Deoxynortryptoquivaline:A unique antiprostate cancer agent  

作　　者：YOHKO YAMAZAKI MANABU KAWADA ISAO MOMOSE 

机构地区：[1]Institute of Microbial Chemistry(BIKAKEN),Numazu Branch,Microbial Chemistry Research Foundation,Numazu,410-0301,Japan [2]Institute of Microbial Chemistry(BIKAKEN),Laboratory of Oncology,Microbial Chemistry Research Foundation,Shinagawa-ku,141-0021,Japan

出　　处：《Oncology Research》2023年第6期845-853,共9页肿瘤学研究（英文）

基　　金：supported by JSPS KAKENHI Grant Number JP24592417.

摘　　要：The androgen receptor (AR) is a critical target in all the clinical stages of prostate cancer. To identify a new ARinhibitor, we constructed a new screening system using the androgen-dependent growth of prostate cancer cell lines as ascreening indicator. We screened 50,000 culture broths of microorganisms using this screening system and found that thefermentation broth produced by a fungus inhibited androgen-dependent growth of human prostate cancer LNCaP cellswithout cytotoxicity. Purification of this culture medium was performed, and this resulted in deoxynortryptoquivaline(DNT) being identified as a novel inhibitor of AR function. DNT showed potent inhibition of androgen-dependentgrowth of human prostate cancer LNCaP cells. The AR competitor assay was performed, and DNT did not act as anAR antagonist. However, DNT inhibited AR-dependent transcriptional activity and AR nuclear translocation, itsuggested that the suppression of AR function leads to inhibition activity against androgen-dependent growth.

关 键 词：Anticancer antibiotics Prostate cancer Androgen receptor Androgen dependency 

分 类 号：R737.25[医药卫生—肿瘤]