase.

RESULTS

The ethyl acetate fraction (EtOAcF) from seed and the dichloromethane fraction (CHClF) and EtOAcF from leaf had high antioxidant capacities (ORAC >5500 μmol trolox eq g, FRAP >1500 μmol trolox eq g and DPPH IC < 35 μg mL) and showed exceptional inhibitory activities against AGEs formation (glycation inhibition above 80% at 10 μg mL) and α-amylase and α-glucosidase (inhibition above 50% at 10 μg mL). The gallated B-types proanthocyanidins were the most active ingredients found in the leaf of E. dysenterica (CHCl and EtOAcF), being responsible for the notorious inhibitory effects against glycation and glycoside hydrolases due to their ortho-hydroxyl groups, which play role in scavenge and quench free radicals and glycated products, and may occupy the enzymes' substrate binding pocket. Furthermore, gallic acid, quercetin and its glycoside derivatives were detected by the first time in the E. dysenterica fruit seed (EtOAcF).

CONCLUSIONS

The results strongly contribute to the understanding of the antidiabetic potential of seeds and leaves from E. dysenterica, a species from a global biodiversity hotspot, which appears to be linked to the prevention of oxidative stress, AGEs production and postprandial hyperglycemia.

摘要

民族药理学相关性

巴西民间常使用不同部位的痢疾杨桃来治疗糖尿病及其并发症。本研究旨在筛选痢疾杨桃的果肉、果皮、种子和叶子的提取物,以寻找具有抗氧化和抗糖化能力的碳水化合物消化酶抑制剂。

材料与方法

对痢疾杨桃的乙醇提取物进行液-液分馏,并用所得馏分评估其抗氧化性能以及对形成晚期糖基化终产物(AGEs)和α-淀粉酶及α-葡萄糖苷酶的抑制潜力。

结果

种子的乙酸乙酯部分(EtOAcF)、叶子的二氯甲烷部分(CHClF)和 EtOAcF 具有较高的抗氧化能力(ORAC>5500 μmol Trolox eq g、FRAP>1500 μmol Trolox eq g 和 DPPH IC<35 μg mL),并且对 AGEs 形成(在 10 μg mL 时抑制率超过 80%)和α-淀粉酶及α-葡萄糖苷酶(在 10 μg mL 时抑制率超过 50%)表现出卓越的抑制活性。叶子中的没食子酰基 B 型原花青素是痢疾杨桃中最活跃的成分(CHCl 和 EtOAcF),由于其邻位羟基,它们对糖化和糖苷水解酶具有显著的抑制作用,这些羟基在清除和淬灭自由基和糖化产物方面发挥作用,并且可能占据酶的底物结合口袋。此外,首次在痢疾杨桃的种子(EtOAcF)中检测到没食子酸、槲皮素及其糖苷衍生物。

结论

这些结果为理解痢疾杨桃种子和叶子的抗糖尿病潜力提供了有力的依据,痢疾杨桃是全球生物多样性热点地区的一种物种,这似乎与预防氧化应激、AGEs 产生和餐后高血糖有关。

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