Inhibitory effects of glycyrrhetic acid and its related compounds on 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol.
Glycyrrhetic acid (GA), aglycone of glycyrrhizin (GL), inhibited potently (I50 = 7 x 10(-6) M) and non-competitively the activity of NAD(P)+-linked 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol. The inhibition was slightly weaker than that of indomethacin, a potent anti-inflammatory agent, but stronger than that of dexamethasone, another anti-inflammatory agent. GL, GA monoglucuronide, and 3-epi-glycyrrhetic acid also inhibited this enzyme activity, but did so less effectively (I50 = 5-8 x 10(-5) M). Carbenoxolone (GA 3-hemisuccinate) and 3-keto-glycyrrhetic acid showed potent inhibitory effects similar to GA, and 18 alpha-GA showed the most powerful inhibition of the activity.
Akao
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Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Japan.
Akao
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Hattori
M
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Namba
T
T
Kobashi
K
K
D015096:3-Hydroxysteroid Dehydrogenases / Q000037:antagonists & inhibitors*; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific); D000818:Animals; D003600:Cytosol / Q000187:drug effects / Q000201:enzymology*; D006034:Glycyrrhetinic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D008099:Liver / Q000187:drug effects / Q000201:enzymology*; D008297:Male; D051381:Rats; D017208:Rats, Wistar
D015096:3-Hydroxysteroid Dehydrogenases; D045002:3-alpha-Hydroxysteroid Dehydrogenase (B-Specific); D006034:Glycyrrhetinic Acid