The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models
3-3′-Diindolylmethane (DIM) is a biologically active dimer derived from the endogenous conversion of indole-3-carbinol (I3C), a naturally occurring glucosinolate found in many cruciferous vegetables (i.e., <i>Brassicaceae</i>). DIM was the first pure androgen receptor antagonist isolated...
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MDPI AG
2023-02-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/4/3620 |
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| author | Paolo Tucci Iain Brown Guy S. Bewick Roger G. Pertwee Pietro Marini |
| author_facet | Paolo Tucci Iain Brown Guy S. Bewick Roger G. Pertwee Pietro Marini |
| author_sort | Paolo Tucci |
| collection | DOAJ |
| description | 3-3′-Diindolylmethane (DIM) is a biologically active dimer derived from the endogenous conversion of indole-3-carbinol (I3C), a naturally occurring glucosinolate found in many cruciferous vegetables (i.e., <i>Brassicaceae</i>). DIM was the first pure androgen receptor antagonist isolated from the <i>Brassicaceae</i> family and has been recently investigated for its potential pharmacological use in prostate cancer prevention and treatment. Interestingly, there is evidence that DIM can also interact with cannabinoid receptors. In this context, by considering the well-known involvement of the endocannabinoid system in prostate cancer, we have pharmacologically characterized the properties of DIM on both CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors in two human prostate cancer cell lines: PC3 (androgen-independent/androgen receptor negative) and LNCaP (androgen-dependent). In the PC3 cell line, DIM was able to activate CB<sub>2</sub> receptors and potentially associated apoptotic pathways. On the other hand, although DIM was also able to activate CB<sub>2</sub> receptors in the LNCaP cell line, no apoptotic effects were observed. Our evidence confirms that DIM is a CB<sub>2</sub> receptor ligand and, moreover, it has a potential anti-proliferative effect on androgen-independent/androgen receptor-negative prostate cancer cells. |
| first_indexed | 2024-03-11T08:43:22Z |
| format | Article |
| id | doaj.art-d29584426abb446cabf0d52373c3c414 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T08:43:22Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-d29584426abb446cabf0d52373c3c4142023-11-16T21:02:38ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-02-01244362010.3390/ijms24043620The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular ModelsPaolo Tucci0Iain Brown1Guy S. Bewick2Roger G. Pertwee3Pietro Marini4Department of Clinical and Experimental Medicine, University of Foggia, 71122 Foggia, ItalyDivision of Applied Medicine, School of Medicine and Dentistry, Foresterhill, University of Aberdeen, Aberdeen AB25 2ZD, UKThe Institute of Medical Sciences, Foresterhill, University of Aberdeen, Aberdeen AB25 2ZD, UKThe Institute of Medical Sciences, Foresterhill, University of Aberdeen, Aberdeen AB25 2ZD, UKInstitute of Education in Healthcare and Medical Sciences, Foresterhill, University of Aberdeen, Aberdeen AB25 2ZD, UK3-3′-Diindolylmethane (DIM) is a biologically active dimer derived from the endogenous conversion of indole-3-carbinol (I3C), a naturally occurring glucosinolate found in many cruciferous vegetables (i.e., <i>Brassicaceae</i>). DIM was the first pure androgen receptor antagonist isolated from the <i>Brassicaceae</i> family and has been recently investigated for its potential pharmacological use in prostate cancer prevention and treatment. Interestingly, there is evidence that DIM can also interact with cannabinoid receptors. In this context, by considering the well-known involvement of the endocannabinoid system in prostate cancer, we have pharmacologically characterized the properties of DIM on both CB<sub>1</sub> and CB<sub>2</sub> cannabinoid receptors in two human prostate cancer cell lines: PC3 (androgen-independent/androgen receptor negative) and LNCaP (androgen-dependent). In the PC3 cell line, DIM was able to activate CB<sub>2</sub> receptors and potentially associated apoptotic pathways. On the other hand, although DIM was also able to activate CB<sub>2</sub> receptors in the LNCaP cell line, no apoptotic effects were observed. Our evidence confirms that DIM is a CB<sub>2</sub> receptor ligand and, moreover, it has a potential anti-proliferative effect on androgen-independent/androgen receptor-negative prostate cancer cells.https://www.mdpi.com/1422-0067/24/4/3620DIMCB<sub>2</sub> cannabinoid receptorsprostate cancer |
| spellingShingle | Paolo Tucci Iain Brown Guy S. Bewick Roger G. Pertwee Pietro Marini The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models International Journal of Molecular Sciences DIM CB<sub>2</sub> cannabinoid receptors prostate cancer |
| title | The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models |
| title_full | The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models |
| title_fullStr | The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models |
| title_full_unstemmed | The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models |
| title_short | The Plant Derived 3-3′-Diindolylmethane (DIM) Behaves as CB<sub>2</sub> Receptor Agonist in Prostate Cancer Cellular Models |
| title_sort | plant derived 3 3 diindolylmethane dim behaves as cb sub 2 sub receptor agonist in prostate cancer cellular models |
| topic | DIM CB<sub>2</sub> cannabinoid receptors prostate cancer |
| url | https://www.mdpi.com/1422-0067/24/4/3620 |
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