Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives

Abstract 10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was repo...

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Main Authors: Joanna Kurek, Krzysztof Myszkowski, Irena Okulicz-Kozaryn, Agnieszka Kurant, Ewa Kamińska, Michał Szulc, Błażej Rubiś, Mariusz Kaczmarek, Przemysław Ł. Mikołajczak, Marek Murias
Format: Article
Language:English
Published: Nature Portfolio 2021-04-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-021-88260-1
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author Joanna Kurek
Krzysztof Myszkowski
Irena Okulicz-Kozaryn
Agnieszka Kurant
Ewa Kamińska
Michał Szulc
Błażej Rubiś
Mariusz Kaczmarek
Przemysław Ł. Mikołajczak
Marek Murias
author_facet Joanna Kurek
Krzysztof Myszkowski
Irena Okulicz-Kozaryn
Agnieszka Kurant
Ewa Kamińska
Michał Szulc
Błażej Rubiś
Mariusz Kaczmarek
Przemysław Ł. Mikołajczak
Marek Murias
author_sort Joanna Kurek
collection DOAJ
description Abstract 10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was reported and tested compounds showed to be more active than commonly used doxorubicin. Some of tested C-10 alkylthiolated colchicines have been found to exhibit cytotoxicity at levels comparable to that of the natural product—colchicine. 10-Methylthiocolchicine has IC50 = 8 nM and 10-ethylthiocolchicine has IC50 = 47 nM in comparison to colchicine IC50 = 37 nM. Moreover for 10-alkylthioderivatives apoptosis test, cyclin B1 and cell cycle tests were performed. 10-n-Butylthiocolchicine was tested for anti-inflammatory and analgesic activities it showed to produce analgesic rather than anti-inflammatory effect.
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spelling doaj.art-26cede43fda54840a3c5a6bd12d371212022-12-21T21:20:38ZengNature PortfolioScientific Reports2045-23222021-04-0111111210.1038/s41598-021-88260-1Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivativesJoanna Kurek0Krzysztof Myszkowski1Irena Okulicz-Kozaryn2Agnieszka Kurant3Ewa Kamińska4Michał Szulc5Błażej Rubiś6Mariusz Kaczmarek7Przemysław Ł. Mikołajczak8Marek Murias9Department of Bioactive Products, Faculty of Chemistry, Adam Mickiewicz UniversityDepartment of Toxicology, Poznań University of Medical SciencesDepartment of Pharmacology, Poznań University of Medical SciencesDepartment of Pharmacology, Poznań University of Medical SciencesDepartment of Pharmacology, Poznań University of Medical SciencesDepartment of Pharmacology, Poznań University of Medical SciencesDepartment of Clinical Chemistry and Molecular Diagnostics, Poznań University of Medical SciencesDepartment of Cancer Immunology, Chair of Medical Biotechnology, Poznan University of Medical SciencesDepartment of Pharmacology, Poznań University of Medical SciencesDepartment of Toxicology, Poznań University of Medical SciencesAbstract 10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was reported and tested compounds showed to be more active than commonly used doxorubicin. Some of tested C-10 alkylthiolated colchicines have been found to exhibit cytotoxicity at levels comparable to that of the natural product—colchicine. 10-Methylthiocolchicine has IC50 = 8 nM and 10-ethylthiocolchicine has IC50 = 47 nM in comparison to colchicine IC50 = 37 nM. Moreover for 10-alkylthioderivatives apoptosis test, cyclin B1 and cell cycle tests were performed. 10-n-Butylthiocolchicine was tested for anti-inflammatory and analgesic activities it showed to produce analgesic rather than anti-inflammatory effect.https://doi.org/10.1038/s41598-021-88260-1
spellingShingle Joanna Kurek
Krzysztof Myszkowski
Irena Okulicz-Kozaryn
Agnieszka Kurant
Ewa Kamińska
Michał Szulc
Błażej Rubiś
Mariusz Kaczmarek
Przemysław Ł. Mikołajczak
Marek Murias
Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
Scientific Reports
title Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
title_full Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
title_fullStr Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
title_full_unstemmed Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
title_short Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives
title_sort cytotoxic analgesic and anti inflammatory activity of colchicine and its c 10 sulfur containing derivatives
url https://doi.org/10.1038/s41598-021-88260-1
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