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

Kong, YQ (Kong, Yaqiong)[ 1 ] ; Chen, F (Chen, Feng)[ 2 ] ; Su, Z (Su, Zhi)[ 1 ] ; Qian, Y (Qian, Yong)[ 1 ]*（钱勇）; Wang, FX (Wang, Fang-xin)[ 3 ] ; Wang, XX (Wang, Xiuxiu)[ 4 ] ; Zhao, J (Zhao, Jing)[ 4 ] ; Mao, ZW (Mao, Zong-Wan)[ 3 ] ; Liu, HK (Liu, Hong-Ke)[ 1 ]*（刘红科）

[ 1 ] Nanjing Normal Univ, Coll Chem & Mat Sci, Collaborat Innovat Ctr Biomed Funct Mat, Nanjing 210046, Jiangsu, Peoples R China

[ 2 ] Univ Warwick, Dept Chem, Gibbet Hill Rd, Coventry CV4 7AL, W Midlands, England

[ 3 ] Sun Yat Sen Univ, Sch Chem & Chem Engn, MOE Key Lab Bioinorgan & Synthet Chem, Guangzhou 510275, Guangdong, Peoples R China

[ 4 ] Nanjing Univ, Inst Chem & Biomed Sci, Sch Life Sci, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China

JOURNAL OF INORGANIC BIOCHEMISTRY，201805,182,194-199

Metal-arene complexes containing bioactive natural-product derived ligands can have new and unusual properties. 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 18 beta-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.

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https://www.sciencedirect.com/science/article/pii/S0162013417307596?via%3Dihub