Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Celastrol attenuates fMLP-induced superoxide anion generation, myeloperoxidase production, and elastase release by human neutrophils

Nipapan Malisorn , Ammara Chaikan

Division of Pharmacology, Preclinical Sciences, Faculty of Medicine, Thammasat University, Pathumthani, Thailand;

For correspondence:- Nipapan Malisorn Email: dr.nipapan@gmail.com Tel:+6629269716

Accepted: 19 August 2019 Published: 30 September 2019

Citation: Malisorn N, Chaikan A. Celastrol attenuates fMLP-induced superoxide anion generation, myeloperoxidase production, and elastase release by human neutrophils. Trop J Pharm Res 2019; 18(9):1805-1809 doi: 10.4314/tjpr.v18i9.3

© 2019 The authors.
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Abstract

Purpose: To investigate the anti-inflammatory effect of celastrol via attenuation of formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation, myeloperoxidase production, and elastase release by peripheral blood neutrophils.

Methods: Cytotoxicity of celastrol on human peripheral blood neutrophils was investigated using a 2H-tetrazolium hydroxide (XTT) assay. Human neutrophils were stimulated with 100-nM fMLP; the effect of celastrol on superoxide generation was determined via ferricytochrome C reduction, the effect on myeloperoxidase production by tetramethylbenzidine oxidation, and the effect on elastase activity by Boc-Ala-ONp hydrolysis.

Results: Treatment of human neutrophils with celastrol showed dose-dependent inhibition of fMLP-induced superoxide generation, myeloperoxidase production, and elastase release with half-maximal inhibitory concentration (IC₅₀) values of 5.9 ± 0.1, 1.9 ± 0.2, and 1.5 ± 0.1 µM, respectively.

Conclusion: These results indicate that celastrol possesses anti-inflammatory properties via attenuation of fMLP-induced superoxide generation, myeloperoxidase production, and elastase release by peripheral blood neutrophils.

Keywords: Celastrol, Anti-inflammatory, Superoxide anion generation, Myeloperoxidase, Neutrophil elastase