Quercetin is a promising pancreatic lipase inhibitor in reducing fat absorption in vivo

2021 ◽  
pp. 101248
Author(s):  
Jian-Feng Zhou ◽  
Wen-Jun Wang ◽  
Zhong-Ping Yin ◽  
Guo-Dong Zheng ◽  
Ji-Guang Chen ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Fat Absorption ◽  
Lipase Inhibitor

scholarly journals Study of Antiobesity Effect through Inhibition of Pancreatic Lipase Activity ofDiospyros kakiFruit andCitrus unshiuPeel

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Gyo-Nam Kim ◽  
Mi-Rae Shin ◽  
Sung Ho Shin ◽  
Ah Reum Lee ◽  
Joo Young Lee ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Dietary Fat ◽  
Inhibitory Effect ◽  
Positive Control ◽  
Diospyros Kaki ◽  
Fat Absorption ◽  
Dietary Fat Absorption

Pancreatic lipase is the enzyme responsible for digestion and absorption of triglycerides, being its inhibition one of the widest studied methods used to determine the potential activity of natural products to inhibit dietary fat absorption. Decrease of energy intake from dietary fat through inhibition of this enzyme may be an excellent strategy to prevent and treat obesity. The inhibitory activity on pancreatic lipase enzyme ofDiospyros kakifruit andCitrus unshiupeel mixture extract (PCM) was evaluatedin vitroand its antiobesity effects were studied based on the serum lipid parameters analysis from high-fat diet- (HFD-) fed micein vivo. PCM was orally administered at a dose of 50 and 200 mg/kg body weight for 6 weeks. In addition, the activity of pancreatic lipase was assessed using orlistat (positive control). PCM exhibited inhibitory effect on lipase activity with IC50value of 507.01 μg/mL. Moreover, serum triacylglycerol, total cholesterol levels, and visceral fat weight were significantly reduced compared to HFD control mice in PCM 200 mg/kg-treated mice (p<0.05). These results suggest that PCM administration may be a novel potential antiobesity agent for reduction of fat absorption via inhibition of pancreatic lipase.

Computational approaches for the discovery of natural pancreatic lipase inhibitors as antiobesity agents

2020 ◽  
Vol 12 (8) ◽  
pp. 741-757
Author(s):  
Ihab M Almasri
Keyword(s):  
Drug Design ◽  
Pancreatic Lipase ◽  
Drug Research ◽  
Fat Absorption ◽  
Computer Aided Drug Design ◽  
Computational Drug Design ◽  
Intestinal Fat Absorption ◽  
Antiobesity Agents ◽  
Pancreatic Lipase Inhibitors ◽  
Antiobesity Drugs

Obesity is becoming one of the greatest threats to global health in the 21st century and therefore the development of novel antiobesity drugs is one of the top priorities of global drug research. An important treatment strategy includes the reduction of intestinal fat absorption through the inhibition of pancreatic lipase (PL). Natural products provide a vast pool of PL inhibitors with novel scaffolds that can possibly be developed into clinical products. Computational drug design methods have become increasingly invaluable in the drug discovery process. In recent years, the discovery of new antiobesity PL inhibitors has been facilitated by the application of computational methods. This review highlights some computer-aided drug design techniques utilized in the discovery of natural PL inhibitors.

Effect of diet on triolein absorption in weanling rats

1990 ◽  
Vol 258 (1) ◽  
pp. G38-G44 ◽  
Author(s):  
C. A. Flores ◽  
P. M. Brannon ◽  
M. A. Wells ◽  
M. Morrill ◽  
O. Koldovsky
Keyword(s):  
Dietary Fat ◽  
Intact Animal ◽  
Fat Intake ◽  
Fat Absorption ◽  
High Fat ◽  
High Carbohydrate ◽  
Weanling Rats ◽  
Low Carbohydrate ◽  
Triton Wr 1339

To determine the effect of altered dietary fat intake on the rate of fat absorption in the intact animal, we fed male weanling rats either a high fat-low carbohydrate (HF-LC) (calories: 67% fat, 10% carbohydrate, 20% protein) or low fat-high carbohydrate (LF-HC) (calories: 10% fat, 67% carbohydrate, 20% protein) diet for 8 days. Absorption of [14C]triolein was estimated by determining 1) 14CO2 expiration in breath, 2) intestinal triglyceride output using Triton WR-1339, an inhibitor of lipoprotein lipase, and 3) quantitating the disappearance of labeled triolein from the gastrointestinal tract. Changes in the activity of pancreatic lipase and amylase confirmed the adaptation to altered fat and carbohydrate intake. Animals fed the HF-LC diet exhibited approximately twofold greater triolein disappearance, oxidation, and intestinal triglyceride output compared with animals fed LF-HC. There was also a highly significant linear relationship between 14CO2 excretion and intestinal triglyceride output in both diet groups. These data show that high dietary fat content markedly enhances in vivo fat absorption in the weanling rat.

scholarly journals Exploring Aurone Derivatives as Potential Human Pancreatic Lipase Inhibitors through Molecular Docking and Molecular Dynamics Simulations

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4657
Author(s):  
Phuong Thuy Viet Nguyen ◽  
Han Ai Huynh ◽  
Dat Van Truong ◽  
Thanh-Dao Tran ◽  
Cam-Van Thi Vo
Keyword(s):  
Molecular Dynamics ◽  
Molecular Dynamics Simulations ◽  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Dynamics Simulation ◽  
Stable Complex ◽  
Catalytic Active Site ◽  
Dynamics Simulations

Inhibition of human pancreatic lipase, a crucial enzyme in dietary fat digestion and absorption, is a potent therapeutic approach for obesity treatment. In this study, human pancreatic lipase inhibitory activity of aurone derivatives was explored by molecular modeling approaches. The target protein was human pancreatic lipase (PDB ID: 1LPB). The 3D structures of 82 published bioactive aurone derivatives were docked successfully into the protein catalytic active site, using AutoDock Vina 1.5.7.rc1. Of them, 62 compounds interacted with the key residues of catalytic trial Ser152-Asp176-His263. The top hit compound (A14), with a docking score of −10.6 kcal⋅mol−1, was subsequently submitted to molecular dynamics simulations, using GROMACS 2018.01. Molecular dynamics simulation results showed that A14 formed a stable complex with 1LPB protein via hydrogen bonds with important residues in regulating enzyme activity (Ser152 and Phe77). Compound A14 showed high potency for further studies, such as the synthesis, in vitro and in vivo tests for pancreatic lipase inhibitory activity.

scholarly journals Short communication: Endophytic actinobacteria isolated from ginger (Zingiber officinale) and its potential as a pancreatic lipase inhibitor and its toxicity

2019 ◽  
Vol 20 (5) ◽  
Author(s):  
SRI RAHAYU ◽  
LENNI FITRI ◽  
YULIA SARI ISMAIL
Keyword(s):  
Pancreatic Lipase ◽  
Short Communication ◽  
Ethanol Extract ◽  
Morphological Diversity ◽  
Zingiber Officinale ◽  
Lipase Inhibitor ◽  
New Information ◽  
Ginger Rhizome ◽  
Pancreatic Lipase Inhibitors ◽  
Endophytic Actinobacteria

Abstract. Rahayu S, Fitri L, Ismail YS. 2019. Short communication: Endophytic actinobacteria isolated from ginger (Zingiber officinale) and its potential as a pancreatic lipase inhibitor and its toxicity. Biodiversitas 20: 1312-1317.  Endophytic actinobacteria from ginger (Zingiber officinale Rosc.) is a bacterium that is capable of producing secondary metabolites that are the same as their hosts. This study aims to look at the potential of endophytic actinobacteria from ginger as a pancreatic lipase inhibitor and its toxicity. Endophytic actinobacteria were isolated, purified, then tested for pancreatic lipase inhibitors and their toxicity using the BSLT method (Brine Shrimp Lethality Test) and phytochemical tested on ethanol extract of selected isolates. Seven endophytic actinobacterial isolates were isolated from the ginger rhizome. The isolates had different morphological diversity based on colony and microscopic observations and 5 isolates had pancreatic lipase inhibitor activity. The highest inhibitors were found in AJ4 isolates (89.9%), compared with pancreatic lipase inhibitors crude extracts of ginger (68.9%) and orlistat (88.1%) as positive controls. The LC50 value of AJ4 isolates was 653,381 ppm and the value of LT50 was 17,569 hours. AJ4 isolates contain terpenoids, phenols, tannins, flavonoids, alkaloids, and saponins. This research data is considered as new information about the potential of endophytic actinobacteria from ginger as pancreatic lipase inhibitors and their toxicity.

scholarly journals In Vitro Pancreatic Lipase Inhibitor Activity of Mangifera foetida Leaves Extract

2021 ◽  
Vol 6 (1) ◽  
pp. 82-92
Author(s):  
Oktira Roka Aji ◽  
Riris Asyhar Hudaya ◽  
Diah Asta Putri
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitor Activity ◽  
Lipase Inhibitor
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