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2,3-环氧原花青素 C1 及其他成分对 α-淀粉酶和 α-葡萄糖苷酶的体外抑制作用评价

In Vitro Evaluation of α-amylase and α-glucosidase Inhibition of 2,3-Epoxyprocyanidin C1 and Other Constituents from Poir.

机构信息

Department of Chemistry, Faculty of Sciences, University of Ngaoundere, Ngaoundere P.O. Box 454, Cameroon.

Department of Chemical Engineering, School of Chemical Engineering and Mineral Industries, University of Ngaoundere, Ngaoundere P.O. Box 454, Cameroon.

出版信息

Molecules. 2022 Dec 23;28(1):126. doi: 10.3390/molecules28010126.

DOI:10.3390/molecules28010126
PMID:36615320
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9822058/
Abstract

Diabetes mellitus is a metabolic disorder which is one of the leading causes of mortality and morbidities in elderly humans. Chronic diabetes can lead to kidney failure, blindness, limb amputation, heart attack and stroke. Physical activity, healthy diets and medications can reduce the incidence of diabetes, so the search for more efficient antidiabetic therapies, most especially from natural products, is a necessity. Herein, extract from roots of the medicinal plant was purified by column chromatography and afforded ten compounds which were characterized by EIMS, HR-FAB-MS, 1D and 2D NMR techniques. Amongst them were, a new trimeric derivative of epicatechin, named 2,3-Epoxyprocyanidin C1 (1); two pentacyclic triterpenoids, friedelin (2) and betulin (3); angolensin (4); flavonoids such as 7-methoxygenistein (5), 7-methoxydaidzein (6), apigenin 7-O-glucoronide (8) and naringenin 7-O-β-D-glucopyranoside (9); and an ellagic acid derivative (10). The extract and compounds were evaluated for their antidiabetic potential by α-amylase and α-glucosidase inhibitory assays. IC values of compound (48.1 ± 0.9 µg/mL), compound (48.6 ± 0.1 µg/mL), compound (50.2 ± 0.5 µg/mL) and extract (40.5 ± 0.8 µg/mL) when compared to that of acarbose (26.4 ± 0.3 µg/mL) indicated good α-amylase inhibition. In the α-glucosidase assay, the extract (IC = 31.2 ± 0.1 µg/mL), compound (IC = 39.5 ± 1.2 µg/mL), compound (IC = 40.9 ± 1.3 µg/mL), compound (IC = 41.6 ± 1.0 µg/mL), Compound (IC = 43.4 ± 0.5 µg/mL), compound (IC = 47.6 ± 0.9 µg/mL), compound (IC = 46.3 ± 0.2 µg/mL), compound (IC = 45.0 ± 0.8 µg/mL), compound (IC = 44.8 ± 0.6 µg/mL) and compound (IC = 47.5 ± 0.4 µg/mL) all had moderate-to-good inhibitions, compared to acarbose (IC = 22.0 ± 0.5 µg/mL). The ability to inhibit α-amylase and α-glucosidase indicates that and its compounds can lower blood glucose levels by delaying hydrolysis of carbohydrates into sugars, thereby providing a source of natural antidiabetic remedy.

摘要

糖尿病是一种代谢紊乱,是导致老年人死亡和发病的主要原因之一。慢性糖尿病可导致肾衰竭、失明、截肢、心脏病发作和中风。体育活动、健康饮食和药物治疗可以降低糖尿病的发病率,因此,寻找更有效的抗糖尿病疗法,特别是从天然产物中寻找,是必要的。在此,从药用植物的根部分离纯化得到十个化合物,通过 EIMS、HR-FAB-MS、1D 和 2D NMR 技术进行了表征。其中包括一种新的表儿茶素三聚体衍生物,命名为 2,3-环氧原花青素 C1(1);两种五环三萜类化合物,即菜油甾醇(2)和白桦脂醇(3);angolensin(4);黄酮类化合物,如 7-甲氧基染料木素(5)、7-甲氧基大豆苷元(6)、芹菜素 7-O-葡萄糖醛酸苷(8)和柚皮素 7-O-β-D-吡喃葡萄糖苷(9);和一个鞣花酸衍生物(10)。通过α-淀粉酶和α-葡萄糖苷酶抑制试验评估提取物和化合物的抗糖尿病潜力。与阿卡波糖(26.4 ± 0.3 µg/mL)相比,化合物 (48.1 ± 0.9 µg/mL)、化合物 (48.6 ± 0.1 µg/mL)、化合物 (50.2 ± 0.5 µg/mL)和提取物(40.5 ± 0.8 µg/mL)的 IC 值表明对α-淀粉酶有良好的抑制作用。在α-葡萄糖苷酶试验中,提取物(IC = 31.2 ± 0.1 µg/mL)、化合物 (IC = 39.5 ± 1.2 µg/mL)、化合物 (IC = 40.9 ± 1.3 µg/mL)、化合物 (IC = 41.6 ± 1.0 µg/mL)、化合物 (IC = 43.4 ± 0.5 µg/mL)、化合物 (IC = 47.6 ± 0.9 µg/mL)、化合物 (IC = 46.3 ± 0.2 µg/mL)、化合物 (IC = 45.0 ± 0.8 µg/mL)、化合物 (IC = 44.8 ± 0.6 µg/mL)和化合物 (IC = 47.5 ± 0.4 µg/mL)均具有中等至良好的抑制作用,而阿卡波糖(IC = 22.0 ± 0.5 µg/mL)。抑制α-淀粉酶和α-葡萄糖苷酶的能力表明,和其化合物可以通过延迟碳水化合物水解成糖来降低血糖水平,从而为天然抗糖尿病疗法提供了一种来源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/9822058/bbb3c424d8e3/molecules-28-00126-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/9822058/ffd11c75b42c/molecules-28-00126-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/9822058/bbb3c424d8e3/molecules-28-00126-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/9822058/ffd11c75b42c/molecules-28-00126-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6db2/9822058/bbb3c424d8e3/molecules-28-00126-g002.jpg

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