Pharmacophore Mapping of Natural Products for Pancreatic Lipase Inhibition

2020 ◽  
pp. 305-338 ◽  
Author(s):  
Matheus Gabriel de Oliveira ◽  
Waléria Ramos Nogueira de Souza ◽  
Ricardo Pereira Rodrigues ◽  
Daniel F. Kawano ◽  
Leonardo Luiz Borges ◽  
...  
Keyword(s):  
Natural Products ◽  
Pancreatic Lipase ◽  
Pharmacophore Mapping ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

scholarly journals Biological activity of alginate and its effect on pancreatic lipase inhibition as a potential treatment for obesity

2015 ◽  
Vol 49 ◽  
pp. 18-24 ◽  
Author(s):  
David Houghton ◽  
Matthew D. Wilcox ◽  
Peter I. Chater ◽  
Iain A. Brownlee ◽  
Chris J. Seal ◽  
...  
Keyword(s):  
Biological Activity ◽  
Pancreatic Lipase ◽  
Potential Treatment ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

scholarly journals Kinetic Behaviour of Pancreatic Lipase Inhibition by Ultrasonicated A. malaccensis and A. subintegra Leaves of Different Particle Sizes

2020 ◽  
Vol 15 (3) ◽  
pp. 818-828
Author(s):  
Miradatul Najwa Muhd Rodhi ◽  
Fazlena Hamzah ◽  
Ku Halim Ku Hamid
Keyword(s):  
Particle Size ◽  
Gallic Acid ◽  
Pancreatic Lipase ◽  
Crude Extract ◽  
Competitive Inhibition ◽  
Treatment Method ◽  
Crude Extracts ◽  
Pre Treatment ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

Gallic acid and quercetin equivalent were determined in the crude extract of matured leaves Aquilaria malaccensis and Aquilaria subintegra. The leaves of both Aquilaria species were dried at 60 °C for 24 hours, ground and sieved into particle size of 250, 300, 400, 500, and 1000 µm. Then, each particle size of leaves was soaked in distilled water with a ratio of 1:100 (w/v) for 24 hours and undergoes the pre-treatment method by using ultrasonicator (37 kHz), at the temperature of 60 °C for 30 minutes. The crude extracts were obtained after about 4 hours of hydrodistillation process. The highest concentration of gallic acid and quercetin equivalent was determined in the crude extract from the particle size of 250 µm. The kinetics of pancreatic lipase inhibition was further studied based using the Lineweaver-Burk plot, wherein the concentration of p-NPP as the substrate and pancreatic lipase were varied. Based on the formation of the lines in the plot, the crude leaves extract of both Aquilaria species exhibit the mixed-inhibition on pancreatic lipase, which indicates that in the reaction, the inhibitors were not only attached to the free pancreatic lipase, but also to the pancreatic lipase-(p-NPP) complex. The reaction mechanism was similar to non-competitive inhibition; however the value of dissociation constant, Ki, for both inhibition pathways was different. The inhibition shows an increment in Michaelis-Menten constant (Km) and a reduction in the maximum pancreatic lipase activity (Vm) compared to the reaction without Aquilaria spp. crude extracts (control). This proved that the inhibition occurred in this reaction. Copyright © 2020 BCREC Group. All rights reserved 

scholarly journals In Vitro Pancreatic Lipase Inhibition by Marine Fungi Purpureocillium lilacinum Associated with Stylissa sp. Sponge as Anti-obesity Agent

2021 ◽  
Vol 29 (1) ◽  
pp. 76-86
Author(s):  
Wendi Nurul Fadillah ◽  
Nampiah Sukarno ◽  
Dyah Iswantini ◽  
Min Rahminiwati ◽  
Novriyandi Hanif ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Pancreatic Lipase ◽  
Metabolite Identification ◽  
Molecular Characteristics ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Purpureocillium Lilacinum ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

This study aimed to evaluate the potential of marine fungus Purpureocillium lilacinum isolated from an Indonesian marine sponge Stylissa sp. as an anti-obesity agent through pancreatic lipase inhibition assay. The fungus was identified as P. lilacinum through morphological and molecular characteristics. The fungal extract’s inhibition activity and kinetics were evaluated using spectrophotometry and Lineweaver-Burk plots. Ethyl acetate and butanol were used for extraction. Both extracts showed pancreatic lipase inhibition in a concentration-dependent manner. Both crude extracts were then fractionated once. All fractionated extracts showed inhibitory activity above 50%, with the highest activity found in fraction 5 of ethyl acetate at 93.41% inhibition. The best fractionated extract had an IC50value of 220.60 µg.mL-1. The most active fraction of P. lilacinum had a competitive-type inhibitor behavior as shown by the value of Vmax not significantly changing from 388.80 to 382.62 mM pNP.min-1, and the Michaelis-Menten constant (KM) increased from 2.02 to 5.47 mM in the presence of 500 µg.mL-1 fractionated extract. Metabolite identification with LC-MS/MS QTOF suggested that galangin, kaempferol, and quercetin were responsible for the observed lipase inhibition.

Pancreatic lipase inhibition of strictinin isolated from Pu’er tea (Cammelia sinensis) and its anti-obesity effects in C57BL6 mice

2018 ◽  
Vol 48 ◽  
pp. 1-8 ◽  
Author(s):  
Tzu-Yin Chen ◽  
Miki M.C. Wang ◽  
Sheng-Kuo Hsieh ◽  
Meng-Huang Hsieh ◽  
Wen-Ying Chen ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

Pancreatic lipase inhibition activity of trilactone terpenes of Ginkgo biloba

2010 ◽  
Vol 26 (4) ◽  
pp. 453-459 ◽  
Author(s):  
Yasser Bustanji ◽  
Ihab M. Al-Masri ◽  
Mohammad Mohammad ◽  
Mohammad Hudaib ◽  
Khaled Tawaha ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Ginkgo Biloba ◽  
Inhibition Activity ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

scholarly journals Synthesis, Drug Likeness and In-vitro Screening of Some Novel Quinazolinone Derivatives for Anti-Obesity Activity

2021 ◽  
pp. 81-92
Author(s):  
Pratik G. Modh ◽  
Laxman J. Patel
Keyword(s):  
Pancreatic Lipase ◽  
Synthesis Method ◽  
Proton Nmr ◽  
Lipolytic Enzyme ◽  
Coupling Reactions ◽  
Lipinski’S Rule ◽  
High Yields ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

Aim: A series of novel quinazolinone derivates was synthesized and assessed for their ability to inhibitory action on pancreatic lipase. The cyclization of quinazolinone-4(3H)-one derivatives was achieved, whereas carbon-carbon cross coupling reactions were carried out on cyclized quinazolinone-4(3H)-one. This synthesis method afforded corresponding 2, 3 and 6 substituted quinazolin-4(3H)-ones (3a to 3m) with moderate to high yields. Methods: Benzamide derivatives (1a-1b) were synthesized from anthranilic acid using acid-amine reaction, followed by cyclization using catalytic p-toluene sulfonic acid and oxidation using (diacetoxyiodo)benzene to give bromo substituted quinazolin-4(3H)-ones (2a-2b), which were cross coupled to suitable boronic acid using Suzuki-Miyaura condition to obtain desired compound (3a-3m). All synthesized compounds were characterized by FTIR, proton NMR, LC-MS analysis, checked for their drug likeness, absorption and evaluated for in vitro pancreatic lipase inhibition activity. Results: Analytical interpretation of all compounds with infrared, proton NMR and LC-MS spectroscopy confirmed their correct structure. All compounds (3a-3m) show good absorption and have reasonably good molecular properties except 3c and 3m which violate two criteria for Lipinski’s rule. Whereas, Compounds 3l and 3m showed IC50 value of 13.13±0.84 µg/mL and 13.80±1.27 µg/mL respectively comparable to the Orlistat (12.72±0.97µg/mL), a US FDA approved drug for the treatment of obesity. Conclusion: Pancreatic lipase is an important lipolytic enzyme, synthesized and secreted through pancreas, plays an important role in dietary trigycerol absorption and metabolism. Therefore, reducing fat absorption through pancreatic lipase inhibition is a promising strategy to treat obesity. Based upon our findings, compounds 3l and 3m can be further developed as potent anti-obesity agents.

scholarly journals Pancreatic Lipase Inhibitory Activity of Cassiamin A, a Bianthraquinone from Cassia siamea

2013 ◽  
Vol 8 (2) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Dilip Kumar ◽  
Aniket Karmase ◽  
Sneha Jagtap ◽  
Ruchi Shekhar ◽  
Kamlesh K Bhutani
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Enzyme Inhibitors ◽  
Etoac Extract ◽  
Cassia Siamea ◽  
Bioassay Guided Fractionation ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition ◽  
Indian Medicinal Plants

In continuation towards the discovery of potential antiobesity lead(s) from natural products, we have screened n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH) extracts of 33 Indian medicinal plants (200 extracts) for in vitro pancreatic lipase inhibitory activity. Of the screened extracts, the EtOAc extract of Cassia siamea roots showed 74.3±1.4% enzyme inhibition at 250 μg/mL concentration. Bioassay guided fractionation of the active extract afforded 6 known compounds viz. chrysophanol (1), physcion (2), emodin (3), cassiamin A (4), friedelin (5) and cycloart-25-en-3β,24-diol (6). These compounds were further evaluated for pancreatic lipase inhibitory activity. Cassiamin A (4), a bianthraquinone, was found to be most active with an IC50 value of 41.8±1.2 μM and compounds 2 and 5 were found to be moderate enzyme inhibitors. Results indicate the antiobesity potential of C. siamea through pancreatic lipase inhibition.

scholarly journals Anti-Obesity Effect of Arq Zeera and Its Main Components Thymol and Cuminaldehyde in High Fat Diet Induced Obese Rats

Drug Research ◽  
2018 ◽  
Vol 68 (11) ◽  
pp. 637-647 ◽  
Author(s):  
Mohammad Haque ◽  
H. Ansari
Keyword(s):  
Body Weight ◽  
Pancreatic Lipase ◽  
High Fat Diet ◽  
Liver Weight ◽  
Fat Pad ◽  
High Fat ◽  
Obese Rats ◽  
Main Components ◽  
Pancreatic Lipase Inhibition ◽  
Lipase Inhibition

AbstractArq zeera is a distillate product that prepared from four different herbs namely Trachyspermum ammi L., apiaceae, Zingiber officinale Roxb., zingiberaceae, Carum carvi L.,apiaceae and Cuminum cyminum L., apiaceae. The present study aims to determine the antiobesity effect of arq zeera and its main components thymol and cuminaldehyde in high fat diet induced obese rats and to explore its mechanism of action. In current study, orlistat was used as positive controls. Male Wistar rats were fed with HFD for 42 days to induce obesity. HFD-fed rats were administered with arq zeera, thymol, cumic aldehyde, thymol + cuminaldehyde and orlistat for 28 days. During the course of treatment, body weight and food intake frequently observed and after end of treatments, liver weight, visceral fat pad weight, plasma lipid proflie, alanine aminotransferase, aspartate aminotransferase, glucose, insulin, leptin levels and pancreatic lipase activity were studied on all treated obese rats. The histopathology of liver was also studied. After the treatments of arq zeera and its main components, body weight, food intake, liver weight, visceral fat pad weight and the level of lipid profile, alanine aminotransferase, aspartate aminotranferase, glucose, insulin, and leptin were found to be decreased and pancreatic lipase inhibition were increased. Arq zeera showed more potential antiobesity effect than orlistat. According to our present findings, arq zeera and its main components possessed potent antiobesity effect on high fat diet -induced obese rats and excreted anti-obesity effect partly via hypolipidemic, hypoglycemic, hypoinsulinemic, hypoleptinemic and pancreatic lipase inhibition action.

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