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Estrogenic and Antiestrogenic Activities of Protocatechic Acid

  • Fang Hu
  • Junzhi Wang
  • Huajun Luo
  • Ling Zhang
  • Youcheng Luo
  • Wenjun Sun
  • Fan Cheng
  • Weiqiao Deng
  • Zhangshuang Deng
  • Kun Zou
Conference paper
Part of the Lecture Notes in Electrical Engineering book series (LNEE, volume 269)

Abstract

Study the estrogenic and antiestrogenic effects of protocatechuic acid with the aim of obtaining a safe and effective natural estrogen replacement drugs. Its estrogenic and antiestrogenic effects were evaluated through cell proliferation experiments. The estrogen-receptor (ER) binding abilities of protocatechuic acid were tested by yeast two-hybrid experiment, and their possible binding sites for ERs were performed by computer-aided molecular docking technology. Protocatechuic acid showed significant effects on the proliferation of estrogen-sensitive ER (+) MCF-7 cells in the absence of estrogen, and resulted in antagonistic effects on E2-induced MCF-7 cell proliferation. However, it could not induce the proliferation of estrogen-negative ER (-) MDA-MB-231 cells. The yeast two-hybrid experiments showed protocatechuic acid had significant but non-selective binding abilities for the two ERs. Protocatechuic acid revealed a double directional adjusting function of estrogenic and antiestrogenic activities, which showed estrogenic agonist activity at low concentration or lack of endogenous estrogen, and the estrogenic antagonistic effect was stimulated at high concentrations or too much endogenous estrogen. Protocatechuic acid had significant binding capacity for ERs. Therefore, protocatechuic acid could be used in the treatment of the estrogen deficiency-related diseases.

Keywords

Protocatechuic acid Phellinus lonicerinus (Bond.) Estrogen Yeast two-hybrid assay 

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Copyright information

© Springer Science+Business Media Dordrecht 2014

Authors and Affiliations

  • Fang Hu
    • 1
  • Junzhi Wang
    • 1
  • Huajun Luo
    • 1
  • Ling Zhang
    • 1
  • Youcheng Luo
    • 1
  • Wenjun Sun
    • 1
  • Fan Cheng
    • 1
  • Weiqiao Deng
    • 2
  • Zhangshuang Deng
    • 1
  • Kun Zou
    • 1
  1. 1.Hubei Key Laboratory of Natural Products Research and Development (China Three Gorges University)College of Chemistry and Life Science, China Three Gorges UniversityYichangPeople’s Republic of China
  2. 2.Dalian Institute of Chemical PhysicsChinese Academy of SciencesDalianPeople’s Republic of China

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