1. Academic Validation
  2. Anti-Cancer Effect of Lambertianic Acid by Inhibiting the AR in LNCaP Cells

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

  • Int J Mol Sci. 2016 Jul 7;17(7):1066. doi: 10.3390/ijms17071066.
Myoung-Sun Lee 1 Seon-Ok Lee 2 Sung-Hoon Kim 3 Eun-Ok Lee 4 Hyo-Jeong Lee 5
Affiliations

Affiliations

  • 1 Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. lmsms14@naver.com.
  • 2 Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. lso4595@naver.com.
  • 3 Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. sungkim7@khu.ac.kr.
  • 4 Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. leook@khu.ac.kr.
  • 5 Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. strong79@khu.ac.kr.
Abstract

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.

Keywords

LNCaP; androgen receptor; anticancer; lambertianic acid.

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