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Inhibition of COX-2 activity and proinflammatory cytokines (TNF-α and IL-1β) production by water-soluble sub-fractionated parts from bee (Apis mellifera) venom

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Bee venom is used as a traditional medicine for treatment of arthritis. The anti-inflammatory activity of then-hexane, ethyl acetate, and aqueous partitions from bee venom (Apis mellifera) was studied using cyclooxygenase (COX) activity and pro-inflammatory cytokines (TNF-α and IL-1β) production,in vitro. COX-2 is involved in the production of prostaglandins that mediate pain and support the inflammatory process. The aqueous partition of bee venom showed strong dose-dependent inhibitory effects on COX-2 activity (IC50 = 13.1 μg/mL), but did not inhibit COX-1 activity. The aqueous partition was subfractionated into three parts by molecular weight differences, namely, B-F1 (above 20 KDa), B-F2 (between 10 KDa and 20 KDa) and B-F3 (below 10 KDa). B-F2 and B-F3 strongly inhibited COX-2 activity and COX-2 mRNA expression in a dose-dependent manner, without revealing cytotoxic effects. TNF-α and IL-1β are potent pro-inflammatory cytokines and are early indicators of the inflammatory process. We also investigated the effects of three subfractions on TNF-α and IL-1β production using ELISA method. All three subfractions, B-F1, B-F2 and B-F3, inhibited TNF-α and IL-1β production. These results suggest the pharmacological activities of bee venom on anti-inflammatory process include the inhibition of COX-2 expression and the blocking of pro-inflammatory cytokines (TNF-α, and IL-1β) production.

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Correspondence to Kung-Woo Nam or Kang-Hoon Je or Jang Hurn Lee or Ho Je Han or Hye Jung Lee or Sung Kil Kang or Woongchon Mar.

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Nam, K., Je, K., Lee, J.H. et al. Inhibition of COX-2 activity and proinflammatory cytokines (TNF-α and IL-1β) production by water-soluble sub-fractionated parts from bee (Apis mellifera) venom. Arch Pharm Res 26, 383–388 (2003). https://doi.org/10.1007/BF02976695

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Key words

  • Bee venom
  • Cyclooxygenase-2
  • Anti-inflammatory activity
  • Tumor necrosis factor-α
  • Interleukin-1β