scholarly journals Characteristics of New Peptides GQLGEHGGAGMG, GEHGGAGMGGGQFQPV, EQGFLPGPEESGR, RLARAGLAQ, YGNPVGGVGH, and GNPVGGVGHGTTGT as Inhibitors of Enzymes Involved in Metabolic Syndrome and Antimicrobial Potential

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2492 ◽  
Author(s):  
Urszula Złotek ◽  
Anna Jakubczyk ◽  
Kamila Rybczyńska-Tkaczyk ◽  
Paula Ćwiek ◽  
Barbara Baraniak ◽  
...  
Keyword(s):  
Metabolic Syndrome ◽  
Antimicrobial Activity ◽  
Inhibitory Activity ◽  
Synthetic Peptides ◽  
Cytotoxic Effect ◽  
Inhibitory Effect ◽  
Converting Enzyme ◽  
Cox 2 ◽  
Enzyme I ◽  
Cox 1

The aim of this study was to determine the cytotoxic properties, influence on enzyme activity involved in metabolic syndrome, and antimicrobial activity of synthetic peptides with GQLGEHGGAGMG, GEHGGAGMGGGQFQPV, EQGFLPGPEESGR, RLARAGLAQ, YGNPVGGVGH, and GNPVGGVGHGTTGT sequences. Peptides have no cytotoxic effect on cells. The highest inhibitory effect on angiotensin converting enzyme I was noted for peptide GT-14 (IC50 = 525.63 µg/mL). None of the tested peptides had an influence on α-glucosidase. The highest α-amylase and lipase inhibitory activity was noted for GG-12 (IC50 = 56.72 and 60.62 µg/mL, respectively). The highest lipoxidase inhibitory activity was determined for peptide ER-13 (IC50 = 84.35 µg/mL). Peptide RQ-9 was characterized by the highest COX inhibitory activity (0.31 and 4.77 µg/mL for COX-1 and COX-2, respectively). Only peptide RQ-9 inhibited S. enteritidis ATCC 4931 growth (42–48%) in all tested concentrations (15.62–250 mg/mL).

scholarly journals In vitro Anti-inflammatory Activity of Ligustrum vulgare Extracts and Their Analytical Characterization

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Anna Macková ◽  
Pavel Mučaji ◽  
Ute Widowitz ◽  
Rudolf Bauer
Keyword(s):  
Inhibitory Activity ◽  
Inhibitory Effect ◽  
Neutrophil Granulocytes ◽  
Cyclooxygenase 1 ◽  
Ligustrum Vulgare ◽  
China And Japan ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 1

Interest in the anti-inflammatory effects of Ligustrum vulgare L., which has been used traditionally in China and Japan prompted us to determine anti-inflammatory effects of the plant's compounds in leukocytes. The leaves of L. vulgare were used to prepare a decoction which was successively extracted with organic solvents (dichloromethane (DCM), n-butanol, ethyl acetate) using liquid-liquid partition. Extracts were tested for inhibition of LTB4, resp. PGE2 biosynthesis. Each extract was evaluated for its in vitro cyclooxygenase-1/2 (COX-1/2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes, as well as for their LTB4 formation inhibitory activity using an assay with activated human neutrophil granulocytes. All extracts reported inhibitory actions against COXs in comparison with the synthetic inhibitors NS-398 (IC50 = 2.6 μM) and indomethacin (IC50 = 0.9 μM). The dichloromethane extract of privet leaves showed a considerable inhibitory effect against COX-1 and COX-2 enzyme activity. The DCM extract revealed 2.7 times higher inhibitory activity against LTB4 formation in comparison with the known specific LT inhibitor zileuton (IC50 = 5.0 μM). Additionally, oleuropein and echinacoside were detected by HPLC-DAD and LC-MS in the Ligustrum vulgare leaves. Both compounds exhibited weak inhibitory activity on cyclooxygenases and leukotriene formation.

New indomethacin analogs as selective COX‐2 inhibitors: Synthesis, COX‐1/2 inhibitory activity, anti‐inflammatory, ulcerogenicity, histopathological, and docking studies

2020 ◽  
Author(s):  
Khaled R. A. Abdellatif ◽  
Eman K. A. Abdelall ◽  
Heba A. H. Elshemy ◽  
El‐Shaymaa El‐Nahass ◽  
Maha M. Abdel‐Fattah ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Studies ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Cox 2 Inhibitors ◽  
Cox 1

scholarly journals Influence of Elicitation and Drying Methods on Anti-Metabolic Syndrome, and Antimicrobial Properties of Extracts and Hydrolysates Obtained from Elicited Lovage (Levisticum officinale Koch)

Nutrients ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 4365
Author(s):  
Anna Jakubczyk ◽  
Urszula Złotek ◽  
Kamila Rybczyńska-Tkaczyk
Keyword(s):  
Metabolic Syndrome ◽  
Antimicrobial Activity ◽  
Biological Activity ◽  
Inhibitory Activity ◽  
Freeze Drying ◽  
Antimicrobial Properties ◽  
Ethanolic Extract ◽  
Microwave Drying ◽  
Drying Methods ◽  
Ethanolic Extracts

This research aims to investigate the influence of elicitation and drying methods (natural, convection, microwave, and freeze-drying), with jasmonic acid (JA) and yeast extract (YE) on the biological activity of extracts and hydrolysates from lovage (Levisticum officinale Koch) leaves. The results indicate that the highest TPC was determined for hydrolysates obtained from JA-elicited microwave-dried lovage (24.96 mg/gDW). The highest ACE and lipase inhibitory activity was noted for PBS extract obtained from JA-elicited lovage after microwave drying (EC50 = 0.16 and 0.12 mg/mL, respectively). Ethanolic extract from JA-elicited lovage after freeze-drying was characterized by the highest α-amylase inhibitory activity (EC50 = 3.92 mg/mL) and the highest α-glucosidase inhibitory activity (EC50 = 1.43 mg/mL) was noted for hydrolysates from control plants subjected to freeze-drying. The highest antimicrobial activity towards C. albicans yeasts was observed for microwave ethanolic extracts with minimal inhibition (MIC) and lethal (MLC) concentrations of 0.625 and 1.25 mg/mL, respectively.

In vitro COX-1, COX-2 and 5-LOX inhibitory activity of plant family Ranunculaceae

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
J Malik ◽  
P Landa ◽  
Z Kutil ◽  
P Marsik ◽  
L Kokoska
Keyword(s):  
Inhibitory Activity ◽  
Plant Family ◽  
Cox 2 ◽  
Cox 1

scholarly journals Kinetic basis for selective inhibition of cyclo-oxygenases

1999 ◽  
Vol 339 (3) ◽  
pp. 607-614 ◽  
Author(s):  
James K. GIERSE ◽  
Carol M. KOBOLDT ◽  
Mark C. WALKER ◽  
Karen SEIBERT ◽  
Peter C. ISAKSON
Keyword(s):  
Inhibitory Activity ◽  
Tight Binding ◽  
Selective Inhibition ◽  
Time Dependent ◽  
Experimental Conditions ◽  
Kinetic Behaviour ◽  
Competitive Kinetics ◽  
Binding Time ◽  
Cox 2 ◽  
Cox 1

Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit the formation of prostaglandins by cyclo-oxygenases (COX). The discovery of a second COX isoform (COX-2) associated with inflammation led to agents that selectively inhibit COX-2, e.g. celecoxib. We evaluated the kinetics of inhibition of celecoxib and several NSAIDs. Celecoxib displays classic competitive kinetics on COX-1 (Ki = 10-16 μM). An initial competitive interaction with COX-2 can also be discerned with celecoxib (Ki = 11-15 μM), followed by a time-dependent interaction leading to potent inhibition, characterized as inactivation (Kinact = 0.03-0.5 s-1). Half-maximal inhibition (IC50) using end-point assays reflects the competitive component on COX-1 (IC50 = 4-19 μM) and the inactivation component on COX-2 (IC50 = 0.003-0.006 μM). NSAIDs exhibit four distinct modes of COX inhibition based on kinetic behaviour: (1) competitive, e.g. ibuprofen; (2) weak binding, time-dependent, e.g. naproxen, oxicams; (3) tight binding, time-dependent, e.g. indomethacin; (4) covalent, e.g. aspirin. In addition, most NSAIDs display different kinetic behaviour for each isoform. Weakly binding inhibitors show variable behaviour in enzyme assays, with apparent inhibitory activity being markedly influenced by experimental conditions; determination of kinetic constants with this class is unreliable and IC50 values are strongly dependent on assay conditions. Although IC50 determinations are useful for structure/activity analyses, the complex and distinct mechanisms of enzyme inhibition of each COX isoform by the NSAIDs renders comparison of inhibitory activity on COX-1 and COX-2 using IC50 ratios of questionable validity.

scholarly journals Ellagic acid inhibits lipopolysaccharide-induced expression of enzymes involved in the synthesis of prostaglandin E2 in human monocytes

2009 ◽  
Vol 103 (8) ◽  
pp. 1102-1109 ◽  
Author(s):  
Sofia Karlsson ◽  
Eewa Nånberg ◽  
Christina Fjaeraa ◽  
Jonny Wijkander
Keyword(s):  
Ellagic Acid ◽  
Inhibitory Effect ◽  
Ionophore A23187 ◽  
Human Monocytes ◽  
Cytosolic Phospholipase ◽  
Natural Polyphenol ◽  
The Subject ◽  
Cox 2 ◽  
Cancer And Inflammation ◽  
Cox 1

Ellagic acid, a natural polyphenol found in certain fruits, nuts and vegetables, has in recent years been the subject of intense research within the fields of cancer and inflammation. Pain, fever and swelling, all typical symptoms of inflammation, are ascribed to elevated levels of PGE2. In the present study, we have investigated the effects of ellagic acid on PGE2 release and on prostaglandin-synthesising enzymes in human monocytes. Ellagic acid was found to inhibit Ca ionophore A23187-, phorbol myristate acetate- and opsonised zymosan-induced release of PGE2 from monocytes pre-treated with the inflammatory agent lipopolysaccharide. Ellagic acid suppressed the lipopolysaccharide-induced increase in protein expression of cyclo-oxygenase-2 (COX-2), microsomal PGE synthase-1 (mPGEs-1) and cytosolic phospholipase A2α (cPLA2α), while it had no effect on the constitutively expressed COX-1 protein. Ellagic acid had no apparent inhibitory effect on these enzymes when the activities were determined in cell-free assays. We conclude that the inhibitory effect of ellagic acid on PGE2 release from monocytes is due to a suppressed expression of COX-2, mPGEs-1 and cPLA2α, rather than a direct effect on the activities of these enzymes.

Flavonoids and Stilbenoids with COX-1 and COX-2 Inhibitory Activity fromDracaena loureiri

Planta Medica ◽  
2002 ◽  
Vol 68 (9) ◽  
pp. 841-843 ◽  
Author(s):  
Kittisak Likhitwitayawuid ◽  
Kanokporn Sawasdee ◽  
Kanyawim Kirtikara
Keyword(s):  
Inhibitory Activity ◽  
Cox 2 ◽  
Cox 1
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