Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers
| Autor: | René Laugier, Andre Fleury, Frédéric Carrière, Christoph Beglinger, Francine Ferrato, Stéphane Ransac, Paul Hadvary, Hans Lengsfeld, Josiane De Caro, Christophe Renou, Patricia Sanwald-Ducray, Véronique Lopez, Robert Verger, Alain De Caro |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Adult
Male medicine.medical_specialty Duodenum Physiology Lipolysis In Vitro Techniques Duodenogastric Reflux Excretion Lactones Pancreatic Juice Physiology (medical) Internal medicine medicine Humans Gastric lipase Obesity Intubation Gastrointestinal Pancreas Orlistat Meal Gastric Juice Hepatology Chemistry digestive oral and skin physiology Gastroenterology Lipase Middle Aged Dietary Fats Endocrinology Gastric Mucosa Lipase inhibitors Pancreatic juice Female Anti-Obesity Agents Digestion medicine.drug |
| Zdroj: | Scopus-Elsevier Europe PubMed Central |
| ISSN: | 1522-1547 0193-1857 |
| DOI: | 10.1152/ajpgi.2001.281.1.g16 |
| Popis: | The inhibition of digestive lipases by the antiobesity drug Orlistat along with lipolysis levels and fecal fat excretion were measured in healthy humans. Orlistat was found to be a powerful gastric lipase inhibitor, achieving 46.6–91.4% enzyme inhibition and thus greatly reducing gastric lipolysis of solid and liquid meals (11–33% of respective controls). Gastric lipase inhibition by Orlistat was extremely fast (half-inhibition time < 1 min). Duodenal lipolysis was reduced significantly by Orlistat given with the solid meal (32.6–37.6% of controls) but was only slightly reduced by Orlistat given with the liquid meal (74.5–100% of controls). Human pancreatic lipase (HPL) inhibition was found to be high (51.2–82.6%), however, regardless of the meal. These paradoxical results were explained when in vitro lipolysis experiments were performed. The rates of HPL inhibition by Orlistat were found to be similar with both types of meals (half-inhibition time 5–6 min), but the preemulsified triglycerides of the liquid meal were rapidly hydrolyzed by HPL before the enzyme was significantly inhibited by Orlistat. With the solid meal, the rate of hydrolysis of the meal triglycerides by HPL was slower than the rate of HPL inhibition by Orlistat. As predicted from the previous results, the effects of Orlistat on fat excretion levels were found to be much greater with the solid (40.5–57.4% of ingested fat) than with the liquid (4.2–18.8%) test meal. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|