Affiliation:
1. School of Bio-Science & Technology, VIT University, Vellore-632014, India
2. School of Chemical Engineering, Yeungnam University, Gyeongsan, 38541, Korea
3. School of Advanced Sciences, VIT University, Vellore, India
Abstract
Background:
Macrophages play a serious part in the instigation, upkeep, and
resolution of inflammation. They are activated or deactivated during inflammation progression.
Activation signals include cytokines (IF-γ, granulocyte-monocyte colonystimulating
factor (GM-CSF), and TNF-α), extracellular matrix proteins, and other chemical
mediators. Activated macrophages are deactivated by anti-inflammatory cytokines (IL-
10 and TGF-β (transforming growth factor-beta) and cytokine antagonists that are mainly
produced by macrophages. Based on this, the present study aimed to develop novel (E)-
Benzylidene-indazolpyridin methanones (Cpd-1-10) as effective anti-inflammatory agents
by analyzing pro- and anti-inflammatory cytokine levels in macrophages.
Objectives:
To determine the anti-inflammatory effect of indazolpyridin-methanones by
examining pro- and anti-inflammatory interleukin levels in J77A.1 macrophages.
Methods:
Expression of cytokines such as TNF-α, IL-1β, IL-6 and IL-10 serum levels
measured by ELISA method. Anti-cancer and cytotoxicity studies were carried out by
MTT assay. COX-2 seems to be associated with cancers and atypical developments in the
duodenal tract. So, 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:
Cytotoxicity effect of the compounds against breast cancer cell lines found
excellent and an extended anticancer study ensured that these compounds are also alternative
therapeutic agents against breast cancer. Among all the tested cancer cell lines, the anti-
cancer effect on breast cancer was exceptional for the most active compounds Cpd5 and
Cpd9.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,General Medicine,Immunology,Immunology and Allergy
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