Integration Center of Traditional Chinese and Modern Medicine, Hualien Tzu Chi Hospital, Hualien 97002, Taiwan.
Department of Chinese Medicine, Hualien Tzu Chi Hospital, Hualien 97002, Taiwan.
Environ Toxicol. 2020 Oct;35(10):1043-1049. doi: 10.1002/tox.22940. Epub 2020 May 16.
In this study, we used ICI 182 780 (ICI), an estrogen receptor (ER) antagonist, to investigate the estrogenic activity of Danshen, and to further explored whether Danshen extract can block Leu27IGF-II-induced hypertrophy in H9c2 cardiomyoblast cells. We first used an IGF-II analog Leu27IGF-II, which specifically activates IGF2R signaling cascades and induces H9c2 cardiomyoblast cell hypertrophy. However, Danshen extract completely inhibited Leu27IGF-II-induced cell size increase, ANP and BNP hypertrophic marker expression, and IGF2R induction. We also observed that Danshen extract inhibited calcineurin protein expression and NFAT3 nuclear translocation, leading to suppression of Leu27IGF-II-induced cardiac hypertrophy. Moreover, the anti-Leu27IGF-II-IGF2R signaling effect of Danshen was totally reversed by ICI, which suggest the cardio protective effect of Danshen is mediated through estrogen receptors. Our study suggests that, Danshen exerts estrogenic activity, and thus, it could be used as a selective ER modulator in IGFIIR induced hypertrophy model.
在这项研究中,我们使用了ICI 182 780(ICI),一种雌激素受体(ER)拮抗剂,来研究丹参的雌激素活性,并进一步探讨丹参提取物是否能阻止 Leu27IGF-II 诱导的 H9c2 心肌细胞肥大。我们首先使用了 IGF-II 类似物 Leu27IGF-II,它特异性地激活 IGF2R 信号级联反应,并诱导 H9c2 心肌细胞肥大。然而,丹参提取物完全抑制了 Leu27IGF-II 诱导的细胞大小增加、ANP 和 BNP 肥大标志物的表达以及 IGF2R 的诱导。我们还观察到丹参提取物抑制了钙调神经磷酸酶蛋白表达和 NFAT3 核易位,从而抑制了 Leu27IGF-II 诱导的心肌肥大。此外,ICI 完全逆转了丹参对 Leu27IGF-II-IGF2R 信号的作用,这表明丹参的心脏保护作用是通过雌激素受体介导的。我们的研究表明,丹参具有雌激素活性,因此,它可以作为 IGFIIR 诱导的肥大模型中的选择性雌激素受体调节剂。