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Purpose <p>A series of imidazolium salts (IMS), substituted with lithocholic acid (LA) and alkyl chains of varying lengths (<b>LA-1</b> to <b>LA-10</b>), were evaluated for their cytotoxic effects against breast cancer (BC).</p> Methods <p>The cytotoxic potential of the tested salts was assessed in estrogen-dependent (MCF‐7) and non-estrogen-dependent (MDA-MB-231) cell lines, as well as in the cardiomyocyte cell line H9C2. The study was also conducted <i>in vivo</i> using a MCF-7 mouse xenograft model.</p> Results <p>The cytotoxicity of IMS increased with the length of the aliphatic chain. A significant effect, compared with the reference drug, was observed for LA-7 and LA-8 (IC<sub>50</sub> = 13.07–13.19&#xa0;µg/ml) in MCF-7 cells and for LA-1-LA-8 (IC<sub>50</sub> = 77.82–21.06&#xa0;µg/mL) in MDA-MB-231 line. LA-8 and doxorubicin showed increased toxicity in MCF-7 cells, reducing HMGB1 concentration and DNA synthesis, while increasing apoptosis and the activation caspase 7 and 8. Most of the tested IMS exhibited significantly lower toxicity toward healthy H9C2 cardiomyocytes (IC<sub>50</sub> = 52.09–105.40&#xa0;µg/mL) compared with doxorubicin (IC<sub>50</sub> = 51.71&#xa0;µg/mL). <i>In vivo</i> studies demonstrated that LA-8 treatment significantly inhibited the growth of MCF-7 tumors.</p> Conclusions <p>LA-based IMS demonstrate significant potential as chemotherapeutic agents for the treatment of breast cancer.</p>

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Lithocholic Acid-Derived Imidazolium Salts Suppress Breast Cancer Growth: In Vitro and In Vivo Evaluation

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年5月11日

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  • Diana Sawicka,
  • Anna Sadowska,
  • Agnieszka Hryniewicka,
  • Beata Skonieczna,
  • Robert Milewski,
  • Katarzyna Guzińska-Ustymowicz,
  • Halina Car

摘要

Purpose

A series of imidazolium salts (IMS), substituted with lithocholic acid (LA) and alkyl chains of varying lengths (LA-1 to LA-10), were evaluated for their cytotoxic effects against breast cancer (BC).

Methods

The cytotoxic potential of the tested salts was assessed in estrogen-dependent (MCF‐7) and non-estrogen-dependent (MDA-MB-231) cell lines, as well as in the cardiomyocyte cell line H9C2. The study was also conducted in vivo using a MCF-7 mouse xenograft model.

Results

The cytotoxicity of IMS increased with the length of the aliphatic chain. A significant effect, compared with the reference drug, was observed for LA-7 and LA-8 (IC50 = 13.07–13.19 µg/ml) in MCF-7 cells and for LA-1-LA-8 (IC50 = 77.82–21.06 µg/mL) in MDA-MB-231 line. LA-8 and doxorubicin showed increased toxicity in MCF-7 cells, reducing HMGB1 concentration and DNA synthesis, while increasing apoptosis and the activation caspase 7 and 8. Most of the tested IMS exhibited significantly lower toxicity toward healthy H9C2 cardiomyocytes (IC50 = 52.09–105.40 µg/mL) compared with doxorubicin (IC50 = 51.71 µg/mL). In vivo studies demonstrated that LA-8 treatment significantly inhibited the growth of MCF-7 tumors.

Conclusions

LA-based IMS demonstrate significant potential as chemotherapeutic agents for the treatment of breast cancer.