Antidyslipidemic and Antioxidant Effects of Novel Lupeol-Derived Chalcones |
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Authors: | Shishir Srivastava Ravi Sonkar Sunil Kumar Mishra Avinash Tiwari Vishal Balramnavar Snober Mir Gitika Bhatia Anil K Saxena Vijai Lakshmi |
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Affiliation: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow, 226 001, India 2. Department of Biochemistry, Central Drug Research Institute, Lucknow, 226 001, India 4. Department of Biotechnology, Integral University, Lucknow, 226 001, India 3. Department of Biochemistry, King George Medical University, Lucknow, 226 003, India
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Abstract: | 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. |
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Keywords: | Chalcones Lupeol Lupenone Lipoprotein lipase (LPL) Antihyperlipidemic activity |
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