An exploration of the estrogen receptor transcription activity of capsaicin analogues via an integrated approach based on in silico prediction and in vitro assays

- 6-I-CPS exerted estrogenic effect through ER-mediated pathway.
- NADA, capsazepine, dihydrocapsaicin, TSA, and capsaicin suppressed ER transactivation activity in MVLN cells.
- Aryl halogenation and long lipophilic carbon chain of capsaicin template may result in increased or depressed ERα transcription activity.
- Species selectivity of ERα transcription activity due to receptor polymorphism cannot be neglected for capsaicin analogues.