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Lipase inhibitors can be found naturally in plants and can also be produced as pharmaceutical drugs.Some lipase inhibitors have been identified in Panax ginseng. [5] [6] Some active compounds with chalcone scaffold found in Glycyrrhiza glabra, Cassia mimosoides, Glycyrrhiza uralensis, Boesenbergia rotunda, apples and Morus alba also had strong effect against lipase.
Pancreatic lipase inhibitor was originally discovered and isolated from fermented broth of the Streptomyces toxytricini bacterium in 1981 and named lipstatin. [7] It is a selective and potent irreversible inhibitor of human gastric and pancreatic lipases.
Lipstatin is a potent, irreversible inhibitor of pancreatic lipase. It is a natural product that was first isolated from the actinobacterium Streptomyces toxytricini. [1] The popular antiobesity drug orlistat (trade names Xenical and alli) is a saturated derivative of lipstatin.
Pancreatic lipase, also known as pancreatic triacylglycerol lipase or steapsin, is an enzyme secreted from the pancreas.As the primary lipase enzyme that hydrolyzes (breaks down) dietary fat molecules in the human digestive system, it is one of the main digestive enzymes, converting triglyceride substrates like 1 found in ingested oils to monoglycerides 3 and free fatty acids 2a and 2b.
Pancreatin is a mixture of several digestive enzymes produced by the exocrine cells of the pancreas. It is composed of amylase, lipase and protease. [11] This mixture is used to treat conditions in which pancreatic secretions are deficient, such as surgical pancreatectomy, pancreatitis and cystic fibrosis.
Blood tests for lipase may be used to help investigate and diagnose acute pancreatitis and other disorders of the pancreas. [32] Measured serum lipase values may vary depending on the method of analysis. [citation needed] Lipase assist in the breakdown of fats in those undergoing pancreatic enzyme replacement therapy (PERT).
Orlistat (Xenical) and cetilistat reduce intestinal fat absorption by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested. [ 31 ]
Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. [9] However, due to its relative simplicity and stability, orlistat was chosen over lipstatin for development as an anti-obesity drug. [10]