The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents

Tucci, Sonia

doi:10.2147/dmso.s7005

Cited by 114 publications

(43 citation statements)

References 167 publications

(211 reference statements)

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“…The inhibitory effect of serum TG elevation may be related to the regulation of intestinal uptake, due in part to the inhibition of TG digestion and/or its absorption mediated by pancreatic lipase, that hydrolyzes dietary triglycerides to mono-and diglycerides and fatty acids which are absorbed by the enterocytes (Tucci et al, 2010). Therefore, the in vitro inhibitory capacity of pancreatic lipase by herbal infusions was tested (Fig.…”

Section: Oral Lipid Tolerance Testmentioning

confidence: 99%

Phytochemical characterization and effect of Calendula officinalis, Hypericum perforatum, and Salvia officinalis infusions on obesity-associated cardiovascular risk

et al. 2015

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Medicinal herb infusions can be used for the treatment of obesity-related metabolic alterations. The aim of this study was to characterize the phytochemical profile and to evaluate the effect of Hypericum perforatum, Salvia officinalis, and Calendula officinalis on the cardiovascular risk developed in diet-induced obese rats. All infusions decreased body weight and abdominal fat mass and reduced serum triglycerides (TG), total cholesterol, lowdensity lipoproteins, and C-reactive protein levels. The anti-obesogenic and hypolipidemic effect of C. officinalis and H. perforatum were associated with the inhibition of triglycerides digestion and absorption. Conversely, the hypolipidemic effect of S. officinalis was not associated with this mechanism. Moreover, seven phenolic acids and nine flavonoids were quantified by HPLC-UV/VIS, hesperidin and epigallocatechin gallate were the majoritarian compounds of H. perforatum and C. officinalis, whereas rosmarinic and ellagic acids were the main compounds in S. officinalis. Additionally, we used HPLC-DAD-MSD to identify 45 phytochemicals, such as anthraquinone and phloroglucinol derivatives, phytosterols, saponins, and alkaloids. Total flavonoids, phytosterols, and alkaloids content were highly correlated with TG levels, AUC values from the oil tolerance test, and pancreatic lipase inhibition. These results suggest that these phytochemical-rich infusions may be used as an alternative for obesity-related cardiovascular risk treatment.

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Section: Oral Lipid Tolerance Testmentioning

confidence: 99%

Phytochemical characterization and effect of Calendula officinalis, Hypericum perforatum, and Salvia officinalis infusions on obesity-associated cardiovascular risk

et al. 2015

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“…It was announced that Cetilistat was moving into Phase III clinical trials for the treatment of obesity. The success of lipase inhibitors has driven investigations into new generations of nutraceuticals, dietary supplements and pharmaceutical agents that inhibit the breakdown of fats and complex carbohydrates within the gastrointestinal tract (9,10). Lipase inhibitors may soon be used for other pharmaceutical applications, such as the treatment of type 2 diabetes (11,12), atherosclerosis (13), tuberculosis (14)(15)(16), and probably cancer, since Orlistat was also found to have anti-tumoral effects via its inhibitory action on fatty acid synthase (17).…”

Section: Introductionmentioning

confidence: 99%

Effects of Surfactants on Lipase Structure, Activity, and Inhibition

et al. 2011

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Lipase inhibitors are the main anti-obesity drugs prescribed these days, but the complexity of their mechanism of action is making it difficult to develop new molecules for this purpose. The efficacy of these drugs is known to depend closely on the physico-chemistry of the lipid-water interfaces involved and on the unconventional behavior of the lipases which are their target enzymes. The lipolysis reaction which occurs at an oil-water interface involves complex equilibria between adsorption-desorption processes, conformational changes and catalytic mechanisms. In this context, surfactants can induce significant changes in the partitioning of the enzyme and the inhibitor between the water phase and lipid-water interfaces. Surfactants can be found at the oil-water interface where they compete with lipases for adsorption, but also in solution in the form of micellar aggregates and monomers that may interact with hydrophobic parts of lipases in solution. These various interactions, combined with the emulsification and dispersion of insoluble substrates and inhibitors, can either promote or decrease the activity and the inhibition of lipases. Here, we review some examples of the various effects of surfactants on lipase structure, activity and inhibition, which show how complex the various equilibria involved in the lipolysis reaction tend to be.

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“…4) which leads to decreased uptake of dietary carbohydrates that suppress postprandial hyperglycemia without increasing insulin level, which is useful to treat diabetic and/or obese patients [59]. Continuous blockade of enzyme by these "starch blockers" results in simultaneous reduction in body weight, HbA1c level and serum triglyceride [60].…”

Section: Chalcones As A-glucosidase Inhibitorsmentioning

confidence: 99%

Chalcones and their therapeutic targets for the management of diabetes: Structural and pharmacological perspectives

Mahapatra

Asati

Bharti

2015

European Journal of Medicinal Chemistry

202

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The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents

Cited by 114 publications

References 167 publications

Phytochemical characterization and effect of Calendula officinalis, Hypericum perforatum, and Salvia officinalis infusions on obesity-associated cardiovascular risk

Phytochemical characterization and effect of Calendula officinalis, Hypericum perforatum, and Salvia officinalis infusions on obesity-associated cardiovascular risk

Effects of Surfactants on Lipase Structure, Activity, and Inhibition

Chalcones and their therapeutic targets for the management of diabetes: Structural and pharmacological perspectives

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