Drugs online research references
Rev Med Liege. 1998 Nov;53(11):646-50.
[Drug clinics. How I treat various metabolic diseases treated by a drug intervention that targets the intestine]
[Article in French]
Scheen AJ.
Departement de Medecine, CHU Sart Tilman, Liege 1.
Besides the classical dietary regimen, it is possible to use specific pharmacological approaches, targeted at the intestine, in order to treat some metabolic disorders. Three approaches will be described: anionic resins for treating hypercholesterolaemia, alpha-glucosidase inhibitors for treating diabetes mellitus and reactive hypoglycaemia, and intestinal lipase inhibitors for treating obesity. All these drugs are based on original concepts, but their clinical use is often limited by the occurrence of digestive side-effects. The latter may generally be reduced by progressive and individual titration of the dosage of each drug and/or by following an appropriate diet.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9887653&dopt=Abstract
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Biochem J. 1999 May 1;339 ( Pt 3):615-20.
Pancreatic lipase/colipase-mediated triacylglycerol hydrolysis is required for cholesterol transport from lipid emulsions to intestinal cells.
Young SC, Hui DY.
Department of Pathology and Laboratory Medicine, University of Cincinnati College of Medicine, 231 Bethesda Avenue, Cincinnati, OH 45267-0529, USA.
This study tested the hypothesis that dietary cholesterol uptake by intestinal cells is dependent on the structure and composition of the lipid carriers in the extracellular milieu. In in vivo experiments with female C57BL/6 mice, cholesterol absorption from phospholipid/triacylglycerol emulsions was significantly reduced by administration of tetrahydrolipstatin, an inhibitor of pancreatic lipase. This inhibitor had no effect on the absorption of cholesterol from phospholipid vesicles. The importance of pancreatic-lipase-mediated triacylglycerol hydrolysis for cholesterol transport from emulsions to intestinal cells was confirmed by in vitro experiments with rat IEC-6 intestinal cells. Cellular uptake of cholesterol from emulsions with a phospholipid/triacylglycerol molar ratio of <0.3 could be stimulated by pancreatic lipase/colipase hydrolysis of the core neutral lipids. However, pancreatic lipase/colipase was ineffective in hydrolysing triacylglycerols in emulsions with a phospholipid/triacylglycerol molar ratio of >0.3. Phospholipase A2-mediated hydrolysis of the surface phospholipids was necessary prior to triacylglycerol hydrolysis in these phospholipid-rich emulsions and to the stimulation of cholesterol transport from these particles to IEC-6 cells. The data also revealed that minimal triacylglycerol hydrolysis was sufficient to significantly increase cholesterol transport from lipid emulsions to the intestinal cells. Thus the products of triacylglycerol hydrolysis, namely monoacylglycerol and non-esterified fatty acids, are key determinants in mediating cholesterol transport from lipid emulsions to intestinal cells. Taken together, these results support the hypothesis that remodelling of the surface and core components of lipid carriers is necessary prior to absorption of dietary cholesterol from the gastrointestinal tract.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10215600&dopt=Abstract
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unav.es
Traditional analysis of the dissolution of lipophilic compounds from aqueous phase into oil is often hampered by the necessity to separate the receiver oil compartment from the aqueous phase. In order to avoid possible artefacts associated with additional separation methods, a procedure was developed to selectively detect the entry of a compound into the oil phase of a oil/water dispersion. When a combination of a primary and secondary scintillator was predissolved in the oil, and solid 14C-tetrahydrolipstatin was added, increasing signals from the same container were measured upon prolonged incubation. The data are consistent with the hypothesis that 14C-THL that has dissolved in the oil phase is essentially responsible for the measured signal. The obtained dissolution profiles of 14C-THL into oil match with parallel experiments using classical procedures.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10699715&dopt=Abstract
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