Susceptible genetic polymorphisms and their association with adverse effects of orlistat therapy

Logesh, Rajan; Radhakrishnan, Arun; Selleppan, Gobi; Mohankumar, Suresh Kumar

doi:10.1016/j.obmed.2021.100360

Cited by 3 publications

(3 citation statements)

References 70 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Using orlistat as a positive control, the IC 50 of orlistat was 0.28 mg mL −1 , implying that the inhibitory ability of orlistat on pancreatic lipase was higher than that of fucoidan. However, long‐term use of orlistat can cause adverse effects such as liver failure and kidney stones 35 …”

Section: Resultsmentioning

confidence: 99%

“…However, long-term use of orlistat can cause adverse effects such as liver failure and kidney stones. 35 The earlier results suggest that fucoidan is a natural plant polysaccharide with pancreatic lipase inhibitory effects and has antiobesity potential. Pancreatic lipase is mainly located in the small intestine.…”

Section: Effect Of Simulated Digestion On the Inhibitory Activity Of ...mentioning

confidence: 99%

See 1 more Smart Citation

Effect of in vitro simulated digestion on the physicochemical properties and pancreatic lipase inhibitory activity of fucoidan

Lu,

Gu,

2024

J Sci Food Agric

View full text Add to dashboard Cite

BACKGROUNDFucoidan has an anti‐obesity effect. However, there are few studies on its mechanism. In this study, we investigated the in vitro and in silico inhibitory properties of fucoidan against pancreatic lipase for the first time. We examined the changes in composition, structure, and pancreatic lipase inhibition of fucoidan during in vitro digestion.RESULTSSimulated saliva‐gastrointestinal digestion resulted in a slight decrease in the molecular weight of fucoidan but no significant changes in the monosaccharide composition, sulfate content, and functional groups. Moreover, the digestion process significantly increased the inhibition of pancreatic lipase by fucoidan. The study on the type of inhibition showed that the inhibition of pancreatic lipase by fucoidan belonged to mixed inhibition with competitive inhibition. Molecular docking analysis showed that fucoidan could bind to the active site of pancreatic lipase.CONCLUSIONThis study indicates that fucoidan can be a potential functional food for anti‐obesity. © 2024 Society of Chemical Industry.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Effect Of Simulated Digestion On the Inhibitory Activity Of ...mentioning

confidence: 99%

Effect of in vitro simulated digestion on the physicochemical properties and pancreatic lipase inhibitory activity of fucoidan

Lu,

Gu,

2024

J Sci Food Agric

View full text Add to dashboard Cite

show abstract

“…Orlistat is a tetrahydrolipstatin, which constrains both pancreatic and gastric lipase enzymes in the gut and avoids the absorption of dietary fats in the intestine. Therefore, it is generally used as an anti-obesity medication to control and manage body weight in obese patients wide-reaching (Rajan et al, 2021).Orlistat items selectively near gastrointestinal lipase by avoiding the hydrolysis of consumed dietary fat into absorbable free fatty acids and glycerol (Othman et al, 2021). For this goal, Orlistat has demonstrated its efficiency in decreasing obesity factors such as BMI, lipid profile, white adipocyte size, and increase fecal fat excretion in animal replicas, as well as the complications of obesity such as metabolic syndrome and endothelial dysfunction in human.…”

Section: Introductionmentioning

confidence: 99%

Effect of lemongrass powder on hyperlipidemia compared to Orlistat using experimental animals

Abd-Elrahman

Omar

2023

Egyptian Journal of Nutrition and Health

View full text Add to dashboard Cite

This study was designed to investigate the effect of lemongrass powder and Orlistat on hyperlipidemia in rats fed on a high fat diet. Twenty four normal male albino rats of Sprague Dawley Strain weighing (15010g), were used in this study and split into 4 equal groups; each group contained 6 rats.One group was conserved as a control negative group (G1), while (G2) were fed on high fat diet, (G3)were fed on high fat diet plus7.5 % lemongrass powder and (G4) fed on high fat diet plus Orlistat (60 mg /Kg body weight). At the end of the experiment, glucose levels, total protein (Albumin and globulin), serum liver functions, and serum lipids were assessed. The results indicated that tests plants improved glucose levels, liver functions, and lipid profile. According to these results, moderate amounts of lemongrass in our diets could be tried for improvement of hyperlipidemic humans.

show abstract

Rapidly screening of pancreatic lipase inhibitors from Clematis tangutica using affinity ultrafiltration‐HPLC‐QTOFMS technique combined with targeted separation, in vitro validation, and molecular docking

Wei,

Chen,

Song

et al. 2024

Phytochemical Analysis

View full text Add to dashboard Cite

IntroductionScreening of novel pancreatic lipase inhibitors from complex natural products is a meaningful task.ObjectivesThrough accurately screening and separating pancreatic lipase inhibitors from Clematis tangutica (C. tangutica), to discover new leading compounds for slimming and accelerate the development and utilization of Tibetan medicine resources.MethodsAn integrated strategy that combines affinity ultrafiltration and high‐performance liquid chromatography‐quadrupole time‐of‐flight mass spectrometry (AU‐HPLC‐QTOFMS), targeted separation, in vitro validation, and molecular docking was developed to screen pancreatic lipase inhibitors from C. tangutica. The AU‐HPLC‐QTOFMS technique was performed to fish for the potential active substances. Macroporous resin, preparative liquid chromatography, and high‐speed countercurrent chromatography were implemented for the accurate and targeted separation of active compounds. The inhibitory activities of target compounds to pancreatic lipase were detected by the inhibition experiments in vitro. The binding affinities and binding sites were analyzed using molecular docking.ResultsA total of eleven kinds of pancreatic lipase inhibitory substances were screened from C. tangutica. Seven triterpenoid saponins were screened for the first time as lipase inhibitors and successfully prepared with purities higher than 97%. Tanguticoside B, clematangoticoside J, hederoside H1, and rutin showed stronger inhibitory effects with IC50 values of 1.539 ± 0.048, 1.661 ± 0.092, 1.793 ± 0.069, and 1.792 ± 0.094 mmol/l. Moreover, they have the lowest ΔG values of −10.84, −9.97, −10.87, and −9.39 kcal/mol to pancreatic lipase.ConclusionThe integrated strategy using AU‐HPLC‐QTOFMS, targeted separation, in vitro validation, and molecular docking was feasible for rapidly screening and directionally isolating pancreatic lipase inhibitors from C. tangutica.

show abstract

Susceptible genetic polymorphisms and their association with adverse effects of orlistat therapy

Cited by 3 publications

References 70 publications

Effect of in vitro simulated digestion on the physicochemical properties and pancreatic lipase inhibitory activity of fucoidan

Effect of in vitro simulated digestion on the physicochemical properties and pancreatic lipase inhibitory activity of fucoidan

Effect of lemongrass powder on hyperlipidemia compared to Orlistat using experimental animals

Rapidly screening of pancreatic lipase inhibitors from Clematis tangutica using affinity ultrafiltration‐HPLC‐QTOFMS technique combined with targeted separation, in vitro validation, and molecular docking

Contact Info

Product

Resources

About