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Biotransformations of anticancer ruthenium(III) complexes: an X-ray absorption spectroscopic study.

Chemistry (Weinheim an der Bergstrasse, Germany) (2013-01-31)
Aviva Levina, Jade B Aitken, Yee Yen Gwee, Zhi Jun Lim, Mimi Liu, Anannya Mitra Singharay, Pok Fai Wong, Peter A Lay

An anti-metastatic drug, NAMI-A ((ImH)[Ru(III) Cl4 (Im)(dmso)]; Im=imidazole, dmso=S-bound dimethylsulfoxide), and a cytotoxic drug, KP1019 ((IndH)[Ru(III) Cl4 (Ind)2 ]; Ind=indazole), are two Ru-based anticancer drugs in human clinical trials. Their reactivities under biologically relevant conditions, including aqueous buffers, protein solutions or gels (e.g, albumin, transferrin and collagen), undiluted blood serum, cell-culture medium and human liver (HepG2) cancer cells, were studied by Ru K-edge X-ray absorption spectroscopy (XAS). These XAS data were fitted from linear combinations of spectra of well-characterised Ru compounds. The absence of XAS data from the parent drugs in these fits points to profound changes in the coordination environments of Ru(III) . The fits point to the presence of Ru(IV/III) clusters and binding of Ru(III) to S-donor groups, amine/imine and carboxylato groups of proteins. Cellular uptake of KP1019 is approximately 20-fold higher than that of NAMI-A under the same conditions, but it diminishes drastically after the decomposition of KP1019 in cell-culture media, which indicate that the parent complex is taken in by cells through passive diffusion.

Product Number
Product Description

Imidazole, ACS reagent, ≥99% (titration)
Imidazole, for molecular biology, ≥99% (titration)
Imidazole, ReagentPlus®, 99%
Imidazole, puriss. p.a., ≥99.5% (GC)
Imidazole buffer Solution, BioUltra, 1 M in H2O
Imidazole, BioUltra, ≥99.5% (GC)
Imidazole hydrochloride
Imidazole, BioUltra, for molecular biology, ≥99.5% (GC)
Imidazole, Pharmaceutical Secondary Standard; Certified Reference Material
Imidazole, ≥99% (titration), crystalline
Imidazole sodium derivative, technical grade
Imidazole, ReagentPlus®, 99%, Redi-Dri, free-flowing
Imidazole, for molecular biology, ≥99% (titration), free-flowing, Redi-Dri
Imidazole, European Pharmacopoeia (EP) Reference Standard

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