Antileishmanial activity of ruthenium(II)tetraammine nitrosyl complexes.
The complexes trans-[Ru(NO)(NH(3))(4)L](X)(3) (X = BF(4)(-), PF(6)(-) or Cl(-) and L = N-heterocyclic ligands, P(OEt)(3), SO(3)(-2)), and [Ru(NO)Hedta)] were shown to exhibit IC(50pro) in the range of 36 (L = imN) to 5000 microM (L = imC). The inhibitory effects of trans-[Ru(NO)(NH(3))(4)imN](BF(4))(3) and of the Angeli's salt on the growth of the intramacrophage amastigote form studied were found to be similar while the trans-[Ru(NH(3))(4)imN(H(2)O)](2+) complex was found not to exhibit any substantial antiamastigote effect. The trans-[Ru(NO)(NH(3))(4)imN](BF(4))(3) compound, administered (500 nmol kg(-1) day(-1)) in BALB/c mice infected with Leishmania major, was found to exhibit a 98% inhibition on the parasite growth. Furthermore, this complex proved to be at least 66 times more efficient than glucantime in in vivo experiments.
Pereira
José Clayston Melo
JC
Departamento de Química e Física Molecular, Instituto de Química de São Carlos-Universidade de São Paulo, São Carlos, SP, Brazil.
Carregaro
Vanessa
V
Costa
Diego Luís
DL
da Silva
João Santana
JS
Cunha
Fernando Q
FQ
Franco
Douglas Wagner
DW
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D020128:Inhibitory Concentration 50; D018320:Leishmania major / Q000166:cytology / Q000187:drug effects* / Q000502:physiology; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D009569:Nitric Oxide / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D012428:Ruthenium / Q000737:chemistry*; D013237:Stereoisomerism
D000981:Antiprotozoal Agents; D009942:Organometallic Compounds; D009569:Nitric Oxide; D012428:Ruthenium