2020年3月15日
STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae.
Bioorganic & medicinal chemistry
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- 巻
- 28
- 号
- 6
- 開始ページ
- 115347
- 終了ページ
- 115347
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmc.2020.115347
The extract of Tabebuia avellanedae has been used as a folk medicine, and the various biological activities of T. avellanedae have been extensively studied. However, few studies have reported which natural products play a role in their biological effects. In this study, we evaluated representative naphthoquinones isolated from T. avellanedae and found that furanonaphthoquinones were the key structures required to exhibit STAT3 phosphorylation inhibitory activities. Our SAR analysis indicated that removal of a hydroxyl group enhanced the STAT3 phosphorylation inhibitory activity. In addition, the combined results of a mobility shift assay, SH2 domain binding assay, and docking simulation by Autodock 4.2.6 suggested that (S)-5-hydroxy-2-(1-hydroxyethyl)naphtho[2,3-b]furan-4,9-dione (1) could directly bind to the hinge region of STAT3.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bmc.2020.115347
- PubMed ID : 32044231