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类黄酮糖苷:体外抑制 DPPIV、醛糖还原酶和对抗氧化应激是介导其抗糖尿病活性的潜在机制。

Flavonol Glycosides: In Vitro Inhibition of DPPIV, Aldose Reductase and Combating Oxidative Stress are Potential Mechanisms for Mediating the Antidiabetic Activity of .

机构信息

Department of Pharmacognosy, College of Pharmacy, King Khalid University, Abha 61441, Saudi Arabia.

Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

出版信息

Molecules. 2020 Dec 11;25(24):5864. doi: 10.3390/molecules25245864.

Abstract

Diabetes is a major health problem that is associated with high risk of various complications. Medicinal plants hold great promise against diabetes. The traditional use of as an antidiabetic agent was correlated to its flavonol glycosides content. In the current study, five major flavonol glycosides appeared on the RP-HPLC chromatogram of the aqueous extract namely; quercetin-3---d-glucosyl-7---rhamnoside (), isorhamnetin-7---neohesperidoside (), isorhamnetin-3---d-glucoside () kaempferol-4'-methoxy-3,7---dirhamnoside (), and isorhamnetin-3---(4″-acetylrhamnoside)-7---rhamnoside (). The inhibitory activities of these compounds were tested in vitro against several enzymes involved in diabetes management. Only the relatively less polar methoxylated flavonol glycosides (, ) showed mild to moderate α-amylase and α-glucosidase inhibitory activities. Compounds - displayed remarkable inhibition of dipeptidyl peptidase IV (DPPIV) enzyme (IC 0.194 ± 0.06, 0.573 ± 0.03, 0.345 ± 0.02 and 0.281 ± 0.05 µg/mL, respectively) comparable to vildagliptin (IC 0.154 ± 0.02 µg/mL). Moreover, these compounds showed high potential in preventing diabetes complications through inhibiting aldose reductase enzyme and combating oxidative stress. Both isorhamnetin glycoside derivatives () exhibited the highest activities in aldose reductase inhibition and compound (IC 5.45 ± 0.26 µg/mL) was even more potent than standard quercetin (IC 7.77 ± 0.43 µg/mL). Additionally, these flavonols exerted excellent antioxidant capacities through 2, 2-diphenyl-1-picrylhydrazil (DPPH) and ferric reducing antioxidant (FRAP) assays.

摘要

糖尿病是一种主要的健康问题,与各种并发症的高风险相关。药用植物在治疗糖尿病方面具有很大的潜力。传统上使用 作为抗糖尿病药物与其类黄酮糖苷的含量有关。在目前的研究中,在水提物的反相高效液相色谱(RP-HPLC)图谱上出现了五种主要的类黄酮糖苷,即槲皮素-3---d-葡萄糖基-7---鼠李糖苷(),异鼠李素-7---新橙皮糖苷(),异鼠李素-3---d-葡萄糖苷(),山柰酚-4'-甲氧基-3,7---二鼠李糖苷()和异鼠李素-3---(4″-乙酰鼠李糖苷)-7---鼠李糖苷()。这些化合物的体外抑制活性在体外针对几种参与糖尿病管理的酶进行了测试。只有相对较少极性的甲氧基化类黄酮糖苷(,)显示出轻度到中度的α-淀粉酶和α-葡萄糖苷酶抑制活性。化合物 - 对二肽基肽酶 IV(DPPIV)酶显示出显著的抑制作用(IC 0.194 ± 0.06、0.573 ± 0.03、0.345 ± 0.02 和 0.281 ± 0.05 µg/mL,分别),与维格列汀(IC 0.154 ± 0.02 µg/mL)相当。此外,这些化合物通过抑制醛糖还原酶酶和对抗氧化应激,显示出预防糖尿病并发症的高潜力。两种异鼠李素糖苷衍生物()在醛糖还原酶抑制中表现出最高的活性,化合物 (IC 5.45 ± 0.26 µg/mL)甚至比标准槲皮素(IC 7.77 ± 0.43 µg/mL)更有效。此外,这些类黄酮通过 2,2-二苯基-1-苦基肼(DPPH)和铁还原抗氧化能力(FRAP)测定法表现出出色的抗氧化能力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/415d/7764826/22d5d8a5d4db/molecules-25-05864-g001.jpg

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