Protective effects of acetylbergenin against carbon tetrachloride-induced hepatotoxicity in rats.
The present study was undertaken to investigate whether or not the hepatoprotective activity of acetylbergenin was superior to bergenin in carbon tetrachloride (CCl4)-intoxicated rat. Acetylbergenin was synthesized by acetylating bergenin, which was isolated from Mallotus japonicus. The hepatoprotective effects of acetylbergenin were examined against CCl4-induced liver damage in rats by means of serum and liver biochemical indices. Acetylbergenin was administered orally once daily for 7 successive days, then a 0.5 ml/kg mixture of CCl4 in olive oil (1:1) was intraperitoneally injected at 12 h and 36 h after the final administration of acetylbergenin. Pretreatment with acetylbergenin reduced the elevated serum enzymatic activities of alanine/aspartate aminotransferase, sorbitol dehydrogenase and gamma-glutamyltransferase in a dose dependent fashion. Acetylbergenin also prevented the elevation of hepatic malondialdehyde formation and depletion of glutathione content dose dependently in CCl4-intoxicated rats. In addition, the decreased activities of glutathione S-transferase and glutathione reductase were restored to almost normal levels. The results of this study strongly suggest that acetylbergenin has potent hepatoprotective activity against CCl4-induced hepatic damage in rats by glutathione-mediated detoxification as well as having free radical scavenging activity. In addition, acetylbergenin doses of 50 mg/kg showed almost the same levels of hepatoprotective activity as 100 mg/kg of bergenin, indicating that lipophilic acetylbergenin is more active against the antihepatotoxic effects of CCl4 than those of the much less lipophilic bergenin.
Lim
H K
HK
College of Pharmacy, Chungbuk National University, Cheongju, Korea.
Kim
H S
HS
Kim
S H
SH
Chang
M J
MJ
Rhee
G S
GS
Choi
J
J
D000818:Animals; D001578:Benzopyrans / Q000737:chemistry / Q000627:therapeutic use*; D002252:Carbon Tetrachloride Poisoning / Q000201:enzymology / Q000378:metabolism / Q000517:prevention & control*; D056486:Chemical and Drug Induced Liver Injury / Q000201:enzymology / Q000378:metabolism / Q000517:prevention & control*; D008111:Liver Function Tests; D019441:Plant Epidermis / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D020011:Protective Agents / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley
D001578:Benzopyrans; D020011:Protective Agents; C418963:acetylbergenin