• Krishna Chaithanya K. Department of Chemistry, College of Natural and Computational Sciences, Aksum University, Axum, Ethiopia
  • Gopalakrishnan V. K. Department of Chemistry, College of Natural and Computational Sciences, Aksum University, Axum, Ethiopia
  • Zenebe Hagos Department of Chemistry, College of Natural and Computational Sciences, Aksum University, Axum, Ethiopia
  • Govinda Rao D. Department of Biochemistry and Molecular Biology, School of Biological Sciences, Central University of Kerala, India


Objective: The main objective of the present study was to evaluate the anti-inflammatory activity of isolated bioactive flavonoid Mesuaferrin-A from the bark of Mesuaferrea L. by in vitro, in vivo and in silico approach.

Methods: To evaluate the effect of isolated bioactive flavonoid Mesuaferrin-A on arachidonic acid metabolizing enzymes (PLA2, COX-2 and 5-LOX) using in vitro methods, followed by carrageenan-induced paw edema model by in vivo and to determine the binding orientation and interactions of Mesuaferrin-A onarachidonic acid metabolizing enzymes (PLA2, COX-2 and 5-LOX) crystal proteins using molecular docking (in silico) studies.

Results: Mesuaferrin-A exhibited a dose-dependent significant 5-LOX inhibitory and considerable COX-2 inhibitory activity by in vitro, The inhibitory activities of 5-LOX and COX-2 at 100µg/ml were found to be 78.67%, 81.03% with IC50 values of 45.22µg/ml and 35.74µg/ml respectively. Whereas Mesuaferrin-A showed less PLA2 inhibitory activity. Mesuaferrin-A showed 68.34% inhibitory activity at 400 mg/kg body weight at the late phase of carrageenan-induced paw edema, and In silico studies demonstrated that Mesuaferrin-A strongly binds with 5-LOX and COX-2, these strong binding affinity of Mesuaferrin-A on active site amino acids of 5-LOX and COX-2 may be responsible for inhibition of enzyme activity. Mesuaferrin-A showeda comparable 5-LOX and COX-2 inhibition activity with (positive control).

Conclusion: It was concluded that Mesuaferrin-A act as 5-LOX and COX dual inhibitor, from the results it was suggests that Mesuaferrin-A, may be an effective preventive and therapeutic approach for patients with inflammatory-related diseases.

Keywords: Mesuaferrin-A, Phospholipase-A2(PLA2), 5-Lipooxygenase (5-LOX), Cyclooxygenase-2 (COX-2), Generic Evolutionary Method for molecular Docking (GEM Dock)


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How to Cite
K., K. C., G. V. K., Z. Hagos, and G. R. D. “MESUAFERRIN A-BIOACTIVE FLAVONOID ISOLATED FROM THE BARK OF MESUA FERREA L. AGAINST PHOSPHOLIPASE A2, CYCLOOXYGENASE AND LIPOXYGENASE: AN IN VITRO, IN VIVO AND IN SILICO APPROACH”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 10, no. 2, Feb. 2018, pp. 102-6, doi:10.22159/ijpps.2018v10i2.23576.
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