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Andrographolide derivative as STAT3 inhibitor that protects acute liver damage in mice
Chen, Shao-Ru1; Li, Feng2; Ding, Mo-Yu1; Wang, Decai2; Zhao, Qi3; Wang, Yitao1; Zhou, Guo-Chun2; Wang, Ying1
2018-10
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
Volume26Issue:18Pages:5053-5061
Abstract

Sustained activation of the Janus kinase-signal transducers and activators of transcription (JAK-STAT) pathway contributed to the progression of cancer and liver diseases. STAT3 signaling inhibitor has been extensively investigated for pharmacological use. We synthesized a series of andrographolide derivatives, and characterized their activity against STAT3 signaling pathway both in vitro and in the CCl4-induced acute liver damage mice model. Among these derivatives, compound 24 effectively inhibited phosphorylation and dimerization of STAT3 but not its DNA binding activity. Compound 24 significantly ameliorated carbon tetrachloride-induced acute liver damage in vivo without changing mice body weight. Treatment with 24 attenuated hepatic pathologic damage and promoted hepatic proliferation and activation of STAT3. Compound 24 inhibited elevated expression of alpha-smooth muscle actin and serum pro-inflammatory cytokines downstream of STAT3 but not those factors that are regulated by NF-kappa B or SMADs. In summary, our results suggest that compound 24 may serve as a potential therapeutic agent for the treatment of hepatic damage or a liver protection agent via regulating STAT3 activation.

KeywordAndrographolide Stat3 Inhibitor Acute Liver Damage Inflammation
DOIhttp://doi.org/10.1016/j.bmc.2018.09.002
URLView the original
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000446669400010
PublisherPERGAMON-ELSEVIER SCIENCE LTD
The Source to ArticleWOS
Citation statistics
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorZhou, Guo-Chun; Wang, Ying
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, Macao SAR, China
2.School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing, Jiangsu 211816, China
3.Faculty of Health Sciences, University of Macau, Avenida da Universidade, Taipa, Macao SAR, China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Chen, Shao-Ru,Li, Feng,Ding, Mo-Yu,et al. Andrographolide derivative as STAT3 inhibitor that protects acute liver damage in mice[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2018,26(18):5053-5061.
APA Chen, Shao-Ru.,Li, Feng.,Ding, Mo-Yu.,Wang, Decai.,Zhao, Qi.,...&Wang, Ying.(2018).Andrographolide derivative as STAT3 inhibitor that protects acute liver damage in mice.BIOORGANIC & MEDICINAL CHEMISTRY,26(18),5053-5061.
MLA Chen, Shao-Ru,et al."Andrographolide derivative as STAT3 inhibitor that protects acute liver damage in mice".BIOORGANIC & MEDICINAL CHEMISTRY 26.18(2018):5053-5061.
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