Acacetin, a flavone with diverse therapeutic potential in cancer, inflammation, infections and other metabolic disorders

Food Chem Toxicol. 2020 Nov;145:111708. doi: 10.1016/j.fct.2020.111708. Epub 2020 Aug 29.


Background: Acacetin is a di-hydroxy and mono-methoxy flavone present in various plants, including black locust, Damiana, Silver birch. Literature information revealed that acacetin exhibits an array of pharmacological potential including chemopreventive and cytotoxic properties in cancer cell lines, prevents ischemia/reperfusion/myocardial infarction-induced cardiac injury, lipopolysaccharide (LPS), 1-methyl-4-phenyl pyridinium ion (MPP+) and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine hydrochloride (MPTP)-induced neuroinflammation, LPS and sepsis-induced lung injury, rheumatoid and collagen-induced arthritis, inhibit the microbial growth, obesity, viral-mediated infections as well as hepatic protection.

Purpose: This review highlights the therapeutic potential of acacetin, with updated and comprehensive information on the biological sources, chemistry, and pharmacological properties along with the possible mechanism of action, safety aspects, and future research opportunities.

Study design: The information was retrieved from various search engines, including Pubmed, SciFinder, Science direct, Inxight:drugs, Google scholar, and Meta cyc.

Result: The first section of this review focuses on the detailed biological source of acacetin, chromatographic techniques used for isolation, chemical characteristics, the method for the synthesis of acacetin, and the available natural and synthetic derivatives. Subsequently, the pharmacological activities, including anti-cancer, anti-inflammatory, anti-viral, anti-microbial, anti-obesity, have been discussed. The pharmacokinetics data and toxicity profile of acacetin are also discussed.

Conclusion: Acacetin is a potent molecule reported for its strong anti-inflammatory and anti-cancer activity, however further scientific evidence is essential to validate its potency in disease models associated with inflammation and cancer. There is limited information available for toxicity profiling of acacetin; therefore, further studies would aid in establishing this natural flavone as a potent candidate for research studies at clinical setup.

Keywords: Acacetin; Anti-cancer; Antioxidants; Flavone; Natural product; Pharmacological activity.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / chemistry
  • Antimetabolites / administration & dosage*
  • Antimetabolites / chemistry
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Flavones / administration & dosage*
  • Flavones / chemistry
  • Humans
  • Inflammation / drug therapy*
  • Metabolic Diseases / drug therapy*
  • Neoplasms / drug therapy*


  • Anti-Inflammatory Agents
  • Antimetabolites
  • Antineoplastic Agents
  • Flavones
  • acacetin