The synthesis and antitumor activity of lithocholic acid and its derivatives

  • Steroids. 2017 Sep:125:54-60. doi: 10.1016/j.steroids.2017.06.009.
Xiao-Long He  1 ,  Yajing Xing  2 ,  Xiang-Zhong Gu  3 ,  Jie-Xin Xiao  1 ,  Ying-Ying Wang  1 ,  Zhengfang Yi  2 ,  Wen-Wei Qiu  4
Affiliations
  • 1. Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Chemical Engineering, East China Normal University, Shanghai 200241, China.
  • 2. Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
  • 3. Department of Research and Development, Jiangsu Jiaerke Pharmaceuticals Group Co Ltd., Zhenglu Town, Changzhou 213111, China.
  • 4. Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Chemical Engineering, East China Normal University, Shanghai 200241, China. Electronic address: [email protected].
PMID: 28648585 DOI: 10.1016/j.steroids.2017.06.009
Abstract

In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and Apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.

Keywords
Antitumor; Apoptosis; Breast cancer; Lithocholic acid; Migration.
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