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从美洲土人参鳞茎中提取的α-葡萄糖苷酶抑制剂。

α-Glucosidase inhibitors from the bulb of Eleutherine americana.

机构信息

Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Kita-ku, Sapporo 060-8589, Japan.

Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Kita-ku, Sapporo 060-8589, Japan.

出版信息

Food Chem. 2011 Sep 15;128(2):308-11. doi: 10.1016/j.foodchem.2011.03.021. Epub 2011 Mar 29.

Abstract

One effective way to treat diabetes is by suppressing carbohydrate digestion due to the utilisation of α-glucosidase inhibitors (AGIs). The determination of prospective herbs, done in vitro by using enzyme assay, resulted in the finding of Eleutherine americana, which showed a potent inhibitory activity. A 50% aqueous methanol-soluble extract of bulbs of E. americana was chromatographed successively and the active fractions were further purified with preparative high performance liquid chromatography (HPLC) to isolate active compounds against α-glucosidase. Structure determination by mass and NMR analysis revealed that these isolated compounds were eleutherol (1), eleutherinoside A (2), and eleuthoside B (3) based on comparisons with the reference data. Considering the amount and the inhibitory activity of each naphthalene in the whole extracts, the bulb of E. americana inhibitory activity against α-glucosidase might be a result of compound 2 (IC50=0.5mM, yield=5mg/50g plant sample, with a characteristic structure which has never been found in other AGIs. AGIs play an important role for the treatment of diabetes, therefore these results may suggest novel alternatives for diabetes treatment management.

摘要

治疗糖尿病的一种有效方法是抑制碳水化合物的消化,这是由于使用了α-葡萄糖苷酶抑制剂(AGIs)。通过酶测定在体外进行的潜在草药的测定,发现美洲麟毛蕨表现出很强的抑制活性。美洲麟毛蕨鳞茎的 50%甲醇水溶液提取物依次进行色谱分离,用制备高效液相色谱(HPLC)进一步纯化活性部分,以分离出针对α-葡萄糖苷酶的活性化合物。通过质谱和 NMR 分析确定这些分离出的化合物为 eleutherol(1)、eleutherinoside A(2)和 eleuthoside B(3),这是基于与参考数据的比较。考虑到全提取物中每个萘的含量和对α-葡萄糖苷酶的抑制活性,美洲麟毛蕨鳞茎对α-葡萄糖苷酶的抑制活性可能是化合物 2 的结果(IC50=0.5mM,产率=5mg/50g 植物样品,具有从未在其他 AGIs 中发现的特征结构。AGIs 对糖尿病的治疗起着重要作用,因此这些结果可能为糖尿病治疗管理提供新的选择。

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