Cucurbitacins: A Systematic Review of the Phytochemistry and Anticancer Activity

Am J Chin Med. 2015;43(7):1331-50. doi: 10.1142/S0192415X15500755. Epub 2015 Oct 27.

Abstract

Cucurbitacins are highly oxidized tetracyclic triterpenoids that are widely present in traditional Chinese medicines (Cucurbitaceae family), possess strong anticancer activity, and are divided into 12 classes from A to T with over 200 derivatives. The eight most active cucurbitacin components against cancer are cucurbitacin B, D, E, I, IIa, L glucoside, Q, and R. Their mechanisms of action include antiproliferation, inhibition of migration and invasion, proapoptosis, and cell cycle arrest promotion. Cucurbitacins are also found to be the inhibitors of JAK-STAT3, Wnt, PI3K/Akt, and MAPK signaling pathways, which play important roles in the apoptosis and survival of cancer cells. Recently, new studies have discovered synergistic anticancer effects by using cucurbitacins together with clinically approved chemotherapeutic drugs, such as docetaxel and methotrexate. This paper provides a summary of recent research progress on the anticancer property of cucurbitacins and the various intracellular signaling pathways involved in the regulation of cancer cell proliferation, death, invasion, and migration. Therefore, cucurbitacins are a class of promising anticancer drugs to be used alone or be intergraded in current chemotherapies and radiotherapies to treat many types of cancers.

Keywords: Anticancer; Cucurbitacins; Mechanism; Phytochemistry.

Publication types

  • Meta-Analysis
  • Research Support, Non-U.S. Gov't
  • Systematic Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic*
  • Apoptosis / drug effects
  • Cell Cycle Checkpoints / drug effects
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Cell Transformation, Neoplastic / drug effects
  • Cucurbitacins / chemistry
  • Cucurbitacins / classification
  • Cucurbitacins / pharmacology*
  • Cucurbitacins / therapeutic use*
  • Docetaxel
  • Drug Therapy, Combination
  • Humans
  • Methotrexate / therapeutic use
  • Molecular Conformation
  • Neoplasm Invasiveness
  • Neoplasms / drug therapy*
  • Neoplasms / pathology*
  • Phytotherapy*
  • Signal Transduction / drug effects
  • Structure-Activity Relationship
  • Taxoids / therapeutic use

Substances

  • Antineoplastic Agents, Phytogenic
  • Taxoids
  • Docetaxel
  • Cucurbitacins
  • Methotrexate