雄性激素和蛋白同化激素（PPT58）课件.ppt

Chapter 11 Hormones（2） 3.Steroid Hormones Male hormones have male activity and protein assimilation (同化) activity. Some structure modified compounds which are called protein anabolic hormones(蛋白同化激素)have very weak male activity but strong protein assimilation activity. Anabolic hormones are drugs derived from the male sex hormone to promote growth or to help the body repair tissues weakened by severe illness or aging, and it subject to abuse to promote muscle mass in athletes. The purpose to modify male hormones is to acquire new protein anabolic hormones . Anabolic Hormones Promote protein anabolism(合成代谢)and reduce its catabolism(分解代谢). Enhance the procedures of protein synthesis from amino acid. Clinical uses of anabolic hormones are treating sickness asthenia(虚弱), cacotrophia(营养不良)of new-born and aged people, consume diseases, osteoporosis and gastric and duodenal ulcer (胃十二指肠溃疡) etc . Side-effect of Anabolic Hormones Male activity is the main side-effect of anabolic hormones. Minor change of structure of Testosterone(睾酮)can cause male activity decrease and anabolic activity increase. For example: De-methyl on C-19; Substitution on ring A Fused rings of ring A No anabolic hormones without male activity . Testosterone Propionate(丙酸睾酮) Chemical name： 17?-Hydroxyandrost-4-en-3-one propionate Structure of Testosterone Propionate Testosterone is a natural male hormones. Separated from male cow testis(睾丸) in 1935. It is △4-3-ketone and 17β-hydroxyl compound, and here it is propionate. UV absorption. Absorption and Pharmacokinetics By oral Testosterone cannot be absorbed in gastrointestinal tract, but Testosterone Propionate oil solution has prolonged effect in vivo because it can be hydrolyzed and release Testosterone slowly. Testosterone propionate — Pro-drug. Biotransformation The ratio of activity: Dihydrotestosterone ：Testosterone ： △4-Androstenedione(雄烯二酮) = 150：100 ：10 Analogues of Testosterone The advantage of 17α-methyl analogue: