从桑科榕中分离的二萜及其α -淀粉酶抑制活性

S. Mikailu, Afieroho Ozadheoghene Eriarie, K. Abo
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摘要

糖尿病的患病率在世界范围内呈上升趋势。目的是研究桑科榕叶对糖尿病民族药中α -淀粉酶的抑制作用。叶粉分别用正己烷、氯仿和70%乙醇浸泡3 d。评估了提取物的植物化学成分和α -淀粉酶的抑制作用。采用猪α-淀粉酶对α-淀粉酶的抑制作用进行评价。用硅胶G(目数60-120)填充柱层析分离生物活性正己烷提取物,用正己烷、乙酸乙酯和乙醇的梯度混合物洗脱。用制备薄层色谱法纯化活性组分(F1 - F5)。对活性纯化合物进行了生物活性评价,并通过光谱(紫外、红外、质谱和核磁共振)进行了鉴定。正己烷提取物的抑制作用最显著(p < 0.05)。在50µg/ml的浓度下,化合物F4的活性最高,具有55%的α -淀粉酶抑制作用,是一种新型的二萜(4,7,10-b-三甲基-苯并二甲苯[c]-6,6-a,8,9,10,10-a-六氢异铬酸-7-羧酸)。本文首次报道了从无花果中分离到的具有α -淀粉酶抑制活性的新型二萜。
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A Diterpene Isolated from Ficus sur Forssk (Moraceae) and it’s Alpha-Amylase Inhibition Activity
The prevalence of diabetes mellitus is increasing worldwide. The objective is to investigate and characterize the alpha-amylase inhibition principles of the leaves of Ficus sur Forssk (Moraceae) used in ethnomedicine for management of diabetes mellitus. Powdered leaves were successively macerated with N-hexane, chloroform and 70% ethanol respectively for three consecutive days. The extracts were assessed for phytochemicals and inhibition of alpha-amylase. Alpha-amylase inhibition was assessed using porcine α-amylase. Bioactive n-hexane extract was fractionated on column chromatography packed with Silica Gel G (mesh 60-120) and eluted with gradient mixture of hexane, ethyl acetate and ethanol. Active fractions (F1 - F5) were purified on preparative thin layer chromatography. Active pure compounds were assessed for bioactivity and identified by spectroscopy (UV, IR, MS and NMR). The n-hexane extracts of the plant exhibited highest significant (p < 0.05) inhibition. Fraction F4 was the most active and was and compound FB was characterized from it as a novel abietane-type diterpene (4,7,10-b-trimethyl-benzofuro[c]-6,6-a,8,9,10,10-a-hexahydroisochromene-7-carboxylic acid) with 55% inhibition of alpha-amylase at 50µg/ml. This work reports for the first time a novel diterpenoid from Ficus sur with alpha-amylase inhibition activity.
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