1. Academic Validation
  2. 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

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

Affiliation

  • 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.

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