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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1.9~20.2μmol/L。
OBJECTIVE To study the chemical constituents and tumor cytotoxicity of Physalis angulata from the genus Physalis. Methods Silica gel, Sephadex LH-20 gel column chromatography and HPLC and other methods, combined with liquid chromatography-mass spectrometry, the active tracking method was used to separate cytotoxic active components from the whole plant. The structures of compounds were identified by physical and chemical constants determination and various spectroscopy (1D and 2D NMR, MS) data analysis. The cytotoxic activity of the compounds was determined by MTT assay. Results A total of 12 compounds were isolated from 95% ethanolic water extracts of Allium mongolicum and identified as berberine A (1), clopidogrel B (2), clopidogrel C (3) Physalitone D (4), Physalis F (5), Physalis H (6), Physalis I (7), 5α-Ethoxy-6β-hydroxy- Physalisone B (8), Physalis O (9), β-sitosterol (10), methyl 2- carboxanilide (11), 2- (acetamido) -benzoic acid (12). Conclusion Compound 11 is a new natural product. Compounds 1 to 3 and 9 are the first to be isolated from bitter gourd. Compounds 1 to 9 are physalins steroid compounds. The results of cytotoxic activity showed that compounds 1 to 9 had strong proliferation inhibitory activity on lung cancer cell line A549, of which the inhibitory activity of 2,3,6,8 was the most significant, with the IC50 of 1.9 ~ 20.2μmol / L .