Berberine inhibits the growth of human colorectal adenocarcinoma in vitro and in vivo

J Nat Med. 2014 Jan;68(1):53-62. doi: 10.1007/s11418-013-0766-z. Epub 2013 Apr 21.


Berberine is an alkaloid isolated from the Chinese herbal medicine Huanglian, and has long been used as an antibiotic. Its antineoplastic properties were subsequently discovered in vitro. The purpose of this study was to investigate the effects of berberine on the growth of human colorectal carcinoma cells in vitro and in vivo. The results showed that berberine inhibited human colorectal adenocarcinoma (LoVo) cell growth in a time- and dose-dependent manner. A WST-1 assay showed that the IC50 value after 72 h was 40.79 ± 4.11 μM. Cell cycle analysis of 40 μM berberine-treated LoVo cells by flow cytometry showed accumulation of cells in the G2/M phase. The inhibition of LoVo cell growth by berberine was associated with the suppression of cyclin B1, cdc2, and cdc25c proteins. Berberine at a dose of 50 mg kg(-1) day(-1) showed inhibitory rates of 45.3% in a human colorectal adenocarcinoma xenograft in nude mice. The combination of berberine and 5-fluorouracil (5-FU) had a higher inhibitory rate (59.8%) than the berberine group (36.4%, P = 0.01), but no significant difference was observed between the 5-FU group (43.0%, P = 0.06) and the combination group. These results support the possibility that berberine may be useful as an alternative therapy for colorectal carcinoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Adenocarcinoma / metabolism
  • Adenocarcinoma / pathology
  • Animals
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Berberine / pharmacology*
  • CDC2 Protein Kinase
  • Cell Proliferation / drug effects*
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / metabolism
  • Colorectal Neoplasms / pathology
  • Cyclin B / metabolism
  • Cyclin B1 / metabolism
  • Cyclin-Dependent Kinases
  • Dose-Response Relationship, Drug
  • Fluorouracil / pharmacology
  • G2 Phase Cell Cycle Checkpoints / drug effects
  • HT29 Cells
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Time Factors
  • Xenograft Model Antitumor Assays
  • cdc25 Phosphatases / metabolism


  • Antineoplastic Agents, Phytogenic
  • CCNB1 protein, human
  • Cyclin B
  • Cyclin B1
  • Berberine
  • CDC2 Protein Kinase
  • CDK1 protein, human
  • Cyclin-Dependent Kinases
  • CDC25C protein, human
  • cdc25 Phosphatases
  • Fluorouracil