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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

allic Acid as a Non-Selective Inhibitor of alpha/beta-Hydrolase Fold Enzymes Involved in the Inflammatory Process: The Two Sides of the Same Coi

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Author(s):
Toyama, Marcos Hikari [1] ; Rogero, Airam [1] ; de Moraes, Laila Lucyane Ferreira [1] ; Fernandes, Gustavo Antonio [1] ; da Cruz Costa, Caroline Ramos [1, 2] ; Belchor, Mariana Novo [1, 2] ; De Carli, Agatha Manzi [1] ; de Oliveira, Marcos Antonio [1]
Total Authors: 8
Affiliation:
[1] Sao Paulo State Univ UNESP, Biosci Inst, BIOMOLPEP Grp, BR-11330900 Sao Vicente, SP - Brazil
[2] Fed Univ ABC, Postgrad Program Biotechnosci, BR-09210580 Santo Andre, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: HARMACEUTIC; v. 14, n. 2 FEB 2022.
Web of Science Citations: 0
Abstract

(1) Background: Gallic acid (GA) has been characterized as an effective anti-inflammatory, antivenom, and promising drug for therapeutic use. (2/3) Methods and Results: GA was identified from ethanolic extract of fresh pitanga (Eugenia uniflora) leaves, which was identified using commercial GA. Commercial GA neutralized the enzymatic activity of secretory PLA2 (sPLA2) by inhibiting the active site and inducing changes in the secondary structure of the enzyme. Pharmacological edema assays showed that GA strongly decreased edema when the compound was previously incubated with sPLA2. However, prior treatment of GA (30 min before) significantly increased the edema and myotoxicity induced by sPLA2. The molecular docking results of GA with platelet-acetylhydrolase (PAF-AH) and acetylcholinesterase reveal that this compound was able to interact with the active site of both molecules, inhibiting the hydrolysis of platelet-activating factor (PAF) and acetylcholine (ACh). (4) Conclusion: GA has a great potential application; however, our results show that this compound can also induce adverse effects in previously treated animals. Additionally, the increased edema and myotoxicity observed experimentally in GA-treated animals may be due to the inhibition of PAF-AH and Acetylcholinesterase. (AU)

FAPESP's process: 20/03297-8 - Screening and bioprospecting of anti-inflammatory compounds in plants Phyllanthus niruri, Eugenia uniflora, Schinus terebinthifolius and Jatropha gossypiifolia bioguided by bioaffinity on the sPLA2 of Crotalus durissus terrificus
Grantee:Gustavo Antonio Fernandes
Support Opportunities: Scholarships in Brazil - Scientific Initiation
FAPESP's process: 17/19942-7 - Search for inhibitors of the peroxirredoxin system from pathogens and humans
Grantee:Marcos Antonio de Oliveira
Support Opportunities: Regular Research Grants
FAPESP's process: 17/20291-0 - Characterization of the proinflammatory activity of a new serine protease (cdtsp-2) purified from the total venom of Crotalus durissus terrificus
Grantee:Marcos Hikari Toyama
Support Opportunities: Regular Research Grants