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Inhibitory Effect of Platinum and Ruthenium Bipyridyl Complexes on Porcine Pancreatic Phospholipase A2

Inhibitory Effect of Platinum and Ruthenium Bipyridyl Complexes on Porcine Pancreatic Phospholipase A2

Tina Kamčeva, Jörg Flemmig, Bojana Damnjanović, Jürgen Arnhold, Aleksandar Mijatović, Marijana Petković

Metallomics. 2011 Oct;3(10):1056-63.

PMID: 21909579

Abstract:

Pancreatic phospholipase A(2) (PLA(2)) plays an important role in cellular homeostasis as well as in the process of carcinogenesis. Effects of metallo-drugs used as chemotherapeutics on the activity of this enzyme are unknown. In this work, the interaction between porcine pancreatic PLA(2) and two selected transition metal complexes--tetrachloro(bipyridine) platinum(IV) ([PtCl(4)(bipy)]) and dichloro (bipyridine) ruthenium(III)chloride ([RuCl(2)(bipy)(2)]Cl)--was studied. Matrix-assisted laser desorption/ionisation time-of-flight mass spectrometry (MALDI-TOF MS) and fluorescence spectroscopy have been used to analyse the enzyme activity in the absence and presence of metal complexes and to verify potential binding of these drugs to the enzyme. The tested metal complexes decreased the activity of phospholipase A(2) in an uncompetitive inhibition mode. A binding of the ruthenium complex near the active site of the enzyme could be evidenced and possible modes of interaction are discussed.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP10049088	Ruthenium(III) chloride		10049-08-8	Price

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