17aα-D-高炔雌二醇-3-乙酯对辐射和化学损伤小鼠的防护作用及其雌活性的实验研究  

EXPERIMENTAL STUDY ON RADIATION AND CHEMICAL DAMAGE PROTECTION AND ESTROGENIC ACTIVITIES OF FRESH ESTROGEN COMPOUND 17aα-D-HOMO-ETHYNYLESTRADIOL-3-ACETATE

作　　者：周则卫[1] 沈秀[1] 唐卫生[1] 吴小霞[1] 王月英[1] 张良安[1] 

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,天津300192

出　　处：《辐射防护》2008年第4期221-225,共5页Radiation Protection

基　　金：天津市自然科学基金重点项目(043802411)

摘　　要：采用我所自行合成的新型雌激素类化合物17aα-D-高炔雌二醇-3-乙酯,观察其对受致死剂量(8.0 Gy)137Csγ射线照射IRM-2小鼠30 d存活率的影响,以及药物对注射环磷酰胺(CY)所致的IRM-2小鼠造血系统损伤的保护作用,比较了其与炔雌二醇(EE2)对昆明种雌性小鼠的雌活性。结果表明,5 mg/kg7、.5 mg/kg、10 mg/kg三个不同剂量17aα-D-高炔雌二醇-3-乙酯药物注射组,30 d存活率分别比单纯照射对照组提高55%、85%、75%(p<0.01),保护指数分别为1.99、2.56、2.46;同时,药物可明显保护环磷酰胺所致的小鼠造血系统功能的损伤。与EE2相比,该药物雌活性约为其1/10000。因此,17aα-D-高炔雌二醇-3-乙酯对γ射线及化学药物损伤均有明显的保护作用,而且该药的雌活性低,毒副作用小。Fresh estrogen compound-17aα-D-homo-ethynylestradiol-3-acetate synthesized by our institute was employed to investigate its protective effect to IRM-2 mice for damages irradiated by lethal dose （8.0 Gy） ^137 Cs γ rays. The influence to 30 d survival rates of the irradiated mice were observed. And protection of the drug to IRM-2 mice hematogenous system damage by injected cyclophosphamide （CY） was studied, as well as in comparison with ethynylestradiol （EE2）, estrogenic activity of the drug was investigated. The resnlts suggest 30 d survival rates of IRM-2 mice for 5 mg/kg, 7.5 mg/kg, 10 mg/kg dosages of the drug 17aα-D-homoethynylestradiol-3-acetate were 55 %, 85 %, 75 % （p 〈 0.01 ）, and protective indexes were 1.99, 2.56 and 2.46, respectively. Also, the drug may has a significant protective effect on the damages resulting from CY to mouse hematogenous system. Compared with EE2, estrogenic activity of the drug was only 1/10000 of it. Therefore, 17aα-D-homo-ethynylestradiol-3-acetate has obviously protective effects to the damages from γ rays radiation and chemical drug. And the drug possesses low estrogenic activity, as well as low side-effect.

关 键 词：17aα-D-高炔雌二醇-3-乙酯 炔雌二醇 辐射损伤防护 药理活性 雌活性 

分 类 号：R96[医药卫生—药理学]