Inflammation is a complex pathological condition associated with exaggerated human immune system involving various activated immune cells and bio-molecules. Treatment of inflammatory diseases particularly chronic inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease etc. has been a big challenge for scientists as there are no safe drugs available for cure. Current therapeutic approaches to the treatment of inflammatory diseases are centered on cycloxygenase (both COX-1 and 2) proinflammatory enzymes but present available drugs of this category are associated with undesirable gastrointestinal and cardiovascular side effects. Recent scientific advents draw out the secrets of inflammation cache and understanding the involvement of several factors acting as stimulators or inhibitors thus opening new avenues for drug discoveries. Several bio-molecules such as proinflammatory cytokines, components of signal transduction and matrix degrading enzymes resolve inflammatory responses, might be new targets for treatment of chronic inflammatory diseases. This review gathers recent advances in drug research focusing interleukin-1, TNF-alpha, p38 kinase, c-Jun N-terminal kinase MAP kinase, NFkappaB, and matrix metalloproteinases. The biological roles of these inflammatory mediators are clearly understood thus offering new targets for design of novel inhibitors for incurable inflammatory diseases. This also provides an overview of the current nonsteroidal antiinflammatory agents.

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Objectives: The aim of this study is to evaluate and compare the antibacterial efficacy of Thymus vulgaris, Salvadora persica, Acacia nilotica, Calendula arvensis , and 5% sodium hypochlorite against Enterococcus faecalis . Methodology: Herbal extracts of T. vulgaris, S. persica, A. nilotica and C. arvensis were prepared. Tryptone soya broth was used to grow E. faecalis and agar plates were prepared. The tested solutions (Group A: 5% NaOCl, Group B: 20% T. vulgaris , Group C: 12.5% S. persica , Group D: 10% A. nilotica , Group E: 10% C. arvensis ) were added to the wells made on agar media. Agar diffusion test was performed. Plates were incubated at 37°C for 24 h. Bacterial zones of inhibition were recorded. Results: The data were analyzed statistically by Analysis of Variance (ANOVA) and post hoc comparison by Tukey's t -test. The highest zone of inhibition against E. faecalis was shown by 5% NaOCl, followed by 10% C. arvensis , 20% T. vulgaris and 10% A. nilotica showed similar comparable antibacterial activity. The least zone of inhibition was showed by S. persica. Conclusion: 5% NaOCl showed the maximum antibacterial activity, and herbal products demonstrated significant antibacterial activity against E. faecalis and can be employed as an alternative to NaOCl.

The p38 protein kinase is a serine-threonine mitogen activated protein kinase, which plays an important role in inflammation and arthritis. A combined study of 3D-QSAR and molecular docking has been undertaken to explore the structural insights of pyrazolyl urea p38 kinase inhibitors. The 3D-QSAR studies involved comparative molecular field analysis (CoMFA) and comparative molecular similarity indices (CoMSIA). The best CoMFA model was derived from the atom fit alignment with a cross-validated r (2 )(q (2)) value of 0.516 and conventional r (2) of 0.950, while the best CoMSIA model yielded a q (2) of 0.455 and r (2) of 0.979 (39 molecules in training set, 9 molecules in test set). The CoMFA and CoMSIA contour maps generated from these models provided inklings about the influence of interactive molecular fields in the space on the activity. GOLD, Sybyl (FlexX) and AutoDock docking protocols were exercised to explore the protein-inhibitor interactions. The integration of 3D-QSAR and molecular docking has proffered essential structural features of pyrazolyl urea inhibitors and also strategies to design new potent analogues with enhanced activity.

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