1 research outputs found
Water-Soluble Ruthenium (II) Chiral Heteroleptic Complexes with Amoebicidal in Vitro and in Vivo Activity
Three
water-soluble RuÂ(II) chiral heteroleptic coordination compounds
[RuÂ(en)Â(pdto)]ÂCl<sub>2</sub> (<b>1</b>), [RuÂ(gly)Â(pdto)]Cl (<b>2</b>), and [RuÂ(acac)Â(pdto)]Cl (<b>3</b>), where pdto =
2,2â˛-[1,2-ethanediylbis-(sulfanediyl-2,1-ethanediyl)]Âdipyridine,
en = ethylendiamine, gly = glycinate, and acac = acetylacetonate,
have been synthezised and fully characterized. The crystal structures
of compounds <b>1</b>â<b>3</b> are described. The
IC<sub>50</sub> values for compounds <b>1</b>â<b>3</b> are within nanomolar range (14, 12, and 6 nM, respectively). The
cytotoxicity for human peripheral blood lymphocytes is extremely low
(>100 ÎźM). Selectivity indexes for RuÂ(II) compounds are in
the
range 700â1300. Trophozoites exposed to RuÂ(II) compounds die
through an apoptotic pathway triggered by ROS production. The orally
administration to infected mice induces a total elimination of the
parasite charge in mice faeces 1â2-fold faster than metronidazole.
Besides, all compounds inhibit the trophozoite proliferation in amoebic
liver abscess induced in hamster. All our results lead us to propose
these compounds as promising candidates as antiparasitic agents