Anti-neurodegenerative, anticancer, anti-inflammatory, and antiobesity activities of theaflavin and its derivatives

Document Type : Narrative Review


1 Department of Pharmacognosy, Faculty of Pharmacy, Lorestan University of Medical Sciences, Lorestan, Iran

2 Department of Microbiology, Faculty of Biological Sciences, Alzahra University, Tehran, Iran

3 Institute for Micromanufacturing, Louisiana Tech University, Ruston, Louisiana, USA

4 Razi Herbal Medicines Research Center, Lorestan University of Medical Sciences, Khorramabad, Lorestan, Iran



Polyphenol metabolites have several hydroxyl groups on aromatic rings. Flavonoids are the main natural groups of polyphenols with numerous therapeutic effects. Theaflavin and its derivatives (theaflavin 3-gallate, theaflavin 3,3′-digallate, and theaflavin 3′-gallate) as one of the major polyphenols of black tea have shown promising anticancer, anti-inflammatory, antiobesity, and anti-neurodegenerative activities. This bioactive compound has the potential capacity to ameliorate coronary heart disease and a healing impact on the density of bone minerals. The emergence of drug resistance in cancer cells and bacteria has caused more endeavors to find novel effective anticancer and antibacterial agents.  In addition, recent studies aim to reduce severe side effects associated with chemotherapy and antimicrobials. In the case of neurodegenerative diseases such as Alzheimer’s, multiple sclerosis, and Parkinson’s, the low efficiency of current expensive drugs is the main problem with therapy for these disorders. In this regard, discovering and designing new anti-neurodegenerative drugs is dispensable.

Graphical Abstract

Anti-neurodegenerative, anticancer, anti-inflammatory, and antiobesity activities of theaflavin and its derivatives


  • Theaflavins modulate growth transcription factors, cell-migration-related proteins, cell-cycle regulatory proteins, and apoptosis-related proteins in cancer cells.
  • Anti-neurodegenerative effects of theaflavin-3,3′-digallate result from its antioxidant capacity via reduction of the cellular oxidative stress.
  • These metabolites regulate glycolipid metabolisms by inhibiting the production and accumulation of lipids in the liver by activation of the SIRT6/ AMPK/SREBP-1/FASN signaling pathway.
  • Theaflavins decrease adipogenic and lipogenic gene expression, adipocyte expansion, and augment lipolytic gene expression.


Main Subjects