TY - JOUR
T1 - In vitro inhibition of Toxoplasma gondii by the anti-malarial candidate, 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol
AU - Xin, Chun Feng
AU - Kim, Hye Sook
AU - Sato, Akira
AU - Lee, Hak Jae
AU - Lee, You Won
AU - Pyo, Kyoung Ho
AU - Shin, Eun Hee
N1 - Funding Information:
This work was supported by 02-2013-080 from the SNUBH research fund.
Publisher Copyright:
© 2016 Elsevier Ireland Ltd
PY - 2016/10/1
Y1 - 2016/10/1
N2 - An anti-malarial candidate, 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251), was studied to characterize its potential as a novel anti-Toxoplasma gondii drug. In the present study, IC50 and LC50 of N-251 on host cells and T. gondii were compared to those of artemisinin and sulfadiazine. The IC50 on Huh-7 cells was 10.19 μg/ml, 67.69 μg/ml and 310.17 μg/ml for N-251, artemisinin, and sulfadiazine, respectively. The LC50 for anti-T. gondii effect was shown to be 1.11 μg/ml, 5.79 μg/ml, and 5.45 μg/ml for N-251, artemisinin and sulfadiazine, respectively. N-251 concentration causing complete parasiticidal effect with minimal cytotoxicity on host cells was determined to be 5 μg/ml. Additionally, the anti-T. gondii effect of N-251 was confirmed by ultrastructural changes, loss of organelles, degenerated morphology and the increase of amylopectin as detected by transmission electron microscope (TEM). Accordingly, the present study suggests that the anti-malarial synthetic endoperoxide, N-251, is an emerging drug candidate more effective than artemisinin and sulfadiazine.
AB - An anti-malarial candidate, 6-(1,2,6,7-tetraoxaspiro[7.11]nonadec-4-yl)hexan-1-ol (N-251), was studied to characterize its potential as a novel anti-Toxoplasma gondii drug. In the present study, IC50 and LC50 of N-251 on host cells and T. gondii were compared to those of artemisinin and sulfadiazine. The IC50 on Huh-7 cells was 10.19 μg/ml, 67.69 μg/ml and 310.17 μg/ml for N-251, artemisinin, and sulfadiazine, respectively. The LC50 for anti-T. gondii effect was shown to be 1.11 μg/ml, 5.79 μg/ml, and 5.45 μg/ml for N-251, artemisinin and sulfadiazine, respectively. N-251 concentration causing complete parasiticidal effect with minimal cytotoxicity on host cells was determined to be 5 μg/ml. Additionally, the anti-T. gondii effect of N-251 was confirmed by ultrastructural changes, loss of organelles, degenerated morphology and the increase of amylopectin as detected by transmission electron microscope (TEM). Accordingly, the present study suggests that the anti-malarial synthetic endoperoxide, N-251, is an emerging drug candidate more effective than artemisinin and sulfadiazine.
KW - Anti-malarial candidate
KW - Anti-protozoal activity
KW - N-251
KW - Synthetic endoperoxide
KW - Toxoplasma gondii
KW - Transmission electron microscopy
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U2 - 10.1016/j.parint.2016.06.013
DO - 10.1016/j.parint.2016.06.013
M3 - Article
C2 - 27380994
AN - SCOPUS:84979534538
SN - 1383-5769
VL - 65
SP - 494
EP - 499
JO - Parasitology International
JF - Parasitology International
IS - 5
ER -
