<i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells
The conversion of betulinic acid (BA) to organic salts is a strategic approach to modulate its physicochemical properties and biological activity. In our previous study, we demonstrated the enhanced cytotoxicity of certain amino acid ethyl ester betulinates ([AAOEt][BA]) compared to BA against hormo...
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2025-01-01
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| author | Sonia Apostolova Irina Georgieva Paula Ossowicz-Rupniewska Joanna Klebeko Svetla Todinova Rumiana Tzoneva Maya Guncheva |
| author_facet | Sonia Apostolova Irina Georgieva Paula Ossowicz-Rupniewska Joanna Klebeko Svetla Todinova Rumiana Tzoneva Maya Guncheva |
| author_sort | Sonia Apostolova |
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| description | The conversion of betulinic acid (BA) to organic salts is a strategic approach to modulate its physicochemical properties and biological activity. In our previous study, we demonstrated the enhanced cytotoxicity of certain amino acid ethyl ester betulinates ([AAOEt][BA]) compared to BA against hormone-dependent breast cancer cells (MCF-7). In this study, we extended our investigation to evaluate the cytotoxic response and thermodynamic properties of hormone-independent breast cancer cells (MDA-MB-231) following 72 h of treatment with the same series of betulinates. Our data reveal a lower cytotoxic response in MDA-MB-231 cells, indicated by higher half-maximal inhibitory concentration (IC<sub>50</sub>) values, which ranged between 31 and 109 μM. Differential scanning calorimetry analysis supported these findings, showing negligible changes in the thermodynamic parameters of the treated MDA-MB-231 cells. However, consistent with our previous observations, [LysOEt][BA]<sub>2</sub>, exhibited the highest cytotoxicity and induced the most pronounced morphological alterations in the cancer cells. Overall, our results suggest that MDA-MB-231 cells are less sensitive to [AAOEt][BA] compared to MCF-7 cells, likely due to their distinct phenotypic and genotypic profiles and differences in oncogenic signalling pathways. Nonetheless, the fact that [LysOEt][BA]<sub>2</sub> enhances the cytotoxic activity of BA even in hormone-independent breast cancer cells underscores its therapeutic potential and warrants further investigation, particularly in the context of adjuvant breast cancer therapy. |
| format | Article |
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| issn | 2413-4155 |
| language | English |
| publishDate | 2025-01-01 |
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| spelling | doaj-art-74a88dc2ef3245679318bafadc5df12f2025-08-20T01:49:07ZengMDPI AGSci2413-41552025-01-0171210.3390/sci7010002<i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer CellsSonia Apostolova0Irina Georgieva1Paula Ossowicz-Rupniewska2Joanna Klebeko3Svetla Todinova4Rumiana Tzoneva5Maya Guncheva6Institute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Bl. 21, 1113 Sofia, BulgariaInstitute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Bl. 21, 1113 Sofia, BulgariaDepartment of Chemical Organic Technology and Polymeric Materials, Faculty of Chemical Technology and Engineering, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065 Szczecin, PolandDepartment of Chemical Organic Technology and Polymeric Materials, Faculty of Chemical Technology and Engineering, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065 Szczecin, PolandInstitute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Bl. 21, 1113 Sofia, BulgariaInstitute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Bl. 21, 1113 Sofia, BulgariaInstitute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., Bl. 9, 1113 Sofia, BulgariaThe conversion of betulinic acid (BA) to organic salts is a strategic approach to modulate its physicochemical properties and biological activity. In our previous study, we demonstrated the enhanced cytotoxicity of certain amino acid ethyl ester betulinates ([AAOEt][BA]) compared to BA against hormone-dependent breast cancer cells (MCF-7). In this study, we extended our investigation to evaluate the cytotoxic response and thermodynamic properties of hormone-independent breast cancer cells (MDA-MB-231) following 72 h of treatment with the same series of betulinates. Our data reveal a lower cytotoxic response in MDA-MB-231 cells, indicated by higher half-maximal inhibitory concentration (IC<sub>50</sub>) values, which ranged between 31 and 109 μM. Differential scanning calorimetry analysis supported these findings, showing negligible changes in the thermodynamic parameters of the treated MDA-MB-231 cells. However, consistent with our previous observations, [LysOEt][BA]<sub>2</sub>, exhibited the highest cytotoxicity and induced the most pronounced morphological alterations in the cancer cells. Overall, our results suggest that MDA-MB-231 cells are less sensitive to [AAOEt][BA] compared to MCF-7 cells, likely due to their distinct phenotypic and genotypic profiles and differences in oncogenic signalling pathways. Nonetheless, the fact that [LysOEt][BA]<sub>2</sub> enhances the cytotoxic activity of BA even in hormone-independent breast cancer cells underscores its therapeutic potential and warrants further investigation, particularly in the context of adjuvant breast cancer therapy.https://www.mdpi.com/2413-4155/7/1/2betulinic acidionic liquidstriple-negative breast cancercytotoxicitydifferential scanning calorimetry |
| spellingShingle | Sonia Apostolova Irina Georgieva Paula Ossowicz-Rupniewska Joanna Klebeko Svetla Todinova Rumiana Tzoneva Maya Guncheva <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells Sci betulinic acid ionic liquids triple-negative breast cancer cytotoxicity differential scanning calorimetry |
| title | <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells |
| title_full | <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells |
| title_fullStr | <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells |
| title_full_unstemmed | <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells |
| title_short | <i>In Vitro</i> Cytotoxicity Assessment of Betulinic Acid Organic Salts on Triple-Negative Breast Cancer Cells |
| title_sort | i in vitro i cytotoxicity assessment of betulinic acid organic salts on triple negative breast cancer cells |
| topic | betulinic acid ionic liquids triple-negative breast cancer cytotoxicity differential scanning calorimetry |
| url | https://www.mdpi.com/2413-4155/7/1/2 |
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