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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Yousefi, Reza Aghevlian, Sadaf Mokhtari, Fatemeh Samouei, Hamidreza Rashidi, Mehdi Nabavizadeh, S. Masoud Tavaf, Zohreh Pouryasin, Zahra Niazi, Ali Faghihi, Reza Papari, Mohammad Mehdi |
| Description | Country affiliation: Iran Author Affiliation: Yousefi R ( Protein Chemistry Laboratory, Department of Biology, College of Sciences, Shiraz University, Iran. ryousefi@shirazu.ac.ir) |
| Abstract | 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. |
| File Format | HTM / HTML |
| ISSN | 02732289 |
| Issue Number | 4 |
| Volume Number | 167 |
| e-ISSN | 15590291 |
| Journal | Applied Biochemistry and Biotechnology |
| Language | English |
| Publisher | Springer |
| Publisher Date | 2012-06-01 |
| Publisher Place | United States |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Biochemistry Discipline Biotechnology Antineoplastic Agents Metabolism Pharmacology Organoplatinum Compounds Serum Albumin Chemistry Cell Line, Tumor Cell Proliferation Drug Effects Humans Protein Binding Protein Denaturation Spectrometry, Fluorescence Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Molecular Biology Environmental Engineering Biochemistry Bioengineering Applied Microbiology and Biotechnology Biotechnology |
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