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Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes

Authorized Users Only
2018
Authors
Dobričić, Vladimir
Drvenica, Ivana
Stancić, Ana
Mihailović, Marija
Čudina, Olivera
Bugarski, Diana
Ilić, Vesna
Article (Published version)
Metadata
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Abstract
The biological activity of three previously synthesized 17 beta-carboxamide glucocorticoids (BG, BEG, and MPEA) was tested in vitro on mitogen stimulated and non-stimulated peripheral blood mononuclear cells (MNCs) and granulocytes from human healthy donors, and the results were compared to the conventional glucocorticoid dexamethasone. The tested 17 beta-carboxamide glucocorticoids did not induce decreases in MNC viability and proliferation, while modulation of reactive oxygen species (ROS) synthesis in granulocytes was dependent on the cell donor. The obtained results indicate the possibility of avoidance of strong lymphocyte suppression, which is generally recognized during administration of conventional glucocorticoids. Furthermore, the metabolism of the tested derivatives was predicted in silico. The predicted metabolites were synthesized and the in silico results were confirmed by in vitro evaluation of the metabolism of BG, BEG, and MPEA in human serum and in cultures of periphe...ral blood MNCs. The results of the biological activity and metabolism evaluation and of previous in vivo evaluations of biological activity indicate the soft drug nature of BG, BEG, and MPEA. In order to be fully considered as soft glucocorticoids, further investigations on the toxicity and activity of the formed metabolites are required.

Keywords:
anti-inflammatory activity / metabolism / peripheral blood mononuclear cells / granulocytes
Source:
Archiv der Pharmazie, 2018, 351, 5
Publisher:
  • Wiley-VCH Verlag GMBH, Weinheim
Funding / projects:
  • Regenerative and modulatory potential of adult stem cells (RS-175062)

DOI: 10.1002/ardp.201700371

ISSN: 0365-6233

PubMed: 29660818

WoS: 000431489000004

Scopus: 2-s2.0-85045727394
[ Google Scholar ]
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/3162
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Dobričić, Vladimir
AU  - Drvenica, Ivana
AU  - Stancić, Ana
AU  - Mihailović, Marija
AU  - Čudina, Olivera
AU  - Bugarski, Diana
AU  - Ilić, Vesna
PY  - 2018
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3162
AB  - The biological activity of three previously synthesized 17 beta-carboxamide glucocorticoids (BG, BEG, and MPEA) was tested in vitro on mitogen stimulated and non-stimulated peripheral blood mononuclear cells (MNCs) and granulocytes from human healthy donors, and the results were compared to the conventional glucocorticoid dexamethasone. The tested 17 beta-carboxamide glucocorticoids did not induce decreases in MNC viability and proliferation, while modulation of reactive oxygen species (ROS) synthesis in granulocytes was dependent on the cell donor. The obtained results indicate the possibility of avoidance of strong lymphocyte suppression, which is generally recognized during administration of conventional glucocorticoids. Furthermore, the metabolism of the tested derivatives was predicted in silico. The predicted metabolites were synthesized and the in silico results were confirmed by in vitro evaluation of the metabolism of BG, BEG, and MPEA in human serum and in cultures of peripheral blood MNCs. The results of the biological activity and metabolism evaluation and of previous in vivo evaluations of biological activity indicate the soft drug nature of BG, BEG, and MPEA. In order to be fully considered as soft glucocorticoids, further investigations on the toxicity and activity of the formed metabolites are required.
PB  - Wiley-VCH Verlag GMBH, Weinheim
T2  - Archiv der Pharmazie
T1  - Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes
VL  - 351
IS  - 5
DO  - 10.1002/ardp.201700371
ER  - 
@article{
author = "Dobričić, Vladimir and Drvenica, Ivana and Stancić, Ana and Mihailović, Marija and Čudina, Olivera and Bugarski, Diana and Ilić, Vesna",
year = "2018",
abstract = "The biological activity of three previously synthesized 17 beta-carboxamide glucocorticoids (BG, BEG, and MPEA) was tested in vitro on mitogen stimulated and non-stimulated peripheral blood mononuclear cells (MNCs) and granulocytes from human healthy donors, and the results were compared to the conventional glucocorticoid dexamethasone. The tested 17 beta-carboxamide glucocorticoids did not induce decreases in MNC viability and proliferation, while modulation of reactive oxygen species (ROS) synthesis in granulocytes was dependent on the cell donor. The obtained results indicate the possibility of avoidance of strong lymphocyte suppression, which is generally recognized during administration of conventional glucocorticoids. Furthermore, the metabolism of the tested derivatives was predicted in silico. The predicted metabolites were synthesized and the in silico results were confirmed by in vitro evaluation of the metabolism of BG, BEG, and MPEA in human serum and in cultures of peripheral blood MNCs. The results of the biological activity and metabolism evaluation and of previous in vivo evaluations of biological activity indicate the soft drug nature of BG, BEG, and MPEA. In order to be fully considered as soft glucocorticoids, further investigations on the toxicity and activity of the formed metabolites are required.",
publisher = "Wiley-VCH Verlag GMBH, Weinheim",
journal = "Archiv der Pharmazie",
title = "Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes",
volume = "351",
number = "5",
doi = "10.1002/ardp.201700371"
}
Dobričić, V., Drvenica, I., Stancić, A., Mihailović, M., Čudina, O., Bugarski, D.,& Ilić, V.. (2018). Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes. in Archiv der Pharmazie
Wiley-VCH Verlag GMBH, Weinheim., 351(5).
https://doi.org/10.1002/ardp.201700371
Dobričić V, Drvenica I, Stancić A, Mihailović M, Čudina O, Bugarski D, Ilić V. Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes. in Archiv der Pharmazie. 2018;351(5).
doi:10.1002/ardp.201700371 .
Dobričić, Vladimir, Drvenica, Ivana, Stancić, Ana, Mihailović, Marija, Čudina, Olivera, Bugarski, Diana, Ilić, Vesna, "Investigation of metabolic properties and effects of 17 beta-carboxamide glucocorticoids on human peripheral blood leukocytes" in Archiv der Pharmazie, 351, no. 5 (2018),
https://doi.org/10.1002/ardp.201700371 . .

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