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白花丹可抑制与 2 型糖尿病相关的关键酶,具有体外和计算机模拟作用;并可调节腹部葡萄糖吸收和肌肉葡萄糖摄取的体外作用。

Boerhaavia diffusa inhibits key enzymes linked to type 2 diabetes in vitro and in silico; and modulates abdominal glucose absorption and muscle glucose uptake ex vivo.

机构信息

Department of Biochemistry, School of Life Sciences, University of KwaZulu-Natal, (Westville Campus), Durban, 4000, South Africa.

Department of Biochemistry, School of Life Sciences, University of KwaZulu-Natal, (Westville Campus), Durban, 4000, South Africa; Department of Pharmacology, University of the Free State, Bloemfontein, 9301, South Africa.

出版信息

Biomed Pharmacother. 2018 Oct;106:1116-1125. doi: 10.1016/j.biopha.2018.07.053. Epub 2018 Jul 17.

DOI:10.1016/j.biopha.2018.07.053
PMID:30119178
Abstract

The present study investigated the in vitro and ex vivo antioxidant, anti-diabetic and anti-obesogenic potentials of different solvent (ethyl acetate, ethanol and water) extracts from the aerial parts of Boerhaavia diffusa. The ferric reducing antioxidant power (FRAP), DPPH scavenging activity and the ameliorative effects of the extracts on Fe-induced oxidative injury was investigated both in vitro and ex vivo. Alpha glucosidase and pancreatic lipase inhibitory potentials of the extracts were examined in vitro, while the effects of the ethanol extract on abdominal glucose intake and muscle glucose uptake were determined in freshly harvested tissues ex vivo. The extracts were subjected to Gas Chromatography-Mass Spectrometry (GC-MS) analysis to identify their possible bioactive components. The ethanol extract showed the most potent FRAP and DPPH radical scavenging activities compared to other extracts. All extracts increased catalase and SOD activities, and GSH levels in oxidative pancreatic injury. Both ethanol and aqueous extracts exhibited remarkable enzyme inhibitory activities, which was significantly higher than ethyl acetate extract and acarbose but was not comparable to orlistat. The ethanol extract portrayed a dose-dependent inhibitory effect on jejunal glucose uptake and enhancement of muscle glucose uptake. 9-(4 methoxyphenyl) xanthene, xanthone and stigmasterol showed strong binding affinities for α-glucosidase and lipase enzymes tested. Data from this study suggest that aerial parts of B. diffusa (particularly the ethanol extract) may not only exhibit antioxidant potentials but may also mediate anti-lipidemic and anti-hyperglycemic effects via inhibiting fat and carbohydrate digestion as well as abdominal glucose intake and enhancing muscle glucose uptake.

摘要

本研究考察了不同溶剂(乙酸乙酯、乙醇和水)从白花丹地上部分提取的抗氧化剂、抗糖尿病和抗肥胖的体外和离体潜力。在体外和离体研究了提取物的铁还原抗氧化能力(FRAP)、DPPH 清除活性以及对 Fe 诱导的氧化损伤的改善作用。还在体外研究了提取物的α-葡萄糖苷酶和胰脂肪酶抑制潜力,而乙醇提取物对新鲜收获组织离体腹部葡萄糖摄取和肌肉葡萄糖摄取的影响。对提取物进行气相色谱-质谱(GC-MS)分析,以鉴定其可能的生物活性成分。与其他提取物相比,乙醇提取物表现出最强的 FRAP 和 DPPH 自由基清除活性。所有提取物均能增加过氧化氢酶和 SOD 活性以及氧化胰腺损伤中的 GSH 水平。乙醇和水提取物均表现出显著的酶抑制活性,明显高于乙酸乙酯提取物和阿卡波糖,但与奥利司他不可比。乙醇提取物对空肠葡萄糖摄取表现出剂量依赖性抑制作用,并增强肌肉葡萄糖摄取。9-(4-甲氧基苯基)呫吨酮、呫吨酮和豆甾醇对α-葡萄糖苷酶和脂肪酶表现出很强的结合亲和力。本研究的数据表明,白花丹地上部分(特别是乙醇提取物)不仅可能具有抗氧化潜力,而且还可能通过抑制脂肪和碳水化合物消化以及腹部葡萄糖摄取和增强肌肉葡萄糖摄取来介导抗血脂和抗高血糖作用。

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