We have conducted to characterize the physico-chemical change and pharmacological transformation of traditional herbal medicines by means of processing. Processed Gardeniae Fructus was prepared by heating of fruit of Gardenia jasminoides(GF) for $30{sim}50;minute$ in the roster designed for herb processing. The contents of drying loss, water extract, diluted ethanol extract, ether extract and geniposide in non-processed GF and processed GF were examined. The contents of drying loss, water extract and geniposide in processed GF showed a decrease as compared with those of non-processed GF, however the contents of dilute ethanol and ether extract showed a increase as compared with those of non-processed GF. The rate of decrease/increase of those index were in proportion to heating time. And, biological activities of methanol extract of non-processed GF and processed GF were investigated. DPPH scavenging effects and inhibitory effect of xanthine oxidate and hemolysis of processed GF exhibited more effective than those of non-processed GF in vitro. Accelerating effect of large intestinal transport and purgative action of non- processed GF were discriminated by processing of GF. Methanol extracts of non-pro- cessed GF and processed GF showed the protective effects against the hepatotoxicity induced by ${alpha}-naphthylisothiocyanate$ in rats. These results suggested that the transformation of biological activities of GF by means of processing may be due to the physico-chemical change of the constituents in GF by heating.