2. Academic Validation
  3. STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae

STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae

  • Bioorg Med Chem. 2020 Mar 15;28(6):115347. doi: 10.1016/j.bmc.2020.115347.
Teruyuki Tahara 1,  Ami Watanabe 1,  Maho Yutani 1,  Yuko Yamano 1,  Mami Sagara 1,  Shizu Nagai 1,  Keita Saito 1,  Mitsuaki Yamashita 1,  Makoto Ihara 1,  Akira Iida 2
Affiliations

Affiliations

  • 1 School of Agriculture, Kindai University, Nakamachi, Nara 631-8505, Japan.
  • 2 School of Agriculture, Kindai University, Nakamachi, Nara 631-8505, Japan. Electronic address: [email protected].
PMID: 32044231 DOI: 10.1016/j.bmc.2020.115347
Abstract

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.

Keywords

BBI 608; Furanonaphthoquinones; JAK-STAT pathway; STAT3 phosphorylation; Tabebuia avellanedae.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-N10472
    STAT3 Inhibitor