Therapeutic aspects of berberine and its derivatives: recent advances and challenges

Document Type : Mini-Review


1 Department of Biological Science, Faculty of Science, University of Kurdistan, Sanandaj, Kurdistan, Iran

2 Department of Biology, Faculty of Science, Razi University, Kermanshah, Iran

3 Lorestan University of Medical Sciences, Khorramabad, Iran



There is an urgent need for the discovery of biocompatible therapeutic drugs that can be administered for long periods without severe side effects. Berberine is an alkaloid metabolite, found in some plant species, commonly applied in animal and clinical productions. This metabolite can be found in the family Ranunculaceae and Berberidaceae. Antibacterial, antiviral, antifungal, and anticancer activities have been identified for this natural hydrophobic cation and its derivatives. As the major limitation for clinical application, the weak pharmacokinetics and quick removal of berberine from the body can result from the poor absorption rate of berberine. Therefore, high doses of this bioactive metabolite are required to obtain acceptable therapeutic activities. However, high concentrations of berberine can lead to some adverse effects. This mini-review has covered the advances and limitations for novel formulations of this metabolite with therapeutic activities considering the recent investigations.

Graphical Abstract

Therapeutic aspects of berberine and its derivatives: recent advances and challenges


  • Berberine promotes cell apoptosis and hinders cell proliferation of cancer cells.
  • Berberine can intercalate into DNA and augment the membrane permeability of bacteria.
  • For antifungal mechanisms of berberine, the up-regulation of oxidative stress genes and dysfunction of mitochondria have been reported.
  • Inhibition of viral attachment/entry, genomic DNA replication, and protein production were the major antiviral mechanisms for berberine.
  • Nanoformulations of berberine with drugs such as doxorubicin lead to a significant synergetic effect.


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