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[摘要]
目的 对酸浆属植物苦蘵Physalis angulata的全草进行化学成分及肿瘤细胞毒活性研究。方法 运用硅胶、Sephadex LH-20凝胶等柱色谱和HPLC等方法,并结合液质联用分析技术,采用活性跟踪的方法从苦蘵全草中分离细胞毒活性成分。根据理化常数测定和各种谱学(1D和2D NMR、MS)数据分析等鉴定化合物结构,MTT法测定化合物的细胞毒活性。结果 从苦蘵全草的95%乙醇水提取物中共分离得到12个化合物,分别鉴定为酸浆苦素A(1)、酸浆苦素B(2)、酸浆苦素C(3)、酸浆苦素D(4)、酸浆苦素F(5)、酸浆苦素H(6)、酸浆苦素I(7)、5α-乙氧基-6β-羟基-5,6-二氢酸浆苦素B(8)、酸浆苦素O(9)、β-谷甾醇(10)、2-羧基苯胺羰酸甲酯(11)、2-(乙酰胺基)-苯甲酸(12)。结论 化合物11 为新天然产物,化合物1~3、9 为首次从苦蘵中分得,化合物1~9 为酸浆苦素类(physalins)甾体化合物。细胞毒活性实验结果显示,化合物1~9 对肺癌细胞株A549均具有较强的增殖抑制活性,其中以2、3、6、8 的抑制活性最为显著,其IC50值为1.9~20.2 μmol/L。
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[Abstract]
Objective To investigate the chemical constituents from whole herb of Physalis angulata and test their cytotoxic activity. Method s Compounds were isolated by chromatography methods and LC-MS guided analysis, structures were determined by spectroscopic techniques of 1D- and 2D-NMR (HSQC, HMBC, 1H-1H COSY, and NOESY), cytotoxic activity experiments were conducted by MTT method. Results Twelve compounds were identified as physalins A (1), B (2), C (3), D (4), F (5), H (6), I (7), O (9), 5α-ethoxy-6β-hydroxy-5,6-dihydrophysalin B (8), β-sitosterol (10), 2-carboxyoxanilic acid methyl ester (11), and acetaminobenzoic acid (12). Conclusion Among these compounds, compound 11 is a new natural product. Compounds 1-3 and 9 are firstly obtained from P. angulata. All compounds are tested for their inhibitory activities against human lung adenocarcinoma strain A-549, with IC50 values of 1.9-20.2 μmol/L, which indicates good cytotoxic activity of these physalins.
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