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Vol. 21, Art. 49 (pp. 603-612)    |    2020       

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Toxicological assessment original clathrate complex 3- (2-phenylethyl) -2-thioxo-1,3-thiazolidine-4-one with a single administration betadeksom rabbits

All-Russian Research Institute of Physiology, Biochemistry and Animal Nutrition - a branch of the Federal Science Center of Animal Husbandry named after Academy Member L.K. Ernst, Kaluga Region, Russian Federation, 249013, Kaluga Region, Borovsk, pos. Institute, 8-495-996-34-15, bifip@kaluga.ru
- Research Center "Park of Active Molecules", Obninsk, Kaluga Region, Russia, 249031, Kaluga Region, Obninsk, ul. Kiev highway, 3, 8-484-39 -9-72-58, biomed@pam-alliance.ru;
- Research Institute of Human Morphology, 117418, Moscow, ul. Tsyurupy, d. 3, 8-499-120-80-65, morfolhum@mail.ru

Brief summary

The clathrate complex 3- (2-phenylethyl) -2-thioxo-1,3 thiazolidin-4-one was first obtained by the solid-phase synthesis method on a planetary ball mill and has a crystalline form in the form of nanoparticles with an average particle size of 40.5 nm. A toxicological assessment of the developed clathrate complex of 3- (2-phenylethyl) -2-thioxo-1,3 thiazolidin-4-one with betadex was carried out with a single intragastric administration to Soviet Chinchilla rabbits in doses of 42 and 84 mg / kg body weight. For the first time, it was revealed that the clathrate complex 3- (2-phenylethyl) -2-thioxo-1,3 thiazolidin-4-one with betadex with a single intragastric administration to rabbits in the studied toxic doses is well tolerated by animals and, according to biochemical tests, does not affect on the functional state of the main internal organs and the morphological composition of peripheral blood.


Key words

rabbits, toxicological assessment, biochemical parameters, blood morphological composition, betadex, 3- (2-phenylethyl) -2-thioxo-1,3 thiazolidin-4-one, clathrate complex.

Reference list

1. Javoronkov L.P. Osnovi prikladnoi mediko-biologicheskoi statistiki. Metodicheskoe posobie. Obninsk: FGBY MRNC Minzdravsocrazvitiya Rossii, 2012. 60 s.


2. Zemlyanoi R.A. Erimbetov K.T., Bondarenko E.V., Goncharova A.Ya., Frog E.S Sozdanie klatratnogo kompleksa β-ciklodekstrina s proizvodnim rodanina // Eksperimentalnaya i klinicheskaya farmakologiya. 2018. Tom 81. s. 91.


3. Kondrasheva I.G., Bondarenko E.V., Erimbetov K.T., Kalashnikova E.E., Goncharova A.Ya. /Issledovanie protivoopyholevoi aktivnosti originalnogo proizvodnogo rodanina PAM-14 na modeli Karcinomi legkogo Lewis // Sbornik tezisov Sechenovskogo Mejdynarodnogo Biomedicinskogo Sammita 2017 (SMBS-2017), 16-20 iunya 2017 g., Moskva. M.: Izdatelstvo FGAOY VO Pervii MGMY im. I.M. Sechenova Minzdrava Rossii, 2017. - 106 s. - c. 69-70.


4. Rykovodstvo po eksperimentalnomy (doklinicheskomy) izycheniu novih farmakologicheskih veshestv / Pod obshei redakciei chlen-korr. RAMN, prof. R.Y.Habrieva. 2-e izd., pererab. i dop. - M. - OAO «Izdatelstvo «Medicina». - 2005. - 832 s.


5. Rykovodstvo po provedeniu doklinicheskih issledovanii lekarstvennih sredstv. Chast pervaya. - Mironov A.N., Bytyanyan N.D., Vasilev A.N.,. Verstakova O.L., Jyravleva M.V., Lepahin V.K., Korobov N.V., Merkylov V.A., Orehov S.N., Sakaeva I.V., Yteshev D.B., Yavorskii A.N. - M.: Grif i K, 2012. - 944 s.


6. Roziev R.A., Goncharova A.Ya., Erimbetov K.T., Podgorodnichenko V.K., Homichenok V.V., Novojilova N.E. Proizvodnoe rodanina i sredstvo dlya profilaktiki opyholevih zabolevanii//Patent na izobretenie RF 2521390. Opyblikovano 27.06.2014 Bul. 18.


7. Roziev R.A., Goncharova A.Ya., Erimbetov K.T., Podgorodnichenko V.K., Homichenok V.V. Sredstvo, obladaushee antiproliferativnim i antimetastaticheskim deistviem, dlya lecheniya opyholevih zabolevanii// Patent na izobretenie RF 2522449. Opyblikovano 10.07.2014 Bul. ? 19.


8. Erimbetov K.T. Phenotypic regulation of animal skeletal muscle protein metabolism / Erimbetov K.T., Obvintseva O.V., Fedorova A.V., Zemlyanoy R.A., Solovieva A.G. // Ukrainian Journal of Ecology. - 2019. - T. 9. - 4. - S. 651-656.


9. Martinez A., Alonso M., Castro A., Dorronsoro I., Gelpí J. L., Luque F. J., Pérez C., Moreno F. J. (2005). SAR and 3D-QSAR Studies on Thiadiazolidinone Derivatives: Exploration of Structural Requirements for Glycogen Synthase Kinase 3 Inhibitors. J Med Chem, 48, 7103-7112.


10. Martinez A., Alonso M., Castro A., Pérez C., Moreno F. J. (2002). First Non-ATP Competitive Glycogen Synthase Kinase 3 â (GSK-3â) Inhibitors:Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer?s. J Med Chem, 45, 1292-1299.


11. Ravinder Singh Bhatti. Recent Pharmacological Developments on Rhodanines and 2,4-Thiazolidinediones / Ravinder Singh Bhatti, Sakshi Shah, Suresh, Pawan Krishan, Jagir S. Sandhu //Int. J. Med. Chem.-2013.-Vol 2013. Article ID 793260 - 16 pages. http://dx.doi.org/10.1155/2013/793260.


REFERENCES


1. Zhavoronkov L.P. Fundamentals of applied biomedical statistics. Toolkit. Obninsk: FSBI MRRC of the Ministry of Health and Social Development of Russia, 2012. 60 p. [In Russian].


2. Zemlyanoy R.A. Erimbetov K.T., Bondarenko E.V., Goncharova A.Ya., Frog E.S. Development of a clathrate complex of β-cyclodextrin with a derivative of rhodanine // Experimental and Clinical Pharmacology. 2018.Vol. 81. p. 91. [In Russian].


3. Kondrasheva I.G., Bondarenko E.V., Erimbetov K.T., Kalashnikova E.E., Goncharova A.Ya. / Study of the antitumor activity of the original PAM-14 throat derivative on the Lewis lung carcinoma model // Abstracts of Sechenov International Biomedical Summit 2017 (SMBS-2017), June 16-20, 2017, Moscow. M .: Publishing house FSAEI HE First MGMU them. THEM. Sechenova of the Ministry of Health of Russia, 2017 .-- 106 p. - c. 69-70. [In Russian].


4. Guidance on the experimental (preclinical) study of new pharmacological substances / Edited by the corresponding member. RAMS, prof. R.U. Khabrieva. 2nd ed., Revised. and add. - M. - JSC "Publishing house" Medicine ". - 2005. - 832 p. [In Russian].


5. Guidelines for preclinical studies of drugs. Part one. - Mironov A.N., Butyanyan N.D., Vasiliev A.N.,. Verstakova O.L., Zhuravleva M.V., Lepakhin V.K., Korobov N.V., Merkulov V.A., Orekhov S.N., Sakaeva I.V., Uteshev D.B., Yavorsky A .N. - M.: Grif and K, 2012 .- 944 p. [In Russian].


6. Roziev R.A., Goncharova A.Ya., Erimbetov K.T., Podgorodnichenko V.K., Khomichenok V.V., Novozhilova N.E. A derivative of rodanin and a means for the prevention of tumor diseases // Patent for the invention of the Russian Federation No. 2521390. Published on June 27, 2014 Bull. Number 18. [In Russian].


7. Roziev R.A., Goncharova A.Ya., Erimbetov K.T., Podgorodnichenko V.K., Khomichenok V.V. An agent with antiproliferative and antimetastatic action for the treatment of tumor diseases // Patent for the invention of the Russian Federation No. 2522449. Published on July 10, 2014 Bull. Number 19. [In Russian].


8. Erimbetov K.T. Phenotypic regulation of animal skeletal muscle protein metabolism / Erimbetov K.T., Obvintseva O.V., Fedorova A.V., Zemlyanoy R.A., Solovieva A.G. // Ukrainian Journal of Ecology. - 2019. - T. 9. - ? 4. - S. 651-656.


9. Martinez A., Alonso M., Castro A., Dorronsoro I., Gelpí J. L., Luque F. J., Pérez C., Moreno F. J. (2005). SAR and 3D-QSAR Studies on Thiadiazolidinone Derivatives: Exploration of Structural Requirements for Glycogen Synthase Kinase 3 Inhibitors. J Med Chem, 48, 7103-7112.


10. Martinez A., Alonso M., Castro A., Pérez C., Moreno F. J. (2002). First Non-ATP Competitive Glycogen Synthase Kinase 3 â (GSK-3â) Inhibitors:Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer?s. J Med Chem, 45, 1292-1299.


11. Ravinder Singh Bhatti. Recent Pharmacological Developments on Rhodanines and 2,4-Thiazolidinediones / Ravinder Singh Bhatti, Sakshi Shah, Suresh, Pawan Krishan, Jagir S. Sandhu //Int. J. Med. Chem.-2013.-Vol 2013. Article ID 793260 - 16 pages. http://dx.doi.org/10.1155/2013/793260.