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目的:研究番荔枝Annona squamosa的化学成分,并对分离化合物进行活性筛选。方法:综合运用各种色谱方法分离纯化番荔枝中的化学成分;采用NMR等波谱方法鉴定其结构;运用SRB法测定化合物对肿瘤细胞体外增殖能力的抑制作用。结果:从番荔枝皮乙醇提取物中分离得到11个化合物,分别是annosquamosin C(1),15,16-epoxy-17-hydroxy-ent-kau-ran-19-oic acid(2),16,17-dihydroxy-ent-kauran-19-oic acid(3),annosquamosin A(4),ent-kaur-16-en-19-oic acid(5),19-nor-ent-kauran-4-ol-17-oic acid(6),16-hydroxy-ent-kau-ran-19-oic acid(7),ent-15β-hydroxy-kaur-16-en-19-oic acid(8),annosquamosin B(9),ent-16β,17-dihydroxykauran-19-al(10),16,17-dihydroxy-ent-kauran-19-oic acid methyl ester(11)。抗肿瘤活性实验表明,化合物1,2,3,5,9对人肺癌95-D细胞的体外增殖能力均具有不同程度的抑制作用,化合物5的活性最强,IC50为7.78μmol.L-1;化合物2,5,9对人卵巢癌A2780细胞有抑制作用,其中化合物2和9的抑制作用较强,IC50分别为0.89,3.10μmol.L-1。结论:化合物2,8,11分别为首次从该科、该属和该种植物分离得到;化合物5对人肺癌95-D细胞的抑制作用较强;化合物2和9对人卵巢癌细胞A2780的抑制作用较强。
OBJECTIVE: To study the chemical constituents of Annona squamosa and to screen the active compounds of the compounds. Methods: The chemical constituents were isolated and purified by various chromatographic methods. The structures were identified by NMR and other spectroscopic methods. The inhibitory effects of the compounds on the proliferation of tumor cells were determined by SRB method. Results: Eleven compounds were isolated from ethanol extract of Annona bark, including annosquamosin C (1), 15,16-epoxy-17-hydroxy-ent-kau- ran-19-oic acid 17-dihydroxy-ent-kauran-19-oic acid (3), annosquamosin A (4), ent-kaur- 17-oic acid (6), 16-hydroxy-ent-kau-ran-19- oic acid (7), ent- 15β-hydroxy-kaur- 16-en-19-oic acid ), ent-16β, 17-dihydroxykauran-19-al (10), 16,17-dihydroxy-ent-kauran-19-oic acid methyl ester (11). The antitumor activity assay showed that the compounds 1, 2, 3, 5 and 9 inhibited the proliferation of human lung cancer 95-D cells to varying degrees in vitro. The activity of compound 5 was the strongest with IC50 of 7.78μmol.L-1 .Compounds 2, 5, and 9 inhibited the proliferation of human ovarian cancer A2780 cells. The inhibitory effects of compounds 2 and 9 were stronger with IC50 of 0.89 and 3.10 μmol·L-1, respectively. CONCLUSION: Compounds 2, 8, and 11 were isolated from this family for the first time, respectively, and from this plant. Compound 5 showed a stronger inhibitory effect on human lung cancer 95-D cells. Compounds 2 and 9 were more effective against human ovarian cancer cells A2780 Strong inhibitory effect.