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Luteolin, a flavone ingredient: Anticancer mechanisms, combined medication strategy, pharmacokinetics, clinical trials, and pharmaceutical researches.

  • Shi, Mingyi1
  • Chen, Zixian2
  • Gong, Hui3
  • Peng, Zhaolei4
  • Sun, Qiang5
  • Luo, Kaipei4
  • Wu, Baoyu1
  • Wen, Chuanbiao1
  • Lin, Wei1
  • 1 School of Intelligent Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China. , (China)
  • 2 College of Ethnic Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China. , (China)
  • 3 School of Clinical Medicine, Chengdu University of Traditional Chinese Medicine, Chengdu, China. , (China)
  • 4 State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China. , (China)
  • 5 Sichuan Provincial Key Laboratory of Individualized Drug Therapy, Sichuan Provincial People's Hospital, University of Electronic Science and Technology of China, Chengdu, China. , (China)
Published Article
Phytotherapy Research
Wiley (John Wiley & Sons)
Publication Date
Feb 01, 2024
DOI: 10.1002/ptr.8066
PMID: 38088265


Current pharmaceutical research is energetically excavating the pharmacotherapeutic role of herb-derived ingredients in multiple malignancies' targeting. Luteolin is one of the major phytochemical components that exist in various traditional Chinese medicine or medical herbs. Mounting evidence reveals that this phytoconstituent endows prominent therapeutic actions on diverse malignancies, with the underlying mechanisms, combined medication strategy, and pharmacokinetics elusive. Additionally, the clinical trial and pharmaceutical investigation of luteolin remain to be systematically delineated. The present review aimed to comprehensively summarize the updated information with regard to the anticancer mechanism, combined medication strategies, pharmacokinetics, clinical trials, and pharmaceutical researches of luteolin. The survey corroborates that luteolin executes multiple anticancer effects mainly by dampening proliferation and invasion, spurring apoptosis, intercepting cell cycle, regulating autophagy and immune, inhibiting inflammatory response, inducing ferroptosis, and pyroptosis, as well as epigenetic modification, and so on. Luteolin can be applied in combination with numerous clinical anticarcinogens and natural ingredients to synergistically enhance the therapeutic efficacy of malignancies while reducing adverse reactions. For pharmacokinetics, luteolin has an unfavorable oral bioavailability, it mainly persists in plasma as glucuronides and sulfate-conjugates after being metabolized, and is regarded as potent inhibitors of OATP1B1 and OATP2B1, which may be messed with the pharmacokinetic interactions of miscellaneous bioactive substances in vivo. Besides, pharmaceutical innovation of luteolin with leading-edge drug delivery systems such as host-guest complexes, nanoparticles, liposomes, nanoemulsion, microspheres, and hydrogels are beneficial to the exploitation of luteolin-based products. Moreover, some registered clinical trials on luteolin are being carried out, yet clinical research on anticancer effects should be continuously promoted. © 2023 John Wiley & Sons, Ltd.

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