Jatwa Rameshwar, Kar Anand
School of Life Science, Devi Ahilya University, Takshashila Campus, Madhya Pradesh Indore-452017, India.
Contraception. 2007 Nov;76(5):408-12. doi: 10.1016/j.contraception.2007.07.005. Epub 2007 Sep 21.
Centchroman, a nonsteroidal oral contraceptive, was evaluated for its hitherto unstudied effect on cardiovascular system, thyroid function and tissue lipid peroxidation in rats.
Wistar sperm-positive female rats were treated with Centchroman (1.5 mg/kg per day, po) for 10 days and the alterations in serum concentration of thyroid hormones [triiodothyronine (T(3)) and thyroxine (T(4))], insulin, glucose, total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), very low-density lipoprotein cholesterol (VLDL-C), triglycerides (TG), aspartate aminotransferase (AST), alanine aminotransferase (ALT) and alkaline phospahatase (ALP) activity, hepatic type-1 iodothyronine 5'-monodeiodinase (5'D) enzyme activity and hepatic, renal, cardiac and serum lipid peroxidation (LPO) were studied. Simultaneously, alterations in endogenous antioxidants [superoxide dismutase (SOD); catalase (CAT) and reduced glutathione (GSH)], relative risk ratio (RR), atherogenic index (AI) and daily rate of food and water consumption were also investigated as supportive parameters.
Centchroman administration resulted in the complete inhibition of pregnancy. It increased serum T(4) marginally and HDL-C levels, hepatic SOD, CAT and GSH; cardiac SOD and GSH and renal SOD and CAT activity significantly. However, it reduced LPO in all tissues; concentrations of other serum lipids; AI; RR and activity of ALP.
As Centchroman administration did not alter the concentrations of most active thyroid hormone, T(3), serum insulin and glucose, it appears that the drug has no side effect on thyroid function and glucose metabolism. Rather, it possesses cardiovascular and anti-peroxidative benefits.
对非甾体类口服避孕药炔雌醚在大鼠心血管系统、甲状腺功能及组织脂质过氧化方面尚未研究的作用进行评估。
用炔雌醚(每天1.5毫克/千克,口服)对Wistar精子阳性雌性大鼠进行10天治疗,研究甲状腺激素[三碘甲状腺原氨酸(T(3))和甲状腺素(T(4))]、胰岛素、葡萄糖、总胆固醇(TC)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)、极低密度脂蛋白胆固醇(VLDL-C)、甘油三酯(TG)、天冬氨酸转氨酶(AST)、丙氨酸转氨酶(ALT)和碱性磷酸酶(ALP)活性的血清浓度变化,肝I型碘甲状腺原氨酸5'-单脱碘酶(5'D)酶活性以及肝、肾、心脏和血清脂质过氧化(LPO)。同时,还研究了内源性抗氧化剂[超氧化物歧化酶(SOD)、过氧化氢酶(CAT)和还原型谷胱甘肽(GSH)]的变化、相对风险比(RR)、动脉粥样硬化指数(AI)以及食物和水的每日消耗率作为支持参数。
给予炔雌醚导致妊娠完全抑制。它使血清T(4)略有升高,HDL-C水平、肝SOD、CAT和GSH、心脏SOD和GSH以及肾SOD和CAT活性显著增加。然而,它降低了所有组织中的LPO、其他血清脂质浓度、AI、RR和ALP活性。
由于给予炔雌醚未改变最具活性的甲状腺激素T(3)、血清胰岛素和葡萄糖的浓度,看来该药物对甲状腺功能和糖代谢无副作用。相反,它具有心血管和抗过氧化益处。