Activities of Pt(II) and Ru(III) triazole-pyrimidine complexes against Trypanosoma cruzi and T. brucei brucei.
We studied the biological activity of three newly synthesized metal complexes of triazole-pyrimidine derivatives that were previously observed to inhibit in vitro growth of epimastigotes of Trypanosoma cruzi and procyclic forms of Trypanosoma brucei brucei. We analyzed the possible inhibitory effect of these compounds on the synthesis of DNA, RNA and protein, ultrastructure and excretion of metabolites by these parasites. RNA synthesis was inhibited by all three complexes assayed. These complexes also led to anomalies of the main organelles (e.g. nucleus, kinetoplast and mitochondria). In addition, these complexes may be capable of altering the excretion of metabolites by the parasites.
Magán
Rosa
R
Instituto de Biotecnología, Facultad de Ciencias, Universidad de Granada, Granada, Spain.
Marín
Clotilde
C
Rosales
Maria Jose
MJ
Barrera
Mario Antonio
MA
Salas
Juan Manuel
JM
Sánchez-Moreno
Manuel
M
D000818:Animals; D001711:Biotransformation; D016054:DNA, Protozoan / Q000096:biosynthesis; D009682:Magnetic Resonance Spectroscopy; D009942:Organometallic Compounds / Q000378:metabolism / Q000494:pharmacology*; D009944:Organoplatinum Compounds / Q000378:metabolism / Q000494:pharmacology*; D015800:Protozoan Proteins / Q000096:biosynthesis; D011743:Pyrimidines / Q000378:metabolism / Q000494:pharmacology*; D016053:RNA, Protozoan / Q000096:biosynthesis; D012428:Ruthenium / Q000378:metabolism / Q000494:pharmacology*; D014230:Triazoles / Q000378:metabolism / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D014529:Uridine / Q000378:metabolism
D016054:DNA, Protozoan; D009942:Organometallic Compounds; D009944:Organoplatinum Compounds; D015800:Protozoan Proteins; D011743:Pyrimidines; D016053:RNA, Protozoan; D014230:Triazoles; D012428:Ruthenium; D014529:Uridine