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Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity
Li, Feng1; Li, Xiao-Min2; Sheng, Dekuan1; Chen, Shao-Ru2; Nie, Xin1; Liu, Zhuyun1; Wang, Decai1; Zhao, Qi3; Wang, Yitao2; Wang, Ying2; Zhou, Guo-Chun1
2018
Source PublicationRSC ADVANCES
ISSN2046-2069
Volume8Issue:17Pages: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-(8'-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 14 beta-(8'-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 INF-alpha/NF-kappa B signaling pathway, whereas 8b1 is selectively active against the TLR4/NE-kappa B signaling pathway; moreover, the compounds 6b17 and 9b are active in inhibiting the IL-6/STAT3, TLR4/NF-kappa B, and TNE-alpha/NE-kappa B 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.

DOIhttp://doi.org/10.1039/c8ra01063c
URLView the original
Indexed BySCI
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000431972600050
PublisherROYAL SOC CHEMISTRY
The Source to ArticleWOS
Fulltext Access
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Institute of Chinese Medical Sciences
Corresponding AuthorWang, Ying; Zhou, Guo-Chun
Affiliation1.School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, PR China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, Macao SAR, PR China
3.Faculty of Health Sciences, University of Macau, Avenida da Universidade, Taipa, Macao SAR, PR China
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Li, Feng,Li, Xiao-Min,Sheng, Dekuan,et al. Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity[J]. RSC ADVANCES,2018,8(17):9440-9456.
APA Li, Feng.,Li, Xiao-Min.,Sheng, Dekuan.,Chen, Shao-Ru.,Nie, Xin.,...&Zhou, Guo-Chun.(2018).Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity.RSC ADVANCES,8(17),9440-9456.
MLA Li, Feng,et al."Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity".RSC ADVANCES 8.17(2018):9440-9456.
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