Relation between biological activity of hydrocortisone analogues and their rates of inactivation by rat liver enzyme systems.
Relation between biological activity of hydrocortisone analogues and their rates of inactivation by rat liver enzyme systems.
复制标题
氢化可的松类似物的生物活性与其被大鼠肝酶系统灭活的速率之间的关系。
DOI:
10.1210/endo-61-1-128
复制
发表时间:
1957
期刊:
影响因子:
4.8
通讯作者:
B. Bowman
中科院分区:
文献类型:
--
作者:
E. M. Glenn;R. O. Stafford;S. C. Lyster;B. Bowman
RECENT studies show that desaturation of the 1, 2 positions of hydro-cortisone and introduction of other substituents (2α-methyl- and 9αfluoro-groups) lead to increased biological activity (1, 2, 3, 4, 5, 6). On the basis of plasma steroid levels, it has been suggested that the prolonged biological half-life of steroid analogues is due to decrease in rate of metabolism by tissues (5, 7, 8, 9). Studies were initiated to determine whether elevated plasma levels and increased glycogen deposition activities of hydrocortisone derivatives are related to rate of inactivation in liver. In summary of much work in this area, it may be stated that C-20 and δ4-3 ketone reduction of hydrocortisone, as well as ketone reduction of a number of other steroids, occurs in a combined microsome-supernatant fraction of rat liver (10, 11, 12, 13). Hydrocortisone is reduced by rat liver enzyme systems to the corresponding dihydro and tetrahydro derivatives (10).