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Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii

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...

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Autores principales: Hao, Pan, Alaraj, Intisar Q. M., Dulayymi, Juma’a R. Al, Baird, Mark S., Liu, Jing, Liu, Qun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Korean Society for Parasitology and Tropical Medicine 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4870972/
https://www.ncbi.nlm.nih.gov/pubmed/27180571
http://dx.doi.org/10.3347/kjp.2016.54.2.139
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author Hao, Pan
Alaraj, Intisar Q. M.
Dulayymi, Juma’a R. Al
Baird, Mark S.
Liu, Jing
Liu, Qun
author_facet Hao, Pan
Alaraj, Intisar Q. M.
Dulayymi, Juma’a R. Al
Baird, Mark S.
Liu, Jing
Liu, Qun
author_sort Hao, Pan
collection PubMed
description 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 μM, compared with EC(50) values of 248-428 μM 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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spelling pubmed-48709722016-05-18 Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii Hao, Pan Alaraj, Intisar Q. M. Dulayymi, Juma’a R. Al Baird, Mark S. Liu, Jing Liu, Qun Korean J Parasitol Original Article 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 μM, compared with EC(50) values of 248-428 μM 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. The Korean Society for Parasitology and Tropical Medicine 2016-04 2016-04-30 /pmc/articles/PMC4870972/ /pubmed/27180571 http://dx.doi.org/10.3347/kjp.2016.54.2.139 Text en © 2016, Korean Society for Parasitology and Tropical Medicine This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/3.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Hao, Pan
Alaraj, Intisar Q. M.
Dulayymi, Juma’a R. Al
Baird, Mark S.
Liu, Jing
Liu, Qun
Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title_full Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title_fullStr Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title_full_unstemmed Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title_short Sterculic Acid and Its Analogues Are Potent Inhibitors of Toxoplasma gondii
title_sort sterculic acid and its analogues are potent inhibitors of toxoplasma gondii
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4870972/
https://www.ncbi.nlm.nih.gov/pubmed/27180571
http://dx.doi.org/10.3347/kjp.2016.54.2.139
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