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Estrogenic and Antiestrogenic Activities of Protocatechic Acid

机译:Protocatechic acid的雌激素和抗雌激酶

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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 E_2-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.
机译:研究Protocatechuic酸的雌激素和抗生素作用,目的是获得安全有效的自然雌激素置换药物的目的。通过细胞增殖实验评估其雌激素和抗生素作用。通过酵母双杂交实验测试了雌激素受体(ER)Protocatechuic酸的结合能力,并且通过计算机辅助分子对接技术进行了它们可能的结合位点。 Protocatechuic acid对没有雌激素的雌激素敏感ER(+)MCF-7细胞的增殖显着影响,导致对E_2诱导的MCF-7细胞增殖产生拮抗作用。但是,它不能诱导雌激素阴性ER( - )MDA-MB-231细胞的增殖。酵母双杂化实验表明ProtocateChuic酸对两者具有显着但不选择性的结合能力。 Protocatechuic acid揭示了雌激素和抗雌激素的双向调节功能,其显示出低浓度或缺乏内源性雌激素的雌激动激动剂活性,并且在高浓度或过多的内源性雌激素刺激雌激素拮抗作用。 Protocatechuic acid对ERS具有显着的结合能力。因此,Protocatechuic酸可用于治疗雌激素缺乏相关疾病。

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