Entecavir as a P2X7R antagonist ameliorates platelet activation and thrombus formation.

Animals Antioxidants Bleeding Time Blood Coagulation / drug effects Cytoprotection / drug effects Disease Models, Animal Guanine / analogs & derivatives Humans Lipid Peroxidation / drug effects Male Mice, Inbred C57BL Molecular Docking Simulation Platelet Activation / drug effects Platelet Aggregation / drug effects Purinergic P2X Receptor Antagonists / pharmacology Receptors, Purinergic P2X7 Thrombosis / blood
Entecavir Mitochondria Oxidative stress P2X7 receptor Platelet

Journal

Journal of pharmacological sciences
ISSN: 1347-8648
Titre abrégé: J Pharmacol Sci
Pays: Japan
ID NLM: 101167001

Informations de publication

Date de publication:
Sep 2020
Historique:
received: 06 11 2019
revised: 24 06 2020
accepted: 29 06 2020
pubmed: 13 7 2020
medline: 30 10 2020
entrez: 13 7 2020
Statut: ppublish

Résumé

Platelet activation is the primary cause of thrombosis. The P2X7 receptor (P2X7R) is a therapeutic target of thrombosis. However, it is still unknown whether P2X7R activation affects platelet thrombus. Our molecular docking results showed that entecavir as a P2X7R antagonist interacted perfectly with the human P2X7R (hP2X7R) in silico simulation studies. Furthermore, our experimental data revealed that entecavir could act as a P2X7R antagonist to exert cytoprotective effects against platelet activation via protecting mitochondrial function, improving lipid peroxidation and increasing antioxidant activity. Correlated with this, entecavir inhibited platelet aggregation, dense-granule secretion, P-selectin expression, integrin activation and Ca

Identifiants

DOI: 10.1016/j.jphs.2020.07.002 PMID: 32653340
pubmed: 32653340
pii: S1347-8613(20)30066-9
doi: 10.1016/j.jphs.2020.07.002
pii:
doi:

Substances chimiques

Antioxidants 0
Purinergic P2X Receptor Antagonists 0
Receptors, Purinergic P2X7 0
entecavir 5968Y6H45M
Guanine 5Z93L87A1R

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

43-51

Informations de copyright

Copyright © 2020 The Authors. Production and hosting by Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest No conflicts of interest to declare.

Auteurs

Yue Ming (Y)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Guang Xin (G)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Beihong Ji (B)

Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pennsylvania, United States.

Chengji Ji (C)

Clinical Laboratory, Hospital of University of Electronic Science and Technology of China and Sichuan Provincial People's Hospital, Chengdu, Sichuan, China.

Zeliang Wei (Z)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Boli Zhang (B)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China; Tianjin University of Traditional Chinese Medicine, Tianjin, China.

Junhua Zhang (J)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China; Tianjin University of Traditional Chinese Medicine, Tianjin, China.

Kui Yu (K)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Xiaoyu Zhang (X)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Shiyi Li (S)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Youping Li (Y)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Zhihua Xing (Z)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Hai Niu (H)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China. Electronic address: niuhai@scu.edu.cn.

Wen Huang (W)

Laboratory of Ethnopharmacology, West China School of Medicine, West China Hospital, Sichuan University, Chengdu, Sichuan, China. Electronic address: huangwen@scu.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Agents protecteurs › Antioxydants › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Temps de saignement › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Hémostase › Coagulation sanguine › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Cytoprotection › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles biologiques › Modèles animaux de maladie humaine › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Purines › Purinones › Hypoxanthines › Guanine › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Métabolisme › Métabolisme énergétique › Oxydoréduction › Peroxydation lipidique › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Hémostase › Activation plaquettaire › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Hémostase › Activation plaquettaire › Agrégation plaquettaire › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents purinergiques › Antagonistes purinergiques › Antagonistes des récepteurs purinergiques P2 › Antagonistes des récepteurs purinergiques P2X › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs purinergiques › Récepteurs purinergiques P2 › Récepteurs purinergiques P2X › Récepteurs purinergiques P2X7 › Entecavir as a P2X7R antagonist ameliorates...
questionsmedicales.fr › Maladies cardiovasculaires › Maladies vasculaires › Embolie et thrombose › Thrombose › Entecavir as a P2X7R antagonist ameliorates...