Bilai I. M., Tsys O. V., Ivanchenko D. G., Romanenko M. I.


About the author:

Bilai I. M., Tsys O. V., Ivanchenko D. G., Romanenko M. I.



Type of article:

Scentific article


The problem of hyperlipidemia is one of the leading risk factors for cardiovascular diseases and the progression of their complications in the population. Despite the high hypolipidemic effect, the group of statins has a few disadvantages associated with both economic feasibility for patients and significant side effects. The creation of new highly effective and low-toxic drugs with a wide range of biological activity and their introduction into clinical practice is an important target of pharmacological and medical science. The purpose of this study is to investigate acute toxicity of synthesized 3-methyl-(1,3-dimethyl)-7-β-hydroxy-γaryloxypropyloxanthiniol-8-tioaxic acid derivatives in laboratory rats. Object and methods of the study. For the study of acute toxicity, 4 groups of animals were used, with 2 observations each with the additional use of one previous and subsequent dose. The compounds were administered to laboratory animals following the aseptic and antiseptic rules in the form of a fine aqueous suspension, which was stabilized with tween-80 at the rate of 0.2 ml tween-80 per 50 mg of the substance. Observations were made after 24 hours. In our studies, the acute toxicity of 20 compounds of 3-methyl-(1,3-dimethyl) -7-β-hydroxy-γ-aryloxypropylxanthinyl8-thioacetic acid derivatives was studied. The analysis of the studies was performed according to the classification of K.K. Sidorov. Results and their discussion. Analysis of the data obtained showed that the acute toxicity of new compounds obtained is in the range of 304–668 mg/kg. According to Sidorov’s classification, all synthesized 3-methyl (1,3-dimethyl)-7-β-hydroxy-γ-aryloxypropylxanthynyl-8-thioacetic acid derivatives turned out to be low toxic substances and belong to the III-IV toxicity classes (low toxic and moderately toxic substances) with intragastric administration. It has been established that among the studied substances, compound 6042 was the most toxic, and the least toxic – 6049. Conclusions.The study has found that synthesized 3-methyl-(1,3-dimethyl)-7-β-hydroxy-γ-aryloxypropylxanthynyl8-thioacetic acid derivatives turned out to be low toxic substances and belong to the III-IV toxicity classes. This experiment reflects the promise of research into this class of safe chemicals in further pharmacological experiments.


xanthines, acute toxicity, hyperlipidemia.


  1. Zodda D, Giammona R, Schifilliti S. Treatment Strategy for Dyslipidemia in Cardiovascular Disease Prevention: Focus on Old and New Drugs. Pharmacy (Basel). 2018 Jan 21;6(1):pii:E10.
  2.  Mihin VP, Vorotyintseva VV, Zhilyaeva YuA, Chernyatina MA, Gromnatskiy NI, Suschenya OA. Gipolipidemicheskaya terapiya segodnya: novyie zadachi i vozmozhnosti statinov. Meditsinskiy sovet. 2018;5:48-53. [in Russiаn].
  3.  Toth P, Patti A, Giglio R, Nikolic D, Castellino G, Rizzo M, et al. Management of Statin Intolerance in 2018: Still More Questions Than Answers. American Journal Of Cardiovascular Drugs. 2018;18(3):157-73.
  4. Bilai IM, Ostapenko AA, Romanenko NI, Krasko NP. Vliyanie 7-(2-gidroksi-3-izopropoksipropil)-3-metil-8-(4-metilpiperidin-1-il)-ksantina na pokazateli lipidnogo obmena. Zaporozhskiy meditsinskiy zhurnal. 2011;13(3):120-3. [in Russiаn].
  5. Lukyanchuk VD. Toksikometriya lekarstvennyih sredstv na doklinicheskom etape: sostoyanie problemyi, diskussionnyie aspektyi (obzor literaturyi). Sovremennyie problemyi toksikologi. 1998;2:12-4. [in Russiаn].
  6. Prozorovskiy VB. Statisticheskaya obrabotka rezultatov farmakologicheskih issledovaniy. Psihofarmakologiya i biologicheskaya narkologiya. 2007;7(3-4):2090-120. [in Russiаn].
  7. Sidorov KK. O klassifikatsii toksichnosti yadov pri parenteralnyih sposobah vvedeniya. Toksikologiya novyih prom. veschestv. 1973;13:45-71. [in Russiаn].

Publication of the article:

«Bulletin of problems biology and medicine» Issue 3 (152), 2019 year, 77-79 pages, index UDK 547.857.4’298.71’53.024’491.4:615.015.35].074