Abstract |
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.
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Authors | Liron Berkovich, Amnon C Sintov, Shimon Ben-Shabat |
Journal | Investigational new drugs
(Invest New Drugs)
Vol. 31
Issue 2
Pg. 247-55
(Apr 2013)
ISSN: 1573-0646 [Electronic] United States |
PMID | 22661288
(Publication Type: Journal Article)
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Chemical References |
- 24-cyclopropyl-9,10-secochola-5,7,10(19),22-tetraene-24-chloro-1,3-diol
- BGP-13 compound
- Dioxoles
- RNA, Messenger
- Receptors, Calcitriol
- VDR protein, human
- Calcitriol
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Topics |
- Animals
- Apoptosis
(drug effects)
- Blotting, Western
- Breast Neoplasms
(drug therapy, metabolism, pathology)
- Calcitriol
(analogs & derivatives, chemical synthesis, pharmacology)
- Cell Cycle
(drug effects)
- Cell Proliferation
(drug effects)
- Dioxoles
(chemical synthesis, pharmacology)
- Female
- HT29 Cells
- Humans
- In Vitro Techniques
- Male
- Mice
- Mice, Inbred BALB C
- Mice, Nude
- Molecular Structure
- Prostatic Neoplasms
(drug therapy, metabolism, pathology)
- RNA, Messenger
(genetics)
- Real-Time Polymerase Chain Reaction
- Receptors, Calcitriol
(genetics, metabolism)
- Reverse Transcriptase Polymerase Chain Reaction
- Tumor Cells, Cultured
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