Skip to main content
SpringerLink
Log in

Experimental Assessment of Additional Hormonal Activity of the Pregnane-Steroid Gestagen Gestobutanoyl

  • MOLECULAR-BIOLOGICAL PROBLEMS OF DRUG DESIGN AND MECHANISM OF DRUG ACTION
  • Published:
Pharmaceutical Chemistry Journal Aims and scope

The ability of gestobutanoyl, a pregnane steroid with progestogenic activity, to exhibit additional glucocorticoid, mineralocorticoid, antiandrogenic, and estrogenic effects in rats has been studied. It was found that gestobutanoyl did not have estrogenic activity because it did not increase the weight of the uterus with prolonged (30 d) administration at a therapeutic dose of 0.25 mg/kg and doses 10 and 100 times higher. Gestobutanoyl at a dose of 2.5 mg/kg for 30 d did not show glucocorticoid activity because the thymus mass did not change. However, the thymus mass decreased by 25% (p ≤ 0.05) when gestobutanoyl was administered at a dose 100 times higher (25 mg/kg) than the therapeutic dose. Gestobutanoyl at a dose of 2.5 mg/kg reduced the expression of androgen receptor (AR) mRNA in the rat uterus by 3 times and, as previously shown, did not increase the weight of the prostate and levator ani muscle. The mineralocorticoid activity of gestobutanoyl tablets was studied using peroral administration for 14 d to female rats at doses 100 and 1000 times (2.5 and 25 mg/kg, respectively) the therapeutic dose. Diuresis did not decrease, water was not retained in the rat body, and electrolytes were excreted in the urine and were present in the urine at constant concentrations in all experimental groups, indicating the absence of side mineralocorticoid effects of gestobutanoyl tablets.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

References

  1. N. L. Shimanovsky, M. A. Epinetov, and M. Ya. Mel’nikov, Molecular and Nanopharmacology [in Russian], Nauka, Moscow (2010).

    Google Scholar 

  2. F. Z. Stanczyk, J. P. Hapgood, S. Winer, et al., Endocr. Rev., 34(2), 171 – 208 (2013); doi: 10.1210/er.2012–1008.

  3. O. A. Zeinalov, T. S. Savinova, V. A. Andryushina, et al., Biomeditsina, 3, 80 – 89 (2018).

    Google Scholar 

  4. P. V. Sergeev, T. A. Fedotcheva, V. M. Rzheznikov, et al., Vestn. Ross. Akad. Med. Nauk, No. 5, 27 – 32 (2007).

  5. T. A. Fedotcheva, V. A. Parshin, et al., RU Pat. No. 2,684,917, Apr. 16, 2019.

  6. N. I. Sheina, V. A. Parshin, V. V. Kolesnikova, et al., Khim. Farm. Zh., 54(5), 11 – 15 (2020); doi: 10.30906/0023-1134-2020-54-5-11-15; Pharm. Chem. J., 54(5), 439 – 443 (2020); doi: 10.1007/s11094-020-02219-6.

  7. E. N. Kareva, O. M. Oleinikova, V. O. Panov, et al., Vestn. Ross. Akad. Med. Nauk, No. 2, 48 – 59 (2012).

  8. A. V. Semeikin, A. S. Dukhanin, R. V. Samoilikov, et al., Eksp. Klin. Farmakol., 69(4), 43 – 46 (2006).

    CAS  PubMed  Google Scholar 

  9. A. V. Semeikin, E. N. Kareva, T. A. Fedotcheva, et al., Eksp. Klin. Farmakol., 79(9), 22 – 24 (2016).

    CAS  PubMed  Google Scholar 

  10. M. W. Pfaffl, Nucleic Acids Rev., 29(9), e45 (2001); doi: https://doi.org/10.1093/nar/29.9.e45.

    Article  CAS  Google Scholar 

  11. A. N. Mironov (ed.), Handbook for Preclinical Drug Trials [in Russian], Part 1, Grif i K, Moscow (2012).

  12. P. V. Sergeev, V. M. Rzheznikov, V. V. Korkhov, et al., Khim.-farm. Zh., 39(7), 20 – 22 (2005); Pharm. Chem. J., 39(7), 358 – 360 (2005).

  13. D. Africander, R. Louw, and J. P. Hapgood, Biochem. Biophys. Res. Commun., 433(3), 305 – 310 (2013); doi: https://doi.org/10.1016/j.bbrc.2013.02.086.

    Article  CAS  PubMed  Google Scholar 

  14. P. A. Arias-Loza, M. Muehlfelder, S. A. Elmore, et al., Toxicol. Pathol., 37(7), 969 – 982 (2009); doi: https://doi.org/10.1177/0192623309350475.

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  15. A. V. Semeikin, T. A. Fedotcheva, E. D. Sveshnikova, et al., Khim.-farm. Zh., 54(11), 3 – 8 (2020); doi: https://doi.org/10.30906/0023-1134-2020-54-11-3-8.

    Article  Google Scholar 

  16. E. S. Stepanova, L. M. Makarenkova, V. V. Chistyakov, et al., Khim.-farm. Zh., 52(12), 55 – 59 (2018); doi: 10.30906/0023-1134-2018-52-12-55-59; Pharm. Chem. J., 52(12), 1016 – 1020 (2019); doi: 10.1007/s11094-019-01944-x.

  17. D. G. McLeod, Cancer, 71, No. S3, 1046 – 1049 (1993); doi: https://doi.org/10.1002/1097-0142(19930201)71:3+

    Article  CAS  PubMed  Google Scholar 

Download references

Acknowledgments

The work was supported by RFBR Grant No. 19-015-00195a.

Author information

Authors and Affiliations

  1. Pirogov Russian National Research Medical University, Ministry of Healthcare, 1 Ostrovityanova St, Moscow, 117997, Russia

    T. A. Fedotcheva, N. I. Sheina, V. A. Parshin, A. V. Semeikin, V. A. Votyakov & N. L. Shimanovsky

Authors
  1. T. A. Fedotcheva
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. N. I. Sheina
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. V. A. Parshin
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. A. V. Semeikin
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. V. A. Votyakov
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. N. L. Shimanovsky
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to T. A. Fedotcheva.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 3, pp. 6 – 9, March, 2021.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Fedotcheva, T.A., Sheina, N.I., Parshin, V.A. et al. Experimental Assessment of Additional Hormonal Activity of the Pregnane-Steroid Gestagen Gestobutanoyl. Pharm Chem J 55, 215–218 (2021). https://doi.org/10.1007/s11094-021-02400-5

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11094-021-02400-5

Keywords

Search

Navigation