Anti-pancreatic lipase and anti-adipogenic effects of 5,7,3′,4′,5′-pentamethoxy and 6,2′,4′-trimethoxy flavone - An in vitro study
In this study, the anti-obesity effects of 5,7,3′,4′,5′ -pentamethoxyflavone (PMF) and 6,2′,4′-trimethoxyflavone (TMF) were evaluated through two distinct mechanisms of action: inhibition of crude porcine pancreatic lipase(PL), and inhibition of adipogenesis in 3T3-L1 pre-adipocytes. Both flavones...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | en |
| Published: |
Elsevier Science Direct
2023
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| Subjects: | |
| Online Access: | http://ir.unimas.my/id/eprint/41472/3/Anti-pancreatic%20-%20Copy.pdf http://ir.unimas.my/id/eprint/41472/ https://www.sciencedirect.com/journal/european-journal-of-pharmacology https://doi.org/10.1016/j.ejphar.2022.175445 |
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| Summary: | In this study, the anti-obesity effects of 5,7,3′,4′,5′
-pentamethoxyflavone (PMF) and 6,2′,4′-trimethoxyflavone
(TMF) were evaluated through two distinct mechanisms of action: inhibition of crude porcine pancreatic lipase(PL), and inhibition of adipogenesis in 3T3-L1 pre-adipocytes. Both flavones show dose dependent, competitive inhibition of PL activity. Molecular docking studies revealed binding of the flavones to the active site of PL. In 3T3-L1 adipocytes, both flavones reduced the accumulation of lipids and triglycerides. PMF and TMF also lowered the expression of adipogenic and lipogenic genes. They both reduced the expression of peroxisome proliferator-activated receptor-gamma (PPAR-γ), CCAAT/enhancer-binding protein α and β (C/EBP α and β),
sterol regulatory element-binding protein 1 (SREBF 1), fatty acid synthase (FASN), adipocyte binding protein 2(aP2), and leptin gene. In addition, these flavones enhanced adiponectin mRNA expression, increased lipolysis and enhanced the expression of lipolytic genes: adipose triglycerides lipase (ATGL), hormone sensitive lipase (HSL) and monoglycerides lipase (MAGL) in mature 3T3-L1 adipocytes. Overall, PMF was seen to be a more potent inhibitor of both PL activity and adipogenesis versus TMF. These results suggest that PMF and TMF possess anti-obesity activities and can be further evaluated for their anti-obesity effects. |
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