Collaborative Innovation Center of Biomedical Functional Materials, College of Chemistry and Materials Science, Nanjing Normal University, Nanjing 210046, China.
Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry CV4 7AL, UK.
J Inorg Biochem. 2018 May;182:194-199. doi: 10.1016/j.jinorgbio.2018.02.004. Epub 2018 Feb 21.
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.
金属芳环配合物含有生物活性天然产物衍生的配体，可以具有新的和不寻常的性质。我们报告了两种新型 Ru(II)芳环配合物的合成、表征和抗增殖活性，它们的咪唑（二氯化物配合物 1）或联吡啶（氯化物配合物 2）配体与 18β-甘草次酸共轭，甘草次酸是甘草的一种活性三萜代谢物。一般来说，共轭配体和配合物对 HeLa（宫颈）、MCF-7（乳腺）和 A2780（卵巢）癌细胞的活性仅为中等，尽管配合物 2 在前两种细胞系中的活性接近顺铂药物。与配合物 1 相比，配合物 2 对革兰氏阳性菌 S. aureus 和革兰氏阴性菌 E. coil 也表现出显著的活性。配合物 2 可以诱导 DNA 凝聚并增强细胞内活性氧 (ROS) 的产生。天然产物与金属有机半夹心配合物中的配体的共轭提供了一种增强其生物活性的策略。
