Advances in Molecular OncologyAdvances in Molecular OncologyУспехи молекулярной онкологии2313-805X2413-3787Publishing House ABV Press7110.17650/2313-805X-2016-3-3-67-72RESEARCH ARTICLESЭКСПЕРИМЕНТАЛЬНЫЕ СТАТЬИAntitumor effect of the curaxin CBL0137 on the models of colon cancerПротивоопухолевое действие кураксина CBL0137 на моделях аденокарциномы толстой кишкиFetisovT. I.ФетисовТ. И.
Russian Federation
TilovaL. R.ТиловаЛ. Р.
Russian Federation
LesovayaE. A.ЛесоваяЕ. А.
Russian Federation
AntoshinaE. E.АнтошинаЕ. Е.
Russian Federation
Gor’kovaT. G.ГорьковаТ. Г.
Russian Federation
TrukhanovaL. S.ТрухановаЛ. С.
Russian Federation
MorozovaO. V.МорозоваО. В.
Russian Federation
ShipaevaE. V.ШипаеваЕ. В.
Russian Federation
IvanovR. V.ИвановР. В.
Russian Federation
PurmalA. A.ПурмальА. А.
Russian Federation
BelitskiyG. A.БелицкийГ. А.
Russian Federation
YakubovskayaM. G.ЯкубовскаяМ. Г.
Russian Federation
GudkovA. V.ГудковА. В.
Russian Federation
GurovaK. V.ГуроваК. В.
Russian Federation
KirsanovK. I.КирсановК. И.
Russian Federation
mrkir@rambler.ruN.N. Blokhin Russian Cancer Reseach Center, Ministry of Health of RussiaФГБУ «Российский онкологический научный центр им. Н. Н. Блохина» Минздрава России24 Kashirskoe Shosse, Moscow, 115478, RussiaРоссия, 115478, Москва, Каширское шоссе, 2424 Kashirskoe Shosse, Moscow, 115478, Russia I.P. Pavlov Ryazan’ State Medical University, Ministry of Health of RussiaРоссия, 115478, Москва, Каширское шоссе, 24 ФГБОУ ВО «Рязанский государственный медицинский университет им. И. П. Павлова» Минздрава России9 Vasokovol’tnaya St., Ryazan, 390026, RussiaРоссия, 390026, Рязань, ул. Высоковольтная, 924 Kashirskoe Shosse, Moscow, 115478, RussiaРоссия, 115478, Москва, Каширское шоссе, 2424 Kashirskoe Shosse, Moscow, 115478, RussiaРоссия, 115478, Москва, Каширское шоссе, 24LLC IncuronООО «Инкурон»6 Stolovyy Pereulok, Moscow, 121069, RussiaРоссия, 121069, Москва, Столовый переулок, 6LLC Incuron6 Stolovyy Pereulok, Moscow, 121069, RussiaООО «Инкурон»Россия, 121069, Москва, Столовый переулок, 6Roswell Park Cancer InstituteBuffalo, USAОнкологический центр Розвел ПаркN.N. Blokhin Russian Cancer Reseach Center, Ministry of Health of RussiaСША, Баффало24 Kashirskoe Shosse, Moscow, 115478, RussiaФГБУ «Российский онкологический научный центр им. Н. Н. Блохина» Минздрава РоссииRoswell Park Cancer InstituteРоссия, 115478, Москва, Каширское шоссе, 24Buffalo, USAОнкологический центр Розвел ПаркRoswell Park Cancer InstituteСША, БаффалоBuffalo, USAОнкологический центр Розвел ПаркN.N. Blokhin Russian Cancer Reseach Center, Ministry of Health of RussiaФГБУ «Российский онкологический научный центр им. Н. Н. Блохина» Минздрава РоссииРоссия, 115478, Москва, Каширское шоссе, 24150920163367723009201630092016Copyright ©; 2016, Fetisov T.I., Tilova L.R., Lesovaya E.A., Antoshina E.E., Gor’kova T.G., Trukhanova L.S., Morozova O.V., Shipaeva E.V., Ivanov R.V., Purmal A.A., Belitskiy G.A., Yakubovskaya M.G., Gudkov A.V., Gurova K.V., Kirsanov K.I.Copyright ©; 2016, Фетисов Т.И., Тилова Л.Р., Лесовая Е.А., Антошина Е.Е., Горькова Т.Г., Труханова Л.С., Морозова О.В., Шипаева Е.В., Иванов Р.В., Пурмаль А.А., Белицкий Г.А., Якубовская М.Г., Гудков А.В., Гурова К.В., Кирсанов К.И.2016Fetisov T.I., Tilova L.R., Lesovaya E.A., Antoshina E.E., Gor’kova T.G., Trukhanova L.S., Morozova O.V., Shipaeva E.V., Ivanov R.V., Purmal A.A., Belitskiy G.A., Yakubovskaya M.G., Gudkov A.V., Gurova K.V., Kirsanov K.I.Фетисов Т.И., Тилова Л.Р., Лесовая Е.А., Антошина Е.Е., Горькова Т.Г., Труханова Л.С., Морозова О.В., Шипаева Е.В., Иванов Р.В., Пурмаль А.А., Белицкий Г.А., Якубовская М.Г., Гудков А.В., Гурова К.В., Кирсанов К.И.https://creativecommons.org/licenses/by/4.0https://umo.abvpress.ru/jour/article/view/71

Curaxins represent low molecular weight carbazole derivatives, which simultaneously activate p53-dependent apoptosis and inhibit NF-kBdependent signal transduction pathways. Antitumor activity of curaxin CBL0137 was demonstrated in vivo on the model of solid transplantable mouse colon adenocarcinoma Akatol. Significant tumor growth inhibition caused by CBL0137 treatment was observed. On the 37th day after tumor transplantation for CBL0137 oral doses 5, 10, 15 and 20 mg/kg the tumor growth inhibition indexes were 53, 50, 56 and 74 %, respectively. CBL0137 treatment extended life span of mice in all study groups receiving this test article. Maximum lifespan increase (81,7 %) was observed in the group of mice treated with 20 mg/kg dose of CBL0137. The cytotoxicity of CBL0137 was assessed on human colon cancer cells in vitro. We demonstrated that CBL0137 inhibits the expression COX2, which in its turn is known to exhibit antiapoptotic, pro-angiogenic and pro- metastatic properties. Thus, we demonstrated antitumor effect of CBL0137 against colon cancer in vitro and in vivo.

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