Biol. Pharm. Bull. 28(11) 2106—2110 (2005)

between synthesis and degradation. When the balance is lost, hyperlipidemia, such as hypertriglyceridemia and hypercholesterolemia, may develop. This can cause variety of serious diseases, such as arteriosclerosis, hypertension, obesity, diabetes, functional depression of some organs, etc. Pancreatic lipase (PL) is a key enzyme for lipid breakdown required to absorb fatty acids. Pancreatic lipase, one of the exocrine enzymes of pancreatic juice, catalyzes the hydrolysis of emulsified esters of glycerol and long-chain fatty acids. Short-chain fatty acids can be directly absorbed into the blood, while long-chain fatty acids and monoglycerides combine with bile salts to form water soluble micelles. The micelles are absorbed into the mucosal cells of the intestine, and the fatty acids and monoglycerides are resynthesized into triglycerides. These triglycerides are formed into small particles known as chylomicrons, which consist of triglycerides, the sterol lipid cholesterol, and apoproteins. These chylomicrons are transported to the muscle and adipose tissue. Dietary triglyceride is usually stored in the adipose tissue. Pharmacological agents that reduce the absorption of dietary triglyceride, thereby reducing the probability of the formation of atherosclerotic plaque, have been developed, such as orlistat and clofibrate. However, the PL-inhibitory activities of natural herbal products have not been studied. As part of our continuing search for biologically active antiarteriosclerosis agents from natural herbal resources, we selected PL-inhibitors from the fructus of Gardenia jasminoides ELLIS (Gardeniae fructus, Family Rubiaceae). Gardeniae fructus (GF) is widely used in Asian countries as a natural colorant, and as a Chinese traditional medicine for its homeostatic, antiphlogistic, analgesic and antipyretic effects. It contains geniposide and crocin as main components. These components exhibit antioxidant, cytotoxic, antitumor and neuroprotective effects. However, antihyperlipidemic effects of GF and its components have not been thoroughly studied. Therefore, we isolated the main components from GF and their metabolites by human intestinal bacteria, and measured their PL-inhibitory activity and their antihyperlipidemic activities on hypertriglyceridemic and hypercholesterolemic mouse models.