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Int. J. Mol. Sci. 2016, 17(7), 1066;

Anti-Cancer Effect of Lambertianic Acid by Inhibiting the AR in LNCaP Cells

Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea
Author to whom correspondence should be addressed.
Academic Editors: Terrence Piva and Dario Marchetti
Received: 8 April 2016 / Revised: 21 June 2016 / Accepted: 28 June 2016 / Published: 7 July 2016
(This article belongs to the Section Molecular Pathology, Diagnostics, and Therapeutics)
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Lambertianic acid (LA) is known to have anti-allergic and antibacterial effects. However, the anticancer activities and mechanism of action of LA have not been investigated. Therefore, the anticancer effects and mechanism of LA are investigated in this study. LA decreased not only AR protein levels, but also cellular and secretory levels of PSA. Furthermore, LA inhibited nuclear translocation of the AR induced by mibolerone. LA suppressed cell proliferation by inducing G1 arrest, downregulating CDK4/6 and cyclin D1 and activating p53 and its downstream molecules, p21 and p27. LA induced apoptosis and the expression of related proteins, including cleaved caspase-9 and -3, c-PARP and BAX, and inhibited BCl-2. The role of AR in LA-induced apoptosis was assessed by using siRNA. Collectively, these findings suggest that LA exerts the anticancer effect by inhibiting AR and is a valuable therapeutic agent in prostate cancer treatment. View Full-Text
Keywords: LNCaP; lambertianic acid; androgen receptor; anticancer LNCaP; lambertianic acid; androgen receptor; anticancer

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Lee, M.-S.; Lee, S.-O.; Kim, S.-H.; Lee, E.-O.; Lee, H.-J. Anti-Cancer Effect of Lambertianic Acid by Inhibiting the AR in LNCaP Cells. Int. J. Mol. Sci. 2016, 17, 1066.

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