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Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules

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2015
636.pdf (1.001Mb)
Authors
Opsenica, Dejan M.
Radivojević, Jelena
Matić, Ivana Z.
Štajner, Tijana
Knežević-Usaj, Slavica
Đurković-Đaković, Olgica
Šolaja, Bogdan
Article (Published version)
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Abstract
New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50 gt 200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment ...of apicomplexan parasites.

Keywords:
antimalarials / antiparasitic / peroxides / cancer / cytotoxicity
Source:
Journal of the Serbian Chemical Society, 2015, 80, 11, 1339-+
Publisher:
  • Srpsko hemijsko društvo, Beograd
Funding / projects:
  • The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-172008)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)

DOI: 10.2298/JSC150430063O

ISSN: 0352-5139

WoS: 000366585800001

Scopus: 2-s2.0-84957567719
[ Google Scholar ]
5
2
URI
http://rimi.imi.bg.ac.rs/handle/123456789/639
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
Institut za medicinska istraživanja
TY  - JOUR
AU  - Opsenica, Dejan M.
AU  - Radivojević, Jelena
AU  - Matić, Ivana Z.
AU  - Štajner, Tijana
AU  - Knežević-Usaj, Slavica
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan
PY  - 2015
UR  - http://rimi.imi.bg.ac.rs/handle/123456789/639
AB  - New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50  gt  200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.
PB  - Srpsko hemijsko društvo, Beograd
T2  - Journal of the Serbian Chemical Society
T1  - Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules
EP  - +
IS  - 11
SP  - 1339
VL  - 80
DO  - 10.2298/JSC150430063O
UR  - conv_3658
ER  - 
@article{
author = "Opsenica, Dejan M. and Radivojević, Jelena and Matić, Ivana Z. and Štajner, Tijana and Knežević-Usaj, Slavica and Đurković-Đaković, Olgica and Šolaja, Bogdan",
year = "2015",
abstract = "New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50  gt  200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.",
publisher = "Srpsko hemijsko društvo, Beograd",
journal = "Journal of the Serbian Chemical Society",
title = "Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules",
pages = "+-1339",
number = "11",
volume = "80",
doi = "10.2298/JSC150430063O",
url = "conv_3658"
}
Opsenica, D. M., Radivojević, J., Matić, I. Z., Štajner, T., Knežević-Usaj, S., Đurković-Đaković, O.,& Šolaja, B.. (2015). Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules. in Journal of the Serbian Chemical Society
Srpsko hemijsko društvo, Beograd., 80(11), 1339-+.
https://doi.org/10.2298/JSC150430063O
conv_3658
Opsenica DM, Radivojević J, Matić IZ, Štajner T, Knežević-Usaj S, Đurković-Đaković O, Šolaja B. Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules. in Journal of the Serbian Chemical Society. 2015;80(11):1339-+.
doi:10.2298/JSC150430063O
conv_3658 .
Opsenica, Dejan M., Radivojević, Jelena, Matić, Ivana Z., Štajner, Tijana, Knežević-Usaj, Slavica, Đurković-Đaković, Olgica, Šolaja, Bogdan, "Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules" in Journal of the Serbian Chemical Society, 80, no. 11 (2015):1339-+,
https://doi.org/10.2298/JSC150430063O .,
conv_3658 .

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