瘤内注射复方中药“99-克星”的活性组分抗肝癌作用及机制

Effect and mechanism of the active compound from Chinese traditional medicine “99-star”on treating liver cancer:experimental study

目的探讨超声引导瘤内注射复方中药“99-克星”的活性组分AG-05体内外抗肝癌作用及机制。方法观察AG-05瘤内注射对小鼠肝癌H22肿瘤生长抑制率的影响;应用磺酰罗丹明(SRB)法检测AG-05对体外培养肝癌HepG2细胞生长的抑制作用,透射电镜观察细胞形态学变化,流式细胞术分析细胞凋亡率。结果AG-05具有较强的抑制小鼠肝癌H22生长的作用,2mg/kg、1mg/kg肿瘤生长抑制率分别达62.8%、37.4%;AG-05对HepG2细胞的生长具有明显的抑制作用,且呈一定的量效、时效关系;AG-05作用48h后癌细胞出现明显的形态学变化,大部分细胞肿胀坏死,部分细胞出现染色质边集、凋亡小体形成等典型的凋亡形态学改变;流式细胞术检测癌细胞凋亡率实验组20μg/ml、10μg/ml两剂量组细胞凋亡率明显升高,分别为(20.1±4.3)%和(13.5±2.1)%。结论复方中药“99-克星”活性组分AG-05具有明显的抗肝癌作用,其作用机理与直接破坏肿瘤细胞及诱导肿瘤细胞凋亡有关。

Objective To probe the treatment effect and the mechanism of the active compound (AG-05) from Chinese traditional medicine “99-star” on liver cancer. Methods Anticancer experiment was done on mice inoculated with the H22 liver cancer cells, and the inhibition of cell proliferation was assayed using sulfur rodamine B (SRB) liguid method. Morphological changes were studied by transmission electron microscopes, and the flow cytometric analysis was performed to detect apoptosis. Results AG-05 could greatly inhibit the tumor growth of the mice. Marked anti-proliferation effect in concentration and time-dependent manners were observed after intervention of AG-05. Morphology changed obviously in that a large number of cells were turgescent and necrotic, and the typical apoptosis phenomena including chromatin margination and apoptotic bodies appeared in part of HepG2 cells. The flow cytometric analysis showed that apoptosis rates of HepG2 cells treated with AG-05 20 μg/mL, 10 μg/mL were (20.1±4.3)% and (13.5± 2.1%), respectively. Conclusions The above findings indicated that the active compound (AG-05) from Chinese traditional medicine “99-star” had strong effect on the liver cancer. Its major mechanisms might be to destroy tumor cells directly and to induce cancer cell apoptosis.