Unprecedented Monoterpenoid Polyprenylated Acylphloroglucinols with a Rare 6/6/5/4 Tetracyclic Core, Enhanced MCF-7 Cells' Sensitivity to Camptothecin by Inhibiting the DNA Damage Response

  • Biomedicines. 2021 Oct 14;9(10):1473. doi: 10.3390/biomedicines9101473.
Xiang-Zhong Liu  1 ,  Mi Zhou  1 ,  Chun-Chun Du  1 ,  Hong-Hong Zhu  1 ,  Xi Lu  1 ,  Shou-Lun He  1 ,  Guang-Hui Wang  1 ,  Ting Lin  1 ,  Wen-Jing Tian  1 ,  Hai-Feng Chen  1
Affiliations
  • 1. Fujian Provincial Key Laboratory of Innovative Drug Target, School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China.
Abstract

(±)-Hypersines A-C (1-3), the three pairs of enantiomerically pure monoterpenoid polyprenylated acylphloroglucinols with an unprecedented 6/6/5/4 fused ring system, were isolated from Hypericum elodeoides. Their structures, including absolute configurations, were elucidated by comprehensive spectroscopic data, single-crystal X-ray diffraction, and quantum chemical calculations. The plausible, biosynthetic pathway of 1-3 was proposed. Moreover, the bioactivity evaluation indicated that 1a might be a novel DNA damage response inhibitor, and could enhance MCF-7 cell sensitivity to the Anticancer agent, camptothecin.

Keywords
DNA damage response inhibitor; Guttiferae; Hypericum elodeoides; acylphloroglucinol; biosynthetic pathway.