Pharmacological Studies of Gardeniae Fructus. I. Effects of Geniposide and Genipin on the Biliary Excretion, the Gastric Juice Secretion, and the Gastric Contraction, and Other Pharmacological Actions

Abstract

Pharmacological studies were made on geniposide, genipin, and gardenia fruit extract on the first general screening test and on their effect on digestive organs, especially on biliary excretion, gastric juice secretion, and gastric contraction. Geniposide is the main component of fruits of gradenia (Gardenia jasminoides ELLIS) and genipin is its aglucone. Gardenia fruit is an important crude drug which is used in prescriptions of Chinese medicine, Shishishi-to ( ?? ?? ?? ?? ), Shishikankyo-to ( ?? ?? ?? ?? ?? ), Inchinko-to ( ?? 〓 ?? ?? ), etc., and may be expected to show sedative, anti-inflammatory, choleretic, antipyretic, and diuretic effects. In the first general screening test, geniposide and genipin inhibited the writhing behavior in mice induced by acetic acid, and genipin showed a weak anti-acetylcholine action and a weak antihistamine action on the isolated mouse. ileum and isolated guinea pig ileum, respectively. Genipin increased biliary excretion by either intravenous, intraduodenal, or oral administration in rats. The choleretic activity of genipin was almost equal to that of sodium dehydrocholate. Genipin inhibited the gastric secretion in the pylorusligated rat, the potency being 1/10 to 1/5 of atropine sulfate. Geniposide and genipin inhibited both the spontaneous contraction and the pilocarpine-induced contraction of the rat stomach. Such an inhibition, however, was transient and geniposide was less potent.