Antioxidant and antiproliferative activity of indigocarpan, a pterocarpan from Indigofera aspalathoides

J Pharm Pharmacol. 2016 Oct;68(10):1331-9. doi: 10.1111/jphp.12609. Epub 2016 Jul 27.

Abstract

Objectives: This study aimed to investigate the anticancer potential of indigocarpan (1), a pterocarpan isolated from Indigofera aspalathoides, a plant found in India which has been used in Ayurveda for centuries for the treatment of oedematous tumours.

Methods: The antiproliferative activity in a panel of four human cancer cell lines was studied. The mechanism of its antiproliferative activity in human colorectal adenocarcinoma LS174T cells was investigated in detail.

Key findings: Indigocarpan (1) showed antiproliferative activity in a panel of four human cancer cell lines with IC50 s ranging from 180 to 250 μm. Indigocarpan induces p53-dependent p21 upregulation and apoptosis in LS174T cells, upregulates p53 and p21(WAF1) protein levels, enhances cleavage of caspase-3 and downregulates cyclin D1, cyclin B1 and PCNA protein levels, indicating its role in modulating cell cycle progression. Indigocarpan also exhibited a strong antioxidative effect in LS174T cells.

Conclusions: Along with the antiproliferative capacity, the strong antioxidative property of the compound makes it a promising candidate for further development as an anticancer and chemopreventive compound.

Keywords: Apoptosis; Indigofera aspalathoides; antioxidant; antiproliferative; indigocarpan.

MeSH terms

  • Adenocarcinoma / drug therapy
  • Adenocarcinoma / metabolism
  • Antioxidants / pharmacology*
  • Apoptosis / drug effects
  • Cell Cycle / drug effects
  • Cell Cycle Proteins / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Colorectal Neoplasms / drug therapy
  • Colorectal Neoplasms / metabolism
  • Cyclin B1 / metabolism
  • Cyclin D1 / metabolism
  • Cyclin-Dependent Kinase Inhibitor p21 / metabolism
  • Down-Regulation / drug effects
  • Humans
  • India
  • Indigofera / chemistry*
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Proliferating Cell Nuclear Antigen / metabolism
  • Pterocarpans / pharmacology*
  • Tumor Suppressor Protein p53 / metabolism
  • Up-Regulation / drug effects

Substances

  • Antioxidants
  • Cell Cycle Proteins
  • Cyclin B1
  • Cyclin-Dependent Kinase Inhibitor p21
  • Plant Extracts
  • Proliferating Cell Nuclear Antigen
  • Pterocarpans
  • Tumor Suppressor Protein p53
  • Cyclin D1