Inhibition of pancreatic lipase by black tea theaflavins: Comparative enzymology and in silico modeling studies

Glisan, Shannon L.; Grove, Kimberly A.; Yennawar, Neela H.; Lambert, Joshua D.

doi:10.1016/j.foodchem.2016.08.052

Cited by 88 publications

(41 citation statements)

References 32 publications

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“…In China, tea has been used as an anti‐obesity therapy for thousands of years, and considerable accumulated evidence has indicated the effects of tea on the prevention of obesity (Glisan, Grove, Yennawar, & Lambert, ). Oolong tea is a semifermented tea that is allowed to partially oxidize to lock‐in the rich flavor that is associated with its high quality.…”

Section: Introductionmentioning

confidence: 99%

Effects of (-)-epigallocatechin 3-O -(3-O -methyl) gallate (EGCG3″Me)- phospholipids complex on pancreatic α-amylase and lipase activities

et al. 2017

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(‐)‐Epigallocatechin 3‐O‐(3‐O‐methyl) gallate (EGCG3″Me) has exhibited various biological activities in oolong tea; however, its absorption is poor. In this study, the role of phospholipids on the digestive enzymes inhibitory effect of EGCG3″Me was investigated. EGCG3″ was purified from oolong tea and used to prepare EGCG3″Me‐phospholipids complex (EPC). The results showed that EPC exhibited relatively higher stability than EGCG3″Me in mimicked digestion conditions, and the presence of phospholipids increased the transepithelial transport of EGCG3″Me. The half inhibitory concentration (IC50) values of EGCG3″Me and EPC for α‐amylase were 0.54 and 1.49 mg/mL, respectively, while the values were 1.14 and 1.69 mg/mL, respectively, for lipase. Lineweaver‐Burk double reciprocal plots indicated the inhibitory types of EPC were competitive for α‐amylase, whereas it was noncompetitive for lipase. Since phospholipids could improve the bioavailability of tea polyphenols, our investigation may be useful in manufacturing functional foods with increased absorption, containing high content of tea polyphenols. Practical applications The findings suggest the potential of phospholipids for the promotion of the inhibitory effect of EGCG3″Me on digestive enzymes. Although the inhibitory effect of EGCG3″Me on a‐amylase and lipase was better than EGCG3″Me‐phospholipids complex (EPC), EPC exhibited better stability and permeability. For good bioavailability, tea polyphenols should have a balance between hydrophilicity and lipophilicity, and the complex we prepared may be used for manufacturing functional foods that support improved tea polyphenols absorption.

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Section: Introductionmentioning

confidence: 99%

Effects of (-)-epigallocatechin 3-O -(3-O -methyl) gallate (EGCG3″Me)- phospholipids complex on pancreatic α-amylase and lipase activities

et al. 2017

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“…In addition, lipases can support the persistence of these strains in the fatty secretions of mammalian skin and thus have an indirect influence on their pathogenic potential . Due to these processes, the pharmacological inhibition of lipases has been pursued by a number studies via the development of new compounds with these characteristics . Currently, the drug tetrahydrolipstatin promotes the inhibition of gastric and pancreatic lipases, and this drug acts on the active serine via covalent binding to inhibit the absorption of fat.…”

Section: Resultsmentioning

confidence: 99%

Effects of cholinium‐based ionic liquids on Aspergillus niger lipase: Stabilizers or inhibitors

Nascimento

Picheli

Lopes

et al. 2019

Biotechnology Progress

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Lipases are well‐known biocatalysts used in several industrial processes/applications. Thus, as with other enzymes, changes in their surrounding environment and/or their thermodynamic parameters can induce structural changes that can increase, decrease, or even inhibit their catalytic activity. The use of ionic compounds as solvents or additives is a common approach for adjusting reaction conditions and, consequently, for controlling the biocatalytic activity of enzymes. Herein, to elucidate the effects of ionic compounds on the structure of lipase, the stability and enzymatic activity of lipase from Aspergillus niger in aqueous solutions (at 0.05, 0.10, 0.50, and 1.00 M) of six cholinium‐based ionic liquids (cholinium chloride [Ch]Cl; cholinium acetate ([Ch][Ac]); cholinium propanoate ([Ch][Prop]); cholinium butanoate ([Ch][But]); cholinium pentanoate ([Ch][Pent]); and cholinium hexanoate ([Ch][Hex])) were evaluated over 24 hr. The enzymatic activity of lipase was maintained or enhanced in the lower concentrations of all the [Ch]+‐ILs (below 0.1 M). [Ch][Ac] maintained the biocatalytic behavior of lipase, independent of the IL concentration and incubation time. However, above 0.1 M, [Ch][Pent] and [Ch][Hex] caused complete inhibition of the catalytic activity of the enzyme, demonstrating that the increase in the anionic alkyl chain length strongly affected the conformation of the lipase. The hydrophobicity and concentration of the [Ch]+‐ILs play an important role in the enzyme activity, and these parameters can be controlled by adjusting the anionic alkyl chain length. The inhibitory effects of [Ch][Pent] and [Ch][Hex] may be of great interest to the pharmaceutical industry to induce pharmacological inhibition of gastric and pancreatic lipases.

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“…EGCG dose-dependently inhibited PL (IC50 = 7.5 lmol L À1 ) in a noncompetitive manner (Grove et al, 2012), while TFs (especially TFdiG) worked in a mixed mode (Glisan et al, 2017). According to the prediction of silico model, all of the TFs could bind to Asn263 and Asp206 residues which would form a pocket adjacent to the enzyme active site, and TFs with galloyl motif would further perturb the protonation of His264 which was a part of the catalytic triad Ser153-His264-Asp177 (Glisan et al, 2017).…”

Section: Enzymes Related To Obesitymentioning

confidence: 99%

Stop for tea? Enzyme inhibitors from tea – what good are they?

Zhao

et al. 2016

Int J of Food Sci Tech

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Summary Tea possesses many bioactive components including polyphenols, theanine and caffeine. Inhibitory effect of these components on the various enzymes involved in some chronic diseases was reviewed in this study. Many studies revealed that anti‐obesity of tea was mainly ascribed to the polyphenols which could inhibit the activity of the enzymes related to diet metabolism such as α‐amylase, α‐glucosidase and lipase. Inhibitory effect of catechins and caffeine against β‐ and γ‐secretase, acetylcholinesterase, protein kinase C and histone deacetylase might be responsible for the prevention from nervous system diseases. Cytochrome P450 enzymes, cytosolic sulfotransferases, cyclooxygenase‐2 and phosphoinositide‐3‐kinase could be efficiently suppressed by catechins, which would decrease the risk of cancer initiation and proliferation; theanine could lower the activity of some anticarcinogen‐activated enzymes and alleviate the adverse effect of cancer cure. Catechins and caffeine exhibited significant inhibition against the matrix metalloproteinases, histidine decarboxylase and many kinases related to inflammation. Thus, catechins, theanine and caffeine might be employed as inhibitors of the enzymes associated with these chronic diseases.

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Inhibition of pancreatic lipase by black tea theaflavins: Comparative enzymology and in silico modeling studies

Cited by 88 publications

References 32 publications

Effects of (-)-epigallocatechin 3-O -(3-O -methyl) gallate (EGCG3″Me)- phospholipids complex on pancreatic α-amylase and lipase activities

Effects of (-)-epigallocatechin 3-O -(3-O -methyl) gallate (EGCG3″Me)- phospholipids complex on pancreatic α-amylase and lipase activities

Effects of cholinium‐based ionic liquids on Aspergillus niger lipase: Stabilizers or inhibitors

Stop for tea? Enzyme inhibitors from tea – what good are they?

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