PMID- 1945747
OWN - NLM
STAT- MEDLINE
DCOM- 19911125
LR  - 20190726
IS  - 0031-6768 (Print)
IS  - 0031-6768 (Linking)
VI  - 418
IP  - 6
DP  - 1991 Jul
TI  - Bile acids and their amidates inhibit 11 beta-hydroxysteroid dehydrogenase 
      obtained from rat kidney.
PG  - 538-43
AB  - Recently it has been demonstrated that interaction of corticosteroids with 
      extraadrenal target cells can effectively be modulated by metabolic 
      transformation of the steroid hormone. As far as 11-hydroxylated glucocorticoids 
      are concerned 11 beta-hydroxysteroid dehydrogenase (11 beta-HSD) is the most 
      important enzyme charged with target cell metabolism. Inhibition of 11 beta-HSD 
      function either by genetically transmitted deficiency or by exogenous enzyme 
      inhibitors causes severe pathophysiological derangements, which result in a 
      syndrome of "apparent mineralocorticoid excess". In the present paper we have 
      tested whether or not endogenous inhibitors of this enzyme system might exist. 
      The effects of the main naturally occurring mono-, di-, and trihydroxylated bile 
      acids in man on 11 beta-HSD have been studied in in vitro experiments. Using rat 
      renal microsomes it could be demonstrated that unconjugated bile acids of all 
      three classes as well as the corresponding glycine and taurine amidates 
      effectively inhibit oxidative as well as reductive activity of 11 beta-HSD, with 
      lithocholic acid and chenodeoxycholic acid being the most potent compounds. It is 
      concluded that bile acids are potent endogenous inhibitors of 11 beta-HSD and, 
      therefore, could participate in abnormalities of cortisol metabolism observed in 
      liver cirrhosis and extrahepatic biliary obstruction and, possibly, after 
      ingestion of bile acids.
FAU - Perschel, F H
AU  - Perschel FH
AD  - Klinikum Steglitz, Freie Universitat Berlin, Federal Republic of Germany.
FAU - Buhler, H
AU  - Buhler H
FAU - Hierholzer, K
AU  - Hierholzer K
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Pflugers Arch
JT  - Pflugers Archiv : European journal of physiology
JID - 0154720
RN  - 0 (Bile Acids and Salts)
RN  - EC 1.1.- (Hydroxysteroid Dehydrogenases)
RN  - EC 1.1.1.146 (11-beta-Hydroxysteroid Dehydrogenases)
SB  - IM
MH  - 11-beta-Hydroxysteroid Dehydrogenases
MH  - Animals
MH  - Bile Acids and Salts/chemistry/*pharmacology
MH  - Hydroxysteroid Dehydrogenases/*antagonists & inhibitors
MH  - In Vitro Techniques
MH  - Kidney Cortex/*drug effects/enzymology
MH  - Male
MH  - Microsomes/enzymology
MH  - Rabbits
MH  - Rats
MH  - Rats, Inbred Strains
MH  - Structure-Activity Relationship
EDAT- 1991/07/01 00:00
MHDA- 1991/07/01 00:01
CRDT- 1991/07/01 00:00
PHST- 1991/07/01 00:00 [pubmed]
PHST- 1991/07/01 00:01 [medline]
PHST- 1991/07/01 00:00 [entrez]
AID - 10.1007/BF00370568 [doi]
PST - ppublish
SO  - Pflugers Arch. 1991 Jul;418(6):538-43. doi: 10.1007/BF00370568.