Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity

UM > Institute of Chinese Medical Sciences

Status	已發表Published
	Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity
	Li, F; Li, XM; Sheng, D; Chen, SR; Nie, X; Liu, Z; Wang, D; Wang, Y. T.; Zhao, Q.; Wang, Y.; Zhou, GC
	2018-03-01
Source Publication	RSC Advances
ISSN	2046-2069
Pages	9440-9456
Abstract	Antibacterials (which restore gut ﬂora balance) and immunosuppressants (which correct immune defects)are two important and eﬀective therapeutic agents for the treatment of inﬂammatory bowel disease (IBD) in clinical use today. Since the structural skeleton of andrographolide, isolated from Andrographis paniculata, has become known as a natural antibiotic with anti-inﬂammation and heat-clearing and detoxifying properties, 14-aryloxy andrographolide derivatives have been designed, synthesized, and tested for their antibacterial eﬀects on E. coli S. aureus, and E. faecalis, which are related to IBD. It has been discovered , in this study that the andrographolide skeleton is more selective against E. faecalis, the 14-aryloxy group with basicity is important for antibacterial functions, and the 14-(80-quinolinyloxy) group is a good pharmacophore with antibacterial activity. In addition, we found that 7b1 and 8b1 are good and selective inhibitors of E. faecalis; two 14b-(80-quinolinyloxy) andrographolide derivatives, 6b17 and 9b, exhibit good activity against E. coli, S. aureus, and E. faecalis. Likewise and importantly, further exploration of immunosuppressant activity for IBD shows that compound 7b1 is a selective inhibitor of the TNF-a/NF- kB signaling pathway, whereas 8b1 is selectively active against the TLR4/NF-kB signaling pathway;moreover, the compounds 6b17 and 9b are active in inhibiting the IL-6/STAT3, TLR4/NF-kB, and TNF-a/ NF-kB signaling pathways. Based on these results, we have further focused on the development of dual function inhibitors of IBD as antibacterial and immunosuppressant agents by structural modiﬁcation of andrographolide.
Keyword	SAR andrographolide antibacterial agents immunosuppressant activity.
Language	英語English
The Source to Article	PB_Publication
PUB ID	35804
Document Type	Journal article
Collection	Institute of Chinese Medical Sciences
Corresponding Author	Wang, Y.; Zhou, GC
Recommended Citation GB/T 7714	Li, F,Li, XM,Sheng, D,et al. Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity[J]. RSC Advances, 2018, 9440-9456.
APA	Li, F., Li, XM., Sheng, D., Chen, SR., Nie, X., Liu, Z., Wang, D., Wang, Y. T.., Zhao, Q.., Wang, Y.., & Zhou, GC (2018). Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity. RSC Advances, 9440-9456.
MLA	Li, F,et al."Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity".RSC Advances (2018):9440-9456.

Files in This Item:
There are no files associated with this item.

If you have any objections to this item, please fill out the form below and the administrator will contact you as soon as possible.
Content:
Email：	*
Affiliation No.
Verification Code:	Refresh

Any comments and suggestions are welcomed.
Title:	*
Content:
Email：	*
Verification Code:	Refresh