The antihepatotoxic effects of gingerols, shogaols, diarylheptanoids and related analogues were assessed utilizing carbon tetrachloride- and galactosamine-induced cytotoxicity in primary cultured rat hepatocytes. Most congeners exhibited significant actions in these assay methods. The carbon tetrachloride assay appeared to be most useful in defining structure-activity relationships. The antihepatotoxic activity of gingerols and shogaols was dependent on the length of the side chain with the - and -companions eliciting the strongest activity. The gingerols exerted more intense activity than the corresponding shogaols. In the diarylheptanoids, introduction of hydroxyl groupings on the phenyl rings caused increased activity; however, the effect of the positions and number of hydroxyls on activity was variable depending on the carbon skeleton.
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