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从水车前中提取的达玛烷型三萜皂苷的抗肿瘤活性。

Antitumor activities of dammarane triterpene saponins from Bacopa monniera.

机构信息

Department of Oncology, Jinling Hospital, Medical School of Nanjing University, Nanjing, Jiangsu Province, PR China.

出版信息

Phytother Res. 2010 Jun;24(6):864-8. doi: 10.1002/ptr.3034.

Abstract

Bioassay-guided methods were used to test the antitumor activity of methanol extract of the whole plant of Bacopa monniera (L.) Wettst. and four different fractions (petroleum ether, CHCl(3), EtOAc, and n-BuOH fractions) of the methanol extract. Among the five crude samples, n-BuOH fraction was noted to have the highest antitumor activity. The dammarane triterpene saponins isolated from n-BuOH fraction, bacopaside E (1) and bacopaside VII (3), had potential antitumor effect. 1 and 3 showed cytotoxicity of all the tested human tumor cell lines MDA-MB-231, SHG-44, HCT-8, A-549 and PC-3M in MTT assay in vitro, and showed 90.52 % and 84.13 % inhibition in mouse implanted with sarcoma S180 in vivo at the concentration of 50 micromol/kg, respectively. The remaining two compounds, bacopaside II (2) and bacopasaponin C (4) were found to be much less potent compared with 1 and 3. 1 and 3 significantly inhibited human breast cancer cell line MDA-MB-231 adhesion, migration and Matrigel invasion in vitro at the concentration of 50 micromol/L. Since no antitumor activities about the monomers from Bacopa monniera (L.) Wettst. have been reported, these results indicate that the mechanism of action of 1 and 3 needs further study.

摘要

采用生物测定法对整个益智(L.) Wettst 植物甲醇提取物和甲醇提取物的四个不同部分(石油醚,CHCl(3),EtOAc 和 n-BuOH 部分)进行了抗肿瘤活性测试。在这五个粗品中,n-BuOH 部分被认为具有最高的抗肿瘤活性。从 n-BuOH 部分分离出的达玛烷三萜皂苷,bacopaside E(1)和 bacopaside VII(3),具有潜在的抗肿瘤作用。1 和 3 在体外 MTT 试验中对所有测试的人肿瘤细胞系 MDA-MB-231、SHG-44、HCT-8、A-549 和 PC-3M 均具有细胞毒性,在 50μm 浓度下对体内植入肉瘤 S180 的小鼠显示出 90.52%和 84.13%的抑制作用。另外两种化合物,bacopaside II(2)和 bacopasaponin C(4)与 1 和 3 相比,发现效力要低得多。1 和 3 在 50μm 浓度下可显著抑制人乳腺癌细胞系 MDA-MB-231 的黏附、迁移和 Matrigel 侵袭。由于从未报道过益智(L.) Wettst 单体的抗肿瘤活性,因此这些结果表明 1 和 3 的作用机制需要进一步研究。

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