scholarly journals Pancreatic Lipase Inhibitory Alkaloids of Murraya koenigii Leaves

2009 ◽  
Vol 4 (8) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Rahul Birari ◽  
Somendu Kumar Roy ◽  
Anubha Singh ◽  
Kamlesh Kumar Bhutani
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Murraya Koenigii ◽  
Etoac Extract ◽  
Inhibitory Potential ◽  
Pancreatic Lipase Inhibitors ◽  
First Time ◽  
Carbazole Alkaloids

In the continuing search for newer pancreatic lipase inhibitors from plants, a total of 63 extracts from 21 different plants were screened to study their pancreatic lipase (PL) inhibitory activity in vitro. All three extracts (DCM, EtOAc and MeOH) of Murraya koenigii (L.) Spreng leaves (Rutaceae) exhibited antilipase activity greater than 80%. Further, bioactivity guided fractionation of the EtOAc extract led to the isolation of four alkaloids, namely mahanimbin, koenimbin, koenigicine and clausazoline-K, with IC50 values of 17.9 μM, 168.6 μM, 428.6 μM and ≤500 μM, respectively. This study reports for the first time the PL inhibitory potential of carbazole alkaloids from plants.

scholarly journals In vitro Antidiabetic, anti-obesity and antioxidant proprities of Rosemary extracts

2014 ◽  
Vol 10 (2) ◽  
pp. 2305-2316 ◽  
Author(s):  
Manel Ben Ali ◽  
Kais Mnafgui ◽  
Abdelfattah Feki ◽  
Mohamed Damak ◽  
Noureddine Allouche
Keyword(s):  
Essential Oil ◽  
Ethyl Acetate ◽  
Pancreatic Lipase ◽  
Antioxidant Properties ◽  
Methanolic Extracts ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Prevention Of Diabetes ◽  
First Time

Diabetes mellitus is a serious health problem worldwide that has adverse and long-lasting consequences for individuals, families, and communities. Hence, this study sought to investigate the inhibitory potential of rosemary extracts on key-enzymes related to diabetes such as α-amylase and pancreatic lipase activities, as well as to assess their antioxidant properties in vitro. The IC50 values of Rosemary essential oil, ethyl acetate and methanolic extracts against α-amylase were 28.36, 34.11 and 30.39 µg/mL respectively, and those against pancreatic lipase were 32.25, 36.64 and 34.07 µg/mL, suggesting strong anti-diabetic and anti-obesity effects of Rosemary. The methanolic extract was found to be the highest in levels of phenolic (282.98 µgGAE/mg extract) and flavonoids (161.05 µg QE /mg extract) contents as well as in the antioxidant activity (IC50 = 15.82 µg/mL) as compared to other extracts ethyl acetate (IC50 = 32.23 µg/mL) and essential oil  (IC50 = 96.12 µg/mL).Antioxidant efficacy of Rosemary extracts has been estimated in the stabilization of sunflower oil (SFO) at three different concentrations, i.e. 200 (SFO-200), 500 (SFO-500) and 1000 ppm (SFO-1000). Results showed the highest efficiency of SFO-1000.The results obtained in this study demonstrated for the first time that Rosemary is a potent source of natural inhibitors of α-amylase and pancreatic lipase with powerful antioxidants proprieties that might be used in the food stabilization and the prevention of diabetes and obesity complications as a complementary pharmacological drug.

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 Pancreatic lipase inhibitory activity of selected pharmaceutical agents

2019 ◽  
Vol 69 (1) ◽  
pp. 1-16 ◽  
Author(s):  
Imad I. Hamdan ◽  
Violet N. Kasabri ◽  
Yusuf M. Al-Hiari ◽  
Dina El-Sabawi ◽  
Hiba Zalloum
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Synergistic Effects ◽  
Docking Studies ◽  
Antagonistic Effect ◽  
Camphor Sulfonic Acid ◽  
Pharmaceutical Agents ◽  
First Time ◽  
The Relationship

Abstract Twenty-five structurally diverse compounds have been tested in vitro for their pancreatic lipase (PL) inhibitory activity. Despite the diversity of tested compounds, the relationship comprising structural attributes of the compounds could be established to correlate with the observed inhibitory activity. Compounds that exerted inhibitory action through surface activity were of different profile from the rest of compounds. When co-incubated with orlistat (OsT), important synergistic effects for some compounds (orphenadrine, gliclazide, cefuroxime and sulfacetamide) were revealed, while antagonistic effects were demonstrated for others (camphor sulfonic acid and dinitro salicylic acid). Docking studies for the most active molecules were performed and molecular interaction forces with the PL active site were identified. The results suggested co-binding of OsT along with the other inhibitor in the binding site in cases of synergistic effect but not in the case of antagonistic effect. These results were additionally supported by affinity capillary electrophoresis. In conclusion, synergistic lipase inhibitory activity between OsT and some other pharmaceutical compounds was demonstrated for the first time, which might help improve the pharmacological effect of OsT.

A review on pancreatic lipase inhibitors from natural sources: a potential target for obesity

2021 ◽  
Vol 17 ◽  
Author(s):  
Bency Baby T ◽  
Murali R ◽  
Suriyaprakash TNK ◽  
Srinivasan N
Keyword(s):  
Natural Products ◽  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Journal Article ◽  
Natural Sources ◽  
Potential Target ◽  
Biological Sources ◽  
Pancreatic Lipase Inhibitors

Background: Obesity is a worldwide lifestyle disorder and its incidence is growing at an alarming rate. Pancreatic lipase (PL) plays a key role in lipid metabolism and hence a potential target for obesity treatment. There have been reports that many bioactive compounds from natural sources are vast pool of PL inhibitors. Objective: In search of natural pancreatic lipase inhibitors, the review summarizes the potential of natural products for their pancreatic lipase inhibitory activity. Methods: In this review the data obtained from literature search across various electronic databases and journal article publications are reviewed. Results: The pancreatic lipase inhibitory activities of 61 biological sources were reviewed in this paper is backed by preclinical experimental evidence, either in vivo or in vitro. Conclusion: This article can be used as a ready to use reference for therapeutic lead molecules from plants, marine and insect derived natural products with PL inhibitory activity. The research is more focused on the discovery of more ingenious pancreatic lipase inhibitors with lesser consequences.

scholarly journals Mammalian Arginase Inhibitory Activity of Methanolic Extracts and Isolated Compounds from Cyperus Species

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Significant Inhibition ◽  
Isolation And Identification ◽  
Vasorelaxant Effect ◽  
Methanolic Extracts ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.

scholarly journals Chemical composition and antifungal activity of essential oils from four Asteraceae plants grown in Egypt

2018 ◽  
Vol 73 (7-8) ◽  
pp. 313-318 ◽  
Author(s):  
Rose Vanessa Bandeira Reidel ◽  
Simona Nardoni ◽  
Francesca Mancianti ◽  
Claudia Anedda ◽  
Abd El-Nasser G. El Gendy ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Inhibitory Activity ◽  
First Time

Abstract The objective of the present paper was the assessment of the chemical composition of the essential oils from four Asteraceae species with a considerable food, medicinal, and agricultural value, collected in Egypt, together with their in vitro inhibitory activity against molds and yeasts. The essential oil of Launaea cornuta flowers was also evaluated for the first time, but because of its very low yield (<0.01%), no antifungal test was performed.

IN VITRO STUDIES OF SOME EDIBLE SPICES ON PANCREATIC LIPASE INHIBITORY ACTIVITY

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 62-68
Author(s):  
S Mhatre ◽  
◽  
A. Bhagit ◽  
R. P Yadav
Keyword(s):  
Pancreatic Lipase ◽  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Syzygium Aromaticum ◽  
High Potency ◽  
Good Source ◽  
Zanthoxylum Armatum ◽  
Methanolic Extracts ◽  
Cinnamomum Tamala

Pancreatic lipase inhibitory effect of some edible spices in light of percent inhibition, efficacy, reversibility/ irreversibility and effect of pH on inhibition is presented here. Lipase inhibitory activities of methanolic extracts of eighteen spices were evaluated. Extracts of Zanthoxylum armatum, Cinnamomum tamala, Syzygium aromaticum and Myristica fragrans were considered to be of high potency in synthetic substrate assay. Only Syzygium aromaticum showed high potency in natural substrate based lipase assay. Zanthoxylum armatum extract displayed lowest IC50 of 9.0 μg/mL. On dialysis, all extracts lost their lipase inhibitory activity indicating reversible nature of inhibition. pH significantly affected the performance of spice extracts during inhibition of pancreatic lipase. Most of the extracts lost their pancreatic lipase inhibitory activity at pH 3.0 with the exception of Brassica nigra and Cinnamomum tamala. Results showed spice are good source of pancreatic lipase inhibitor and its potential as drug for obesity can be explored by addressing various issues.

scholarly journals Development of an Efficient Protocol for Cimifugin Isolation from Peucedanum schottii and Evaluation of Enzyme Inhibitory Activity

2016 ◽  
Vol 11 (8) ◽  
pp. 1934578X1601100
Author(s):  
Ewelina Kozioł ◽  
Ilkay Erdogan Orhan ◽  
F. Sezer Senol ◽  
Kalina Alipieva ◽  
Milen Georgiev ◽  
...  
Keyword(s):  
Nmr Spectroscopy ◽  
Ethyl Acetate ◽  
Crude Extract ◽  
Inhibitory Activity ◽  
High Performance ◽  
Performance Counter ◽  
Inhibitory Potential ◽  
Counter Current ◽  
First Time ◽  
Analytical Scale

The dichloromethane (DCM) extract of the fruits of Peucedanum schottii Besser ex DC. (Apiaceae) was subjected to high-performance counter-current chromatography (HPCCC) for the efficient and fast separation (30 min) and isolation of cimifugin using an ethyl acetate: water (1:1 v/v, K = 1.01) system. The analytical scale-optimized separation was easily scaled to semi-preparative conditions. Cimifugin (11.25% yield, 96.5% purity) was isolated for the first time from P. schottii and characterized by NMR spectroscopy. Cimifugin and the crude DCM extract were evaluated using ELISA microtiter assays for their inhibitory potential against the cholinesterases (acetylcholinesterase - AChE and butyrylcholinesterase - BChE), and tyrosinase (TYR), which are key enzymes for the treatment of some neurodegenerative diseases, i.e. Alzheimer's and Parkinson's. The crude extract exhibited a weak inhibitory activity against AChE, BChE, and TYR (4.2, 35.5, and 0% at 100 μg mL−1 and 10.3, 40.0, and 12.2% at 200 μg mL−1, respectively), while cimifugin displayed low to moderate inhibition towards AChE and BChE (3.1 and 21.6%, respectively) at 200 μg mL−1.

scholarly journals Pharmacologic Activities¬ of 3’-Hydroxypterostilbene: Cytotoxic, Anti-Oxidant, Anti-Adipogenic, Anti-Inflammatory, Histone Deacetylase and Sirtuin 1 Inhibitory Activity

2015 ◽  
Vol 18 (4) ◽  
pp. 713 ◽  
Author(s):  
Jody K Takemoto ◽  
Connie M. Remsberg ◽  
Neal M. Davies
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Sirtuin 1 ◽  
In Vitro Assays ◽  
Naturally Occurring ◽  
Anti Oxidant ◽  
Anti Inflammatory ◽  
First Time ◽  
Stilbene Compounds

Purpose: Delineate the selected pharmacodynamics of a naturally occurring stilbene 3’-Hydroxypterostilbene. Objective: Characterize for the first time the pharmacodynamics bioactivity in several in-vitro assays with relevant roles in heart disease, inflammation, cancer, and diabetes etiology and pathophysiology. Methods: 3’-Hydroxypterostilbene was studied in in-vitro assays to identify possible bioactivity. Results: 3’-Hydroxypterostilbene demonstrated anti-oxidant, anti-inflammatory, cytotoxic, anti-adipogenic, histone deacetylase, and sirtuin-1 inhibitory activity. Conclusions: The importance of understanding individual stilbene pharmacologic activities were delineated.  Small changes in chemical structure of stilbene compounds result in significant pharmacodynamic differences. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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