Abstract
The aim of this study was to determine the pancreatic lipase (PL) inhibitory effect of cocoa protein (CP) hydrolysates (CPH) using in silico and in vitro approaches, and an in vivo high-fat diet (HF) obese rat model. The results showed better theoretical affinity on PL for cocoa peptides EEQR, GGER, QTGVQ, and VSTDVNIE released from vicilin and albumins (−6.5, −6.3, −6.2, and −6.1 kcal/mol, respectively). Absorption, distribution, metabolism, and excretion (ADMET) prediction showed the human intestinal absorption (HIA) capacity of orlistat and eight cocoa peptides, demonstrating that they presented a low probability of toxicity with values lower than 0.6, while the orlistat has a high probability of hepatotoxicity with a mean value of 0.9. CPH (degree of hydrolysis of 55%) inhibited PL with an IC50 (concentration needed to inhibit 50% of enzyme activity) value of 1.38 mg/mL. The intragastric administration of 150 mg CP/kg/day to rats increased total lipids and triglycerides excretion in feces, ranging from 11% to 15% compared to the HF-diet. The HF + CP-diet also significantly decreased (p < 0.05) the apparent rate of fat absorption compared with the HF group. These results suggest that CP has anti-obesity potential by inhibiting PL, thus helping to prevent the development of non-communicable diseases.
Highlights
Obesity and obesity-associated diseases have reached epidemic proportions worldwide
The only pancreatic lipase (PL) inhibitor approved by the Food and Drug Administration (FDA) is orlistat, recommended for long-term use to reduce the absorption of dietary fat
In other studies carried out with fish tripeptides from Larimichthys crocea or Oncorhynchus mykiss, good absorption BBB and human intestinal absorption (HIA) values were obtained [30]. Another in silico assay with ADMET was performed with soybean tripeptides, highlighting that seven peptides had a good probability of absorption in HIA and four in BBB [31]
Summary
Obesity and obesity-associated diseases have reached epidemic proportions worldwide. According to the World Health Organization (WHO), in 2016, at least 1.9 billion adults showed obesity or overweight, being equivalent to more than 25 percent of the world’s population. A molecular target of much interest in the prevention and treatment of obesity is the pancreatic lipase (PL) This enzyme is responsible for the intestinal digestion of triacylglycerols from the diet, limiting their absorption in the gastrointestinal tract. This enzyme has become an important therapeutic target in the development of anti-obesity agents [2,3]. Proteins and peptides produced from vegetal food sources by in vitro digestion have been reported to inhibit PL activity in in vitro and in vivo studies, including soybean [7], cumin seed [8], soy milk [9], bean seeds Peptides from natural origin, as components of the daily diet, could have potential therapeutic use to ameliorate obesity with low side effects
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