A comprehensive review on the pancreatic lipase inhibitory peptides: A future anti-obesity strategy

Abstract

Dysregulation of lipid homeostasis contributes to obesity and can directly lead to several critical public health concerns globally. This paper aimed to present a brief review of related properties and the use of pancreatic lipase inhibitors as the future weight loss drug discovery and development procured from a wide range of natural sources. A total of 176 pancreatic lipase inhibitory peptides were identified from recent publications and peptide databases. These peptides were classified into three categories according to their peptide length and further analyzed using bioinformatic approaches to identify their structural activity relationship. Molecular docking analyses were conducted for each amino acid at the terminal position of the peptides to predict the binding affinity between peptide-enzyme protein complexes based on intermolecular contact interactions. Overall, the observations revealed the features of the inhibitory peptides and their inhibitory mechanisms and interactions. These findings strived to benefit scientists whose research may be relevant to anti-obesity drug development and/or discovery thereby support effective translation of preclinical research for humans’ health being.

New insight on antioxidants and anti-obesity properties of two seagrasses Thalassia hemprichii and Zostera marina: an integrated molecular docking simulation with in vitro study

“…33 Departing from this concept, the anti-obesity approach using lipase enzyme inhibitors or lipase inhibitors is expected to reduce the number of lipids absorbed to minimize the accumulation of fatty acids, cholesterol, and lipoproteins in the blood and adipose tissue deposition in the body. 34 Lipase inhibitors work by binding to residues located at the active binding site of pancreatic and gastric lipase so that the ability of triglycerides to bind to lipase becomes inhibited. Due to its selective nature, weak absorption rate, and low risk of systemic side effects, there is potential to develop lipase inhibitors further into mainstream anti-obesity.…”

Quantitative HPLC analysis and isolation of tiliroside from Alcea biennis Winterl and determination of total flavonoid content and biological activities

“…After these biomolecules are absorbed in the small intestine, they pass into the blood circulation and reach the adipose tissue and are used in the synthesis of triacylglycerol in adipocyte cells. Since inhibition of PL controls the level of free fatty acid accumulation by delaying/blocking dietary fat absorption, PL inhibitors play an important role in prevention and treatment of obesity (Chia et al 2023). Orlistat, which is currently used clinically for the treatment of obesity and acts as a PL inhibitor, has serious side effects.…”

“…Trakya Univ J Nat Sci, 25(1): [11][12][13][14][15][16][17][18][19]2024 Quantitative analysis of ABA-E1 (Tiliroside) by HPLC Method…”

Synthesis and Characterization of Short α and β-Mixed Peptides with Excellent Anti-Lipase Activities

“…In the 1 HNMR spectrum, a singlet at 5.1 ppm integrated for two protons (-CH 2 -Ar monosubstituted) and another singlet at 3.6 ppm integrated for three protons (-OCH 3 ) confirmed the synthesis of dipeptide 14. The synthesis of tetrapeptide 17 was established by the presence of a singlet at 1.39 ppm integrated for nine protons (C(CH 3 ) 3 ) and a broad singlet at 6.95 ppm (-NH) combined for one proton in its 1 HNMR spectrum (Scheme 3). It is evident that our desired α, β-mixed peptides were synthesized successfully with good yield.…”

“…In 2021, 1.9 billion adults were heavy, and 650 million were obese. According to the global burden of disease, over 4 million people die each year due to this widespread disease [ 1 ]. Notably, obesity is a healthcare and socioeconomic disadvantage due to associated health issues.…”