Indole-based fibrates as potential hypolipidemic and antiobesity agents. 2012

Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute (CSIR-CDRI), Lucknow 226 001, India. sashidhar123@gmail.com

Hypolipidemic and antiobesity effects of the newly synthesized indole-based fibrates were evaluated in Triton WR-1339 and high fat diet (HFD)-induced hyperlipidemic rats. Preliminary screening of all the synthesized compounds was done by using an acute model (Triton model), in which compounds 3f and 3l showed significant antidyslipidemic activity. Furthermore, these compounds 3f and 3l were found to induce significant weight loss in the visceral fat mass of HFD-fed hyperlipidemic rats without affecting the normal feeding behavior. Histological examination of the liver of rats supplemented with 3f and 3l revealed a significant decrease in steatosis when compared to the effect of the standard drug fenofibrate. Additional effects such as an increase in lecithin cholesterol acyl-transferase (LCAT) enzyme level and increased receptor mediated catabolism of I(131)-low density lipoproteins (LDL) confirm and reinforce the efficacy of both of these compounds as a new class of dual-acting hypolipidemic and antiobesity agents.

UI MeSH Term Description Entries
D006949 Hyperlipidemias Conditions with excess LIPIDS in the blood. Hyperlipemia,Hyperlipidemia,Lipemia,Lipidemia,Hyperlipemias,Lipemias,Lipidemias
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D007862 Phosphatidylcholine-Sterol O-Acyltransferase An enzyme secreted from the liver into the plasma of many mammalian species. It catalyzes the esterification of the hydroxyl group of lipoprotein cholesterol by the transfer of a fatty acid from the C-2 position of lecithin. In familial lecithin:cholesterol acyltransferase deficiency disease, the absence of the enzyme results in an excess of unesterified cholesterol in plasma. Lecithin Cholesterol Acyltransferase,Cholesterol Ester Lysolecithin Acyltransferase,Lecithin Acyltransferase,Phosophatidylcholine-Sterol Acyltransferase,Acyltransferase, Lecithin,Acyltransferase, Lecithin Cholesterol,Acyltransferase, Phosophatidylcholine-Sterol,Cholesterol Acyltransferase, Lecithin,O-Acyltransferase, Phosphatidylcholine-Sterol,Phosophatidylcholine Sterol Acyltransferase,Phosphatidylcholine Sterol O Acyltransferase
D008077 Lipoproteins, LDL A class of lipoproteins of small size (18-25 nm) and light (1.019-1.063 g/ml) particles with a core composed mainly of CHOLESTEROL ESTERS and smaller amounts of TRIGLYCERIDES. The surface monolayer consists mostly of PHOSPHOLIPIDS, a single copy of APOLIPOPROTEIN B-100, and free cholesterol molecules. The main LDL function is to transport cholesterol and cholesterol esters to extrahepatic tissues. Low-Density Lipoprotein,Low-Density Lipoproteins,beta-Lipoprotein,beta-Lipoproteins,LDL(1),LDL(2),LDL-1,LDL-2,LDL1,LDL2,Low-Density Lipoprotein 1,Low-Density Lipoprotein 2,LDL Lipoproteins,Lipoprotein, Low-Density,Lipoproteins, Low-Density,Low Density Lipoprotein,Low Density Lipoprotein 1,Low Density Lipoprotein 2,Low Density Lipoproteins,beta Lipoprotein,beta Lipoproteins
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D011422 Propionates Derivatives of propionic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxyethane structure. Propanoate,Propanoic Acid,Propionate,Propanoates,Propanoic Acid Derivatives,Propanoic Acids,Propionic Acid Derivatives,Propionic Acids,Acid, Propanoic,Acids, Propanoic,Acids, Propionic,Derivatives, Propanoic Acid,Derivatives, Propionic Acid
D002087 Butyrates Derivatives of BUTYRIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxypropane structure. Butyrate,n-Butyrate,Butanoic Acids,Butyric Acids,Acids, Butanoic,Acids, Butyric,n Butyrate
D004041 Dietary Fats Fats present in food, especially in animal products such as meat, meat products, butter, ghee. They are present in lower amounts in nuts, seeds, and avocados. Fats, Dietary,Dietary Fat,Fat, Dietary
D005234 Fatty Liver Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS. Liver Steatosis,Steatohepatitis,Steatosis of Liver,Visceral Steatosis,Liver Steatoses,Liver, Fatty,Steatohepatitides,Steatoses, Liver,Steatoses, Visceral,Steatosis, Liver,Steatosis, Visceral,Visceral Steatoses

Related Publications

Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
December 2018, Bioorganic & medicinal chemistry letters,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
January 2012, TheScientificWorldJournal,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
December 2019, Bioorganic & medicinal chemistry letters,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
June 2014, European journal of medicinal chemistry,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
July 2021, Bioorganic & medicinal chemistry letters,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
June 2015, Natural products and bioprospecting,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
August 2013, Molecular diversity,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
January 2015, European journal of medicinal chemistry,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
January 2019, Frontiers in nutrition,
Koneni V Sashidhara, and Manoj Kumar, and Ravi Sonkar, and Bhanu Shankar Singh, and A K Khanna, and Gitika Bhatia
March 1969, Journal of pharmaceutical sciences,
Copied contents to your clipboard!