Abstract

Background: Inflammatory response is the body’s first-line defence mechanism in which the immune system recognises, counters the antigens, and aids in healing the disease. The World Health Organisation suggests that inflammation is one of the greatest causes of death in the world. Inflammation could be acute or chronic due to the release of inflammatory mediators, i.e. prostaglandins, leukotrienes due to mitogens, and antigens or cytokines found in the body.

Methods: The detailed studies and conceptual framework of dual COX/LOX inhibitors of natural origin have attracted great attention. A bibliographic database using PubMed cites for peer-reviewed research articles with titles containing dual COX-2 and 5-LOX enzyme inhibitors, heterocyclic moieties, with AND Boolean operator's terms for the last ten years was searched. The quality papers reviewing the natural or synthetic lead compounds were extracted.

Results: Out of 127 research and review articles evaluated, 54 articles were cited for providing high-quality data regarding the pharmacoactive molecules having anti-inflammatory activity via dual COX-2/5-LOX inhibition. In addition, in silico and experimental studies on dual COX/LOX inhibitors in increasing hierarchical order over the past decade were illustrated.

Conclusion: This review provides details of isolated bioactive compounds, such as pyrazole, coumaperine, indoles, and phenanthrene derivatives, that have been significantly reported for anti- inflammatory activities.

Keywords: Dual COX-2 and 5-LOX enzyme inhibitors, heterocyclic, in-vivo, in-silico, anti-inflammatory, pyrazole.

Graphical Abstract