Dearomatized Isoprenylated Acylphloroglucinol Derivatives with Potential Antitumor Activities from Hypericum henryi

Abstract

Abstract A series of dearomatized isoprenylated acylphloroglucinols derivatives, hyperhenols A–E (1–5), as well as seven known analogues (6–12), were characterized from Hypericum henryi. Their structures were determined by combination of NMR, ECD spectroscopy, and X-ray diffraction analysis. Compounds 1 and 6–8 were tested to exhibit potential antitumor properties, of which 6 and 7 inhibited cell growth through inducing apoptosis and cell cycle arrest. In addition, these compounds could induce autophagy and PINK1/Parkin-mediated mitophagy in cancer cell lines, as well as suppress lung cancer A549 cells metastasis in vitro.

Keywords

• Hypericum henryi
• Dearomatized isoprenylated acylphloroglucinols (DIAPs)
• Apoptosis
• Cell cycle arrest