p-Carborane-based androgen antagonists active in LNCaP cells with a mutated androgen receptor

MedChemComm ◽  
2011 ◽  
Vol 2 (9) ◽  
pp. 877 ◽  
Author(s):  
Shinya Fujii ◽  
Ayumi Yamada ◽  
Keiko Tomita ◽  
Mao Nagano ◽  
Tokuhito Goto ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Lncap Cells ◽  
Androgen Antagonists

scholarly journals Role of Testosterone Levels on the Combinatorial Effect of Boswellia serrata Extract and Enzalutamide on Androgen Dependent LNCaP Cells and in Patient Derived Cells

2021 ◽  
Vol 20 ◽  
pp. 153473542199682
Author(s):  
Prathesha Pillai ◽  
Ginil Kumar Pooleri ◽  
Shantikumar V. Nair
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Early Stage ◽  
Therapeutic Option ◽  
Specific Antigen ◽  
Cell Killing ◽  
Receptor Expression ◽  
Lncap Cells ◽  
Boswellia Serrata ◽  
Physiological Serum

Co-therapy with herbal extracts along with current clinical drugs is being increasingly recognized as a useful complementary treatment for cancer. The anti-cancer property of the phyto-derivative acetyl-11 keto β boswellic acid (AKBA) has been studied in many cancers, including prostate cancer. However, the whole extract of the gum resin Boswellia serrata (BS) and anti-androgen enzalutamide has not been explored in prostate cancer to date. We hypothesized that the BS extract containing 30% (AKBA) with enzalutamide acted synergistically in the early phase of cancer, especially in LNCaP cells, by inhibiting androgen receptor (AR) and by reducing cell proliferation, and further, that the extract would be superior to the action of the active ingredient AKBA when used alone or in combination with enzalutamide. To test our hypothesis, we treated LNCaP cells with BS extract or AKBA and enzalutamide both individually and in combination to analyze cell viability under different levels of dihydrotestosterone (DHT). The inhibition of androgen receptor (AR) followed by the expression of prostate-specific antigen (PSA) and the efflux mechanism of the cells were analyzed to determine the effect of the combination on the cellular mechanism. Cells derived from prostate cancer patients were also tested with the combination. Only 6 µM enzalutamide along with BS in the range of 4.1 µg/ml to 16.4 µg/ml gave the best synergistic results with nearly 50% cell killing even though standard enzalutamide doses were as high as 48 µM. Cell killing was most effective at intermediate DHT concentrations of approximately 1 nM, which corresponds to normal physiological serum levels of DHT. The Pgp expression level and the androgen receptor expression levels were reduced under the combination treatment; the former helping to minimize drug efflux and the latter by reducing the sensitivity to hormonal changes. Furthermore, the combination reduced the PSA level secreted by the cells. In contrast, AKBA could not achieve the needed synergism for adequate cell killing at equivalent concentrations. The combination of enzalutamide and BS extract containing 30% AKBA because of their synergistic interaction is an attractive therapeutic option for treating early stage (hormone-dependent) prostate cancer and is superior to the use of AKBA alone.

Anti-androgen receptor activity of apoptotic CK2 inhibitor CX4945 in human prostate cancer LNCap cells

2012 ◽  
Vol 22 (17) ◽  
pp. 5470-5474 ◽  
Author(s):  
Byung Jun Ryu ◽  
Seung-hwa Baek ◽  
Jiyeon Kim ◽  
Su Jung Bae ◽  
Sung-Youn Chang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Receptor Activity ◽  
Human Prostate ◽  
Human Prostate Cancer ◽  
Lncap Cells ◽  
Androgen Receptor Activity ◽  
Ck2 Inhibitor

Ethanolic extract of Algerian propolis decreases androgen receptor transcriptional activity in cultured LNCaP cells

2019 ◽  
Vol 189 ◽  
pp. 108-115 ◽  
Author(s):  
Nada Zabaiou ◽  
Allan Fouache ◽  
Amalia Trousson ◽  
Julio Buñay-Noboa ◽  
Geoffroy Marceau ◽  
...  
Keyword(s):  
Androgen Receptor ◽  
Transcriptional Activity ◽  
Ethanolic Extract ◽  
Lncap Cells

Androgen Receptor Regulation by Physiological Concentrations of the Isoflavonoid Genistein in Androgen-Dependent LNCaP Cells Is Mediated by Estrogen Receptor β

2004 ◽  
Vol 45 (2) ◽  
pp. 245-251 ◽  
Author(s):  
Jasmin Bektic ◽  
Andreas P Berger ◽  
Karina Pfeil ◽  
Gabriele Dobler ◽  
Georg Bartsch ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Androgen Receptor ◽  
Estrogen Receptor Β ◽  
Receptor Regulation ◽  
Lncap Cells
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