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目的本文报告新型雌激素化合物17aα-D-高炔雌二醇-3-乙酯对多种瘤谱的抑瘤活性及对肿瘤辐射抑瘤的增效作用;并通过对胸腺、脾等指标综合考察17aα-D-高炔雌二醇-3-乙酯的高抑瘤活性和低副作用特征。方法选择小鼠宫颈癌(U14)瘤株分别接种于IRM-2小鼠,腹腔给予17aα-D-高炔雌二醇-3-乙酯。对辐射抑瘤的增效作用以肉瘤(S180)加以1×5Gy照射,比较对给药组抑瘤的增效作用。结果宫颈癌(U14)使用17aα-D-高炔雌二醇-3-乙酯有明显的抑瘤效果,最佳抑瘤率为U1464.3%,并且17aα-D-高炔雌二醇-3-乙酯对小鼠的造血系统(脾指数)、免疫系统(胸腺指数)几乎无影响;而阳性对照环磷酰胺(CCP)组对小鼠的肝、脾指数、胸腺指数有着明显的损伤(P<0.01)。对肉瘤(S180)辐射抑瘤的增效作用,各剂量组均有较明显抑瘤增效作用。结论17aα-D-高炔雌二醇-3-乙酯有可能成为一种低毒、高效且有辐射增效作用的多功效抗肿瘤新药。
OBJECTIVE: To report the antitumor activity of a new estrogen compound 17aα-D-homovinyl-estradiol-3-ethyl ester on various tumor patterns and its synergistic effect on tumor radiation and tumor inhibition. Through the combination of thymus, spleen and other indicators To investigate the high inhibitory activity and low side effects of 17aα-D-ethinyl estradiol-3-ethyl ester. Methods Mice cervical cancer (U14) were inoculated into IRM-2 mice and intraperitoneally administered with 17aα-D-ethinyl estradiol-3-ethyl ester. The antitumor effect of radiation on the inhibition of sarcoma (S180) to 1 × 5Gy irradiation, compared to the administration group antitumor synergies. Results Uterine cervix cancer (U14) had obvious antitumor effect with 17aα-D-homoserine estradiol-3-ethyl ester. The best inhibition rate was U1464.3%, and 17aα-D-high ethinyl estradiol- 3-Ethyl ester has almost no effect on the hematopoietic system (spleen index) and immune system (thymus index) in mice, while the positive control cyclophosphamide (CCP) group has obvious damage to the liver, spleen index and thymus index in mice (P <0.01). On the sarcoma (S180) inhibition of radiation synergies, each dose group were more obvious anti-tumor synergy. Conclusion 17aα-D-high-ethinyl estradiol-3-ethyl ester may become a multi-functional anti-tumor drug with low toxicity, high efficiency and radiation synergism.