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

Abstract:

: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 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.

journal_name

J Inorg Biochem

authors

Kong Y,Chen F,Su Z,Qian Y,Wang FX,Wang X,Zhao J,Mao ZW,Liu HK

doi

10.1016/j.jinorgbio.2018.02.004

subject

Has Abstract

pub_date

2018-05-01 00:00:00

pages

194-199

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(17)30759-6

journal_volume

182

pub_type

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