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Investigational New Drugs

, Volume 31, Issue 2, pp 247–255 | Cite as

Inhibition of cancer growth and induction of apoptosis by BGP-13 and BGP-15, new calcipotriene-derived vitamin D3 analogs, in-vitro and in-vivo studies

  • Amnon C. Sintov
  • Liron Berkovich
  • Shimon Ben-ShabatEmail author
PRECLINICAL STUDIES

Summary

One of the most innovative approaches to the treatment of cancer entails the use of 1α,25-dihydroxyvitamin D3 (calcitriol) analogs to inhibit cancer cell growth. We demonstrate here that BGP-13, a new calcipotriene-based 1α,25-dihydroxyvitamin D3 analog that we synthesized in our laboratory, inhibits the growth of prostate cancer (LNCaP), breast cancer (MCF-7), and colon cancer (HT-29) cell lines. Moreover, we also show that BGP-13 causes cells both to accumulate in G0-G1 and to activate caspase-3 and undergo apoptosis. In addition, we observed elevated vitamin D receptor (VDR) mRNA and protein levels in both LNCaP and MCF-7 cells following the exposure of the two cell lines to BGP-13. Importantly, we found that both the new analog BGP-13 and also BGP-15, another calcipotriene-based analog we synthesized previously and about which we published recently, inhibit the growth of HT-29 tumor xenografts in nude mice.

Keywords

Calcipotriene Vitamin D3 Vitamin D receptor Apoptosis Tumor xenografts 

Notes

Conflict of interest

The authors declare that they have no conflict of interest.

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Copyright information

© Springer Science+Business Media, LLC 2012

Authors and Affiliations

  • Amnon C. Sintov
    • 2
  • Liron Berkovich
    • 1
  • Shimon Ben-Shabat
    • 1
    Email author
  1. 1.Department of Pharmacology, Faculty of Health SciencesBen-Gurion University of the NegevBeer-ShevaIsrael
  2. 2.Department of Biomedical Engineering, Faculty of Engineering SciencesBen-Gurion University of the NegevBeer-ShevaIsrael

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