Coptidis rhizoma and berberine as anti-cancer drugs: A 10-year updates and future perspectives

Pharmacol Res. 2025 Jun:216:107742. doi: 10.1016/j.phrs.2025.107742. Epub 2025 Apr 19.

Abstract

Cancer continues to be among the most substantial health challenges globally. Among various natural compounds, berberine, an isoquinoline alkaloid obtained from Coptidis Rhizoma, has garnered considerable attention for its broad-spectrum biological activities, including anti-inflammatory, antioxidant, anti-diabetic, anti-obesity, and anti-microbial activities. Furthermore, berberine exhibits a broad spectrum of anti-cancer efficacy against various malignancies, such as ovarian, breast, lung, gastric, hepatic, colorectal, cervical, and prostate cancers. Its anti-cancer mechanisms are multifaceted, encompassing the inhibition of cancer cell proliferation, the prevention of metastasis, the induction of apoptosis, the facilitation of autophagy, the modulation of the tumor microenvironment and gut microbiota, and the enhancement of the efficacy of conventional therapeutic strategies. This paper offers an exhaustive overview of the cancer-fighting characteristics of Coptidis Rhizoma and berberine, while also exploring recent developments in nanotechnology aimed at enhancing the bioavailability of berberine. Furthermore, the side effects and safety of berberine are addressed as well. The potential role of artificial intelligence in optimizing berberine's therapeutic applications is also highlighted. This paper provides precious perspectives on the prospective application of Coptidis Rhizoma and berberine in the prevention and management of cancer.

Keywords: Anti-cancer; Berberine; Coptidis Rhizoma.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic* / adverse effects
  • Antineoplastic Agents, Phytogenic* / pharmacokinetics
  • Antineoplastic Agents, Phytogenic* / pharmacology
  • Antineoplastic Agents, Phytogenic* / therapeutic use
  • Berberine* / adverse effects
  • Berberine* / pharmacokinetics
  • Berberine* / pharmacology
  • Berberine* / therapeutic use
  • Coptis chinensis
  • Drugs, Chinese Herbal* / adverse effects
  • Drugs, Chinese Herbal* / pharmacology
  • Drugs, Chinese Herbal* / therapeutic use
  • Humans
  • Neoplasms* / drug therapy
  • Neoplasms* / pathology

Substances

  • Berberine
  • Drugs, Chinese Herbal
  • Coptidis rhizoma extract
  • Antineoplastic Agents, Phytogenic