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榄仁树成分的抗糖尿病活性。

Antidiabetic activity of Terminalia sericea constituents.

作者信息

Nkobole Nolitha, Houghton Peter James, Hussein Ahmed, Lall Namrita

机构信息

Department of Plant Science, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa.

出版信息

Nat Prod Commun. 2011 Nov;6(11):1585-8.

Abstract

Diabetes mellitus is an endocrine disorder that affects more than 100 million people worldwide. South African plants namely Terminalia sericea, Euclea natalensis, Warbugia salutaris, Aloe ferox, Artemisia afra, Sclerocarya birrea, Spirostachys africana and Psidium guajava were investigated for their in vitro alpha-glucosidase and alpha-amylase properties, and antioxidant activities. Terminalia sericea stem bark extract showed the best results against alpha-glucosidase and alpha-amylase enzymes. Bioassay-guided fractionation of an acetone extract of T. sericea stem bark led to the isolation of four known compounds namely beta-sitosterol (1), beta-sitosterol-3-acetate (2), lupeol (3), and stigma-4-ene-3-one (4), in addition to two inseparable sets of mixtures of isomers [epicatechin-catechin (M1), and gallocatechin-epigallocatechin (M2). 1 and 3 showed the best inhibitory activity on alpha-glucosidase (IC50:54.5 and 66.5 microM). Bio-evaluation of the inhibitory activity of the purified compounds on alpha-amylase showed that 3 and 1 exhibited IC50 values of 140.7 and 216.02 microM, respectively against alpha-amylase. Compounds 2, M1, 3 and M2 were found to be non-toxic to Vero cells. This study is the first to report alpha-glucosidase and alpha-amylase activity of M1, M2, 2 and 4 isolated from T. sericea, which validated the traditional use of the bark of T. sericea for diabetes in South Africa.

摘要

糖尿病是一种内分泌紊乱疾病,全球有超过1亿人受其影响。对南非植物绢毛榄仁树、纳塔尔真核木、药用沃伯格樟、好望角芦荟、南非蒿、南非硬核李、非洲螺旋麻和番石榴进行了体外α-葡萄糖苷酶和α-淀粉酶特性以及抗氧化活性的研究。绢毛榄仁树茎皮提取物对α-葡萄糖苷酶和α-淀粉酶表现出最佳效果。对绢毛榄仁树茎皮丙酮提取物进行生物测定导向的分级分离,除了得到两组无法分离的异构体混合物[表儿茶素-儿茶素(M1)和没食子儿茶素-表没食子儿茶素(M2)]外,还分离出四种已知化合物,即β-谷甾醇(1)、β-谷甾醇-3-乙酸酯(2)、羽扇豆醇(3)和豆甾-4-烯-3-酮(4)。1和3对α-葡萄糖苷酶表现出最佳抑制活性(IC50:54.5和66.5微摩尔)。对纯化化合物对α-淀粉酶的抑制活性进行生物评价表明,3和1对α-淀粉酶的IC50值分别为140.7和216.02微摩尔。发现化合物2、M1、3和M2对非洲绿猴肾细胞无毒。本研究首次报道了从绢毛榄仁树中分离出的M1、M2、2和4的α-葡萄糖苷酶和α-淀粉酶活性,证实了南非传统上使用绢毛榄仁树皮治疗糖尿病的做法。

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