https://orcid.org/0000-0003-0609-9200
Abstract
Aim: Inducible nitric oxide synthase (iNOS) is a validated target for anti-inflammatory treatment. Based on the authors' previous work, novel aza-ursolic acid derivatives were designed and synthesized and their inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) release from RAW264.7 cells was evaluated. Materials & results: 16 novel derivatives were screened for their in vitro inhibitory activity against NO release using Griess assays and the cytotoxicity was evaluated using MTT assays. The presence of furoxan joined to the A-ring of ursolic acid and N-methylpiperazine groups in the lead compound was identified for anti-inflammatory activity, and compound 21b showed 94.96% inhibition of NO release at 100 μM with an IC50 value of 8.58 μM. Conclusion: Compound 21b has potential anti-inflammatory activity with low cytotoxicity that warrants further preclinical study and evaluation.
Graphical Abstract
Supplementary data
To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184
Author contributions
Q Meng and F Zhao are responsible for the research planning. M Luan, Y Xu, X Zhang, D Li and M Yan participated in experimental research. M Luan and Y Xu are responsible for thesis writing. G Hou and F Zhao are responsible for thesis revision.
Financial & competing interests disclosure
This work was financially supported by the Science and Technology Innovation Development Plan of Yantai (no. 2020XDRH105) and the National Natural Science Foundation of China (no. 81473104). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.