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从水瓜柳中提取小檗碱的纯化、生化特性分析及其对 DPP-IV 和 α-淀粉酶的抑制活性。

Purification, biochemical characterization, and DPP-IV and α-amylase inhibitory activity of Berberine from Cardiospermum halicacabum.

机构信息

Centre for Bio-Separation Technology, Vellore Institute of Technology, Vellore, India.

Department of Pharmacognosy, King Saud University College of Pharmacy, Riyadh, Saudi Arabia.

出版信息

J Mol Recognit. 2022 Nov;35(11):e2983. doi: 10.1002/jmr.2983. Epub 2022 Aug 26.

Abstract

Diabetes mellitus (DM) has spread across the globe, increasing the risk of obesity, cardiovascular disease, and other comorbidities. Despite substantial research into the development of diabetic treatments that are effective in lowering blood glucose levels, their efficiency is short-lived due to unpleasant side effects such as weight gain and hypoglycemia. The discovery of secondary metabolites in the prevention and treatment of diabetes and its complications has an incentive to take interest in plant-based medications, and enzyme inhibitors have the potential to aid in the treatment and management of DM. This study aims to isolate, characterize, and analyse the influence of berberine-like alkaloids from alcoholic Cardiospermum halicacabum extract in vitro and in silico, as a possible inhibitor of Dipeptidyl peptidase-IV (DPP-IV) and α-amylase, two essential enzymes involved in diabetes. The alkaloid from C. halicacabum was identified as berberine, with an m/z of 336.1263. Purified berberine inhibits DPP-IV with an IC of 16.328 ± 1.344 μM and inhibits α-amylase by 72% at 10 μg/mL. In-silico studies demonstrated that berberine was found to bind to the active site of both DPP-IV and α-amylase. The precise mechanism underlying the observation has to be researched further in order to investigate C. halicacabum's anti-diabetic effects and argue for its possible application as alternative medicine.

摘要

糖尿病(DM)在全球范围内蔓延,增加了肥胖、心血管疾病和其他合并症的风险。尽管有大量研究致力于开发有效降低血糖水平的糖尿病治疗方法,但由于体重增加和低血糖等不良反应,其效果是短暂的。在预防和治疗糖尿病及其并发症方面发现的次生代谢物,激发了人们对植物性药物的兴趣,酶抑制剂有可能有助于糖尿病的治疗和管理。本研究旨在从 Cardiospermum halicacabum 的酒精提取物中分离、表征和分析黄连素样生物碱,并在体外和计算机模拟中研究其作为二肽基肽酶-IV(DPP-IV)和α-淀粉酶抑制剂的可能性,这两种酶是糖尿病中两种重要的酶。从 C. halicacabum 中分离出的生物碱被鉴定为小檗碱,其质荷比为 336.1263。纯化的小檗碱对 DPP-IV 的抑制 IC 为 16.328 ± 1.344 μM,对α-淀粉酶的抑制率在 10 μg/mL 时为 72%。计算机模拟研究表明,小檗碱被发现与 DPP-IV 和α-淀粉酶的活性部位结合。为了研究 C. halicacabum 的抗糖尿病作用并论证其作为替代医学的可能应用,需要进一步研究观察到的精确机制。

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