Department of Pharmacology, Harbin Medical University, Baojian Road 157, Harbin, Heilongjiang 150081, People's Republic of China.
Naunyn Schmiedebergs Arch Pharmacol. 2010 Feb;381(2):137-45. doi: 10.1007/s00210-009-0484-y. Epub 2010 Jan 6.
Scutellarin is a flavonoid extracted from a traditional Chinese herb, Erigeron breviscapus Hand Mazz, which has been broadly used in treating various cardiovascular diseases. In this study, we investigated its effect on cardiac hypertrophy and the underlying mechanism. Both in vitro and in vivo cardiac hypertrophy models were employed to explore the anti-hypertrophic action of scutellarin. We found that scutellarin significantly suppressed the hypertrophic growth of neonatal cardiac myocytes exposed to phenylephrine (PE) and mouse heart subjected to pressure overload induced by aortic banding, accompanied with the decreased expression of hypertrophic markers beta-myosin heavy chain and atrial natriuretic peptide. We then measured the change of free intracellular calcium using laser scanning confocal microscope. We found that scutellarin alleviated the increment of free intracellular calcium during cardiac hypertrophy either induced by PE or aortic banding. The expression of calcium downstream effectors calcineurin and phosphorylated calmodulin kinase II (CaMKII) were significantly suppressed by scutellarin. Our study indicated that scutellarin exerts its anti-hypertrophic activity via suppressing the Ca(2+)-mediated calcineurin and CaMKII pathways, which supports the observation that clinical application of scutellarin is beneficial for cardiovascular disease patients.
野黄芩苷是一种从传统中药灯盏细辛中提取的黄酮类化合物，广泛用于治疗各种心血管疾病。在本研究中，我们研究了它对心肌肥厚的作用及其潜在机制。我们采用体外和体内心肌肥厚模型来研究野黄芩苷的抗肥厚作用。结果发现，野黄芩苷显著抑制了去甲肾上腺素（PE）诱导的新生大鼠心肌细胞和主动脉缩窄诱导的小鼠心脏的心肌肥厚，同时降低了肥厚标志物β-肌球蛋白重链和心钠肽的表达。然后，我们使用激光共聚焦显微镜测量了细胞内游离钙的变化。结果发现，野黄芩苷减轻了由 PE 或主动脉缩窄引起的心肌肥厚过程中细胞内游离钙的增加。野黄芩苷显著抑制了钙调神经磷酸酶和磷酸化钙调蛋白激酶 II（CaMKII）这两种钙下游效应物的表达。我们的研究表明，野黄芩苷通过抑制 Ca(2+)-介导的钙调神经磷酸酶和 CaMKII 通路发挥抗肥厚作用，这支持了野黄芩苷的临床应用有益于心血管疾病患者的观察结果。
