Lee Myoung-Sun, Lee Seon-Ok, Kim Sung-Hoon, Lee Eun-Ok, Lee Hyo-Jeong
Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea.
Int J Mol Sci. 2016 Jul 7;17(7):1066. doi: 10.3390/ijms17071066.
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.
已知兰伯蒂酸（LA）具有抗过敏和抗菌作用。然而，LA的抗癌活性和作用机制尚未得到研究。因此，本研究对LA的抗癌作用及其机制进行了研究。LA不仅降低了AR蛋白水平，还降低了PSA的细胞水平和分泌水平。此外，LA抑制了米勃酮诱导的AR核转位。LA通过诱导G₁期阻滞、下调CDK4/6和细胞周期蛋白D1以及激活p53及其下游分子p21和p27来抑制细胞增殖。LA诱导细胞凋亡及相关蛋白的表达，包括裂解的caspase-9和-3、c-PARP和BAX，并抑制BCl-2。通过使用siRNA评估AR在LA诱导的细胞凋亡中的作用。总的来说，这些发现表明LA通过抑制AR发挥抗癌作用，是前列腺癌治疗中有价值的治疗药物。
