Cytostatic Activity and Ligand-Receptor Interaction Energy of the Novel Russian-Produced Gestagen Gestobutanoil and its Metabolites

Semeikin, A. V.; Федотчева, Т. А.; Sveshnikova, E. D.; Shilov, B. V.; Smirnov, A. S.; Шимановский, Н. Л.

doi:10.1007/s11094-021-02326-y

Cited by 4 publications

(2 citation statements)

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“…Based on the previously obtained data on IC 50 in various cell cultures for steroids with different substituents at the C3 carbon atom of the cyclopentane perhydrophenanthrene ring, which ranged from 7 to 87 μM with 48 h incubation [ 40 , 43 ], we used a fixed concentration of steroids of 10 μM for the primary screening of cytotoxicity.…”

Section: Resultsmentioning

confidence: 99%

“…Solutions of the compounds were added to final concentrations of 10 −5 M and incubated for 24 h. The DMSO concentration did not exceed 0.01%, and the control wells contained an equal volume of DMSO at each point. Thereafter, culture viability was assessed using a standard MTT assay [ 40 ]. After the completion of the incubation of cells with the compounds, the medium was taken from the wells of the plate, after which 200 µL of DMEM F12 1:1 medium and 10 µL of the stock MTT solution (10 mg/mL, Diam, Moscow, Russia) were added to the wells.…”

Section: Methodsmentioning

confidence: 99%

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The Effects of the Steroids 5-Androstenediol and Dehydroepiandrosterone and Their Synthetic Derivatives on the Viability of K562, HeLa, and Wi-38 Cells and the Luminol-Stimulated Chemiluminescence of Peripheral Blood Mononuclear Cells from Healthy Volunteers

Sokolov,

Rozhkov,

Uspenskaya

et al. 2024

Biomolecules

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In order to evaluate the role of substituents at 3-C and 17-C in the cytotoxic and cytoprotective actions of DHEA and 5-AED molecules, their derivatives were synthesized by esterification using the corresponding acid anhydrides or acid chlorides. As a result, seven compounds were obtained: four DHEA derivatives (DHEA 3-propionate, DHEA 3-butanoate, DHEA 3-acetate, DHEA 3-methylsulfonate) and three 5-AED derivatives (5-AED 3-butanoate, 5-AED 3,17-dipropionate, 5-AED 3,17-dibutanoate). All of these compounds showed micromolar cytotoxic activity toward HeLa and K562 human cancer cells. The maximum cytostatic effect during long-term incubation for five days with HeLa and K562 cells was demonstrated by the propionic esters of the steroids: DHEA 3-propionate and 5-AED 3,17-dipropionate. These compounds stimulated the growth of normal Wi-38 cells by 30–50%, which indicates their cytoprotective properties toward noncancerous cells. The synthesized steroid derivatives exhibited antioxidant activity by reducing the production of reactive oxygen species (ROS) by peripheral blood mononuclear cells from healthy volunteers, as demonstrated in a luminol-stimulated chemiluminescence assay. The highest antioxidant effects were shown for the propionate ester of the steroid DHEA. DHEA 3-propionate inhibited luminol-stimulated chemiluminescence by 73% compared to the control, DHEA, which inhibited it only by 15%. These data show the promise of propionic substituents at 3-C and 17-C in steroid molecules for the creation of immunostimulatory and cytoprotective substances with antioxidant properties.

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Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%