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从两面针根皮中提取的α-淀粉酶和α-葡萄糖苷酶抑制剂。

α-Amylase and α-glucosidase inhibitors from Zanthoxylum chalybeum Engl. root bark.

机构信息

Department of Chemistry, Maseno University, Maseno, Kenya.

Department of Chemistry, Maseno University, Maseno, Kenya.

出版信息

Fitoterapia. 2020 Oct;146:104719. doi: 10.1016/j.fitote.2020.104719. Epub 2020 Sep 2.

DOI:10.1016/j.fitote.2020.104719
PMID:32889048
Abstract

A systematic analysis of the root bark of Zanthoxylum chalybeum was conducted to establish the antidiabetic potential of isolated compounds based on its ethnomedicinal use to manage diabetes. Chromatographic separation of alkaloid extracts led to isolation of three undescribed amides, chaylbemide A (1), chalybemide B (2) and chalybemide C (3) alongside the known fagaramide (4); four known benzophenanthridine alkaloids skimmianine (5), norchelerythrine (6), 6-acetonyldihydrochelerythrine (7) and 6-hydroxy-N-methyl decarine (8). The alkaloid free extracts yielded three known lignans, ailanthoidol (9), 2,3-epoxy-6,7-methylenedioxy coniferyl alcohol (10), sesamine (11), together with five known triterpenoids, lupeol (12), lupanone (13), 3α,20-dihydroxy-28-lupanoic acid (14), 20-hydroxy-3-oxo-28-lupanoic acid (15) and 3α,20,28-trihydroxylupane (16). The structures of the compounds were established based on 1D and 2D NMR spectroscopic and mass spectrometric experiments. Compounds 1-8 displayed inhibitory activities against both α-amylase and α-glycosidase in the range of IC = 43.22-49.36 μM which showed no significant (P > 0.05) difference to the positive control acarbose (IC = 42.67; 44.88 μM). The results confirmed anti-hyperglycemic potential of alkaloids from Z. chalybeum which lends credence to its use towards management of diabetes susceptibilities.

摘要

对两面针(Zanthoxylum chalybeum)的根皮进行了系统分析,以根据其在管理糖尿病方面的民族医学用途,确定分离化合物的降血糖潜力。生物碱提取物的色谱分离导致分离出三种未描述的酰胺,即 chaylbemide A(1)、chalybemide B(2)和 chalybemide C(3)以及已知的 fagaramide(4);四种已知的苯并菲啶生物碱 skimmianine(5)、norchelerythrine(6)、6-乙酰基二氢 chelerythrine(7)和 6-羟基-N-甲基 decarine(8)。生物碱游离提取物得到三种已知的木脂素,ailanthoidol(9)、2,3-环氧-6,7-亚甲二氧基松柏醇(10)、芝麻素(11),以及五种已知的三萜,羽扇豆醇(12)、羽扇豆酮(13)、3α,20-二羟基-28-齐墩果酸(14)、20-羟基-3-氧代-28-齐墩果酸(15)和 3α,20,28-三羟基羽扇烷(16)。根据 1D 和 2D NMR 光谱和质谱实验确定了化合物的结构。化合物 1-8 对α-淀粉酶和α-糖苷酶均显示出抑制活性,其 IC 50 值在 43.22-49.36 μM 范围内,与阳性对照阿卡波糖(IC 50 值分别为 42.67 和 44.88 μM)无显著差异(P > 0.05)。结果证实了两面针生物碱的抗高血糖潜力,这为其用于糖尿病易感性管理提供了依据。

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