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1. Appl Biochem Biotechnol. 2012 May 24. [Epub ahead of print]

The Anticancer Activity and HSA Binding Properties of the Structurally Related
Platinum (II) Complexes.

Yousefi R, Aghevlian S, Mokhtari F, Samouei H, Rashidi M, Nabavizadeh SM, Tavaf
Z, Pouryasin Z, Niazi A, Faghihi R, Papari MM.

Protein Chemistry Laboratory (PCL), Department of Biology, College of Sciences,
Shiraz University, Shiraz, 71454, Iran, ryousefi@shirazu.ac.ir.

The development of resistance and unwanted harmful interaction with other
biomolecules instead of DNA are the major drawbacks for application of platinum
(Pt) complexes in cancer chemotherapy. To conquer these problems, much works have
been done so far to discover innovative Pt complexes. The objective of the
current study was to evaluate the anti cancer activities of a series of four and
five-coordinated Pt(II) complexes, having deprotonated 2-phenyl pyridine
(abbreviated as C^N), biphosphine moieties, i.e., dppm = bis(diphenylphosphino)
methane (Ph(2)PCH(2)PPh(2)) and dppa = bis(diphenylphosphino)amine
(Ph(2)PNHPPh(2)), as the non-leaving carrier groups. The growth inhibitory effect
of the Pt complexes [Pt(C^N)(dppm)]PF(6): C ( 1 ), [Pt(C^N)(dppa)]PF(6): C ( 2 ),
and [Pt(C^N)I(dppa)]: C ( 3 ), toward the cancer cell lines was measured using
3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. In addition,
the florescence quenching experiments of the interaction between human serum
albumin (HSA) and the Pt complexes were performed in order to obtain the binding
parameters and to evaluate the denaturing properties of these complexes upon
binding to the general carrier protein of blood stream. The structure-activity
relationship studies reveal that four-coordinated Pt complexes C ( 1 ) and C ( 2
) with both significant hydrophobic and charge characteristics, not only exhibit
strong antiproliferation activity toward the cancer cell lines, but also they
display lower denaturing effect against carrier protein HSA. On the other hand,
five-coordinated C ( 3 ) complex with the unusual intermolecular NH…Pt hydrogen
binding and the intrinsic ability for oligomerization, exhibits poor anticancer
activity and strong denaturing property. The current study reveals that the
balance between charge and hydrophobicity of the Pt complexes, also their
hydrogen binding abilities and coordination mode are important for their
anticancer activities. Moreover, this study may suggest C ( 1 ) and C ( 2 ) as
the potential template structures for synthesis of new generation of
four-coordinated Pt complexes with strong anticancer activities and weak
denaturing effects against proteins.

PMID: 22622643 [PubMed - as supplied by publisher]