An exploration of the estrogen receptor transcription activity of capsaicin analogues via an integrated approach based on in silico prediction and in vitro assays
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- 作者：Juan Li ; Duo Ma ; Yuan Lin ; Jianjie Fu ; Aiqian Zhang ; aqzhang@rcees.ac.cn" class="auth_mail
- 关键词：ER transcription activity ; Capsaicin analogs ; MVLN assay ; Molecular docking ; Receptor polymorphism analysis
- 刊名：Toxicology Letters
- 出版年：16 June 2014
- 年：2014
- 卷：227
- 期：3
- 页码：179-188
- 全文大小：2385 K
文摘
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6-I-CPS exerted estrogenic effect through ER-mediated pathway.
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NADA, capsazepine, dihydrocapsaicin, TSA, and capsaicin suppressed ER transactivation activity in MVLN cells.
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Aryl halogenation and long lipophilic carbon chain of capsaicin template may result in increased or depressed ER伪 transcription activity.
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Species selectivity of ER伪 transcription activity due to receptor polymorphism cannot be neglected for capsaicin analogues.