Identification of methysticin as a potent and non-toxic NF-κB inhibitor from kava, potentially responsible for kava's chemopreventive activity

Ahmad Ali Shaik, David Lee Hermanson, Chengguo Xing

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

Nuclear factor-κB (NF-κB) is a transcription factor that plays an essential role in cancer development. The results of our recent chemopreventive study demonstrate that kava, a beverage in the South Pacific Islands, suppresses NF-κB activation in lung adenoma tissues, potentially a mechanism responsible for kava's chemopreventive activity. Methysticin is identified as a potent NF-κB inhibitor in kava with minimum toxicity. Other kava constituents, including four kavalactones of similar structures to methysticin, demonstrate minimum activities in inhibiting NF-κB.

Original languageEnglish (US)
Pages (from-to)5732-5736
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number19
DOIs
StatePublished - Oct 1 2009

Bibliographical note

Funding Information:
This investigation was supported by Grant R03CA125844 from National Cancer Institute , NIH (C. Xing). We thank Thomas E. Johnson for synthesizing flavokawains A, B, and C for HPLC confirmation and Sonia Das for evaluating the cytotoxicity of methysticin in HL-60 and CCRF cell lines.

Keywords

  • Cancer
  • Kava
  • Methysticin
  • Nuclear factor-κB

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