Abstract
Background: Cholesterol cholelithiasis is a multifactorial hepatobiliary disease.
Methods: Interactions between genetic and environmental factors play a critical role in biliary cholesterol homeostasis and its imbalance enhances cholelithogenesis. Results: In patients developing symptoms or complications of gallstone disease, laparoscopic cholecystectomy is recommended for treatment of gallstones. In a subgroup of patients with small, radiolucent pure cholesterol gallstones, the hydrophilic bile acid, ursodeoxycholic acid (UDCA) is still considered the only pharmacological therapy able to induce oral litholysis. Identifying novel and effective pharmacological therapies is being investigated. Conclusions: We propose that the specific intestinal Niemann-Pick C1-like 1 protein inhibitor ezetimibe is a potential agent for preventing gallstone formation by reducing bioavailability of intestine- derived cholesterol to the liver for biliary secretion and desaturating bile through the inhibition of intestinal absorption of cholesterol.Keywords: Brush border, ezetimibe, gallstones, intestinal cholesterol absorption, Niemann-Pick C1-like 1 protein.
Medicinal Chemistry
Title:Effect of Inhibition of Intestinal Cholesterol Absorption on the Prevention of Cholesterol Gallstone Formation
Volume: 13 Issue: 5
Author(s): Piero Portincasa*David Q.-H. Wang
Affiliation:
- University of Bari Medical School, Clinica Medica ,Italy
Keywords: Brush border, ezetimibe, gallstones, intestinal cholesterol absorption, Niemann-Pick C1-like 1 protein.
Abstract: Background: Cholesterol cholelithiasis is a multifactorial hepatobiliary disease.
Methods: Interactions between genetic and environmental factors play a critical role in biliary cholesterol homeostasis and its imbalance enhances cholelithogenesis. Results: In patients developing symptoms or complications of gallstone disease, laparoscopic cholecystectomy is recommended for treatment of gallstones. In a subgroup of patients with small, radiolucent pure cholesterol gallstones, the hydrophilic bile acid, ursodeoxycholic acid (UDCA) is still considered the only pharmacological therapy able to induce oral litholysis. Identifying novel and effective pharmacological therapies is being investigated. Conclusions: We propose that the specific intestinal Niemann-Pick C1-like 1 protein inhibitor ezetimibe is a potential agent for preventing gallstone formation by reducing bioavailability of intestine- derived cholesterol to the liver for biliary secretion and desaturating bile through the inhibition of intestinal absorption of cholesterol.Export Options
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Cite this article as:
Portincasa Piero*, Wang Q.-H. David, Effect of Inhibition of Intestinal Cholesterol Absorption on the Prevention of Cholesterol Gallstone Formation, Medicinal Chemistry 2017; 13 (5) . https://dx.doi.org/10.2174/1573406413666170209122851
DOI https://dx.doi.org/10.2174/1573406413666170209122851 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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