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Antidyslipidemic and Antioxidant Effects of Novel Lupeol-Derived Chalcones

Srivastava, Shishir, Sonkar, Ravi, Mishra, Sunil Kumar, Tiwari, Avinash, Balramnavar, Vishal, Mir, Snober, Bhatia, Gitika, Saxena, Anil K., Lakshmi, Vijai
Lipids 2013 v.48 no.10 pp. 1017-1027
adipogenesis, antioxidant activity, chalcones, lipolysis, lipoprotein lipase, phospholipids, rats, triacylglycerols
A series of Lupeol-based chalcones have been synthesized aiming to enhance the therapeutic efficacy of parent compound, the novel compounds were evaluated for their antidyslipidemic activity in triton-WR 1339 induced hyperlipidemic rats. Among the ten synthesized chalcones, the most active K4, K8, and K9 reversed the plasma levels of TC by (24, 25, 27 %), phospholipid by (25, 26, 25 %) and triacylglycerol by (27, 24, 24 %) respectively. In addition, the compounds showed significant in vitro antioxidant activity. The lipid lowering activity of these compounds were mediated through lipoprotein lipase activation (12–21 %) and enhanced post-heparin lipolytic activity (15–16 %). The compounds also displayed noteworthy inhibitory effect on 3-hydroxy-3-methyl-glutaryl reductase activity (in vitro). The in vitro effect of the most active compounds on MDI-induced adipogenesis using 3T3-L1 preadipocytes at 10 and 20 μM concentrations showed significant inhibition (20–32 %) of adipogenesis.