Antitumor and anti-nematode activities of α-mangostin

Eur J Pharmacol. 2019 Nov 15:863:172678. doi: 10.1016/j.ejphar.2019.172678. Epub 2019 Sep 19.

Abstract

α-Mangostin, one of the major xanthones isolated from pericarp of mangosteen (Garcinia mangostana Linn), exhibits a wide range of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial as well as anticancer, both in in vitro and in vivo studies. In the present study, α-mangostin' anti-cancer and anti-parasitic properties were tested in vitro against three human cell lines, including squamous carcinoma (SCC-15) and glioblastoma multiforme (U-118 MG), compared to normal skin fibroblasts (BJ), and in vivo against Caenorhabditis elegans. The drug showed cytotoxic activity, manifested by decrease of cell viability, inhibition of proliferation, induction of apoptosis and reduction of adhesion at concentrations lower than 10 μM (the IC50 values were 6.43, 9.59 and 8.97 μM for SCC-15, U-118 MG and BJ, respectively). The toxicity, causing cell membrane disruption and mitochondria impairment, was selective against squamous carcinoma with regard to normal cells. Moreover, for the first time anti-nematode activity of α-mangostin toward C. elegans was described (the LC50 = 3.8 ± 0.5 μM), with similar effect exerted by mebendazole, a well-known anthelmintic drug.

Keywords: Biological activity; Caenorhabditis elegans; Glioblastoma multiforme; Squamous carcinoma; α-Mangostin.

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Animals
  • Antinematodal Agents / chemistry
  • Antinematodal Agents / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Caenorhabditis elegans / drug effects
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Inhibitory Concentration 50
  • Xanthones / chemistry
  • Xanthones / pharmacology*

Substances

  • Antinematodal Agents
  • Antineoplastic Agents
  • Xanthones
  • Adenosine Triphosphate
  • mangostin