chapter14hormones要点.pptVIP

Metabolism of hydrocortisone 在肝脏、肌肉及红细胞中代谢 –首先通过5β或5α还原酶使△4，5被还原 –进一步在3α或3β酮基还原酶的作用下3-酮被还原成5β-孕甾烷， –大部分C-20侧链断裂形成C-19甾体 –经葡萄糖醛酸化或单硫酸酯化成水溶性盐后从尿及胆汁中排出 Structure Modification of glucocorticoid: 1、C-21 2、C-1??3、C-6位 4、C-9 5、C-17 1. Structure modification of C- 21 　 用常规方法进行酯化时，只有C-21羟基能被酯化，位阻使其它羟基不能成酯：C-11羟基因C-10及C-18角甲基，C-17羟基因侧链。 The prodrugs of C-21 ester The increasing of enduration time and better stability. - Long-chain fatty acid ester can extend acting time - Multi-acid monoester salt, can be made in aqueous solution for injection C-21 modification does not change the activity of glucocorticoid Derivatives of Hydrocortisone C-21 ester 2. Structure modification of C-1 　 Hydrocortisone acetate as lead C 1-2脱氢（A环引入双键）得到醋酸氢化泼尼松 (Prednisolone acetate) 醋酸地塞米松 Dexamethasone acetate　 9-α-氟-11β，17α，21-三羟基-16α-甲基孕甾-1，4-二烯-3-20二酮-21-醋酸酯 9-α-fluoro-11β, 17α, 21 - trihydroxy-16α-methyl-pregna-1,4 - dione -3-20 diene -21 - acetate * Chapter 14 Adrenocorticotropic hormones and sex hormones Hormones are chemicals released by cells that affect cells in other parts of the body. Only a small amount of hormone is required to alter cell metabolism. It is essentially a chemical messenger that transports a signal from one cell to another. All multicellular organisms produce hormones; plant hormones are also called phytohormones. Hormones in animals are often transported in the blood. Cells respond to a hormone when they express a specific receptor for that hormone. The hormone binds to the receptor protein, resulting in the activation of a signal transduction mechanism that ultimately leads to cell type-specific responses. Introduction: Hormones have the following effects on the body: (1) stimulation or inhibition of growth (2) mood swings (3) induction or suppression of apoptosis (programmed cell death) (3) activation or inhibition of the immune system (4) regulation of metabolism (5) preparation of the body for fighting ,fleeing, mating and other activ