Isorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studies

Ressaissi, Asma; Attia, Nebil; Falé, Pedro L.; Pacheco, Rita; Victor, Bruno L.; Machuqueiro, Miguel; Serralheiro, Maria Luísa

doi:10.1007/s12272-017-0959-1

Cited by 40 publications

(26 citation statements)

References 37 publications

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“…This extract also has the potential to decrease the permeation of the cholesterol through a simulated intestinal barrier, with a similar value to those obtained with medicinal plants aqueous extracts containing phenolic compounds [33,34,51]. Cholesterol permeation may be affected because of the competition of bioactive compounds for membrane transporters like NPC1L1, which transport cholesterol into the intestinal cell or by increasing the efflux from inside the cells, through the ABCG5 and ABCG8 transporters [48].…”

Section: Discussionsupporting

confidence: 55%

Effect of Food Preparations on In Vitro Bioactivities and Chemical Components of Fucus vesiculosus

André

Guedes

Melo

et al. 2020

Foods

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Fucus vesiculosus is a brown macroalgae used in food and generally considered safe to be consumed, according to EU Directive (EC 258/97). The aim of this study is to analyze the effect of food preparation on F.vesiculosus of different origins on what concerns its chemical constituents and final bioactivities. The aqueous extract of the seaweeds were obtained at different temperatures, similar to food preparation and then purified by SPE. The compound identification was carried out by Liquid Chromatography High Resolution Mass Spectrometry (LC-HRMS/MS) and algae extracts microstructure were observed by Scanning Electron Microscopy (SEM). The activities were determined by using antioxidant activity, inhibition of acetylcholinesterase (AChE) and 3-hidroxi-3-methyl-glutaril-CoA (HMG-CoA) reductase (HMGR) together with Caco-2 cells line simulating the intestinal barrier. The activity of AChE and the HMGR were inhibited by the extracts giving IC50 values of 15.0 ± 0.1 µg/mL and 4.2 ± 0.1 µg/mL, respectively and 45% of the cholesterol permeation inhibition. The main compounds identified were phlorotannins and peptides derivatives. The mode of preparation significantly influenced the final bioactivities. Moreover, the in vitro results suggest that the preparation of F. vesiculosus as a soup could have hypercholesterolemia lowering effect.

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Section: Discussionsupporting

confidence: 55%

Effect of Food Preparations on In Vitro Bioactivities and Chemical Components of Fucus vesiculosus

André

Guedes

Melo

et al. 2020

Foods

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“…The cytotoxicity of Zls extracts were performed using the MTT viability test, against the human tumor cell lines HepG 2 (ATCC#HB-8065), from human hepatocellular liver carcinoma cell lines, and MCF-7 HTB-22), from breast cancer, were cultured in DMEM supplemented with 10% FBS, 100 U/mL Pen-Strep, and 2 mM L-glutamine at 37 • C in an atmosphere containing 5% CO 2 every 48 to 72 h before reaching confluence, the medium was changed [10]. For each concentration of extract, the assays were done in 8 × 12 replicates and the cell viability percentage was calculated by the following equation (Equation 4…”

Section: Anti-proliferative Activities On Hepg 2 and Mcf-7 Cellsmentioning

confidence: 99%

“…The β-Hydroxy-β-methylglutaryl coenzyme A reductase (HMGR, E.C. 1.1.1.88), a rate-limiting enzyme in cholesterol biosynthesis, which catalyzes the reductive deacylation of HMG-CoA to mevalonate pathway, the metabolic pathway that produces cholesterol and other isoprenoids [10,11]. The high risk of coronary heart diseases or hyperlipidemia were found to be caused by elevated serum-blood cholesterol levels [12].…”

Section: Introductionmentioning

confidence: 99%

Ultrasound Assisted Extraction of Phenolic Compounds from a Jujube By-Product with Valuable Bioactivities

et al. 2020

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Jujube plant is a potential source of polyphenols with biological propreties. The purpose of this study was to investigate the application of ultrasound technique for extracting phenolic compounds (TPC) from seeds of Zizyphus lotus under optimization conditions based on response surface methodology. A maximum TPC, total flavonoids content (TFC), and total condensed tannins content (TTC) of 2383.10 ± 0.87 mg GAE/100g, 486.50 ± 0.38 mg QE/100g and 15,787.10 ± 0.10 mg CE/100g, respectively obtained under ethanol concentration 50.16%, sonication temperature 29.01 °C, sonication time 15.94 min and solvent-to-solid ratio 34.10:1 mL/g. The optimized extract was then evaluated for its antioxidant, antiacethylcholinesterase, antihypercholesterolemia, and antiproliferative activities. The results showed that ultrasound method is a green and safe method that can be used to effectively extract TPC from jujube seeds. The biological activity of Zizyphus extract exhibited a very good antioxidant against DPPH (EC50 = 0.39 µg/mL) and FRAP (1670.42 ± 6.5 mg/100 g). Additionally, it possesses acetylcholinesterase (AChE) inhibitory effect (IC50 = 0.93 ± 0.01 mg/mL) and HMGR inhibition (45.41%) using 100 µg/mL. The extract significantly inhibits cell proliferation on the MCF-7 and HepG2 tumor cell lines with an IC50 values of <0.05 and 3 ± 0.55 mg/mL, respectively. Therefore, the ultrasound method can be considered a method for obtaining a significant anticancer activity with respect to the lines and therefore makes it possible to recover a maximum of phenolic compounds in less time with an AChE and HMGR inhibitory activity. Thus, it can be suggested that Zls extract is a promising fruit for the development of supplementary dietary due to its potential behaviour as nutraceutical.

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“…Although it has been quantified in extracts that exhibit anti‐inflammatory activity, its contribution to this bioactivity has not been studied. Until now, the reported bioactivity is its effect on hypercholesterolemia management as an inhibitor of cholesterol permeation …”

Section: Introductionmentioning

confidence: 99%

“…Until now, the reported bioactivity is its effect on hypercholesterolemia management as an inhibitor of cholesterol permeation. 11 Prickly pears have also been studied as a therapeutic approach for treating type II diabetes by lowering glucose absorption by inhibiting intestinal carbohydrate-hydrolyzing enzymes -amylase and -glucosidase. 12 Several Opuntia species have been reported to reduce glycemia and insulin requirements by acting on glucose homeostasis-related systems and energy metabolism.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory potential of prickly pears and their isolated bioactives against digestive enzymes linked to type 2 diabetes and inflammatory response

et al. 2019

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BACKGROUND Prickly pears are potential candidates for the development of low‐cost functional foods because they grow with low water requirements in arid regions of the world. They are sources of betalains and phenolic compounds, which have been reported to contribute to human health. The study of the biological activity of different varieties and of their isolated bioactive constitutes is fundamental in the design of functional foods. In this context, our objective is the assessment of the ability of Spanish and Mexican prickly‐pear cultivars to inhibit enzymes related to type 2 diabetes and the inflammatory response, and the contribution of their bioactive compounds to their nutra‐pharmaceutical potential. RESULTS Prickly pear peels presented the highest antioxidant activity due to their high isorhamnetin glycoside content. Isorhamnetin glycosides showed significantly higher antioxidant and anti‐inflammatory activity than aglycone, particularly isorhamnetin glucosyl‐rhamnosyl‐pentoside (IG2), which also reported antihyperglycemic activity. Morada, Vigor, and Sanguinos whole fruits exhibited moderate α‐amylase inhibition and higher α‐glucosidase inhibition, which is ideal for lowering glucose absorption in hyperglycemia management. Sanguinos peels presented the highest anti‐inflammatory activity because of their high indicaxanthin content and isorhamnetin glycoside profile. CONCLUSIONS In the design of prickly pear functional foods, technological processing should prioritize the retention or concentration of these bioactive compounds to preserve (or increase) their natural antioxidant, antihyperglycemic and anti‐inflammatory activity. Peels of red and orange varieties should be further evaluated for antioxidant and anti‐inflammatory purposes while whole fruits of red and purple varieties could be considered possible candidates for hyperglycemia management. © 2019 Society of Chemical Industry

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Isorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studies

Cited by 40 publications

References 37 publications

Effect of Food Preparations on In Vitro Bioactivities and Chemical Components of Fucus vesiculosus

Effect of Food Preparations on In Vitro Bioactivities and Chemical Components of Fucus vesiculosus

Ultrasound Assisted Extraction of Phenolic Compounds from a Jujube By-Product with Valuable Bioactivities

Inhibitory potential of prickly pears and their isolated bioactives against digestive enzymes linked to type 2 diabetes and inflammatory response

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