105 巻 (1985) 2 号 p. 109-118
There are a variety of crude drugs which are reputed to be effective for liver disorders. To evaluate liver-protective activity and to elucidate active constituents of those drugs, it is essential that appropriate assay methods are provided. Antihepatotoxic activity has hitherto been assessed by in vivo assay methods employing whole animals which, however, are costly in animals, require fairly large amounts of samples and give marked variation and poor reproducibility of the results, and, therefore, are not suitable for activity-guided fractionation of plant extracts. For primary screening of antihepatotoxic activity of extracts, fractions and constituents of liver-protective crude drugs, carbon tetrachloride-, D-galactosamine-, peroxide- and ionophore-produced cytotoxicity models utilizing primary cultured rat hepatocytes have been established. The antihepatotoxic effects of the known natural products have been evaluated using these methods thus devised. A number of crude drugs have been screened by means of the in vitro assay methods using carbon tetrachloride- and D-galactosamine-induced cytotoxicity models to reveal that some exhibited significant antihepatotoxic effects. A survey for the antihepatotoxic constituents in the active drugs has been conducted and the antihepatotoxic actions of the active constituents of Artemisia capillaris buds, Salvia plebeia herbs, Curcuma longa rhizomes, Zingiber officinale rhizomes, Schizandra chinensis fruits, Atractylodes rhizomes, Swertia japonica herbs, Tetrapanax papyriferum leaves, Dianthus superbus var. longicalycinus herbs, Panax ginseng roots, Aeginetia indica herbs and Ephedra roots have been assessed. The mechanisms of antihepatotoxic actions of glycyrrhizin, atractylon and wuweizisu C have been examined.