Abstract
Purpose: To synthesize and evaluate the anti-hyperlipidemic activity of a novel series of N- (benzoylphenyl)-2-furamides ( 3a , 3b , 4a , 4b and 4c ). Methods: Compounds ( 3a , 3b , 4a , 4b and 4c ) were successfully synthesized by reacting activated furan-2-carbonyl-chloride derivatives with aminobenzophenones at 60 °C for 36 h. Hyperlipidemia was induced in overnight fasted rats by intraperitoneal administration of Triton WR-1339 (300 mg/kg). to overnight fasted rats. The rats were divided into six groups: control, hyperlipidemic, hyperlipidemic plus compounds 3b , 4b , 4c , and hyperlipidemic plus bezafibrate-treated. Eighteen hours later, blood samples were collected and plasma lipid profile determined using enzymatic methods. Results: At a dose of 15 mg/kg body weight, the elevated plasma triglyceride (TG) levels, total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) levels were significantly reduced by compounds 4b (p < 0.001) and 4c (p < 0.0001) 18 h later, compared to the hyperlipidemic group. Furthermore, compounds 4b and 4c significantly increased high density lipoprotein cholesterol (HDL-C) levels by 29 and 34 %, respectively. Conclusion: The findings indicate the high potency of N-(benzolphenyl)-2-furamides ( 4b and 4c ) as lipid-lowering agents. Thus, these compounds 4b and 4c may used as lead compounds for the development of new derivatives and agents for targeting dyslipidemia and cardiovascular diseases. Keywords: Triton WR-1339-induced hyperlipidemic rats, N-(benzoylphenyl)-2-furamides, Lipid-lowering activity, Cardiovascular disease, Synthesis
Highlights
Cardiovascular diseases have become a major health problem in developing countries
Epidemiological studies demonstrate that hyperlipidemia is the most prevalent indicator of susceptibility to atherosclerosis and heart diseases [3,4,5]
The results of the present study revealed the potential anti-hyperlipidemic activity of novel series of N-(benzoylphenyl)-2-furamides using Triton WR-1339-induced hyperlipidemic rats as a model for screening the lipid lowering potential [22]
Summary
Cardiovascular diseases have become a major health problem in developing countries. Hyperlipidemia is defined as high levels of lipids (fat, cholesterol and triglycerides) circulating in the bloodstream [1,2]. Epidemiological studies demonstrate that hyperlipidemia is the most prevalent indicator of susceptibility to atherosclerosis and heart diseases [3,4,5]. Decreasing plasma lipid levels play a major role in the treatment and prevention of coronary heart diseases [6]. For this reason, many studies have been conducted to evaluate the potential lipidlowering activity of synthetic and naturally compounds. Triton WR-1339, a non-ionic detergent (oxyethylated tertiary octylphenol formaldehyde polymer) has been widely used in in vivo studies to produce acute hyperlipidemia in animal models in order to study the lipid-lowering effect of natural or chemical drugs [7]. Triton WR-1339 has been found to prevent the catabolism of triglycerol-rich lipoprotein by lipoprotein lipase [8,9]
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