Jiang T L, Salmon S E, Liu R M
Eur J Cancer Clin Oncol. 1983 Feb;19(2):263-70. doi: 10.1016/0277-5379(83)90425-x.
The antitumor activity of four investigational natural products (camptothecin, harringtonin, cantharidin and curcumae) obtained from China were tested on human tumor biopsies in an in vitro soft agar clonogenic assay system. Significant antitumor activity was seen with camptothecin against human ovarian cancer and some other adenocarcinomas. Antitumor activity was also observed for harringtonin against adenocarcinoma and sarcoma. Both drugs also appeared to show activity in melanoma and mesothelioma. However, cantharidin and curcumae were relatively ineffective on the human tumors tested. For purposes of comparing the intensity of antitumor effects with standard cytotoxic drugs to those of the four new agents, the ID50 values were calculated. The ratio of ID50S of new drugs to the standard agents doxorubicin, cis-platinum and vinblastine (ID50 of the standard drug/ID50 of tested drug) were 10.2, 64.1 and 1.9 for camptothecin and 1.5, 10.3 and 0.9 for harrington respectively. A relationship was observed between the duration of drug exposure (1 hr prior to plating vs continuous contact in the agar) and inhibition of clonogenic tumor cells for camptothecin, harringtonin and doxorubicin.
对从中国获取的四种研究用天然产物(喜树碱、三尖杉酯碱、斑蝥素和莪术)进行了体外软琼脂克隆形成试验系统的人体肿瘤活检抗肿瘤活性测试。喜树碱对人卵巢癌和其他一些腺癌显示出显著的抗肿瘤活性。三尖杉酯碱对腺癌和肉瘤也观察到了抗肿瘤活性。这两种药物在黑色素瘤和间皮瘤中似乎也表现出活性。然而,斑蝥素和莪术对所测试的人体肿瘤相对无效。为了将这四种新药与标准细胞毒性药物的抗肿瘤作用强度进行比较,计算了ID50值。喜树碱与标准药物阿霉素、顺铂和长春碱的ID50比值(标准药物的ID50/受试药物的ID50)分别为10.2、64.1和1.9,三尖杉酯碱分别为1.5、10.3和0.9。观察到喜树碱、三尖杉酯碱和阿霉素的药物暴露持续时间(接种前1小时与琼脂中的持续接触)与克隆形成肿瘤细胞的抑制之间存在关系。