Deoxyelephantopin and Isodeoxyelephantopin as Potential Anticancer Agents with Effects on Multiple Signaling Pathways

Molecules. 2017 Jun 21;22(6):1013. doi: 10.3390/molecules22061013.

Abstract

Cancer is the 2nd leading cause of death worldwide. The development of drugs to target only one specific signaling pathway has limited therapeutic success. Developing chemotherapeutics to target multiple signaling pathways has emerged as a new prototype for cancer treatment. Deoxyelephantopin (DET) and isodeoxyelephantopin (IDET) are sesquiterpene lactone components of "Elephantopus scaber and Elephantopus carolinianus", traditional Chinese medicinal herbs that have long been used as folk medicines to treat liver diseases, diabetes, diuresis, bronchitis, fever, diarrhea, dysentery, cancer, and inflammation. Recently, the anticancer activity of DET and IDET has been widely investigated. Here, our aim is to review the current status of DET and IDET, and discuss their anticancer activity with specific emphasis on molecular targets and mechanisms used by these compounds to trigger apoptosis pathways which may help to further design and conduct research to develop them as lead therapeutic drugs for cancer treatments. The literature has shown that DET and IDET induce apoptosis through multiple signaling pathways which are deregulated in cancer cells and suggested that by targeting multiple pathways simultaneously, these compounds could selectively kill cancer cells. This review suggests that DET and IDET hold promising anticancer activity but additional studies and clinical trials are needed to validate and understand their therapeutic effect to develop them into potent therapeutics for the treatment of cancer.

Keywords: Elephantopus carolinianus; Elephantopus scaber; apoptosis; cancer; deoxyelephantopin; inflammation; isodeoxyelephantopin.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects*
  • Asteraceae / chemistry
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Humans
  • Lactones / chemistry
  • Lactones / metabolism
  • Lactones / pharmacology*
  • Lactones / therapeutic use*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Plant Extracts / chemistry
  • Plant Extracts / metabolism
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use
  • Plants, Medicinal / chemistry
  • Sesquiterpenes / chemistry
  • Sesquiterpenes / metabolism
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use*
  • Signal Transduction / drug effects
  • Transcription Factors / drug effects
  • Transcription Factors / metabolism
  • Transcription Factors / therapeutic use

Substances

  • Antineoplastic Agents
  • Lactones
  • Plant Extracts
  • Sesquiterpenes
  • Transcription Factors
  • deoxyelephantopin