RESEARCH OF HEPATOPROTECTIVE ACTIVITY OF PYRIMIDINE DERIVATIVES IN VITRO

E. R. Kudoyarov; Кудояров Э. Р.; D. D. Karimov; Каримов Д. Д.; T. G. Kutlina; Кутлина Т. Г.; D. O. Karimov; Каримов Д. О.; G. F. Mukhammadieva; Мухаммадиева Г. Ф.; N. Yu. Khusnutdinova; Хуснутдинова Н. Ю.; K. V. Danilko; Данилко К. В.; A. R. Gimadieva; Гимадиева А. Р.; A. B. Bakirov; Бакиров А. Б.

doi:10.36946/0869-7922-2019-4-38-42

RESEARCH OF HEPATOPROTECTIVE ACTIVITY OF PYRIMIDINE DERIVATIVES IN VITRO

作者: Kudoyarov E.R.¹, Karimov D.D.¹, Kutlina T.G.¹, Karimov D.O.¹, Mukhammadieva G.F.¹, Khusnutdinova N.Y.¹, Danilko K.V.², Gimadieva A.R.³, Bakirov A.B.¹
隶属关系:
1. Ufa Research Institute of Occupational Medicine and Human Ecology
2. Bashkir State Medical University
3. Ufa Institute of Chemistry, Ufa Branch of RAS
期: 编号 4 (2019)
页面: 38-42
栏目: Articles
##submission.datePublished##: 04.06.2020
URL: https://innoscience.ru/0869-7922/article/view/641197
DOI: https://doi.org/10.36946/0869-7922-2019-4-38-42
ID: 641197

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The article presents data on experimental study of the hepatoprotective activity of pyrimidine derivatives (5-amino-6-methyluracil, 5-methylamino-6-methyluracil, 1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl N-phtalyl valinate, 5-piperidinomethyl-6-methyluracil, 3-morpholinomethyl-5-nitro-6-methyluracil) by incubation of mouse hepatocytes МН-22а poisoned with carbon tetrachloride. MTT-test was used to determine cell viability. Positive control was cells treated only with carbon tetrachloride (100 mM, 1% DMSO). Among compounds studied in this experiment 5-amino-6-methyluracil (400 µM) and 3-morpholinomethyl-5-nitro-6-methyluracil (50 µM) were the most effective for the survival of liver cells under seeding conditions. The increase in cell survival (relative to the values in the positive control group) under the conditions of tetrachloromethane priming and treatment with these drugs was up to 27,5% (p < 0,05) for 5-amino-6-methyluracil and 22,42% (p < 0,05) for 3-morpholinomethyl-5-nitro-6-methyluracil. The compounds 5-methylamino-6-methyluracil and 1,3,6-trimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl N-phtalyl valinate have low toxicity, but did not show antioxidant properties. The derivative 5-piperidinomethyl-6-methyluracil (400 µM) showed high toxicity (30,04 ± 0.90%; p < 0,05) and the survival of the cells treated with carbon tetrachloride was lower or equal to the values of positive control, which does not allow it to be used as an antioxidant.

关键词

pyrimidine, uracil, survival, antioxidant, in vitro

参考

Mashkovsky M.D. Medicines. Moscow: New wave; 2002 (in Russian).
Gimadieva A.R., Chernyshenko Yu.N., Abdrakhmanov I.B., Mustafin A.G. Synthesis, modifications and biological activity of uracils. Ufa: Gilem; 2013 (in Russian).
Myshkin V.A., Ibatullina R.B., Bakirov A.B. Liver damage by chemicals (functional and metabolic disorders, pharmacological correction). Ufa: Gilem; 2007 (in Russian).
Petrova I.V., Kataev V.A., Meshcheryakova S.A., Nikolaeva K.V., Munasipova D.A., Farkhutdinov R.R. Antioxidant properties of pyrimidine derivatives. Medical Bulletin of Bashkortostan. 2013; 8(4):64-7 (in Russian).
Samotrueva M.A., Tsibizova A.A., Yasenyavskaya A.L., Ozerov A.A., Tyurenkov I. N. Pharmacological activity of pyrimidine derivatives. Astrakhan Medical Journal. 2067(4):44-6 (in Russian).
Zimin Yu.S., Borisova N.S., Timerbaeva G.R., Gimadieva A.R., Mustafin A.G. Complexes of uracil derivatives with polyfunctional acids: preparation, toxicity and anti-inflammatory activity. Chemical and Pharmaceutical Journal. 2016; 50(10):226 (in Russian).
Grivennikova V.G., Vinogradov A.D. Generation of reactive oxygen species by mitochondria. // Advances in biological chemistry. 2013; 53:245-96 (in Russian).
de Fouw J. Environmental Health Criteria 208, Carbon Tetrachloride. Available at: http://www.inchem.org/documents/ehc/ehc/ehc208.htm. (Accessed 9 March 2019).
Gimadieva A.R., Khazimullina Yu.Z., Belaya E.A., Zimin Yu.S., Abdrakhmanov I.B., Mustafin A.G. Rapid assessment of antioxidant activity of uracil derivatives. Biomedical chemistry. 2015; 61(6):765-9 (in Russian).
STP-14.621.21.0008.12-20Methods of determining the cytotoxicity of MTT-test substances on the culture of normal human cells HEK-2Chernogolovka: IPAC Publ., 2015 (in Russian)

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RESEARCH OF HEPATOPROTECTIVE ACTIVITY OF PYRIMIDINE DERIVATIVES IN VITRO

全文:

详细

关键词

作者简介

E. Kudoyarov

D. Karimov

T. Kutlina

D. Karimov

G. Mukhammadieva

N. Khusnutdinova

K. Danilko

A. Gimadieva

A. Bakirov

参考

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