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.
出处
《辐射防护》
CAS
CSCD
北大核心
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)
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
17aα- D-homo-ethynylestradiol-3-acetate, Ethynylestradiol（ EE＇2）, Radiation Damage Protection, Pharmacolog- ical Activities, Estrogenic Activity
