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Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice
Bao-Jian Guo1,3; Zhuyun Liu2,4; Mo-Yu Ding1; Feng Li2; Mei Jing3; Li-Peng Xu3; Yu-Qiang Wang3; Zai-Jun Zhang3; Yitao Wang1; Decai Wang2; Guo-Chun Zhou2; Ying Wang1
2019-05
Source PublicationBIOCHEMICAL PHARMACOLOGY
ISSN0006-2952
Volume163Pages:416-424
Abstract

The therapeutic efficacy of immunosuppressive agents has been intensively studied for colitis management. We synthesized a series of andrographolide derivatives and reported their structure-activity-relationship and anti-inflammatory activity in our previous studies. Among these derivatives, compound 3b exhibited the most potent immunosuppressive activity. In the present study, we assessed the efficacy of 3b in dextran sulfate sodium (DSS)-induced model of acute colitis. Compound 3b was administered intragastrically. The therapeutic effect of 3b was evaluated using disease score and immune cell infiltration. The effect of 3b on Toll-like receptor 4/NF-κB and β-catenin signaling was primarily determined by using immunohistochemistry staining and quantitative real-time PCR. The crosstalk between NF-κB and β-catenin signaling was then assessed in HCT-116 cells. Treatment with 3b significantly downregulated the disease activity index and suppressed the histologic evidence of inflammation in DSS-induced model of acute colitis. Compound 3b inhibited proinflammatory cytokine expression at both the serum and transcription levels. Treatment with 3b also upregulated the number of PCNA-positive and goblet cells in the intestinal crypt and the intestinal expression of mRNA levels of β-catenin target genes. β-Catenin level regulation affected the antiinflammation and anti-apoptotic activities of 3b. This study demonstrated that 3b, a novel andrographolide derivative, suppressed inflammation and significantly reversed colitis pathology. The outcome of colitis treatment with an immunosuppressive agent depends upon the intestinal expression and mutation status of β-catenin.

KeywordAndrographolide Analog Colitis Ibd Nf-κb Β-catenin
DOIhttps://doi.org/10.1016/j.bcp.2019.03.019
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000466060000040
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorGuo-Chun Zhou; Ying Wang
Affiliation1.Institute of Chinese Medical Sciences and State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Avenida da Universidade, Taipa, Macao
2.School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing, Jiangsu 211816, China
3.Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou 510632, China
4.School of Pharmacy, Taizhou Polytechnic College, Taizhou 225300, Jiangsu, China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Bao-Jian Guo,Zhuyun Liu,Mo-Yu Ding,et al. Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice[J]. BIOCHEMICAL PHARMACOLOGY,2019,163:416-424.
APA Bao-Jian Guo.,Zhuyun Liu.,Mo-Yu Ding.,Feng Li.,Mei Jing.,...&Ying Wang.(2019).Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice.BIOCHEMICAL PHARMACOLOGY,163,416-424.
MLA Bao-Jian Guo,et al."Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice".BIOCHEMICAL PHARMACOLOGY 163(2019):416-424.
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