Huang C C, Han C S, Yue X F, Shen C M, Wang S W, Wu F G, Xu B
J Natl Cancer Inst. 1983 Oct;71(4):841-7.
Growth inhibition in the Chinese hamster cell line V79 and in the human lymphoid cell line Raji and induction of sister chromatid exchange(s) (SCE) in V79 cells after treatment with six anticancer drugs [harringtonine (HRT), homoharringtonine (HHRT), camptothecin (CPT), hydroxycamptothecin (HCPT), lycobetaine (LBT), and oxalysine (OXL)] developed in the People's Republic of China were studied. OXL is a new antibiotic; all other drugs are plant extracts. All drugs caused a dose-dependent growth inhibition in both cell types, as evidenced by decreases in plating efficiencies of V79 cells and in viable cell counts of Raji. However, the degree of inhibition differed widely among the drugs. HRT, HHRT, CPT, and HCPT were the most potent growth inhibitors, LBT was next, and OXL was the least effective inhibitor. SCE analyses were made in V79 cells treated with a drug in the presence or absence of the metabolic activation system S9 mixture (S9 mix), except for the HRT assay in which the S9 mix was not used. CPT, HCPT, and LBT induced a dose-dependent increase in SCE frequencies, while HRT, HHRT, and OXL caused no SCE induction at any dose level used. CPT was the most powerful SCE inducer. HCPT induced SCE but at a much reduced rate when compared to that of CPT. LBT was a weak SCE inducer; SCE induction was seen only in cultures treated with 40 micrograms or more LBT/ml. Addition of the S9 mix did not alter SCE frequencies, indicating that the drugs were direct-acting agents. HRT and HHRT were highly toxic, but they induced no increases in SCE frequency, indicating that cytotoxicity of a compound does not necessarily correlate with SCE induction.
研究了六种中国研制的抗癌药物（三尖杉酯碱（HRT）、高三尖杉酯碱（HHRT）、喜树碱（CPT）、羟基喜树碱（HCPT）、石蒜碱（LBT）和草赖氨酸（OXL））对中国仓鼠细胞系V79和人淋巴样细胞系Raji的生长抑制作用，以及对V79细胞姐妹染色单体交换（SCE）的诱导作用。OXL是一种新抗生素；其他所有药物均为植物提取物。所有药物均导致两种细胞类型出现剂量依赖性生长抑制，V79细胞平板接种效率降低以及Raji活细胞计数减少即证明了这一点。然而，不同药物之间的抑制程度差异很大。HRT、HHRT、CPT和HCPT是最有效的生长抑制剂，LBT次之，OXL是最无效的抑制剂。除未使用S9混合物（S9 mix）进行HRT检测外，对在有或无代谢激活系统S9 mix存在的情况下用药物处理的V79细胞进行了SCE分析。CPT、HCPT和LBT诱导SCE频率呈剂量依赖性增加，而HRT、HHRT和OXL在所用的任何剂量水平下均未引起SCE诱导。CPT是最强大的SCE诱导剂。HCPT诱导SCE，但与CPT相比速率大大降低。LBT是一种弱SCE诱导剂；仅在用40微克或更多LBT/ml处理的培养物中观察到SCE诱导。添加S9 mix未改变SCE频率，表明这些药物是直接作用剂。HRT和HHRT毒性很高，但它们未诱导SCE频率增加，表明化合物的细胞毒性不一定与SCE诱导相关。
