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Pro- and Anti-Inflammatory Cytokine Expression Levels in Macrophages; An Approach to Develop Indazolpyridin-Methanones as a Novel Inflammation Medication

Author(s):

Manikandan Alagumuthu, Vanshika Srivastava, Manisha Shah, Sivakumar Arumugam, Mohandoss Sonaimuthu and Napoleon Ayyakannu Arumugam *   Pages 1 - 11 ( 11 )

Abstract:


Background: Indented to develop novel (E)-Benzylidene-indazolpyridin methanones (Cpd-1-10) as effective anti-inflammatory agents, a molecular-based therapeutic investigation executed in order to measure the druggability possibilities of these compounds.

Objectives: To determine pro-inflammatory and anti-inflammatory interleukin levels in J77A.1 macrophages, the TNF-α, IL-1β, IL-6 and IL-10 serum levels measured by ELISA method.

Method: Their cytotoxicity effect against breast cancer cell lines found excellent and an extended anticancer study ensured that these compounds are also alternative therapeutic agents against breast cancer. In fact, COX-2 seems to be associated with cancers and atypical developments in the duodenal tract. A competitive ELISA based COX-2 inhibition assay was done. To validate the inhibitory potentials and to get more insight into the interaction of COX-2 with Cpd1-10, molecular docking was performed.

Results: Briefly, the COX-2 inhibitory relative activity was found to be in between the range of 80-92 % (Diclofenac showed 84 %, IC50 0.95 µM).

Conclusion: Among all the tested cancer cell lines, the anti-cancer effect on breast cancer was exceptional for the most active compounds Cpd5 and Cpd9.

Keywords:

Anti-inflammation, Benzylidene-indazolpyridin methanones, COX-2, Cytotoxicity, HRBC membrane stabilization

Affiliation:

School of Bio-Science & Technology, VIT University, Vellore-632014, School of Bio-Science & Technology, VIT University, Vellore-632014, School of Bio-Science & Technology, VIT University, Vellore-632014, School of Bio-Science & Technology, VIT University, Vellore-632014, Nano-biomedicine Lab, National Sun Yat-Sen University, Kaohsiung-80424, School Advanced Sciences, VIT University, Vellore



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