Polymethoxyflavones

Chemistry and Molecular Mechanisms for Cancer Prevention and Treatment

Yen Chen Tung, Ya Chun Chou, Wei Lun Hung, An Chin Cheng, Roch Chui Yu, Chi Tang Ho, Min Hsiung Pan

Research output: Contribution to journalReview article

2 Citations (Scopus)

Abstract

Polymethoxyflavones (PMFs) are one group of the flavonoid compounds, with tangeretin (Tan) and nobiletin (Nob) being the most abundant PMFs in citrus peel. Numerous biological activities of PMFs have been intensively studied, including anti-inflammatory and anticancer activities. Because of their methoxy groups, PMFs are more lipophilic than hydroxyl flavones, which may affect their biological activities. In addition, researchers found that hydroxylated PMFs (HPMFs) are one of the major metabolites of PMFs in animal urine and feces. Although PMF and HPMFs do show anticancer activity against different types of cancers, but their low hydrophilicity is still a crucial factor that may affect their biological effectiveness. Therefore, from the pharmaceutical aspect, chemical modifications of PMFs have been carried out to obtain acetylated PMFs (Ac-PMFs) for enhancing their biological effects. From the past centuries to the present, cancer is still a critical disease that needs to be solved. Carcinogenesis can be simply divided into three stages: initiation, promotion, and progression. These three stages involve different biological events, such as DNA mutation, cell proliferation, cell growth, and metastasis. In this paper, we aim to illustrate the biological effects of different PMFs, HPMFs, PMF derivatives, and metabolites against different types of cancer and related molecular mechanisms.

Original languageEnglish
JournalCurrent Pharmacology Reports
DOIs
Publication statusPublished - Jan 1 2019

Fingerprint

Metabolites
Bioactivity
Flavones
Chemical modification
Hydrophilicity
Cell proliferation
Cell growth
Flavonoids
Hydroxyl Radical
Neoplasms
Animals
Anti-Inflammatory Agents
Citrus
Derivatives
Hydrophobic and Hydrophilic Interactions
Feces
DNA
Carcinogenesis
Research Personnel
Cell Proliferation

Keywords

  • Anticancer
  • Citrus peel
  • Hydroxylated polymethoxyflavone
  • Metabolites
  • Polymethoxyflavone derivatives
  • Polymethoxyflavones

ASJC Scopus subject areas

  • Biochemistry
  • Genetics
  • Pharmacology
  • Drug Discovery

Cite this

Polymethoxyflavones : Chemistry and Molecular Mechanisms for Cancer Prevention and Treatment. / Tung, Yen Chen; Chou, Ya Chun; Hung, Wei Lun; Cheng, An Chin; Yu, Roch Chui; Ho, Chi Tang; Pan, Min Hsiung.

In: Current Pharmacology Reports, 01.01.2019.

Research output: Contribution to journalReview article

Tung, Yen Chen ; Chou, Ya Chun ; Hung, Wei Lun ; Cheng, An Chin ; Yu, Roch Chui ; Ho, Chi Tang ; Pan, Min Hsiung. / Polymethoxyflavones : Chemistry and Molecular Mechanisms for Cancer Prevention and Treatment. In: Current Pharmacology Reports. 2019.
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abstract = "Polymethoxyflavones (PMFs) are one group of the flavonoid compounds, with tangeretin (Tan) and nobiletin (Nob) being the most abundant PMFs in citrus peel. Numerous biological activities of PMFs have been intensively studied, including anti-inflammatory and anticancer activities. Because of their methoxy groups, PMFs are more lipophilic than hydroxyl flavones, which may affect their biological activities. In addition, researchers found that hydroxylated PMFs (HPMFs) are one of the major metabolites of PMFs in animal urine and feces. Although PMF and HPMFs do show anticancer activity against different types of cancers, but their low hydrophilicity is still a crucial factor that may affect their biological effectiveness. Therefore, from the pharmaceutical aspect, chemical modifications of PMFs have been carried out to obtain acetylated PMFs (Ac-PMFs) for enhancing their biological effects. From the past centuries to the present, cancer is still a critical disease that needs to be solved. Carcinogenesis can be simply divided into three stages: initiation, promotion, and progression. These three stages involve different biological events, such as DNA mutation, cell proliferation, cell growth, and metastasis. In this paper, we aim to illustrate the biological effects of different PMFs, HPMFs, PMF derivatives, and metabolites against different types of cancer and related molecular mechanisms.",
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