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Evaluation of PTA-derived ruthenium(II) and iridium(III) quinoline complexes against chloroquine-sensitive and resistant strains of the Plasmodium falciparum malaria parasite

Stringer, Tameryn LU ; Quintero, Maria Alejandra Silva; Wiesner, Lubbe; Smith, Gregory S. and Nordlander, Ebbe LU (2019) In Journal of Inorganic Biochemistry 191. p.164-173
Abstract

Cationic 1,3,5‑triaza‑phosphaadamantane (PTA) quinoline ruthenium(II) and iridium(III) complexes were successfully synthesized and characterized using standard spectroscopic and analytical techniques. The complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (CQS) NF54 and chloroquine-resistant (CQR) K1 strains of the Plasmodium falciparum species of the malaria parasite and were found to exhibit good activities in the sensitive strain but moderate activities in the resistant strain, suggesting a resistance mechanism similar to chloroquine (CQ). Selected samples were screened for their ability to inhibit synthetic haemozoin formation and were found to be inhibitors with similar activity... (More)

Cationic 1,3,5‑triaza‑phosphaadamantane (PTA) quinoline ruthenium(II) and iridium(III) complexes were successfully synthesized and characterized using standard spectroscopic and analytical techniques. The complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (CQS) NF54 and chloroquine-resistant (CQR) K1 strains of the Plasmodium falciparum species of the malaria parasite and were found to exhibit good activities in the sensitive strain but moderate activities in the resistant strain, suggesting a resistance mechanism similar to chloroquine (CQ). Selected samples were screened for their ability to inhibit synthetic haemozoin formation and were found to be inhibitors with similar activity to CQ. The complexes also exhibit moderate to low cytotoxicity when evaluated against the Chinese Hamster Ovarian (CHO) cell-line in vitro, suggesting selectivity towards the malaria parasite rather than mammalian cells.

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organization
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Contribution to journal
publication status
published
subject
keywords
1,3,5‑Triaza‑phosphaadamantane, Antiplasmodial activity, Iridium, Plasmodium falciparum, Quinoline, Ruthenium
in
Journal of Inorganic Biochemistry
volume
191
pages
10 pages
publisher
Elsevier
external identifiers
  • scopus:85057600257
ISSN
0162-0134
DOI
10.1016/j.jinorgbio.2018.11.018
language
English
LU publication?
yes
id
463ba9e6-1388-4d89-bbb9-8a627d010928
date added to LUP
2018-12-17 14:50:30
date last changed
2019-02-20 11:40:08
@article{463ba9e6-1388-4d89-bbb9-8a627d010928,
  abstract     = {<p>Cationic 1,3,5‑triaza‑phosphaadamantane (PTA) quinoline ruthenium(II) and iridium(III) complexes were successfully synthesized and characterized using standard spectroscopic and analytical techniques. The complexes were evaluated for their in vitro antiplasmodial activities against the chloroquine-sensitive (CQS) NF54 and chloroquine-resistant (CQR) K1 strains of the Plasmodium falciparum species of the malaria parasite and were found to exhibit good activities in the sensitive strain but moderate activities in the resistant strain, suggesting a resistance mechanism similar to chloroquine (CQ). Selected samples were screened for their ability to inhibit synthetic haemozoin formation and were found to be inhibitors with similar activity to CQ. The complexes also exhibit moderate to low cytotoxicity when evaluated against the Chinese Hamster Ovarian (CHO) cell-line in vitro, suggesting selectivity towards the malaria parasite rather than mammalian cells.</p>},
  author       = {Stringer, Tameryn and Quintero, Maria Alejandra Silva and Wiesner, Lubbe and Smith, Gregory S. and Nordlander, Ebbe},
  issn         = {0162-0134},
  keyword      = {1,3,5‑Triaza‑phosphaadamantane,Antiplasmodial activity,Iridium,Plasmodium falciparum,Quinoline,Ruthenium},
  language     = {eng},
  pages        = {164--173},
  publisher    = {Elsevier},
  series       = {Journal of Inorganic Biochemistry},
  title        = {Evaluation of PTA-derived ruthenium(II) and iridium(III) quinoline complexes against chloroquine-sensitive and resistant strains of the Plasmodium falciparum malaria parasite},
  url          = {http://dx.doi.org/10.1016/j.jinorgbio.2018.11.018},
  volume       = {191},
  year         = {2019},
}