In-vitro antitumor activity of new quaternary phosphonium salts, derivatives of 3-hydroxypyridine
Iksanova A. G., Gabbasova R. R., Kupriyanova T. V., Akhunzyanov A. A., Pugachev M. V., Vafiva R. M., Shtyrlin N. V., Balakin K. V., Shtyrlin Y. G.
Anti-Cancer Drugs
Vol.29, Issue7, P. 682-690
Опубликовано: 2018
Тип ресурса: Статья
DOI:10.1097/CAD.0000000000000642
Аннотация:
This work presents the results of in-vitro biological activity studies of three novel anticancer agents, phosphonium salts based on the 3-hydroxypyridine scaffold, including one derivative of 4-deoxypyridoxine. Proliferation and viability of cells treated with these compounds was assessed by the colony formation and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Effects of the compounds on apoptosis and cell cycle were studied by flow cytometry using annexin V-FITC/propidium iodide and propidium iodide staining, respectively. The influence of the compounds on mitochondrial membrane potential and intracellular reactive oxygen species was evaluated using tetramethyl rhodamine ethyl and DCFHA staining. Western blot analysis was used to study the changes in the expression of Bcl-xL, Bax, and caspase-3 apoptotic proteins. The treatment of ovarian adenocarcinoma cells OVCAR-4 with the tested compounds inhibited the growth and induced cell cycle arrest in the G1 phase. 3
Ключевые слова:
3-hydroxypiridine; 4-deoxypyridoxine; apoptosis; cell cycle; cytotoxicity; OVCAR-4
3 hydroxypyridine derivative; antineoplastic agent; caspase 3; doxorubicin; phosphonium derivative; protein Bax; protein bcl xl; reactive oxygen metabolite; tetramethylrhodamine ethyl ester; antineoplastic activity; Article; cell cycle G1 phase; cell cycle M phase; cell cycle S phase; colony formation; controlled study; female; flow cytometry; G1 phase cell cycle checkpoint; human; human cell; in vitro study; mitochondrial membrane potential; ovary adenocarcinoma; priority journal; propidium iodide assay; protein expression; Western blotting
Язык текста: Английский
ISSN: 1473-5741
Iksanova A. G.
Gabbasova R. R.
Kupriyanova T. V.
Akhunzyanov A. A.
Pugachev M. V.
Vafiva R. M.
Shtyrlin N. V.
Balakin K. V. Konstantin Valeryevich 1970-
Shtyrlin Y. G.
Иксанова А. Г.
Габбасова Р. Р.
Куприянова Т. В.
Ахунзянов А. А.
Пугачев М. В.
Вафива Р. М.
Штyрлин Н. В.
Балакин К. В. Константин Валерьевич 1970-
Штyрлин Y. Г.
In-vitro antitumor activity of new quaternary phosphonium salts, derivatives of 3-hydroxypyridine
Текст визуальный непосредственный
Anti-Cancer Drugs
Lippincott Williams & Wilkins
Vol.29, Issue7 P. 682-690
2018
Статья
3-hydroxypiridine 4-deoxypyridoxine apoptosis cell cycle cytotoxicity OVCAR-4
3 hydroxypyridine derivative antineoplastic agent caspase 3 doxorubicin phosphonium derivative protein Bax protein bcl xl reactive oxygen metabolite tetramethylrhodamine ethyl ester antineoplastic activity Article cell cycle G1 phase cell cycle M phase cell cycle S phase colony formation controlled study female flow cytometry G1 phase cell cycle checkpoint human human cell in vitro study mitochondrial membrane potential ovary adenocarcinoma priority journal propidium iodide assay protein expression Western blotting
This work presents the results of in-vitro biological activity studies of three novel anticancer agents, phosphonium salts based on the 3-hydroxypyridine scaffold, including one derivative of 4-deoxypyridoxine. Proliferation and viability of cells treated with these compounds was assessed by the colony formation and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Effects of the compounds on apoptosis and cell cycle were studied by flow cytometry using annexin V-FITC/propidium iodide and propidium iodide staining, respectively. The influence of the compounds on mitochondrial membrane potential and intracellular reactive oxygen species was evaluated using tetramethyl rhodamine ethyl and DCFHA staining. Western blot analysis was used to study the changes in the expression of Bcl-xL, Bax, and caspase-3 apoptotic proteins. The treatment of ovarian adenocarcinoma cells OVCAR-4 with the tested compounds inhibited the growth and induced cell cycle arrest in the G1 phase. 3