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Evaluation of Ruthenium(II) N -Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity.

Ibrahim S Al NasrWaleed S KokoTariq A KhanNevin Gürbüzİsmail ÖzdemirNaceur Hamdi
Published in: Molecules (Basel, Switzerland) (2023)
A series of [RuCl 2 (p-cymene)(NHC)] complexes were obtained by reacting [RuCl 2 (p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the biological activities of these compounds as antienzymatic, antioxidant, antibacterial, anticancer, and antiparasitic agents. The results revealed that complexes 3b and 3d were the most potent inhibitors against AchE with IC 50 values of 2.52 and 5.06 μM mL -1 . Additionally, 3d proved very good antimicrobial activity against all examined microorganisms with IZ (inhibition zone) over 25 mm and MIC (minimum inhibitory concentration) < 4 µM. Additionally, the ligand 2a and its corresponding ruthenium (II) complex 3a had good cytotoxic activity against both cancer cells HCT-116 and HepG-2, with IC 50 values of (7.76 and 11.76) and (4.12 and 9.21) μM mL -1 , respectively. Evaluation of the antiparasitic activity of these complexes against Leishmania major promastigotes and Toxoplasma gondii showed that ruthenium complexes were more potent than the free ligand, with an IC 50 values less than 1.5 μM mL -1 . However, 3d was found the best one with SI (selectivity index) values greater than 5 so it seems to be the best candidate for antileishmanial drug discovery program, and much future research are recommended for mode of action and in vivo evaluation. In general, Ru-NHC complexes are the most effective against L. major promastigotes.
Keyphrases
  • drug discovery
  • anti inflammatory
  • toxoplasma gondii
  • cell proliferation
  • cell death
  • quantum dots
  • mass spectrometry
  • room temperature
  • highly efficient