| 番荔枝皮化学成分及其抗肿瘤活性的研究 |
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| 引用本文： | 孙丽蕊,朱虹,甘礼社,莫建霞,冯锋,周长新.番荔枝皮化学成分及其抗肿瘤活性的研究[J].中国中药杂志,2012,37(14):2100-2104. |
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| 作者姓名： | 孙丽蕊 朱虹 甘礼社 莫建霞 冯锋 周长新 |
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| 作者单位： | 1. 中国药科大学天然药物化学教研室,江苏南京,210009
2. 浙江大学药学院,浙江杭州,310058 |
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| 基金项目： | 浙江省自然科学基金项目 (Y208602) |
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| 摘 要： | 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7.78 μmol·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0.89,3.10 μmol·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.
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| 关 键 词： | 番荔枝 贝壳杉烷型二萜 抗肿瘤活性 |
| 收稿时间： | 2011/11/17 0:00:00 |
Constituents from the bark of Annona squamosa and their anti-tumor activity |
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| SUN Lirui,ZHU Hong,GAN Lishe,MO Jianxi,FENG Feng and ZHOU Changxin.Constituents from the bark of Annona squamosa and their anti-tumor activity[J].China Journal of Chinese Materia Medica,2012,37(14):2100-2104. |
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| Authors: | SUN Lirui ZHU Hong GAN Lishe MO Jianxi FENG Feng and ZHOU Changxin |
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| Institution: | Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China;College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China;College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China;Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;College of Pharmaceutical Science, Zhejiang University, Hangzhou 310058, China |
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| Abstract: | Objective: To investigate the constituents of the Annona squamosa and evaluate their anti-tumor activity.Method: The compounds were isolated and purified by various column chromatography.Their structures were elucidated by spectral data analysis.Their anti-tumor activity was assayed by SRB method.Result: Eleven compounds were obtained from the 95% EtOH extract.The structures were determined as: 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 me thyl ester(11).Compounds 1,2,3,5,9 showed different inhibitory activities against 95-D lung cancer cells,the effect of compound 5 was strongest with the IC50 value 7.78 μmol·L-1;Compounds 2,5,9 showed inhibitory activities against A2780 ovarian cancer cells,the effects of compounds 2 and 9 were strong with the IC50 values being 0.89,3.10 μmol·L-1,respectively.Conclusion: Compound 2 was firstly isolated from this family,while compound 8 and 10 were first found from this genus and the title species,respectively.The in vitro anti-tumor test showed compound 5 significantly inhibited 95-D lung cancer cells and compounds 2 and 9 exhibited remarkbale activity against A2780 ovarian cancer cells. |
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| Keywords: | Annona squamosa kaurane-type diterpene anti-tumor activity |
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