雷公藤红素对裸鼠肝癌皮下移植瘤抑制作用的研究

目的 研究天然活性化合物雷公藤红素（celastrol）对裸鼠移植肿瘤的抑制作用。方法 建立人源肝癌HepG2细胞的裸鼠皮下移植肿瘤模型。20只裸鼠随机分为4组,即空白对照组和雷公藤红素高剂量组、中剂量组和低剂量组,每组分别按4.0 mg/kg、2.0 mg/kg、1.0 mg/kg雷公藤红素腹腔给药,每日一次,每周5 d,共给药30 d,实验中每5 d测量一次肿瘤体积的变化。结果 雷公藤红素高剂量组、中剂量组和低剂量组的体积抑瘤率分别是89.52%、65.60%和12.21%,与空白对照组相比,高剂量组、中剂量组的差异具有统计学意义（P〈0.05）。高剂量雷公藤红素给药后对裸鼠肝脏和肾脏等产生严重的毒性反应。结论 雷公藤红素对裸鼠肝癌皮下移植瘤具有良好的体内抗肿瘤效果,应进一步开展药物新剂型及分子结构优化方面的研究,减少其毒副反应。

Celastrol-mediated growth inhibition of subcutaneously transplanted hepatocarcinoma in nude mice

Objective To study the potential of celastrol to inhibit growth of transplanted tumors in nude mice. Methods Nude mice（n=20）subcutaneously injected with HepG2 cells were randomly divided into 4 groups and treated by abdominal injection with 0,1.0,2.0 and 4.0 mg/kg once daily five times per week. Tumor size was measured every five days. Results Tumor volume inhibition was 12.21% for 1.0 mg/kg,65.60% for 2.0 mg/kg and 89.52% for 4.0 mg/kg,and tumor volume was significantly smaller in animals treated with 2.0 or 4.0 mg/kg than in control animals. Severe liver and kidney toxicity were observed in animals treated with 4.0 mg/kg. Conclusion Celastrol shows good anticancer activity in this mouse model of liver cancer. Studies are needed to optimize dosing and drug structure to reduce toxicity.