Cyanidin and cyanidin-3-glucoside derived from Vigna unguiculata act as noncompetitive inhibitors of pancreatic lipase

Abstract

The consumption of legumes positively correlated with the reduction of body weight. In the present study, we identified and evaluated pancreatic lipase inhibitors from Vigna unguiculata and unraveled their mode of inhibition. The highly sensitive fluorometric method was adopted to access the pancreatic lipase activity and the ethanolic extract of Vigna unguiculata showed the maximum inhibition (IC50 of 15.2 µg/ml). Cyanidin and cyanidin‐3‐glucoside are the major anthocyanins observed in Vigna unguiculata. The IC50 value of cyanidin was 28.29 µM which was 6.5‐fold higher than the cyanidin‐3‐glucoside (188.28 µM). We determined an apparent Ki of 27.28 µM for cyanidin and cyanidin‐3‐glucoside (88.97 µM) with noncompetitive inhibition. Collectively, these results suggest that the glycosylation of the anthocyanidins significantly reduces lipase inhibition. The noncompetitive inhibition of pancreatic lipase by Vigna unguiculata anthocyanins may exert significant pharmacological activities toward obesity complications by calorie restriction. Practical applications The results of this study emphasize the importance of legumes in our diet to combat obesity‐related complications. Consumption of legumes minimizes fat absorption by inhibiting the action of the fat‐digesting enzyme.

Inhibitory Activities of Polyphenolic Extracts of Bangladeshi Vegetables against α-Amylase, α-Glucosidase, Pancreatic Lipase, Renin, and Angiotensin-Converting Enzyme

“…The water solubility properties of the phenolic compounds could enhance their interactions with target enzymes within the hydrophilic environment of the gastrointestinal tract. For example, the aqueous extracts of some bean varieties were shown to have stronger lipase inhibition than the ethanolic extracts [ 28 ]. Inhibition of α-amylase was mainly dose-dependent except for brinjal and stem amaranth, where their decreases occurred at higher sample concentrations.…”

“…Lipase is secreted in the pancreas and is used as a catalyst to aid triglyceride hydrolysis in the stomach, and this hydrolysis is completed by intestinal lipase in the small intestine [ 28 , 37 ]. It has been estimated that about 50–70% of total dietary fats are hydrolyzed for absorption by PL [ 38 ], which emphasizes the importance of this enzyme in calorie release from diets.…”

Obesity-associated Pathways of Anthocyanins

“…Pancreatic lipase enzyme is required for the dietary fat absorption. Therefore, it is important to inhibit pancreatic lipase enzyme in order to reduce obesity development (Vijayaraj et al, 2019). Anthocyanin-rich fruits and vegetables contain significant anthocyanins that are able to inhibit pancreatic lipase enzyme, thus, some fruits and vegetables rich in anthocyanins have significant effects on preventing obesity.…”

“…In the research in which the effect of litchi flower extract in the Mediterranean diet containing anthocyanin-rich fruit and vegetables was investigated, it was determined that the extract samples have a suppressive effect on pancreatic lipase. In the researches in which some anthocyanin-containing fruits were used, it was found that pomegranate and blood orange juices have significant pancreatic lipase inhibition due to the high anthocyanin content (Chen et al, 2018;Xie et al, 2018;Vijayaraj et al, 2019). In another research, black rice extract containing cyanidin 3-glucoside and peonidin 3-glucoside anthocyanins in the arrest of cholesterol absorption in Caco-2 cells has been tested.…”

The Influence of Supplementation of Anthocyanins on Obesity-Associated Comorbidities: A Concise Review

“…Moreover, anthocyanins treatment improved insulin sensitivity and suppressed the comorbidities of obesity in vitro [ 83 ]. Cyanidin and C3G-rich ethanolic extract of Vigna unguiculata showed significant pancreatic lipase inhibition in vitro, which indicated that V. unguiculata anthocyanins have anti-obesity potential [ 84 ] ( Table 3 ).…”