Canthin-6-one ameliorates TNBS-induced colitis in rats by modulating inflammation and oxidative stress. An in vivo and in silico approach

doi:10.1016/j.bcp.2021.114490

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	Canthin-6-one ameliorates TNBS-induced colitis in rats by modulating inflammation and oxidative stress. An in vivo and in silico approach
	Arunachalam,Karuppusamy ; Damazo,Amilcar Sabino ; Macho,Antonio ; Matchado,Monica Steffi ; Pavan,Eduarda ; Figueiredo,Fabiana de Freitas ; Oliveira,Darley Maria ; Duckworth,Carrie A.; Thangaraj,Parimelazhagan ; Leonti,Marco ; de Oliveira Martins,Domingos Tabajara
	2021
发表期刊	BIOCHEMICAL PHARMACOLOGY
ISSN	0006-2952
卷号	186 页码:114490
摘要	Canthin-6-one (Cant) is an indole alkaloid found in several botanical drugs used as medicines, reported to be gastroprotective, anti-inflammatory, anti-microbial, anti-diarrheal and anti-proliferative. We aimed to explore Cant in the management of colitis using a trinitrobenzenesulfonic acid (TNBS)-induced rat model. Cant (1, 5 and 25 mg/kg) was administered by oral gavage to Wistar rats followed by induction of colitis with TNBS. Macroscopic and histopathological scores, myeloperoxidase (MPO), malondialdehyde (MDA) and reduced glutathione (GSH) were assessed in colon tissues. Pro- (TNF-?, IL-1(i and IL-12p70) and anti-inflammatory (IL-10) cytokines, and vascular endothelial growth factor (VEGF) were also quantified. Mitogen-activated protein kinase 14 (MAPK14) and Toll-like receptor-8 (TLR8), as putative targets, were considered through in silico analysis. Cant (5 and 25 mg/kg) reduced macroscopic and histological colon damage scores in TNBS-treated rats. MPO and MDA were reduced by up to 61.69% and 92.45%, respectively, compared to TNBS-treated rats alone. Glutathione concentration was reduced in rats administered with TNBS alone (50.00% of sham group) but restored to 72.73% (of sham group) with Cant treatment. TNF-?, IL-1(i, IL-12p70 and VEGF were reduced, and anti-inflammatory IL10 was increased following Cant administration compared to rats administered TNBS alone. Docking ligation results for MAPK14 (p38?) and TLR8 with Cant, confirmed that these proteins are feasible putative targets. Cant has an anti-inflammatory effect in the intestine by down-regulating molecular immune mediators and decreasing oxidative stress. Therefore, Cant could have therapeutic potential for the treatment of inflammatory bowel disease and related syndromes.
关键词	Canthin-6-one Inflammatory bowel disease TNBS Cytokines Colitis BOWEL-DISEASE PROINFLAMMATORY CYTOKINES CLINICAL-ASPECTS ACTIVITY SPECTRA PATHOGENESIS DOCKING CELLS ACCUMULATION PREDICTION MODEL
DOI	10.1016/j.bcp.2021.114490
WOS记录号	WOS:000640413600003
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73790
专题	中国科学院昆明植物研究所
作者单位	1.Univ Fed Mato Grosso UFMT, Fac Med, Dept Ciencias Basicas Saude, Area Farmacol, Av Fernando Correa da Costa 2367, BR-78060900 Cuiaba, MT, Brazil 2.Chinese Acad Sci, Kunming Inst Bot, Key Lab Econ Plants & Biotechnol, Kunming 650201, Yunnan, Peoples R China 3.Chinese Acad Sci, Kunming Inst Bot, Yunnan Key Lab Wild Plant Resources, Kunming 650201, Yunnan, Peoples R China 4.Univ Fed Mato Grosso UFMT, Fac Med, Dept Ciencias Basicas Saude, Area Histol & Biol Celular, Cuiaba, MT, Brazil 5.Univ Brasilia UnB, Fac Med, Programa Posgrad Ciencias Med, Brasilia, DF, Brazil 6.Ganga Orthopaed Res & Educ Fdn GOREF, Coimbatore, Tamil Nadu, India 7.Univ Fed Mato Grosso UFMT, Fac Med, Inst Ciencias Saude, Campus Sinop, MT, Brazil 8.Duckworth, Carrie A.] Univ Liverpool, Inst Syst, Dept Mol Physiol & Cell Signalling, Liverpool, Merseyside, England 9.Bharathiar Univ, Sch Life Sci, Dept Bot, Coimbatore, Tamil Nadu, India 10.Univ Cagliari, Dept Biomed Sci, I-09042 Monserrato, CA, Italy
推荐引用方式 GB/T 7714	Arunachalam,Karuppusamy,Damazo,Amilcar Sabino,Macho,Antonio,et al. Canthin-6-one ameliorates TNBS-induced colitis in rats by modulating inflammation and oxidative stress. An in vivo and in silico approach[J]. BIOCHEMICAL PHARMACOLOGY,2021,186:114490.
APA	Arunachalam,Karuppusamy.,Damazo,Amilcar Sabino.,Macho,Antonio.,Matchado,Monica Steffi.,Pavan,Eduarda.,...&de Oliveira Martins,Domingos Tabajara.(2021).Canthin-6-one ameliorates TNBS-induced colitis in rats by modulating inflammation and oxidative stress. An in vivo and in silico approach.BIOCHEMICAL PHARMACOLOGY,186,114490.
MLA	Arunachalam,Karuppusamy,et al."Canthin-6-one ameliorates TNBS-induced colitis in rats by modulating inflammation and oxidative stress. An in vivo and in silico approach".BIOCHEMICAL PHARMACOLOGY 186(2021):114490.