Protective Effect of A2B Receptor Antagonist (TRP 1) on Acetic Acid Induced Ulcerative Colitis in Rats: in vitro, in vivo and in silico Methods (Record no. 9787)

MARC details
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fixed length control field a
003 - CONTROL NUMBER IDENTIFIER
control field OSt
005 - DATE AND TIME OF LATEST TRANSACTION
control field 20191019122054.0
008 - FIXED-LENGTH DATA ELEMENTS--GENERAL INFORMATION
fixed length control field 191019b xxu||||| |||| 00| 0 eng d
040 ## - CATALOGING SOURCE
Original cataloging agency AIKTC-KRRC
Transcribing agency AIKTC-KRRC
100 ## - MAIN ENTRY--PERSONAL NAME
9 (RLIN) 9995
Author Pasala, Praveen Kumar
245 ## - TITLE STATEMENT
Title Protective Effect of A2B Receptor Antagonist (TRP 1) on Acetic Acid Induced Ulcerative Colitis in Rats: in vitro, in vivo and in silico Methods
250 ## - EDITION STATEMENT
Volume, Issue number Vol.52(1), Jan-Mar
260 ## - PUBLICATION, DISTRIBUTION, ETC.
Place of publication, distribution, etc. Karnataka
Name of publisher, distributor, etc. Indian journal of pharmaceutical education and research
Year 2018
300 ## - PHYSICAL DESCRIPTION
Pagination 101-109p.
520 ## - SUMMARY, ETC.
Summary, etc. Aim: Present study was elucidate the protective effect of pyridinone derivatives such as 7-amino-5-oxo-2- Phenyl-5H, 8H-dihydro-[1, 2, 4] triazolo [1, 5-α] pyridine - 6- carbonitril (TRP 1) by in vitro, in vivo and in silico.Methods: Radioligand binding assay was performed on human adenosine receptors (A2B) and assess A2B antagonist effect by adenylyl cyclase activity. In vitro study was carried out to determine the neutralize capacity against DPPH*, NO*, SO*, LPO* free radicals. TRP 1 at the doses 1 mg/kg bd.wt. and 10 mg/kg bd.wt p.o, was administered consecutively for 14 days in albino rats. Ulcerative colitis was induced with single dose of 2 ml of 3% acetic acid intrarectal on 14th day in treated rats. At the end of treatment, colonic tissue was collected and subjected for estimation of macroscopic score, glutathione, catalase, MPO and inflammatory parameters such as IL 1β, TNF α and IL 6. In silico study was carried out to evaluate the binding energy and IC50 toward IL 1β, TNF α and IL 6. Results: TRP 1 was antagonized the A2B receptors at the concentration of 30000 nM. In vitro study was revealed that TRP1 (1 mg/ml) was significantly neutralizes the free radicals of DPPH*, SO*, NO*and LPO*. In in vivo studies, intrarectal administration of acetic acid caused significantly (***P<0.001) increased macroscopic score, colon weight, colonic MPO, IL 6, IL 1β and TNF-α (*P<0.05), while TRP 1 treated colitis rats antioxidants system such as GSH (**P<0.01), catalase (*P<0.05) activity was significantly improved, decreases inflammatory mediators such TNF α (*P<0.05), IL 1β (**P<0.01) , IL 6 (**P< 0.01) and also suppresses the MPO activity (*P<0.05). In silico study was reported that the IC50 of TPR 1 against IL 1β, IL 6 and TNF-α was 7.5 mM, 28.65 mM and 45.87 mM respectively. Conclusion: Our data demonstrated thatthe TRP 1 treatment improved clinical score in acetic acid induced colitis in rats. It also inhibited the proinflammatory cytokine IL-6, IL 1β and TNF α and improvements of antioxidant in colitis rats through A2B receptor antagonist property.
650 #0 - SUBJECT ADDED ENTRY--TOPICAL TERM
9 (RLIN) 4639
Topical term or geographic name entry element PHARMACEUTICS
700 ## - ADDED ENTRY--PERSONAL NAME
9 (RLIN) 9996
Co-Author Alluri, Ramesh
773 0# - HOST ITEM ENTRY
Place, publisher, and date of publication Bengluru Association of Pharmaceutical Teachers of India (APTI)
Title Indian journal of pharmaceutical education and research
International Standard Serial Number 0019-5464
856 ## - ELECTRONIC LOCATION AND ACCESS
URL https://www.ijper.org/sites/default/files/IndJPhaEdRes_52_1_101.pdf
Link text Click here
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    Dewey Decimal Classification     School of Pharmacy School of Pharmacy Archieval Section 19/10/2019   2019940 19/10/2019 19/10/2019 Articles Abstract Database
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