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目的:研究芙蓉菊全草中具有抑制α-葡萄糖苷酶活性的化学成分。方法:采用体外α-葡萄糖苷酶抑制活性跟踪方法和各种柱色谱技术进行化学成分的分离和纯化;应用各种谱学方法鉴定化合物的结构;对单体化合物进行α-葡萄糖苷酶抑制活性试验,确定活性成分。结果:芙蓉菊70%乙醇提取物的醋酸乙酯萃取部分和水溶性部分对α-葡萄糖苷酶活性具有较强的抑制作用,从两部分分离鉴定了5,7-二羟基-3,′4,′5′-三甲氧基黄酮(1),东莨菪素(2),艾菊素,粗毛豚草素(3),5,5,′7-三羟基-3,′4′-二甲氧基黄酮(4),柯伊利素(5),万寿菊黄素-3,6,7-三甲基醚(6),石杉黄素(7),东莨菪苷(8)和槲皮万寿菊素-3,6-二甲醚(9)。其中,化合物2,3,5~7,9对α-葡萄糖苷酶活性具有较强的抑制作用,IC50(μmol.L-1)值分别为(34.36±2.06),(146.28±12.44),(246.26±8.73),(74.06±3.83),(42.19±5.25),(136.20±25.73),强于同条件下的阳性对照药阿卡波糖[IC50=(489.25±38.55)μmol.L-1]。化合物1,4,8和艾菊素的IC50值皆大于1 000μmol.L-1。结论:化合物5和9为首次从该属植物中分离得到;化合物2,3,5~7,9对α-葡萄糖苷酶活性具有较强的抑制作用,其抑制作用类型属于竞争性抑制作用,它们可能是芙蓉菊防治糖尿病的物质基础。
Objective: To study the chemical constituents that inhibit the activity of α-glucosidase in the whole plant of Methods: The chemical constituents were isolated and purified by in vitro α-glucosidase inhibition assay and various column chromatographic techniques. The structures of compounds were identified by various spectroscopic methods. The inhibitory activity of α-glucosidase Test to determine the active ingredient. Results: The extraction of 70% ethanol extract of Eriantha arborese and ethyl acetate extract of water had a strong inhibitory effect on the activity of α-glucosidase. Isolation and identification of 5,7-dihydroxy-3, 4 , 3’-trimethoxyflavone (1), scopolamine (2), tanshinone, abamectin (3), 5,5 ’ Flavonoids (4), krelin (5), marigoldin-3,6,7-trimethylether (6), dextrins (7), scopol (8) Marigold-3,6-dimethyl ether (9). Compounds 2,3,5 ~ 7,9 had a strong inhibitory effect on the activity of α-glucosidase. The values of IC50 (μmol.L-1) were (34.36 ± 2.06), (146.28 ± 12.44), 246.26 ± 8.73), (74.06 ± 3.83), (42.19 ± 5.25) and (136.20 ± 25.73), respectively, which was higher than that of acarbose, a positive control drug [IC50 = (489.25 ± 38.55) μmol.L-1] . Compounds 1, 4, 8 and tanshin with IC50 values above 1 000 μmol.L-1. Conclusion: Compounds 5 and 9 are isolated from this genus for the first time. Compounds 2,3,5 ~ 7,9 have a strong inhibitory effect on the activity of α-glucosidase, and their inhibitory effects belong to the competitive inhibition. They may be the material basis for prevention and treatment of diabetes mellitus.