Chalcones as Potential Inhibitors of Pancreatic Lipase
Obesity is a global disease that has been escalating to epidemic proportions over the past years. A recent report from World Obesity Federation predicts that, in 2030, 1 billion people will be obese. Thus, it is mandatory to develop new therapeutic options that can manage and control obesity. One of...
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MDPI AG
2022-11-01
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| Online Access: | https://www.mdpi.com/2673-9992/14/1/116 |
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| author | Sílvia Rocha Álvaro Tomé Ana Teresa Rufino Marisa Freitas Félix Carvalho Artur Silva Eduarda Fernandes |
| author_facet | Sílvia Rocha Álvaro Tomé Ana Teresa Rufino Marisa Freitas Félix Carvalho Artur Silva Eduarda Fernandes |
| author_sort | Sílvia Rocha |
| collection | DOAJ |
| description | Obesity is a global disease that has been escalating to epidemic proportions over the past years. A recent report from World Obesity Federation predicts that, in 2030, 1 billion people will be obese. Thus, it is mandatory to develop new therapeutic options that can manage and control obesity. One of the most promising research paths is the inhibition of pancreatic lipase (PL), responsible for the hydrolysis of 50 to 70% of total dietary triglycerides. Chalcones are the precursors of flavonoids, consisting of two benzene rings connected by a three-carbon α, β-unsaturated carbonyl structure. The goal of the present work was to evaluate the activity of seven chalcones with hydroxy (OH) and chloride (Cl) substituents, as potential inhibitors of PL. For this purpose, spectrophotometric and fluorometric microanalysis systems were used, based on the enzymatic metabolization of <i>p</i>-nitrophenyl butyrate and 4-methylumbeliferyl oleate, respectively. The obtained results showed that chalcones inhibit PL activity, and that the fluorometric method can reach higher inhibition rates with fewer compounds than the spectrophotometric method. These findings bring new insights into the structure design for the modulation of PL, but further studies are still needed to further explore these compounds as potential anti-obesity molecules. |
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| issn | 2673-9992 |
| language | English |
| last_indexed | 2024-03-11T06:06:32Z |
| publishDate | 2022-11-01 |
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| spelling | doaj.art-c832c7a6a27a48318e031181f26cf84c2023-11-17T12:58:28ZengMDPI AGMedical Sciences Forum2673-99922022-11-0114111610.3390/ECMC2022-13413Chalcones as Potential Inhibitors of Pancreatic LipaseSílvia Rocha0Álvaro Tomé1Ana Teresa Rufino2Marisa Freitas3Félix Carvalho4Artur Silva5Eduarda Fernandes6Associated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalAssociated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalAssociated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalAssociated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalApplied Molecular Biosciences Unit (UCIBIO), Network of Chemistry and Technology (REQUIMTE), Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalAssociated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Department of Chemistry, University of Aveiro, 3810-193 Aveiro, PortugalAssociated Laboratory for Green Chemistry (LAQV), Network of Chemistry and Technology (REQUIMTE), Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, PortugalObesity is a global disease that has been escalating to epidemic proportions over the past years. A recent report from World Obesity Federation predicts that, in 2030, 1 billion people will be obese. Thus, it is mandatory to develop new therapeutic options that can manage and control obesity. One of the most promising research paths is the inhibition of pancreatic lipase (PL), responsible for the hydrolysis of 50 to 70% of total dietary triglycerides. Chalcones are the precursors of flavonoids, consisting of two benzene rings connected by a three-carbon α, β-unsaturated carbonyl structure. The goal of the present work was to evaluate the activity of seven chalcones with hydroxy (OH) and chloride (Cl) substituents, as potential inhibitors of PL. For this purpose, spectrophotometric and fluorometric microanalysis systems were used, based on the enzymatic metabolization of <i>p</i>-nitrophenyl butyrate and 4-methylumbeliferyl oleate, respectively. The obtained results showed that chalcones inhibit PL activity, and that the fluorometric method can reach higher inhibition rates with fewer compounds than the spectrophotometric method. These findings bring new insights into the structure design for the modulation of PL, but further studies are still needed to further explore these compounds as potential anti-obesity molecules.https://www.mdpi.com/2673-9992/14/1/116obesitypancreatic lipasechalconesinhibitionspectrophotometryfluorometry |
| spellingShingle | Sílvia Rocha Álvaro Tomé Ana Teresa Rufino Marisa Freitas Félix Carvalho Artur Silva Eduarda Fernandes Chalcones as Potential Inhibitors of Pancreatic Lipase Medical Sciences Forum obesity pancreatic lipase chalcones inhibition spectrophotometry fluorometry |
| title | Chalcones as Potential Inhibitors of Pancreatic Lipase |
| title_full | Chalcones as Potential Inhibitors of Pancreatic Lipase |
| title_fullStr | Chalcones as Potential Inhibitors of Pancreatic Lipase |
| title_full_unstemmed | Chalcones as Potential Inhibitors of Pancreatic Lipase |
| title_short | Chalcones as Potential Inhibitors of Pancreatic Lipase |
| title_sort | chalcones as potential inhibitors of pancreatic lipase |
| topic | obesity pancreatic lipase chalcones inhibition spectrophotometry fluorometry |
| url | https://www.mdpi.com/2673-9992/14/1/116 |
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