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Sterculic acid and its analogues are potent inhibitors of Toxoplasma gondii
HAO Pan 1,ALARAJ Intisar Q. M. 2,AL DULAYYMI Juma’a R. 2,BAIRD S. Mark 2,LIU Jing 1,LIU Qun 1 * #
1.National Animal Protozoa Laboratory, College of Veterinary Medicine, China Agricultural University, Beijing 100193, China
2.School of Chemistry, Bangor University, Bangor, UK
*Correspondence author
#Submitted by
Subject:
Funding: Ph.D. Program Foundation of the Ministry of Education of China （No.No. 20110008110006）, National Natural Science Foundation of China （No.No. 31372424）
Opened online: 9 December 2015
Accepted by: none
Citation: HAO Pan,ALARAJ Intisar Q. M.,AL DULAYYMI Juma’a R..Sterculic acid and its analogues are potent inhibitors of Toxoplasma gondii[OL]. [ 9 December 2015] http://en.paper.edu.cn/en_releasepaper/content/4667291
 
 
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 Toxoplasma gondii. Stearoyl-CoA desaturase (SCD), a key enzyme for the synthesis of unsaturated fatty acid, was 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 effect in vitro. T. gondii- infected Vero cells disintegrated at 36h 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 its 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 EC50 value of 36.2 μM, compared with EC50 values of 248-428 uM for the methyl esters. Our study demonstrated that sterculic acid and its analogues are effective in the inhibition of T. gondii growth in vitro, suggesting these compounds or analogues targeting SCD could be effective agents for the treatment of toxoplasmosis.
Keywords:sterculic acid; anti-Toxoplasma gondii; stearoyl-CoA desaturase
 
 
 

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