17aα-D-高炔雌二醇-3-乙酯抗肿瘤活性及辐射增效作用研究  

Study on Anti-tumor Activities & Tumor Radio-sensitivity of 17aα-D-Homo-Ethynylestradiol-3-Acetate

作　　者：周则卫[1] 张良安[1] 沈秀[1] 王月英[1] 王晓雪[1] 向前[2] 胡晓年[2] 

机构地区：[1]中国医学科学院/中国协和医科大学放射医学研究所,300192 [2]中国医学科学院/中国协和医科大学基础医学研究所

出　　处：《医学研究杂志》2006年第8期49-51,共3页Journal of Medical Research

基　　金：天津市自然科学基金重点项目资助(043802411)

摘　　要：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 The paper reports anti - tumor activities and tumor radio - sensitivity research of the novel Estrogen compound 17aα - D - Homo Ethynylestradiol -3 - Acetate to U14 and S180 sarcomas ; and overall test high - activity and low toxicity traits of 17aα - D -Homo Ethynylestradiol- 3 -Acetate by the indexes of thymus gland, spleen, etc. Methods The mouse cervical cancer U14 was selected and implanted in IRM - 2 mice for anti - tumor assay, and sarcoma S180 was selected for tumor radio - sensitivity assay, the drug was administered to all mice by i.v. way. Results 17aα - D - Homo Ethynylestradiol - 3 - Acetate has obvious anti - tumor activity to U14 tumor,the best inhibitory rates is U14 64.3% , andlTaα- D- Homo Ethynylestradiol- 3 -Acetate has hardly any influence to hematogenous system （spleen index）, immune system （thymus index） ; Nevertheless, the positive control drug CCP has obvious damage to spleen index and thymus index （ P 〈 0.01 ）. For tumor radio - sensitivity assay, obvious effect - increasing activity is shown in all drug administered group. Conclusions 17aα - D - Homo Ethynylestradiol - 3 - Acetate may be made into a multi - functional new drug with lower toxicity, high anti - tumor and tumor radio - sensitivity activities, etc.

关 键 词：17aα—D-高炔雌二醇-3-乙酯 抗肿瘤 辐射增效 药理活性 

分 类 号：R285.5[医药卫生—中药学] R979.1[医药卫生—中医学]