Identification of a new natural gastric lipase inhibitor from star anise

Kamoun, Jannet; Rahier, Renaud; Sellami, Mohamed; Koubaa, Imed; Mansuelle, Pascal; Lebrun, Régine; Berlioz‐Barbier, Alexandra; Fiore, Michele; Alvarez, Karine; Abousalham, Abdelkarim; Carrière, Frédéric; Aloulou, Ahmed

doi:10.1039/c8fo02009d

Cited by 18 publications

(10 citation statements)

References 43 publications

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“…This effect may be due to the enhancement of TG-rich lipoproteins elimination through the improvement of lipoprotein lipase activity, and the enhancement of the uptake of TG carried in VLDL by peripheral organs [39]. Another mechanism may be related to the regulation of intestinal uptake of TG mediated by pancreatic lipase that catalyzes the hydrolysis of TG to mono-and diglycerides, which are uptaken by the intestinal cells [40]. Although the direct implication of TG in atherosclerosis is not confirmed yet, it has been reported that the reduction of serum TG level is effective in preventing hyperlipidemia and treating heart diseases [41].…”

Section: Discussionmentioning

confidence: 99%

Effect of polyphenol, flavonoid, and saponin fractions from Thymus atlanticus on acute and chronic hyperlipidemia in mice

Ramchoun¹,

Khouya²,

Harnafi³

et al. 2020

Futur J Pharm Sci

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Background Thymus atlanticus is an endemic plant of the Mediterranean region, which has been used in the Moroccan mountain area to treat several diseases. This study aimed to investigate the effect of polyphenol, flavonoid, and saponin fractions derived from this plant on acute and chronic hyperlipidemia in male albino mice. Results The results indicated that the injection of Triton WR-1339 (20 mg/100 g body weight (B.wt.)) and 6-week administration of a high-fat diet (which is an 81.8% standard diet supplemented with 2% cholesterol, 16% lard, and 0.2% cholic acid) significantly increased plasma total cholesterol, triglycerides and low-density lipoprotein cholesterol (LDL-C), but did not affect high-density lipoprotein cholesterol (HDL-C) levels in mice. Administration of a single dose (2 mg/kg B.wt.) of polyphenol, flavonoid, or saponin fractions significantly suppressed the effect of Triton injection on plasma total cholesterol, triglycerides, and LDL-C. In addition, the supplementation of the high-fat diet with polyphenol fraction (2 mg/kg B.wt./day) prevented the increase of total cholesterol, triglycerides, and LDL-C, and effectively increased HDL-C level when compared to mice feeding only the high-fat diet. Conclusion In conclusion, phenolic compounds from Thymus atlanticus possess a significant hypocholesterolemic and hypotriglyceridemic effects and, therefore, could have an important role in the management of dyslipidemia.

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Section: Discussionmentioning

confidence: 99%

Effect of polyphenol, flavonoid, and saponin fractions from Thymus atlanticus on acute and chronic hyperlipidemia in mice

Ramchoun¹,

Khouya²,

Harnafi³

et al. 2020

Futur J Pharm Sci

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“…Indeed, KAE showed reliable inhibitory effects against C. rugosa and C. albicans lipases [21,22]. A recent report described a possible covalent bound created between a gastric lipase and the rhamnosylated myricetin [48]. Molecular docking modeling indicated that the hydroxy group of the catalytic Ser153 residue of gastric lipase lead to a nucleophilic attack on the mentioned flavonol, which induced the addition of 1,4 nucleophilic on the double bound to form an enol function.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of CpLIP2 Lipase Hydrolytic Activity by Four Flavonols (Galangin, Kaempferol, Quercetin, Myricetin) Compared to Orlistat and Their Binding Mechanisms Studied by Quenching of Fluorescence

et al. 2019

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The inhibition of recombinant CpLIP2 lipase/acyltransferase from Candida parapsiolosis was considered a key model for novel antifungal drug discovery and a potential therapeutic target for candidiasis. Lipases have identified recently as potent virulence factors in C. parapsilosis and some other yeasts. The inhibition effects of orlistat and four flavonols (galangin, kaempferol, quercetin and myricetin) characterized by an increasing degree of hydroxylation in B-ring, were investigated using ethyl oleate hydrolysis as the model reaction. Orlistat and kaempferol (14 µM) strongly inhibited CpLIP2 catalytic activity within 1 min of pre-incubation, by 90% and 80%, respectively. The relative potency of flavonols as inhibitors was: kaempferol > quercetin > myricetin > galangin. The results suggested that orlistat bound to the catalytic site while kaempferol interacted with W294 on the protein lid. A static mechanism of interactions between flavonols and CpLIP2 lipase was confirmed by fluorescence quenching analyses, indicating that the interactions were mainly driven by hydrophobic bonds and electrostatic forces. From the Lehrer equation, fractions of tryptophan accessibility to the quencher were evaluated, and a relationship with the calculated number of binding sites was suggested.

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“…This effect may be due to the improved elimination of triglyceride-rich lipoproteins through the improved activity of lipase lipoproteins and improved absorption of triglycerides transported in VLDL by peripheral organs [37]. Another mechanism may be related to the regulation of intestinal uptake of TG mediated by pancreatic lipase that catalyzes the hydrolysis of triglycerides into mono-and diglycerides, which are captured by intestinal cells [38]. Although the direct involvement of TG in atherosclerosis is not yet confirmed, it has been reported that reducing serum TG levels is effective in preventing hyperlipidemia and treating heart disease [39].…”

Section: β-Carotene Bleaching Testmentioning

confidence: 99%

Antihyperlipidemic and Antioxidant Activities of Flavonoid-Rich Extract of Ziziphus lotus (L.) Lam. Fruits

et al. 2021

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Ziziphus lotus (L.) Lam. (Z. lotus) is a medicinal plant species that is widely distributed throughout the Mediterranean basin. Moroccans traditionally use it to treat many illnesses thanks to its beneficial medicinal properties. The purpose of this study is to assess the anti-hyperlipidemic and antioxidant activities of a flavonoid-rich aqueous extract of Z. lotus fruits (ZLF). The 2-2-diphenyl-1-picrylhydrazyl (DPPH) scavenging assay and the β-carotene bleaching test were used to determine the antioxidant activity of ZLF. The anti-hyperlipidemic effect of the aqueous extract of ZLF (200 and 400 mg/kg) was evaluated in albino mice exposed to the chronic high-fat diet, based on lipid profile, blood sugar, and changes in growth performance. The results showed that the aqueous extract of ZLF rich in flavonoids (2242.89 ± 25 µg QE (quercitin equivalent)/mg), and has a considerable antioxidant power against DPPH radicals (IC50 = 116 ± 0.02 µg/mL) and β-carotene oxidation. The aqueous extract of ZLF also showed a significant anti-hyperlipidemic effect by improving abnormal changes in lipid profile and blood glucose levels in albino mice exposed to a chronic high-fat diet. Our findings suggest that the anti-hyperlipidemic activities of ZLF aqueous extract are correlated with its flavonoid content and antioxidant activity. Therefore, the aqueous extract of ZLF could be an essential therapeutic candidate for hyperlipidemia patients, thanks to its richness in bioactive molecules.

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Identification of a new natural gastric lipase inhibitor from star anise

Abstract: The flavonoid myricitrin-5-methyl ether is a potential drug candidate as a gastric lipase inhibitor for the treatment of obesity.

Cited by 18 publications

References 43 publications

Effect of polyphenol, flavonoid, and saponin fractions from Thymus atlanticus on acute and chronic hyperlipidemia in mice

Effect of polyphenol, flavonoid, and saponin fractions from Thymus atlanticus on acute and chronic hyperlipidemia in mice

Inhibition of CpLIP2 Lipase Hydrolytic Activity by Four Flavonols (Galangin, Kaempferol, Quercetin, Myricetin) Compared to Orlistat and Their Binding Mechanisms Studied by Quenching of Fluorescence

Antihyperlipidemic and Antioxidant Activities of Flavonoid-Rich Extract of Ziziphus lotus (L.) Lam. Fruits

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