Potential role of genipin in cancer therapy

Muthu K. Shanmugam, Hongyuan Shen, Feng Ru Tang, Frank Arfuso, Mohanraj Rajesh, Lingzhi Wang, Alan Prem Kumar, Jinsong Bian, Boon Cher Goh, Anupam Bishayee, Gautam Sethi

Research output: Contribution to journalReview articlepeer-review

97 Citations (Scopus)


Genipin, an aglycone derived from the iridoid glycoside, geniposide, is isolated and characterized from the extract of Gardenia jasminoides Ellis fruit (family Rubiaceae). It has long been used in traditional oriental medicine for the prevention and treatment of several inflammation driven diseases, including cancer. Genipin has been shown to have hepatoprotective activity acting as a potent antioxidant and inhibitor of mitochondrial uncoupling protein 2 (UCP2), and also reported to exert significant anticancer effects. It is an excellent crosslinking agent that helps to make novel sustained or delayed release nanoparticle formulations. In this review, we present the latest developments of genipin as an anticancer agent and briefly describe its diverse mechanism(s) of action. Several lines of evidence suggest that genipin is a potent inhibitor of UCP2, which functions as a tumor promoter in a variety of cancers, attenuates generation of reactive oxygen species and the expression of matrix metalloproteinase 2, as well as induces caspase-dependent apoptosis in vitro and in in vivo models. These finding suggests that genipin can serve as both a prominent anticancer agent as well as a potent crosslinking drug that may find useful application in several novel pharmaceutical formulations.

Original languageEnglish
Pages (from-to)195-200
Number of pages6
JournalPharmacological Research
Publication statusPublished - Jul 2018


  • Anticancer
  • Crosslinking
  • Genipin
  • Metastasis
  • Nano-formulations
  • UCP2

ASJC Scopus subject areas

  • Pharmacology


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