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首页> 外文期刊>World Journal of Gastroenterology >Anti-hepatoma activity and mechanism of ursolic acid and its derivatives isolated from Aralia decaisneana.
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Anti-hepatoma activity and mechanism of ursolic acid and its derivatives isolated from Aralia decaisneana.

机译：乌alia中乌索酸及其衍生物的抗肝癌活性及其作用机理。

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AIM:To investigate the anti-tumor activity of ursolic acid (UA) and its derivatives isolated from Aralia decaisneana on hepatocellular carcinoma both in vitro and in vivo.METHODS:In vivo cytotoxicity was first screened by 3-[4,5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide (MTT) assay. Morphological observation, DNA ladder, flow cytometry analysis, Western blot and real time PCR were employed to elucidate the cytotoxic mechanism of UA. Implanted mouse hepatoma H(22) was used to evaluate the growth inhibitory effect of UA in vivo.RESULTS:UA could significantly inhibit the proliferation of HepG2 and its drug-resistance strain, R-HepG2 cells, but had no inhibitory effect on primarily cultured normal mouse hepatocytes whereas all the six derivatives of UA could not inhibit the growth of all tested cell lines. Further study on mechanism demonstrated that apoptosis and G(0)/G(1) arrest were involved in the cytotoxicity and cleavage of poly-(ADP-ribose)-polymerase (PARP). Downregulation of cyclooxygenase-2 (COX-2) protein and upregulation of heat shock protein (HSP) 105 mRNA correlated to the apoptosis of HepG2 cells treated with UA. In addition, UA also could inhibit the growth of H(22) hepatoma in vivo.CONCLUSION:UA is a promising anti-tumor agent, but further work needs to be done to improve its solubility.
机译：目的：研究熊果中的熊果酸及其衍生物对肝癌的体外和体内抗肿瘤活性。方法：首先通过3- [4,5-二甲基噻唑- 2-yl] -2，5-二苯基四唑溴化物（MTT）分析。通过形态学观察，DNA阶梯分析，流式细胞术分析，Western印迹和实时PCR来阐明UA的细胞毒性机制。结果：UA可以显着抑制HepG2及其耐药株R-HepG2细胞的增殖，但对原代培养的HepG2细胞无抑制作用。正常小鼠肝细胞，而UA的所有六种衍生物均不能抑制所有测试细胞系的生长。进一步的机制研究表明，凋亡和G（0）/ G（1）逮捕参与聚（ADP-核糖）-聚合酶（PARP）的细胞毒性和裂解。环氧合酶2（COX-2）蛋白的下调和热休克蛋白（HSP）105 mRNA的上调与UA处理的HepG2细胞的凋亡有关。此外，UA还可以在体内抑制H（22）肝癌的生长。结论：UA是一种有前途的抗肿瘤药，但需要做进一步的工作以提高其溶解度。

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