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Latest research progress on anticancer effect of baicalin and its aglycone baicalein


Cancer, which is a leading cause of deaths around the world, is characterized by genetic mutations and epigenetic changes. Baicalin and its aglycone baicalein, the major bioactive flavones derived from the dried root of Scutellaria baicalensis Georigi, belong to flavonoid compounds. Many studies demonstrated that both of them exhibited remarkable promising anticancer activities. This study summarized potential anticancer mechanisms of baicalin and baicalein including induction of apoptosis, initiation of cell cycle arrest, suppression of metastasis, induction of autophagy, and regulation of immunity. Combination strategies involving baicalin or baicalein as chemotherapeutic adjuvants, clinical trial and safety were also discussed. In addition, we compared the difference in their anticancer effects. Interestingly, baicalein showed quicker and stronger inhibitory effects on multiple cancers than those of baicalin, probably due to its smaller size and high lipophilicity which contribute to fast absorption and improve ability to penetrate cells. Taken together, both baicalin and baicalein are effective in treating cancer with good tolerance. However, deglycosylation of baicalin to baicalein was found to have stronger anticancer potential.

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This study was supported by the Cooperative Scientific Research Project of Chunhui Plan of the Ministry of Education of China (N0. 2020-703), the Youth Science and Technology Innovation Research Team (No.2021JDTD0008) and the Basic Research Fund (No.2020YJ0336, 2020YJ0373) of the Science and Technology Department of Sichuan province of China, Science and Technology Innovation Team from Jiucheng Science and Technology Talent Cultivation Plan in Luzhou City (No. 2019-1). Key Research and Development Projectors of Office of Science & Technology and Talent Work of Luzhou (No. 2021-SYF-26).

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Correspondence to Yumeng Wei or Ling Zhao.

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Wang, L., Feng, T., Su, Z. et al. Latest research progress on anticancer effect of baicalin and its aglycone baicalein. Arch. Pharm. Res. 45, 535–557 (2022).

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  • Anticancer effect
  • Baicalein
  • Baicalin
  • Mechanisms
  • Combination strategy