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Lipases inhibition

Achieving specific and covalent inhibition of hpolytic enzymes is a difficult task, because of mutuaUy non-exclusive processes such as interfacial denaturation, changes in interfacial quahty [45], and surface dilution phenomena [46]. Further- [Pg.159]

In Fig. 9.4 are depicted the chemical structures of all inhibitors we will discuss diethyl p-nitrophenyl phosphate (Egoo), orlistat and O-mefhyl-O-(p-nitrophenyl) n-undecylphosphonate (Cll-P). In order to study the effects of these reagents, which can in principle modify covalently several essential amino acid residues of the lipases, we have proposed four different methods [50-52], depending upon the order of addition of lipase, substrate and inhibitor (Fig. 9.5). [Pg.160]

This method (Fig. 9.5 A) was set up to test, in aqueous medium and in the absence of substrate, the possible reactions between lipases and all the reagents to be tested [53, 54]. Residual lipase activity was measured separately using an emulsified substrate. Sometimes the inhibitor is incorporated into a solution of a tensio-active agent in order to create a mixed micellar interface, containing the incorporated inhibitor, and described as method A by Cudrey et al. [52]. [Pg.162]


In 1987, scientists at Hoffmann-La Roche described their discovery of hpstatin (5), a secondary metabolite isolated from Strptomyces toxytricini, and demonstrated that it is a potent inhibitor of pancreatic lipase.Simple hydrogenation of 5 formed terahydrolipstatin (1,USAN, orlistat) which possesses comparable biological activity but is more stable than 5. Orlistat (1, Xenical ) works through pancreatic lipase inhibition. Pancreatic lipase is the key enzyme of dietary triglyceride absorption, exerting its activity... [Pg.150]

An extensive study of the effects of formaldehyde in milk lipase inhibition showed that formaldehyde acts as a competitive inhibitor and, under the proper conditions, selectively inhibits the lipases of raw skim milk (Schwartz et al. 1956A). This study showed that the inhibitory effect of formaldehyde was dependent on such factors as pH, time of addition of the inhibitor, length of the incubation period, concentration... [Pg.230]

Sundheim, G., Bengtsson-Olivecrona, G. 1987b. Hydrolysis of bovine milk fat globules by lipoprotein lipase inhibition by proteins extracted from milk fat globule membrane. J. Dairy Sci. 70, 1815-1821. [Pg.554]

Quistad, G.B., Klintenberg, R., Caboni, P., Liang, S.N., Casida, J.E. (2006). Monoacylglycerol lipase inhibition by organophosphorus compounds leads to elevation of brain 2-arachidonoylglycerol and the associated hypomotilify in mice. Toxicol. Appl. Pharmacol. 211 78-83. [Pg.89]

DDT can be determined in microgram amounts by its inhibition of carbonic anhydrase (69). Several of the chlorinated insecticides as well as the carbamate insecticide, Sevin, are potent lipase inhibitors. As little as 0.1-1 /Ag/ml of Sevin, aldrin, heptachlor, lindane, 10 / g/ml of DDT, and 2,4-d can be determined fluorimetrically with 2-3% precision by the lipase inhibition when 4-methyl umbelliferone heptanoate is used as substrate (70). The lipase inhibition procedure for DDT determination is much easier to carry out than the carbonic anhydrase assay which involves monitoring gaseous COo production. [Pg.48]

M48. Mori, M., Yamaguchi, K., and Abe, K. Purification of a lipoprotein lipase-inhibiting protein produced by a melanoma cell line associated with cancer cachexia. Biochem. Biophys. Res. Commun. 160, 1085-1092 (1989). [Pg.76]

Increased expression of high-affinity LDL receptors Increased lipid hydrolysis by lipoprotein lipase Inhibition of secretion of VLDL by the liver Reduction of secretion of HDL by the liver When used as monotherapy, a major toxicity of gemfibrozil is increased risk of (A) Bloating and constipation Cholelithiasis Hyperuricemia Liver damage Severe cardiac arrhythmia... [Pg.320]

Bomser, J. A., Quistad, G. B., and Casida, J. E. (2002). Chlorpyrifos oxon potentiates diacylglycerol-induced extracellular signal-regulated kinase (ERK 44/42) activation, possibly by diacylglycerol lipase inhibition. Toxical. Appl. Pharmacol. 17ft, 29-36. [Pg.242]

Inhibition of Lipid Absorption - Agents which decrease the absorption of dietary lipids specifically by inhibiting pancreatic lipase may be suitable for the treatment of obesity. The reduced rate of lipid absorption produced by fenfluramine in rats is probably due to an inhibition of pancreatic lipase. The structural features of a series of phenethylamines, including fenfluramine, required for lipase inhibition have been described using partially purified rat and human pancreatic lipase. Pluronic L-101, a hydrophobic surfactant is a potent inhibitor of pancreatic lipase vitro and reduces body weight gain and carcass lipid after chronic administration to rats. Fecal excretion of dietary lipid is enhanced by Pluronic L-101, thus supporting its action as a lipase inhibitor. [Pg.162]

Orlistat binds to intestinal and pancreatic lipases, inhibiting their action and reduces dietary fat absorption by about 30%. The typical dose of orlistat is 120 mg three times per day with meals. Less than 1% of the drug is taken up. Thus, most of the drug is excreted unchanged in faeces. [Pg.168]

Pancreatic lipase is a key enzyme for TAG absorption and many studies have associated polyphenols with lipase inhibition. Sugiyama et al. (2007) showed that oligomeric apple procyanidins had an inhibitory effect on pancreatic lipase activity in vitro which was higher than other polyphenolic compounds of an apple extract. These results were also confirmed in both an animal and a human study where oligomeric apple procyanidins inhibited postprandial TAG absorption. ... [Pg.184]

Satouchi, K., and Matsushita, S., 1976, Purification and properties of a lipase inhibiting protein from soybean cotyledons,... [Pg.319]


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See also in sourсe #XX -- [ Pg.227 , Pg.228 , Pg.229 , Pg.230 ]

See also in sourсe #XX -- [ Pg.148 ]

See also in sourсe #XX -- [ Pg.148 ]




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