The aim of this paper was to investigate the effect of chlorogenic acid (5-caffeoylquinic acid, 5CQA), isolated from Baccharis oxyodonta, on the structure and pharmacological effect of secretory phospholipase A2 (sPLA2) from Crotalus durissus terrificus. All in vitro and in vivo experiments were conducted using a purified sPLA2 compared under the same experimental conditions with sPLA2 : 5CQA. 5CQA induced several discrete modifications in the secondary structure and the hydrophobic characteristics of native sPLA2 that induced slight changes in the α-helical content, increase in the random coil structure, and decrease of fluorescence of native sPLA2. Moreover, 5CQA significantly decreased the enzymatic activity and the oedema and myonecrosis induced by native sPLA2. As the catalytic activity of sPLA2 plays an important role in several of its biological and pharmacological properties, antibacterial activity was used to confirm the decrease in its enzymatic activity by 5CQA, which induced massive bacterial cell destruction. We found that 5CQA specifically abolished the enzymatic activity of sPLA2 and induced discrete protein unfolding that mainly involved the pharmacological site of sPLA2. These results showed the potential application of 5CQA in the snake poisoning treatment and modulation of the pathological effect of inflammation induced by secretory PLA2.
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http://dx.doi.org/10.1155/2014/726585 | DOI Listing |
J Lipid Res
January 2025
Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, University of Graz, Graz, Austria; Field of Excellence BioHealth - University of Graz, Graz, Austria. Electronic address:
Phospholipids containing oxidized esterified PUFA residues (OxPLs) are increasingly recognized for multiple biological activities and causative involvement in disease pathogenesis. Pharmacokinetics of these compounds in blood plasma is essentially not studied. Human plasma contains both genuine phospholipases A (PAF-AH (also called Lp-PLA) and sPLA) and multifunctional enzymes capable of removing sn-2 residues in native and oxidized PLs (LCAT, PRDX6).
View Article and Find Full Text PDFMar Drugs
July 2019
Laboratório de Bioquímica e Biologia Molecular de Peptídeos (BIOMOLPEP), Instituto de Biociências, UNESP, Campus do Litoral Paulista, São Vicente 11330-900, São Paulo, Brazil.
Ellagitannins constitute the largest group of hydrolyzable tannins of plants, and, from this group, casuarictin (Casu) was identified in some plant species. However, to our knowledge, no investigation of secretory phospholipase A2 (sPLA2) inhibition by Casu has been performed yet. Casuarictin was isolated by chromatography n-butanol (n-BuOH) partition of leaves.
View Article and Find Full Text PDFBiochem Biophys Res Commun
July 2019
Departments of Health Sciences and Biological Sciences, Faculties of Applied Health Sciences and Mathematics & Science, Brock University, St. Catharines, ON, L2S 3A1, Canada. Electronic address:
The canonical Phospholipase A (PLA) metabolites lysophosphatidylcholine (LPC) and arachidonic acid (ARA) affect regulated exocytosis in a wide variety of cells and are proposed to directly influence membrane merger owing to their respective spontaneous curvatures. According to the Stalk-pore hypothesis, negative curvature ARA inhibits and promotes bilayer merger upon introduction into the distal or proximal monolayers, respectively; in contrast, with positive curvature, LPC has the opposite effects. Using fully primed, release-ready native cortical secretory vesicles (CV), well-established fusion assays and standardized lipid analyses, we show that exogenous ARA and LPC, as well as their non-metabolizable analogous, ETYA and ET-18-OCH3, inhibit the docking/priming and membrane merger steps, respectively, of regulated exocytosis.
View Article and Find Full Text PDFSaudi J Biol Sci
December 2018
Instituto de Química del Noroeste Argentino (INQUINOA, CONICET), Argentina.
Cav. (Fabaceae), a native plant from Argentina has been used traditionally as medicinal species. The aim of the study was to validate the antibiotic and anti-inflammatory potential of organic extract (ZpE) and the major compounds; 2',4'-dihydroxy-3'-methoxychalcone (DHMC), 2',4'-dihydroxychalcone (DHC), 7-hydroxyflavanone (7-HF) and 3,7-dihydroxyflavone (DHF); using an model.
View Article and Find Full Text PDFSci Rep
August 2017
Institute of Experimental and Clinical Pharmacology, Medical University of Graz, Graz, Austria.
Levels of secretory phospholipases A (sPLA) highly increase under acute and chronic inflammatory conditions. sPLA is mainly associated with high-density lipoproteins (HDL) and generates bioactive lysophospholipids implicated in acute and chronic inflammatory processes. Unexpectedly, pharmacological inhibition of sPLA in patients with acute coronary syndrome was associated with an increased risk of myocardial infarction and stroke.
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