17β-雌二醇-3位衍生物抗辐射活性研究

An Experimental Research on Anti-radiation Activities of 17β-estrogen-3-derivatives

目的研究新雌激素衍生物17β-雌二醇-3-烯丙基醚(ES-1)、17β-雌二醇-3-异戊烯基醚(ES-2)的抗辐射活性。方法以炔雌二醇和茜草双酯为阳性对照药,小鼠接受铯137(137Cs)γ-射线6.5Gy一次性全身照射,观察各给药组白细胞数(WBC)、股骨有核细胞计数(BMNC)及DNA含量、脾结节数(CFU-S)、脾指数、胸腺指数等相关指标变化。结果与对照组比较,ES-1和ES-2各给药剂量组小鼠在WBC、BMNC及DNA含量、CFU-S、脾指数、胸腺指数均明显升高(P<0.05或P<0.01),WBC变化非常明显,ES-1和ES-2两组均差异有极显著性(均P<0.01)。结论ES-1、ES-2具有明显的抗辐射活性,有可能成为高效、低毒、口服的辐射防护药。

Objective To study the anti-radiation effects produced by 17β-estradiol-3- allyl ether （ES-I） and 17β- estradiol-3-isopentenyl ether（ES-2）. Methods Using ethinylestradiol and rubidate as positive control, the mice receive 6.5 Gy y-rays emitted from the 137Cs radiation resource. The number of white blood cell（WBC）, the number of nucleated cells in bone marrow（BMNC）, DNA content, colony forming unit-spleen （CFUS） , spleen index and thymus index were detected to evaluate the protection of ES-1 and ES-2 to the mice against radiation. Results Compared with the control group, the three dosage groups of both ES-1 and ES-2 exhibit better anti-radiation effects, including the aspects of WBC, BMNC, DNA content, CFU-S, spleen index and thymus index （P 〈 0.05, P 〈 0. 01 ）, especially, the improvement of the WBC （ P 〈 0. 01 ）. Therefore, we can conclude that the two compounds can protect the hematopoietic function and promote the immunity of the mice. Conclusion ES-1, ES-2 have the effects of anti-radiation and may become an oral anti-radiation protector with higher efficiency, lower toxieity.