Inhibitory effects of apple polyphenol extract (AP) and procyanidin contained in AP on in vitro pancreatic lipase activity and in vivo triglyceride absorption in mice and humans were examined. AP and procyanidin considerably inhibited in vitro pancreatic lipase activity. However, polyphenols, except for procyanidin, in AP (i.e., catechins, chalcones, and phenol carboxylic acids) showed weak inhibitory activities on pancreatic lipase. Procyanidins separated by normal-phase chromatography according to the degree of polymerization were also examined. Inhibitory effects of procyanidins increased according to the degree of polymerization from dimer to pentamer. On the other hand, pentamer or greater procyanidins showed maximal inhibitory effects on pancreatic lipase. These results suggested that with respect to in vitro pancreatic lipase inhibition, the degree of polymerization was an important factor and oligomeric procyanidin mainly contributed. Next, we performed a triglyceride tolerance test in mice and humans. Simultaneous ingestion of AP and triglyceride significantly inhibited an increase of plasma triglyceride levels in both models. These results suggested that the oligomeric procyanidins contained in AP inhibited triglyceride absorption by inhibiting pancreatic lipase activity in mice and humans.

Oligomeric Procyanidins in Apple Polyphenol Are Main Active Components for Inhibition of Pancreatic Lipase and Triglyceride Absorption [Erratum: 2007 July 11, v. 55, no. 14, p. 5906.]

Pancreatic lipase (PL) is a critical enzyme associated with hyperlipidemia and obesity. A previous study of ours suggested that persimmon tannin (PT) was the main component accounting for the antihyperlipidemic effects of persimmon fruits, but the underlying mechanisms were unclear. In this present study, the inhibitory effect of PT on PL was studied and the possible mechanisms were evaluated by fluorescence spectroscopy, circular dichroism (CD) spectra, isothermal titration calorimetry (ITC), and molecular docking. PT had a high affinity to PL and inhibited the activity of PL with the half maximal inhibitory concertation (IC50) value of 0.44 mg/mL in a noncompetitive way. Furthermore, molecular docking revealed that the hydrogen bonding and π–π stacking was mainly responsible for the interaction. The strong inhibition of PT on PL in the gastrointestinal tract might be one mechanism for its lipid-lowering effect.

Inhibitory Effect of Persimmon Tannin on Pancreatic Lipase and the Underlying Mechanism in Vitro

Qingzhuan tea (QZT), a post-fermented tea, has been reported to have anti-obesity and anti-hyperglycemic effects, perhaps due to bioactive compounds that inhibit lipase and α-amylase. It is unknown what chemical constituents' changes and what bioactive compounds occur during the manufacture of QZT. The aim of this study was to determine the secondary metabolites changes that occur during post-fermentation and how these changes affect the ability of QZT to inhibit the activities of lipase and α-amylase. During the processing steps, metabolites levels and their inhibitory effects on lipase and α-amylase were assessed. Changes in content and activities suggested that the first turn over or the second turn over was critical for the formation and conversion of bioactive compounds responsible for the anti-obesity and hypoglycemic effects. The relationship between constituents and activities was further evaluated by correlation analysis, which showed that amino acids and flavonoids might be responsible for the anti-obesity and anti-hyperglycemic effects of QZT. This study clarified that compounds were altered during pile fermentation of QZT and tentatively identified the bioactive compounds formed during QZT manufacture.

/pdf/chemical-profile-changes-during-pile-fermentation-of-2pm7m48qdt.pdf

Chemical profile changes during pile fermentation of Qingzhuan tea affect inhibition of α-amylase and lipase.

Secondary metabolites from plants and fungi are stimulating growing interest in consumers and, consequently, in the food and supplement industries. The beneficial effects of these natural compounds are being thoroughly studied and there are frequent updates about the biological activities of old and new molecules isolated from plants and fungi. In this article, we present a review of the most recent literature regarding the recent discovery of secondary metabolites through isolation and structural elucidation, as well as the in vitro and/or in vivo evaluation of their biological effects. In particular, the possibility of using these bioactive molecules in the prevention and/or treatment of widely spread pathologies such as cardiovascular and neurodegenerative diseases is discussed.

https://www.mdpi.com/2304-8158/10/1/29/pdf

Natural Compounds for the Prevention and Treatment of Cardiovascular and Neurodegenerative Diseases.

https://link.springer.com/content/pdf/10.1186/s43141-021-00120-7.pdf

Molecular docking studies of some selected gallic acid derivatives against five non-structural proteins of novel coronavirus.

/pdf/in-silico-investigation-of-black-tea-components-on-and-945-5f3tfanv9c.pdf

In silico investigation of black tea components on and #945;-amylase, and #945;-glucosidase and lipase

Black tea is one of the most widely consumed beverages in the world and traditionally known for its antidiabetic and antiobese property. However, the underlying mechanisms of these properties are not studied widely. In this work, we hypothesize that the reason could be because of the inhibition of gut enzymes by the tea derived phytochemicals. Molecular docking was used to explore the efficacy of tea components to inhibit the key enzymes related with Type II diabetes and obesity; α-glucosidase, α-amylase and lipase. Autodock4.2 molecular docking software that applies Lamarckian Genetic Algorithm was used. The ligand structures were retrieved from PubChem and KNApSAcK-3D database. PreADMET web server was used for Toxicity and ADME predictions. Based on this analysis, it has been found that 8-c-ascorbyl-(-)-epigallocatechin, rutin and orientin could be the putative molecules for amelioration of post-prandial hyperglycaemia whereas 8-c-ascorbyl-(-)-epigallocatechin, 8-c-ascorbyl epigallocatechin 3-o-gallate and schaftoside could be used to reduce fat absorption in obese persons. It can be concluded that these phytochemicals or their derivatives can be used for further in-vitro and in-vivo studies to design valuable drugs.

/pdf/in-silico-investigation-of-black-tea-components-on-a-amylase-3131w25gu3.pdf

Farhan Haque

Papers

In silico investigation of black tea components on and #945;-amylase, and #945;-glucosidase and lipase

In silico investigation of black tea components on α-amylase, α-glucosidase and lipase