View : 19 Download: 0

Pharmacokinetics and hepatoprotective effects of 2-methylaminoethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2-carboxyli c acid-2'-carboxylate monohydrochloride in rats with CCl 4-induced acute hepatic failure

Title
Pharmacokinetics and hepatoprotective effects of 2-methylaminoethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2-carboxyli c acid-2'-carboxylate monohydrochloride in rats with CCl 4-induced acute hepatic failure
Authors
Oh S.Y.Lee C.H.Ku Y.S.
Ewha Authors
구영순
SCOPUS Author ID
구영순scopusscopus
Issue Date
2000
Journal Title
Journal of Pharmacy and Pharmacology
ISSN
0022-3573JCR Link
Citation
vol. 52, no. 9, pp. 1099 - 1103
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
The pharmacokinetics and hepatoprotective effects of 2-methylaminoethyl-4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2-carboxyli c acid-2'-carboxylate monohydrochloride (DDB-S) have been investigated in rats with CCl 4-induced acute hepatic failure. To study the pharmacokinetics of DDB-S, rats were divided into a control group and a CCl 4-intoxicated group. DDB-S 50 mg kg -1 was administered by intravenous bolus injection to both groups of rats. In the CCl 4-intoxicated rats the plasma concentrations of DDB-S were significantly higher, the area under the plasma concentration-time curve from time zero to time infinity was significantly greater (6.46 vs 3.34 mg min mL -1), and the total body (7.74 vs 15.0 mL min -1 kg -1), renal (2.55 vs 5.10 mL min -1 kg -1), nonrenal (5.07 vs 9.65 mL min -1 kg -1), and biliary (1.48 vs 2.69 mL min -1 kg -1) clearances were significantly slower compared with the control rats. This could be due to decreased hepatic cytochrome P450 activity and impaired kidney function induced by CCl 4. To study the hepatoprotective effects of DDB-S, rats were divided into three groups, control rats and CCl 4-intoxicated rats with or without DDB-S pretreatment (50 mg kg -1, i.p.). The effects of DDB-S pretreatment on CCl 4-induced liver injury were considerable; the serum levels of alanine transaminase, aspartate transaminase, and alkaline phosphatase were significantly lower by 54.3, 44.6 and 67.2%, respectively, compared with the CCl 4-intoxicated-only group. In an in-vitro study, rat hepatocytes were exposed to fresh medium containing 10 mM CCl 4 and various concentrations of DDB-S (10 or 100 μg mL -1). The levels of alanine transaminase and aspartate transaminase in the medium were measured as an indicator of hepatocyte injury. DDB-S dose-dependently decreased the levels of alanine transaminase and aspartate transaminase compared with CCl 4-intoxication only. These results indicate that DDB-S has hepatoprotective activity.
Appears in Collections:
약학대학 > 약학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE