| Project/Area Number |
62570508
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
内分泌・代謝学
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| Research Institution | School of Medicine, Kanazawa University |
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Principal Investigator |
TAKEDA Ryoyu School of Medicine, Kanazawa University, 医学部, 教授 (50019535)
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| Co-Investigator(Kenkyū-buntansha) |
MORISE Toshio Kanazawa University Hospital, 医学部付属病院, 助手 (40191027)
MIYAMORI Isamu School of Medicine, Kanazawa University, 医学部, 講師 (40142278)
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| Project Period (FY) |
1987 – 1988
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| Project Status |
Completed (Fiscal Year 1988)
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| Budget Amount *help |
¥1,900,000 (Direct Cost: ¥1,900,000)
Fiscal Year 1988: ¥500,000 (Direct Cost: ¥500,000)
Fiscal Year 1987: ¥1,400,000 (Direct Cost: ¥1,400,000)
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| Keywords | Glycyrrhizin / Mg^+-HCO -ATPase / Mineralocorticoid / mineralocorticoid receptor / Electrical potential of rectal mucosa / RU 28362 / )3>ATPase / ミネ ラロコルチコイド / ミネラロコルチコイド・レセプター / RU28362 / ZK91587 / グリチルレチン酸 / 甘草 / ミネラロコルチコイド受容体 |
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| Research Abstract |
In order to elucidate the sodium-retaining and hypertensionogenic action of glycyrrhizin; an active principle of liquorice, minaralocorticoid (MC) activity of glycyrrhetinic acid (GR) which was newly synthesized, was studied in vitro and in vivo. The results were summarized as follows: (1) Scatchard analysis of [^3H] aldosterone showed that Kd of higher affinity site (type I) 6.0X10^<-9>, Bnac 1.0X10^<-14> mol/mg/protein, and Kd of lower affinity site (type II) 1.6X10^<-7>M, Bmax 7.5X10^<-14> mol/mg protein. GR competed for [^3H] aldosterone binding site in kidney sitosol at the concentration of 10^4 times as that of unlabeled aldosterone. RU-28362; glucocorticoid receptor blocker displaced aldosterone binding curve, whereas GR binding kinetic was not affected by the compound. GR competed with ZK 91587; MC receptor blocker, for [^3H]aldos teronekidney cytosol binding. (2) Decreased activity of Mg^<2+>-HCO^-_ -ATPase in brush border of the small instestine in adrenalectomized rats was partially restored by GR administration. (3) However, electrical potential differences in the adrenalectomized rats were increased in a dose-dependent manner with long-term administration of GR. (4) The oral administration of GR, in a dose of 225 mg a day for a week, caused significant decrease of the ratio of urinary cortisone to cortisol, suggesting the inhibitory effect of GR on 11-hydroxysteroid dehydrogenase activity.
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