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- Cholesterol transporter proteins in HepG2 cells can be modulated by phenolic compounds present in Opuntia ficus-indica aqueous solutionsPublication . RESSAISSI, Asma; ATTIA, Nebil; Pacheco, Rita; Fale, Pedro; Serralheiro, Maria LuisaIncreased blood cholesterol is a risk factor for atherosclerotic cardiovascular disease. This study tested the hypothesis that phenolic compounds can modulate the level of cholesterol transporters including Niemann-Pick C1-like 1 (NPC1L1) and ATP-binding cassette transporters in liver cells. HepG2 cells, used as a model of hepatocytes, showed a decrease in the abundance of cholesterol transporters comparatively to the control when treated with the Opuntia ficus-indica's cladodes decoction. The decrease was between 13-70%, 25-60%, 9-60% and 23-60% for NPC1L1, ABCA1, ABCG5 and ABCG8 transporters, respectively, when using between 0.15 and 0.35 mg/mL of decoction in the culture medium. FTIR analysis showed changes in the amount of RNA, which may be the cause of the decrease in the level of several proteins. These in vitro results pave the way to a molecular explanation for the decoction of cladodes effect on cholesterol levels as it reduced the membrane cholesterol transporter proteins, NPC1L1, ABCG5/ABCG8 and ABCA1, in HepG2 cells.
- Isorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studiesPublication . RESSAISSI, Asma; ATTIA, Nebil; Falé, Pedro Luís; Pacheco, Rita; Victor, Bruno L.; Machuqueiro, Miguel; Serralheiro, Maria Luísa M.Bioactive compounds, such as isorhamnetin and piscidic acid, were obtained from decoctions of cladodes (stem pads from Opuntia ficus-indica). The effect of these phenolic compounds, in a fiber-free extract, were evaluated as inhibitors of cholesterol permeation through a Caco-2 cell monolayer and as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. A reduction of 38% in cholesterol permeation through the Caco-2 cell monolayer was obtained, and the phenolic compounds all permeated between 6 and 9%. A mixture of these compounds showed an IC50 of 20.3 mu g/mL as an enzyme inhibitor, whereas piscidic acid alone showed an IC50 of 149.6 mu g/mL; this was slightly outperformed by the isorhamnetin derivatives. Docking studies confirmed that both piscidic acid and isorhamnetin derivatives, present in the decoction, could adequately bind to the enzyme active site. These results reveal that O. ficus-indica, and cladodes derived there from, is a promising plant for use in the development of new functional foods and pharmaceutical products.