INVIVO STUDY OF THE ACTION OF ANTI-GLUCOCORTICOIDS ON THYMUS WEIGHT RATIO, ANTIBODY TITER AND THE ADRENAL-PITUITARY-HYPOTHALAMUS AXIS

被引：60

作者：

DUNCAN, MR ^{[1
]}

DUNCAN, GR ^{[1
]}

机构：

[1] UNIV TORONTO,FAC PHARM,TORONTO M5S 1A1,ONTARIO,CANADA

来源：

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY | 1979年 / 10卷 / 03期

关键词：

17-O-methylethisterone; 17α-ethynyl-17β-methoxy-4-androsten-3-one; 17-O-methylnorethindrone; 17α-ethynyl-; 17β-methoxy-19-nor-4-androsten-3-one; 19-nortestosterone 17β-hydroxy-19-nor-4-androsten-3-one(Si); 20α-dihydroprogesterone 20(S)-hydroxy-4-pregnene-3-one(Si); 20β-dihydroprogesterone 20(R)-hydroxy-4-pregnene-3-one(Si); 21-hydroxymelhylprednisolone acetonide 21-homo-11β,17-dihydroxy-21,22-isopropylidenedioxy-1,4-pregnadiene-3,20-dione; 5β-dihydrocortexolone 17,21-dihydroxy-5β-pregnane-3,20-dione(Ik); cortexolone 17,21-dihydroxy-4-pregnene-3,20-dione (S-M); cortexone 21-hydroxy-4-pregnene-3,20-dione (S-M); dehydrospirocortisol; 11β-hydroxy-4-androstene-3-one-; 17(R)-spiro-2'-(2'; 3'-dihydroxol-3'-one); ethisterone 17α-ethynyl-17β-hydroxy-4-androstene-3-one(C-G); fluoxymesterone; 9α-fluoro-17α-methyl-11β; 17β-dihydroxy-4-androstene-3-one; (Up); medroxyprogesterone acetate 6α-methyl-17-hydroxy-4-pregnene-3,20-dione (17-acetate) (Up); mestranol 17α-ethynyl-3-methoxy-17β-hydroxy-1,3,5(10)-estratriene(Si); methandrostenolone 17α-methyl-17β-hydroxy-1,4-androstadien-3-one(C-G); norethindrone 17α-ethynyl-17β-hydroxy-19-nor-4-androsten-3-one(Si); norethynodrel 17α-ethynyl-17β-hydroxy-19-nor-5-(10)-androsten-3-one(Si); sodium cortexolone hemisuccinate sodium (17,21-dihydroxy-4-pregnene-3,20-dione) 21-succinate; sodium cortexone hemisuccinate sodium (21-hydroxy-4-pregnene-3,20-dione) 21-succinate; sodium corticosterone hemisuccinate sodium (11β,21-dihydroxy-4-pregnene-3,20-dione) 21-succinate; sodium cortisol hemisuccinate sodium (11β, 17,21-trihydroxy-4-pregnene-3,20-dione) 21-succinate (S-M); tetrahydrocortexolone; 3α; 17; 21-trihydroxy-5β-pregnan-20-one(Ik); tetrahydrocortisol 3α,11β,17,21-tetrahydroxy-5β-pregnan-20-one(Si); tetrahydroprogesterone 3α-hydroxy-5β-pregnan-20-one(Si);

D O I：

10.1016/0022-4731(79)90250-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Forty-one steroids were assayed for their ability to act as antiglucocorticoids in viro in intact rats using thymus weight, antibody titre and plasma ACTH and corticosterone levels to assess such activity. Progesterone, an antiglucocorticoid extensively studied in vitro, demonstrated significant in viro antagonism of endogenous corticosterone by increasing all the measured parameters except thymus weight. Competition studies against exogenous corticosterone using adrenalectomized rats indicated that the increased corticosterone blood levels mask progesterone antagonism on the thymus. Like progesterone. several other compounds including cortexolone, 17α-hydroxyprogesterone, 16α-methylprogesterone and 16α-ethynylprogesterone demonstrated multi-site antiglucocorticoid activity in vivo. One previously untested compound, 17α-methylprogesterone demonstrated in vivo an ability to significantly elevate antibody titres and increase thymus weight while simultaneously having no effect on ACTH and corticosterone blood levels. The possible therapeutic use of such selective antiglucocorticoids as immunopotentiators is discussed. © 1979.

引用

页码：245 / 259

页数：15

共 64 条

[1] EFFECTS OF LATE THYMECTOMY ON IMMUNOSUPPRESSIVE ACTION OF CORTISONE AND TESTOSTERONE IN RATS IMMUNIZED TO SHEEP RED BLOOD-CELLS [J].