Open Access

ARTICLE

Deoxynortryptoquivaline: A unique antiprostate cancer agent

YOHKO YAMAZAKI^1,*, MANABU KAWADA², ISAO MOMOSE¹

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

* Corresponding Author: YOHKO YAMAZAKI. Email:

(This article belongs to the Special Issue: Approach from Chemical Biology for Cancer Research)

Oncology Research 2023, 31(6), 845-853. https://doi.org/10.32604/or.2023.030266

Received 24 April 2023; Accepted 26 June 2023; Issue published 15 September 2023

Abstract

The androgen receptor (AR) is a critical target in all the clinical stages of prostate cancer. To identify a new AR inhibitor, we constructed a new screening system using the androgen-dependent growth of prostate cancer cell lines as a screening indicator. We screened 50,000 culture broths of microorganisms using this screening system and found that the fermentation broth produced by a fungus inhibited androgen-dependent growth of human prostate cancer LNCaP cells without 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-dependent growth of human prostate cancer LNCaP cells. The AR competitor assay was performed, and DNT did not act as an AR antagonist. However, DNT inhibited AR-dependent transcriptional activity and AR nuclear translocation, it suggested that the suppression of AR function leads to inhibition activity against androgen-dependent growth.

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Graphical Abstract

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