title: Anti-Cancer Effect of Lambertianic Acid by Inhibiting the AR in LNCaP Cells.
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.
authors.affiliation: Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. lmsms14@naver.com.
authors.forename: Myoung-Sun
authors.initials: MS
authors.lastname: Lee
authors.affiliation: Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. lso4595@naver.com.
authors.forename: Seon-Ok
authors.initials: SO
authors.lastname: Lee
authors.affiliation: Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. sungkim7@khu.ac.kr.
authors.forename: Sung-Hoon
authors.initials: SH
authors.lastname: Kim
authors.affiliation: Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. leook@khu.ac.kr.
authors.forename: Eun-Ok
authors.initials: EO
authors.lastname: Lee
authors.affiliation: Department of Cancer Preventive Material Development, Graduate School, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul 130-701, Korea. strong79@khu.ac.kr.
authors.forename: Hyo-Jeong
authors.initials: HJ
authors.lastname: Lee
mesh_terms: D000970:Antineoplastic Agents / Q000633:toxicity*; D017209:Apoptosis / Q000187:drug effects; D002264:Carboxylic Acids / Q000633:toxicity*; D053148:Caspase 3 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D018797:Cell Cycle Proteins / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D019938:Cyclin D1 / Q000378:metabolism; D051358:Cyclin-Dependent Kinase 4 / Q000378:metabolism; D051361:Cyclin-Dependent Kinase 6 / Q000378:metabolism; D015536:Down-Regulation / Q000187:drug effects; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects; D006801:Humans; D009277:Nandrolone / Q000031:analogs & derivatives / Q000494:pharmacology; D009281:Naphthalenes / Q000633:toxicity*; D017430:Prostate-Specific Antigen / Q000378:metabolism; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D034622:RNA Interference; D034741:RNA, Small Interfering / Q000378:metabolism; D011944:Receptors, Androgen / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D018797:Cell Cycle Proteins; D009281:Naphthalenes; D019253:Proto-Oncogene Proteins c-bcl-2; D034741:RNA, Small Interfering; D011944:Receptors, Androgen; D016159:Tumor Suppressor Protein p53; D051028:bcl-2-Associated X Protein; D019938:Cyclin D1; C421442:lambertianic acid; D009277:Nandrolone; C100075:mibolerone; D051358:Cyclin-Dependent Kinase 4; D051361:Cyclin-Dependent Kinase 6; D017430:Prostate-Specific Antigen; D053148:Caspase 3; D053453:Caspase 9
keywords: LNCaP; androgen receptor; anticancer; lambertianic acid