Parasites, Hosts and Diseases

The Korea Society for Parasitology and Tropical Medicine (대한기생충학·열대의학회)
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Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii

  • Hao, Pan (National Animal Protozoa Laboratory, College of Veterinary Medicine, China Agricultural University) ;
  • Alaraj, Intisar Q.M. (School of Chemistry, Bangor University) ;
  • Al Dulayymi, Juma'a R. (School of Chemistry, Bangor University) ;
  • Baird, Mark S. (School of Chemistry, Bangor University) ;
  • Liu, Jing (National Animal Protozoa Laboratory, College of Veterinary Medicine, China Agricultural University) ;
  • Liu, Qun (National Animal Protozoa Laboratory, College of Veterinary Medicine, China Agricultural University)
  • Received : 2015.12.02
  • Accepted : 2016.03.13
  • Published : 2016.04.30
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Abstract

Toxoplasmosis is a serious disease caused by Toxoplasma gondii, one of the most widespread parasites in the world. Lipid metabolism is important in the intracellular stage of T. gondii. Stearoyl-CoA desaturase (SCD), a key enzyme for the synthesis of unsaturated fatty acid is predicted to exist in T. gondii. Sterculic acid has been shown to specifically inhibit SCD activity. Here, we examined whether sterculic acid and its methyl ester analogues exhibit anti-T. gondii effects in vitro. T. gondii-infected Vero cells were disintegrated at 36 hr because of the propagation and egress of intracellular tachyzoites. All test compounds inhibited tachyzoite propagation and egress, reducing the number of ruptured Vero cells by the parasites. Sterculic acid and the methyl esters also inhibited replication of intracellular tachyzoites in HFF cells. Among the test compounds, sterculic acid showed the most potent activity against T. gondii, with an $EC_{50}$ value of $36.2{\mu}M$, compared with $EC_{50}$ values of $248-428{\mu}M$ for the methyl esters. Our study demonstrated that sterculic acid and its analogues are effective in inhibition of T. gondii growth in vitro, suggesting that these compounds or analogues targeting SCD could be effective agents for the treatment of toxoplasmosis.

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