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Probing the selective antitumor activity of 22-oxo-26-selenocyanocholestane derivatives
María A Fernández-Herrera1, Jesús Sandoval-Ramírez1, Luis Sánchez-Sánchez2
1Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, Ciudad Universitaria, 72570 Puebla, PUE, Mexico.
Abstract:
Diverse steroidal compounds have shown antiproliferative activity on certain tumor cell lines; however, their complete role on cancer cells has not been extensively established since the research is quite recent. Hence, deeper study in this field is required. Due to the importance of selenium in animal and human health; herein, we report the synthesis, characterization, and biological evaluation of two novel 22-oxo-26-selenocyanocholestanic steroids on cervicouterine cancer cells and non-tumor cells. The title compounds were straightforward prepared from diosgenin and hecogenin in excellent overall yields. We determined their effect on cell proliferation on HeLa, CaSki, and ViBo cell cultures. Their cytotoxic effect on tumor cells, as well as on peripheral blood lymphocytes was also evaluated. The increase in the expression of active caspase-3 along with the fragmentation of DNA confirm that the new 22-oxo-26-selenocyanocholestane frameworks potentiate apoptosis in tumor cells. The antiproliferative activity on tumor cells affects to some extent the proliferative potential of peripheral blood lymphocytes, so an immunosuppressive effect has also been established. The novel 22-oxo-26-selenocyanocholestane compounds show selective antitumor activity and therefore are promising lead candidates for further in vivo evaluation.
Insights
Two novel selenium-containing steroids demonstrate selective antiproliferative effects against cervicouterine cancer cells by inducing apoptosis. These compounds show potential for cancer treatment with a noted, but limited, immunosuppressive effect on lymphocytes.
Area of Science:
- Steroid chemistry
- Cancer biology
- Medicinal chemistry
Background:
- Steroidal compounds exhibit antiproliferative properties against cancer cell lines.
- The role of steroids in cancer is an emerging area of research requiring further investigation.
- Selenium is vital for human and animal health, prompting interest in selenium-containing compounds.
Purpose of the Study:
- To synthesize and characterize novel 22-oxo-26-selenocyanocholestane steroids.
- To evaluate the biological activity of these novel steroids on cervicouterine cancer cells (HeLa, CaSki, ViBo) and non-tumor cells.
- To assess the apoptotic potential and cytotoxic effects on tumor cells versus peripheral blood lymphocytes.
Main Methods:
- Synthesis of two novel 22-oxo-26-selenocyanocholestane steroids from diosgenin and hecogenin.
- Cell proliferation assays on HeLa, CaSki, and ViBo cancer cell lines.
- Evaluation of cytotoxic effects and apoptosis induction (caspase-3 activation, DNA fragmentation) in tumor and non-tumor cells.
Main Results:
- The novel selenocyanocholestane compounds were synthesized in excellent yields.
- These compounds demonstrated antiproliferative and cytotoxic effects specifically on cervicouterine cancer cells.
- Apoptosis was confirmed through increased active caspase-3 expression and DNA fragmentation in tumor cells.
- A moderate immunosuppressive effect was observed on peripheral blood lymphocytes.
Conclusions:
- The novel 22-oxo-26-selenocyanocholestane steroids exhibit selective antitumor activity.
- These compounds induce apoptosis in cervicouterine cancer cells.
- The observed immunosuppressive effect warrants further investigation for potential therapeutic applications.
