Bioactive ruthenium(II)-arene complexes containing modified 18 β-glycyrrhetinic acid ligands.

We report the synthesis, characterization and antiproliferative activity of two new Ru(II) arene complexes with imidazole (dichlorido complex 1) or bipyridyl (chlorido complex 2) ligands conjugated to 18β-glycyrrhetinic acid, an active triterpenoid metabolite of Glycyrrhiza glabra. In general, the conjugated ligands and complexes showed only moderate activity against HeLa (cervical), MCF-7 (breast) and A2780 (ovarian) cancer cells, although the activity of complex 2 in the former two cell lines approached that of the drug cisplatin. Complex 2 (in contrast to complex 1) also exhibited significant activity towards both Gram-positive S. aureus and Gram-negative E. coil bacteria. Complex 2 can induce condensation of DNA and enhances the generation of intracellular reactive oxygen species (ROS). The conjugation of natural products to ligands in organometallic half-sandwich complexes provides a strategy to enhance their biological activities.
PMID: 29501980 [PubMed - as supplied by publisher]

Source: Journal of Inorganic Biochemistry - February 21, 2018 Category: Biochemistry Authors: Kong Y, Chen F, Su Z, Qian Y, Wang FX, Wang X, Zhao J, Mao ZW, Liu HK Tags: J Inorg Biochem Source Type: research