1. Biological effect and molecular docking of anticancer palladium and platinum complexes with morpholine dithiocarbamate on human serum albumin as a blood carrier protein
- Author
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Hosseini, Seyed Ali, Moghadam, Mahboube Eslami, Saeidifar, Maryam, and Saboury, Ali Akbar
- Subjects
Health aspects ,Palladium -- Health aspects ,Platinum compounds -- Health aspects ,Serum albumin -- Health aspects ,Chronic myeloid leukemia ,Cancer treatment ,Albumin ,Spectroscopy ,Antibacterial agents ,Pharmacology ,Fluorescence ,Microorganisms - Abstract
IntroductionCancer is a deadly disease and the second most common cause of death after cardiovascular disease. Various factors are responsible for the increasing incidence of cancer, of which modernization of [...], The aim of this study was to examine the interaction of [Pd (2,2'-bipyridine) (morpholinedithiocarbamate)] N[O.sub.3] and [Pt (2,2'-bipyridine)(morpholinedithiocarbamate)]N[O.sub.3] with human serum albumin under physiological conditions by using fluorescence, absorption, and circular dichroism spectroscopic techniques. Spectroscopic analysis of the emission quenching at different temperatures demonstrated that the quenching mechanism was static quenching. From the circular dichroism results, thermal stability study, it was found that the interaction of the complexes with human serum albumin caused a conformational change of the protein reversibly. These 2 anticancer Pd and Pt complexes were activated against chronic myelogenous leukemia cell line K562, so that 50% cytotoxic concentration values of 16 and 26 [micro]M for Pd and Pt complexes, respectively, were observed, which were much lower than that of cisplatin (154 [micro]M). Biological activities of both Pd and Pt complexes were also assayed against selective microorganisms by the disc diffusion method. These results showed that the Pd(II) complex is antifungal agent but Pt(II) complex has antibacterial activity. Also, the interaction of both metal derivative complexes was studied by molecular docking. Complementary molecular docking results may be useful to determine the binding mechanism of human serum albumin in pharmaceutical and biophysical studies providing new insight in the novel pharmacology.Key words: dithiocarbamate, Pt and Pd complexes, HSA binding, fluorescence and circular dichroism spectroscopy, antifungal and antibacterial activity, molecular docking.Cette etude a pour but d'examiner l'interaction des complexes [Pd(2,2'-bipyridine) (morpholinedithiocarbamate)] N[O.sub.3] et [Pt (2,2'-bipyridine) (morpholinedithiocarbamate)] N[O.sub.3] avec l'albumine serique humaine (ASH) en conditions physiologiques, a l'aide de techniques spectroscopiques de fluorescence, d'absorption et de dichroisme circulaire. L'analyse spectroscopique de l'extinction de remission a differentes temperatures a montre que le mode d'action de l'extinction etait de nature statique. A partir des resultats sur le dichroisme circulaire, l'etude de stabilite thermique, nous avons observe que l'interaction entre les complexes et l'ASH provoquait un changement conformationnel reversible de la proteine. Ces deux complexes Pd et Pt anticancereux etaient actifs contre des lignees cellulaires K562 de leucemie myeloide chronique, de telle sorte que nous observions des valeurs de concentrations demi-cytotoxiques des complexes Pd et Pt de 16 et de 26 [micro]M, respectivement, ce qui correspond a des chiffres beaucoup moins eleves qu'avec le cisplatine (154 [micro]M). A l'aide de la methode de diffusion sur disque, nous avons aussi etudie l'activite biologique des complexes Pd et Pt contre des microorganismes selectifs. Ces resultats ont montre que le complexe Pd(II) correspond a un agent antifongique, mais que le complexe Pt(II) est dote d'une activite antibacterienne. En outre, nous avons etudie l'interaction avec les deux complexes derives de metaux a l'aide de techniques d'arrimage moleculaire. Les resultats complementaires avec l'arrimage moleculaire pourraient se reveler etre utiles en vue d'etablir les modes d'action de la liaison avec l'ASH dans le cadre d'etudes pharmaceutiques et biophysiques permettant d'obtenir de nouvelles donnees pouvant contribuer a l'innovation en pharmacologie. [Traduit par la Redaction]Mots-cles: dithiocarbamate, complexes Pt et Pd, liaison a l'albumine serique humaine, spectroscopie par fluorescence et dichroisme circulaire, activite antifongique et antibacterienne, arrimage moleculaire.
- Published
- 2018
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