Bioassay-guided isolation of α-glucosidase inhibitors from Byrsonima garcibarrigae Cuatrec.

Tallita Marques Machado, Carolina Queiroz Valentim, Leonard Domingo Rosales Acho, Emerson Silva Lima, Hector Henrique Ferreira Koolen, F. Guilhon-Simplicio
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Abstract

Introduction:Byrsonima garcibarrigae is an endemic tree of Amazonas state, Brazil, with pharmacological and chemical knowledge poorly understood. Aim: To investigate the antidiabetic potential of the B. garcibarrigae stem bark. Methods: The stem bark was sequentially extracted by maceration with hexane (EHBG), ethyl acetate (EABG), and methanol (EMBG). The antioxidant capacity, α-glucosidase inhibitory potentials and anti-glycation capacities were evaluated. A bio-guided fractionation gave compounds that were characterized by MS and NMR. Results: 8 compounds were identified by HPLC-MS. EMBG showed the highest α-glucosidase inhibitory activity (1.09±0.32 μg/mL), antioxidant activity (9.2±0.23 μg/mL) and phenolic compounds content (61.43±0.50%), thus was fractionated producing hexane (FHX), chloroform (FCL) and hydromethanolic (FHM) fractions. After additional anti-α-glucosidase assays, FHM (1.02±0.49 μg/mL) was fractionated giving quercitrin and epicatechin. The anti-glycation assay showed that EMBG, FHM and quercitrin presented higher activities in comparison to the positive control, aminoguanidine. Conclusions:B. garcibarrigae displayed antidiabetic potential since inhibited α-glucosidase, as well as presented expressive antioxidant and anti-glycation activities were recorded.
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生物测定法分离枸杞子α-葡萄糖苷酶抑制剂。
garcibarrigae是巴西亚马逊州的一种特有乔木,对其药理和化学知识了解甚少。目的:研究菝葜茎皮的抗糖尿病作用。方法:采用正己烷(EHBG)、乙酸乙酯(EABG)、甲醇(EMBG)浸渍法提取茎皮。对其抗氧化能力、α-葡萄糖苷酶抑制能力和抗糖化能力进行了评价。生物引导分馏得到了经质谱和核磁共振表征的化合物。结果:HPLC-MS鉴定出8个化合物。EMBG的α-葡萄糖苷酶抑制活性最高(1.09±0.32 μg/mL),抗氧化活性最高(9.2±0.23 μg/mL),酚类化合物含量最高(61.43±0.50%),经分馏得到己烷(FHX)、氯仿(FCL)和氢甲醇(FHM)三组分。经抗-α-葡萄糖苷酶检测后,提取FHM(1.02±0.49 μg/mL),给予槲皮素和表儿茶素。抗糖化实验表明,EMBG、FHM和槲皮素的活性高于阳性对照氨基胍。结论:B。Garcibarrigae具有抑制α-葡萄糖苷酶的抗糖尿病作用,并表现出明显的抗氧化和抗糖化活性。
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