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

Tameryn Stringer; Maria Alejandra Silva Quintero; Lubbe Wiesner; Gregory S. Smith; Ebbe Nordlander

doi:10.1016/j.jinorgbio.2018.11.018

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

Tameryn Stringer, Maria Alejandra Silva Quintero, Lubbe Wiesner, Gregory S. Smith, Ebbe Nordlander

Chemical Physics

Research output: Contribution to journal › Article › peer-review

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 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.

Original language	English
Pages (from-to)	164-173
Number of pages	10
Journal	Journal of Inorganic Biochemistry
Volume	191
DOIs	https://doi.org/10.1016/j.jinorgbio.2018.11.018
Publication status	Published - 2019

Subject classification (UKÄ)

Pharmaceutical Sciences
Physical Chemistry (including Surface- and Colloid Chemistry)

Free keywords

1,3,5‑Triaza‑phosphaadamantane
Antiplasmodial activity
Iridium
Plasmodium falciparum
Quinoline
Ruthenium

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.jinorgbio.2018.11.018

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

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 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.",

keywords = "1,3,5‑Triaza‑phosphaadamantane, Antiplasmodial activity, Iridium, Plasmodium falciparum, Quinoline, Ruthenium",

author = "Tameryn Stringer and Quintero, {Maria Alejandra Silva} and Lubbe Wiesner and Smith, {Gregory S.} and Ebbe Nordlander",

year = "2019",

doi = "10.1016/j.jinorgbio.2018.11.018",

language = "English",

volume = "191",

pages = "164--173",

journal = "Journal of Inorganic Biochemistry",

issn = "0162-0134",

publisher = "Elsevier",

}

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; Quintero, Maria Alejandra Silva; Wiesner, Lubbe et al.
In: Journal of Inorganic Biochemistry, Vol. 191, 2019, p. 164-173.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Evaluation of PTA-derived ruthenium(II) and iridium(III) quinoline complexes against chloroquine-sensitive and resistant strains of the Plasmodium falciparum malaria parasite

AU - Stringer, Tameryn

AU - Quintero, Maria Alejandra Silva

AU - Wiesner, Lubbe

AU - Smith, Gregory S.

AU - Nordlander, Ebbe

PY - 2019

Y1 - 2019

N2 - 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.

AB - 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.

KW - 1,3,5‑Triaza‑phosphaadamantane

KW - Antiplasmodial activity

KW - Iridium

KW - Plasmodium falciparum

KW - Quinoline

KW - Ruthenium

U2 - 10.1016/j.jinorgbio.2018.11.018

DO - 10.1016/j.jinorgbio.2018.11.018

M3 - Article

C2 - 30529881

AN - SCOPUS:85057600257

SN - 0162-0134

VL - 191

SP - 164

EP - 173

JO - Journal of Inorganic Biochemistry

JF - Journal of Inorganic Biochemistry

ER -

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

Abstract

Subject classification (UKÄ)

Free keywords

UN SDGs

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