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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.
[25] [26] The pancreatic lipase is secreted to the small intestine where it is most active, at pH 7-7,5. [20] Pancreatic lipase hydrolyses triglycerides and diglycerides by cleaving acyl chains at the sn-1 and sn-3 position [21] and releases free fatty acids and 2-monoglycerides. [23] The pancreatic lipase consists of 465 amino acids.
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.
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]
These lipases, unlike alkaline lipases (such as pancreatic lipase), do not require bile acid or colipase for optimal enzymatic activity. Acidic lipases make up 30% of lipid hydrolysis occurring during digestion in the human adult, with gastric lipase contributing the most of the two acidic lipases.
pancreatic lipase: PNLIP: digestive juice: Human pancreatic lipase (HPL) is the main enzyme that breaks down dietary fats in the human digestive system. [5] To exhibit optimal enzyme activity in the gut lumen, PL requires another protein, colipase, which is also secreted by the pancreas. [18] lysosomal lipase: LIPA: interior space of organelle ...
It produces the pancreatic lipase inhibitor lipstatin, [1] of which the antiobesity drug orlistat is a derivative. [2] References