Effects of 20-hydroxyecdysone, Leuzea carthamoides extracts, dexamethasone and their combinations on the NF-κB activation in HeLa cells

J Pharm Pharmacol. 2011 Nov;63(11):1483-95. doi: 10.1111/j.2042-7158.2011.01349.x.


Objectives: The plant steroid 20-hydroxyecdysterone (20E) and 20E-containing extracts from Leuzea carthamoides (Willd.) DC are sold with claims of anabolic and immunomodulatory effects. Yet their effect on the activation of nuclear factor kappa B (NF-κB), a key player in immune response and cell fate, and their influence on the NF-κB-inhibiting activity of steroidal anti-inflammatory drugs is still unknown.

Methods: The ability of 20E, Leuzea extracts and selected steroidal/non-steroidal anti-inflammatory drugs to influence the activation of NF-κB was explored using, as the experimental model, human cervical cancer HeLa-IL-6 cells stably transfected with an IL-6-bound reporter gene. Effects on cell viability and proliferation were monitored (MTT assay). HPLC-DAD was used to establish links between chemical patterns of Leuzea extracts and their bioactivities.

Key findings: 20E inhibited NF-κB activation (IC50 31.8 µm) but was less active than other plant metabolites (xanthohumol 3.8 µm, withaferin A 1.4 µm). Leuzea extracts with high content in 20E had a fair activating effect, but in contrast, some extracts with low 20E content significantly inhibited NF-κB activation at IC50s ranging from 3.5 to 6.2 µg/ml. Combination tests confirmed that 20E does not explain the NF-κB modulation achieved by Leuzea extracts. The extracts but not 20E itself showed a significant modulation of the NF-κB inhibitory effect of dexamethasone.

Conclusions: 20E is unlikely a major player in the NF-κB inhibitory effects displayed by some Leuzea extracts in vitro. If confirmed in vivo, caution should prevail towards marketed Leuzea extracts that are non-standardised or standardised on 20E only, since different starting materials and extracts may even cause opposite effects. More importantly, our results indicate the interaction potential of Leuzea with steroidal anti-inflammatory drugs.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Dexamethasone / pharmacology*
  • Drug Combinations
  • Ecdysterone / pharmacology*
  • HeLa Cells / drug effects
  • HeLa Cells / metabolism
  • Humans
  • Leuzea / chemistry*
  • NF-kappa B / metabolism*
  • Plant Preparations / pharmacology*


  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Combinations
  • NF-kappa B
  • Plant Preparations
  • Ecdysterone
  • Dexamethasone