AI Article Synopsis
- Three new chiral water-soluble Ru(II) coordination compounds have been synthesized and characterized, showing promising crystal structures and very low cytotoxicity in human lymphocytes.
- The compounds exhibit strong anticancer activity with IC values in the nanomolar range and a high selectivity index.
- They induce apoptosis in trophozoites through reactive oxygen species (ROS) production and effectively eliminate parasites in infected mice, outperforming the commonly used metronidazole.
Article Abstract
Three water-soluble Ru(II) chiral heteroleptic coordination compounds [Ru(en)(pdto)]Cl (1), [Ru(gly)(pdto)]Cl (2), and [Ru(acac)(pdto)]Cl (3), where pdto = 2,2'-[1,2-ethanediylbis-(sulfanediyl-2,1-ethanediyl)]dipyridine, en = ethylendiamine, gly = glycinate, and acac = acetylacetonate, have been synthezised and fully characterized. The crystal structures of compounds 1-3 are described. The IC values for compounds 1-3 are within nanomolar range (14, 12, and 6 nM, respectively). The cytotoxicity for human peripheral blood lymphocytes is extremely low (>100 μM). Selectivity indexes for Ru(II) compounds are in the range 700-1300. Trophozoites exposed to Ru(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 1-2-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.
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| http://dx.doi.org/10.1021/acs.jmedchem.6b00795 | DOI Listing |
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