Fundamental Toxicological Sciences

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Fundamental Toxicological Sciences
Vol. 6 No. 2 March 19, 2019 p.57-63
Original Article
Effects of benzotriazole ultraviolet stabilizers on rat PXR, CAR and PPARα transcriptional activities
  • Shigeyuki Kitamura (Nihon Pharmaceutical University / kitamura@nichiyaku.ac.jp)
Yoko Watanabe 1) , Shoko Hattori 1) , Chieri Fujino 2) , Ken Tachibana 3) , Hiroyuki Kojima 4) , Kouichi Yoshinari 5) , Shigeyuki Kitamura 1)
1) Nihon Pharmaceutical University , 2) Graduate School of Biomedical and Health Sciences, Hiroshima University , 3) Faculty of Pharmaceutical Sciences, Sanyo-Onoda City University , 4) Hokkaido Institute of Public Health , 5) School of Pharmaceutical Sciences, University of Shizuoka
Keywords: Benzotriazole UV stabilizer, CAR, Nuclear receptor activation, PPARα, PXR
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Abstracts

Benzotriazole ultraviolet stabilizers (BUVSs) are widely used as ultraviolet filters in various consumer and industrial products. For this purpose, we examined the effects of 10 BUVSs and benzotriazole itself on transcriptional activation mediated by nuclear receptors: pregnane X receptor (PXR), constitutive androstane receptor (CAR) and peroxisome proliferator-activated receptor alpha (PPARα). UV-090 and UV-9 showed rat PXR-agonistic activity in the concentration range of 1-30 μM in reporter gene assay using simian kidney COS-1 cells. UV-090 showed the highest activity (REC20 value: 3.85 × 10-6 M). UV-090 was also positive in rat CAR activation assay, while UV-P showed inverse agonistic activity towards CAR. In the presence of the CAR agonist artemisinin (10 μM), UV-P also showed dose-dependent CAR-antagonistic activity in the concentration range of 10-30 μM. UV-090 and UV-9 activated rat PPARα. Overall, these results suggest that UV-090, UV-9 and UV-P modulate PXR, CAR and/or PPARα activation.

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