Teprenone ameliorates diclofenac-induced small intestinal injury via inhibiting protease activated receptors 1 and 2 activity

OBJECTIVE: This study aimed to investigate specific protein expression of injured intestinal mucosa induced by diclofenac, and explore the protective effects of teprenone on it.

METHODS: Intestinal damage of Sprague Dawley male rats was gradually induced by the intragastric administration of diclofenac. After the last drug administration, the intestinal mucosa was taken off with an interval of 24 h, subsequently, its general histological injury and ultrastructure were observed and analysed by a transmission electron microscope. The expression levels of PAR1 and PAR2 protein were detected by immunohistochemistry and real-time polymerase chain reaction (PCR).

RESULTS: The Reuter and Chiu scores of small intestinal damage were 5.63 ± 1.30 and 4.25 ± 0.70 respectively in the model group, which could be protected by teprenone (100 mg/kg⋅day) with the degree of 55.7% and 44%. Optical microscopy and transmission electron microscope showed that intestinal mucosa and ultrastructure were severely damaged. Distributed in the cytoplasm or aligned with the nucleus, the expression of PAR1 and PAR2 was significantly upregulated after the administration of diclofenac, while it was relieved after the treatment of teprenone.

CONCLUSION: Our study presents a new view that teprenone might protect NSAIDs-induced (diclofenac) intestinal injury via suppressing the expression of PAR1 and PAR2.

Medienart:

E-Artikel

Erscheinungsjahr:

2021

Erschienen:

2021

Enthalten in:

Zur Gesamtaufnahme - volume:26

Enthalten in:

Biomarkers : biochemical indicators of exposure, response, and susceptibility to chemicals - 26(2021), 1 vom: 03. Feb., Seite 38-44

Sprache:

Englisch

Beteiligte Personen:

Chao, Guanqun [VerfasserIn]
Wang, Zhaojun [VerfasserIn]
Yang, Chaoyu [VerfasserIn]
Qian, Yanna [VerfasserIn]
Zhang, Shuo [VerfasserIn]

Links:

Volltext

Themen:

144O8QL0L1
Anti-Inflammatory Agents, Non-Steroidal
Diclofenac
Diterpenes
EC 2.7.11.1
F2r protein, rat
Geranylgeranylacetone
Journal Article
PAR1
PAR2
Protein Serine-Threonine Kinases
Receptor, PAR-2
S8S8451A4O
Small intestinal injury
Teprenone

Anmerkungen:

Date Completed 15.10.2021

Date Revised 04.12.2021

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/1354750X.2020.1849405

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM317441000