ArticleBMC pharmacology2004
Inhibition of pancreatic cholesterol esterase reduces cholesterol absorption in the hamster.
Article in BMC pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 74 citations in OpenAlex.
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- Cyanidin-3-rutinoside acts as a natural inhibitor of intestinal lipid digestion and absorption.BMC complementary and alternative medicine · 2019Article
- Siamese neem flower extract suppresses cholesterol absorption by interfering NPC1L1 and micellar propertyResearch in pharmaceutical sciences · 2019Article
- Antidiabetic Effects of the Ethanolic Root Extract ofAdvances in pharmacological sciences · 2018Article
- Antidiabetic and hypolipidemic activities of hydroethanolic root extract of Uvaria chamae in streptozotocin induced diabetic albino rats.BMC complementary and alternative medicine · 2016Article
- Antidiabetic activities of aqueous ethanol and n-butanol fraction of Moringa stenopetala leaves in streptozotocin-induced diabetic rats.BMC complementary and alternative medicine · 2015Article
- Intestinal α-glucosidase and some pancreatic enzymes inhibitory effect of hydroalcholic extract of Moringa stenopetala leaves.BMC complementary and alternative medicine · 2014Article
- New insights in the activation of human cholesterol esterase to design potent anti-cholesterol drugs.Molecular diversity · 2014Article
- Isocoumarin-based inhibitors of pancreatic cholesterol esterase.Bioorganic & medicinal chemistry · 2008Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundPancreatic cholesterol esterase has three proposed functions in the intestine: 1) to control the bioavailability of cholesterol from dietary cholesterol esters; 2) to contribute to incorporation of cholesterol into mixed micelles; and 3) to aid in transport of free cholesterol to the enterocyte. Inhibitors of cholesterol esterase are anticipated to limit the absorption of dietary cholesterol.
resultsThe selective and potent cholesterol esterase inhibitor 6-chloro-3-(1-ethyl-2-cyclohexyl)-2-pyrone (figure 1, structure 1) was administered to hamsters fed a high cholesterol diet supplemented with radiolabeled cholesterol ester. Hamsters were gavage fed 3H-labeled cholesteryl oleate along with inhibitor 1, 0-200 micromoles. Twenty-four hours later, hepatic and serum radioactive cholesterol levels were determined. The ED50 of inhibitor 1 for prevention of the uptake of labeled cholesterol derived from hydrolysis of labeled cholesteryl oleate was 100 micromoles. The toxicity of inhibitor 1 was investigated in a 30 day feeding trial. Inhibitor 1, 100 micromoles or 200 micromoles per day, was added to chow supplemented with 1% cholesterol and 0.5% cholic acid. Clinical chemistry urinalysis and tissue histopathology were obtained. No toxicity differences were noted between control and inhibitor supplemented groups.
conclusionsInhibitors of cholesterol esterase may be useful therapeutics for limiting cholesterol absorption.
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