Simple Trans-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin

Following previous studies devoted to trans−Pt(3-af)2Cl2, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures...

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Main Authors:	Małgorzata Fabijańska, Magdalena Orzechowska, Agnieszka J. Rybarczyk-Pirek, Justyna Dominikowska, Alicja Bieńkowska, Maciej Małecki, Justyn Ochocki
Format:	Article
Language:	English
Published:	MDPI AG 2020-03-01
Series:	International Journal of Molecular Sciences
Subjects:	anticancer drugs coordination compounds gene expression platinum structure–activity relationships
Online Access:	https://www.mdpi.com/1422-0067/21/6/2116

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spelling	doaj-4661f53d6cd44ead97a0a22fcd7597a92020-11-25T02:20:10ZengMDPI AGInternational Journal of Molecular Sciences1422-00672020-03-01216211610.3390/ijms21062116ijms21062116Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with CisplatinMałgorzata Fabijańska0Magdalena Orzechowska1Agnieszka J. Rybarczyk-Pirek2Justyna Dominikowska3Alicja Bieńkowska4Maciej Małecki5Justyn Ochocki6Department of Bioinorganic Chemistry, Medical University of Lodz, 1 Muszynskiego St., 90-151 Łódź, PolandDepartment of Applied Pharmacy, Medical University of Warsaw, 1 Banacha St., 02–097 Warsaw, PolandTheoretical and Structural Chemistry Group, Department of Physical Chemistry, Faculty of Chemistry, University of Łódź, Pomorska 163/165, 90-236 Łódź, PolandTheoretical and Structural Chemistry Group, Department of Physical Chemistry, Faculty of Chemistry, University of Łódź, Pomorska 163/165, 90-236 Łódź, PolandDepartment of Applied Pharmacy, Medical University of Warsaw, 1 Banacha St., 02–097 Warsaw, PolandDepartment of Applied Pharmacy, Medical University of Warsaw, 1 Banacha St., 02–097 Warsaw, PolandDepartment of Bioinorganic Chemistry, Medical University of Lodz, 1 Muszynskiego St., 90-151 Łódź, PolandFollowing previous studies devoted to <i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures are presented in the Cambridge Structural Database (CSD). Molecular Hirshfeld surface analysis and computational methods were used to examine a possible relationship between the structure and anticancer activity of <i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>. The purpose of the article was also to investigate the effect of hyperthermia on the anticancer activity of cisplatin, cytostatics used in the treatment of patients with ovarian cancer and a new analogue of cisplatin-<i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>. The study was conducted on two cell lines of ovarian cancer sensitive to Caov-3 cytostatics and the OVCAR-3 resistant cisplatin line. The study used the MTT (3-(4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide) cell viability assay, LDH (lactate dehydrogenase), and the quantitative evaluation method for measuring gene expression, i.e., qPCR with TagMan probes. Reduced survivability of OVCAR-3 and Caov-3 cells exposed to cytostatics at elevated temperatures (37 °C, 40 °C, 43 °C) was observed. Hyperthermia may increase the sensitivity of cells to platinum-based antineoplastic drugs and paclitaxel, which may be associated with the reduction of gene expression related to apoptotic processes.https://www.mdpi.com/1422-0067/21/6/2116anticancer drugscoordination compoundsgene expressionplatinumstructure–activity relationships
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Małgorzata Fabijańska Magdalena Orzechowska Agnieszka J. Rybarczyk-Pirek Justyna Dominikowska Alicja Bieńkowska Maciej Małecki Justyn Ochocki
spellingShingle	Małgorzata Fabijańska Magdalena Orzechowska Agnieszka J. Rybarczyk-Pirek Justyna Dominikowska Alicja Bieńkowska Maciej Małecki Justyn Ochocki Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin International Journal of Molecular Sciences anticancer drugs coordination compounds gene expression platinum structure–activity relationships
author_facet	Małgorzata Fabijańska Magdalena Orzechowska Agnieszka J. Rybarczyk-Pirek Justyna Dominikowska Alicja Bieńkowska Maciej Małecki Justyn Ochocki
author_sort	Małgorzata Fabijańska
title	Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin
title_short	Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin
title_full	Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin
title_fullStr	Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin
title_full_unstemmed	Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin
title_sort	simple <i>trans</i>-platinum complex bearing 3-aminoflavone ligand could be a useful drug: structure-activity relationship of platinum complex in comparison with cisplatin
publisher	MDPI AG
series	International Journal of Molecular Sciences
issn	1422-0067
publishDate	2020-03-01
description	Following previous studies devoted to <i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>, in this paper, the molecular structure and intermolecular interactions of the title complex are compared with other cisplatin analogues of which the crystal structures are presented in the Cambridge Structural Database (CSD). Molecular Hirshfeld surface analysis and computational methods were used to examine a possible relationship between the structure and anticancer activity of <i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>. The purpose of the article was also to investigate the effect of hyperthermia on the anticancer activity of cisplatin, cytostatics used in the treatment of patients with ovarian cancer and a new analogue of cisplatin-<i>trans</i>−Pt(3-af)<sub>2</sub>Cl<sub>2</sub>. The study was conducted on two cell lines of ovarian cancer sensitive to Caov-3 cytostatics and the OVCAR-3 resistant cisplatin line. The study used the MTT (3-(4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide) cell viability assay, LDH (lactate dehydrogenase), and the quantitative evaluation method for measuring gene expression, i.e., qPCR with TagMan probes. Reduced survivability of OVCAR-3 and Caov-3 cells exposed to cytostatics at elevated temperatures (37 °C, 40 °C, 43 °C) was observed. Hyperthermia may increase the sensitivity of cells to platinum-based antineoplastic drugs and paclitaxel, which may be associated with the reduction of gene expression related to apoptotic processes.
topic	anticancer drugs coordination compounds gene expression platinum structure–activity relationships
url	https://www.mdpi.com/1422-0067/21/6/2116
work_keys_str_mv	AT małgorzatafabijanska simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT magdalenaorzechowska simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT agnieszkajrybarczykpirek simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT justynadominikowska simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT alicjabienkowska simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT maciejmałecki simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin AT justynochocki simpleitransiplatinumcomplexbearing3aminoflavoneligandcouldbeausefuldrugstructureactivityrelationshipofplatinumcomplexincomparisonwithcisplatin
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Simple <i>Trans</i>-Platinum Complex Bearing 3-Aminoflavone Ligand Could Be a Useful Drug: Structure-Activity Relationship of Platinum Complex in Comparison with Cisplatin

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