5-Demethyltangeretin is more potent than tangeretin in inhibiting dimethylbenz(a)anthracene (DMBA)/12-O-tetradecanoylphorbol-13-acetate (TPA)-induced skin tumorigenesis

Nianhan Ma, Ching Shu Lai, Chih Han Chung, Jinn Moon Yang, Kai Cheng Hsu, Chin Yu Chen, Tao Sheng Chung, Shiming Li, Chi Tang Ho, Min Hsiung Pan

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)


5-Demethyltangeretin (5-DTAN), an autohydrolysis product of tangeretin (TAN) found in citrus peel, exhibited more potent anti-proliferative activity in human cancer cells than TAN itself. In this study, we investigated the anti-tumor promoting effect and underlying molecular mechanism of 5-DTAN on 7,12-dimethyl-benz(a)anthracene (DMBA)-induced and 12-. O-tetradecanoylphorbol-13-acetate (TPA)-promoted skin carcinogenesis. Application of 5-DTAN prior to each TPA-treatment was more effective than that of TAN on reducing the number, incidence and size of papillomas in DMBA-initiated mouse skin. Moreover, 5-DTAN suppressed cyclooxygenase-2 (COX-2) protein expression more strongly than TAN through interfering with phosphatidylinositiol 3-kinase (PI3K)/Akt signaling and further activation of transcription factor NF-κB. Taken together, these results revealed for the first time the in vivo chemopreventive efficacy of 5-DTAN on inhibition of skin carcinogenesis through promoting apoptosis and molecular interactions with residues of PI3K, COX-2, and AKT that may potentially serve as a novel functional agent capable of preventing inflammation-associated tumorigenesis.

Original languageEnglish
Pages (from-to)528-537
Number of pages10
JournalJournal of Functional Foods
Issue numberC
Publication statusPublished - 2014
Externally publishedYes


  • 5-Demethyltangeretin
  • DMBA
  • Inflammation
  • TPA
  • Tangeretin

ASJC Scopus subject areas

  • Food Science
  • Medicine (miscellaneous)
  • Nutrition and Dietetics


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