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Anti-pancreatic lipase and anti-adipogenic effects of 5, 7, 3′,4′,5’ -pentamethoxy and 6, 2′,4′-trimethoxy flavone - An In vitro study

Ahmad, Bilal, Friar, Emily P., Taylor, Emerald, Vohra, Muhammad Sufyan, Serpell, Christopher J., Garrett, Michelle D., Ee Loo, Jason Siau, Fong, Isabel Lim, Wong, Eng Hwa (2023) Anti-pancreatic lipase and anti-adipogenic effects of 5, 7, 3′,4′,5’ -pentamethoxy and 6, 2′,4′-trimethoxy flavone - An In vitro study. European Journal of Pharmacology, 938 . Article Number 175445. ISSN 0014-2999. (doi:10.1016/j.ejphar.2022.175445) (KAR id:98984)

Abstract

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 pre-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.

Item Type: Article
DOI/Identification number: 10.1016/j.ejphar.2022.175445
Additional information: For the purpose of open access, the author has applied a CC BY public copyright licence (where permitted by UKRI, an Open Government Licence or CC BY ND public copyright licence may be used instead) to any Author Accepted Manuscript version arising
Uncontrolled keywords: Adipogenesis, Obesity, Pancreatic lipase, Cell Differentiation, 3T3-L1 Cells, Animals, Swine, Triglycerides - metabolism, Anti-adipogenic, PPAR gamma - genetics - metabolism, Anti-Obesity, Molecular Docking Simulation, CCAAT-Enhancer-Binding Protein-alpha - genetics, Lipase - metabolism, Polymethoxy flavones, Mice, Flavones - pharmacology
Subjects: Q Science
Divisions: Divisions > Division of Natural Sciences > Chemistry and Forensics
Funders: Engineering and Physical Sciences Research Council (https://ror.org/0439y7842)
University of Kent (https://ror.org/00xkeyj56)
SWORD Depositor: JISC Publications Router
Depositing User: JISC Publications Router
Date Deposited: 09 Dec 2022 11:41 UTC
Last Modified: 20 Dec 2022 12:40 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/98984 (The current URI for this page, for reference purposes)

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