Detoxification of Bee Venom Increases Its Anti-inflammatory Activity and Decreases Its Cytotoxicity and Allergenic Activity

Bee venom is a medicinal product that is widely used in traditional therapies owing to its excellent anti-inflammatory activity. However, the use of bee venom has shown adverse effects. Therefore, there is a need for research that can remove the cytotoxicity of bee venom and enhance its efficacy. In this study, we hydrolyzed melittin, the main component of bee venom, and removed the other components to eliminate the toxicity of bee venom. To compare the efficacy of bee venom and detoxified bee venom, we examined their antioxidant effects using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. In addition, cytotoxicity was confirmed in MCF 10A and RAW 264.7 cells, using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay. Detoxified bee venom showed a strong antioxidant activity and decreased a cytotoxicity in MCF 10A and RAW 264.7 cells. The anti-inflammatory activity of detoxified bee venom and bee venom were assessed by comparison of the expression of inflammatory cytokine mRNA and phosphorylation of IκBα in RAW 264.7 cells. Degranulation in RBL-2H3 cells was analyzed through β-hexosaminidase release assay to confirm the allergenic activity of bee venom and detoxified bee venom. Treatment of the detoxified bee venom inhibited inflammatory cytokine mRNA expression, IκBα phosphorylation, and β-hexosaminidase release. Taken together, the results indicated that compared to bee venom, detoxified bee venom exhibited decreased cytotoxicity and allergenicity and increased anti-inflammatory activity. In conclusion, detoxification of bee venom efficiently decreases the adverse effects, making it suitable for medicinal applications. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s12010-021-03653-2.