Andrographolide Derivative as STAT3 Inhibitor to Treat Acute Liver Damage in Mice

UM > Institute of Chinese Medical Sciences

Status	已發表Published
	Andrographolide Derivative as STAT3 Inhibitor to Treat Acute Liver Damage in Mice
	Chen, S.R.; Li, F; Ding, M.Y.; Wang, D; Zhao, Q.; Wang, Y. T.; Zhou, G.C.; Wang, Y.
	2018-10-01
Source Publication	Bioorganic & Medicinal Chemistry
ISSN	0968-0896
Pages	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 α-smooth muscle actin and serum pro-inflammatory cytokines downstream of STAT3 but not those factors that are regulated by NF-κB 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.
Keyword	andrographolide STAT3 acute liver damage.
URL	View the original
Language	英語English
The Source to Article	PB_Publication
PUB ID	39719
Document Type	Journal article
Collection	Institute of Chinese Medical Sciences
Corresponding Author	Wang, Y.
Recommended Citation GB/T 7714	Chen, S.R.,Li, F,Ding, M.Y.,et al. Andrographolide Derivative as STAT3 Inhibitor to Treat Acute Liver Damage in Mice[J]. Bioorganic & Medicinal Chemistry, 2018, 5053-5061.
APA	Chen, S.R.., Li, F., Ding, M.Y.., Wang, D., Zhao, Q.., Wang, Y. T.., Zhou, G.C.., & Wang, Y. (2018). Andrographolide Derivative as STAT3 Inhibitor to Treat Acute Liver Damage in Mice. Bioorganic & Medicinal Chemistry, 5053-5061.
MLA	Chen, S.R.,et al."Andrographolide Derivative as STAT3 Inhibitor to Treat Acute Liver Damage in Mice".Bioorganic & Medicinal Chemistry (2018):5053-5061.

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