Antiandrogenic and Estrogenic Activity Evaluation of Oxygenated and Nitrated Polycyclic Aromatic Hydrocarbons Using Chemically Activated Luciferase Expression Assays

Overview

Journal Int J Environ Res Public Health

Publisher MDPI

Specialties Environmental Health
Public Health

Date 2023 Jan 8

PMID 36612408

Authors

Kentaro Misaki

Nguyen Minh Tue

Takeji Takamura-Enya

Hidetaka Takigami

Go Suzuki

Le Huu Tuyen

Shin Takahashi

Shinsuke Tanabe

Affiliations

Soon will be listed here.

Abstract

To establish the risk of the endocrine disrupting activity of polycyclic aromatic compounds, especially oxygenated and nitrated polycyclic aromatic hydrocarbons (oxy-PAHs and nitro-PAHs, respectively), antiandrogenic and estrogenic activities were determined using chemically activated luciferase expression (CALUX) assays with human osteoblast sarcoma cells. A total of 27 compounds including 9 oxy-PAHs (polycyclic aromatic ketones and quinones) and 8 nitro-PAHs was studied. The oxy-PAHs of 7-benz[]anthracen-7-one (BAO), 11-benzo[]fluoren-11-one (B[]FO), 11-benzo[]fluoren-11-one (B[]FO), and phenanthrenequinone (PhQ) exhibited significantly the potent inhibition of AR activation. All nitro-PAHs exhibited high antiandrogenic activities (especially high for 3-nitrofluoranthene (3-NFA) and 3-nitro-7-benz[]anthracen-7-one (3-NBAO)), and the AR inhibition was confirmed as noncompetitive for 3-NFA, 3-NBAO, and 1,3-dinitropyrene (1,3-DNPy). Antiandrogenic activity of 3-NFA demonstrated characteristically a U-shaped dose-response curve; however, the absence of fluorescence effect on the activity was confirmed. The prominent estrogenic activity dependent on dose-response curve was confirmed for 2 oxy-PAHs (i.e., B[]FO and B[]FO). Elucidating the role of AR and ER on the effects of polycyclic aromatic compounds (e.g., oxy- and nitro-PAHs) to endocrine dysfunctions in mammals and aquatic organisms remains a challenge.

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