Isorhamnetin, a natural flavonol aglycone, can inhibit xanthine oxidase with IC50 of 400nM and stabilize β-catenin as well as up-regulate the Wnt signaling pathway. Isorhamnetin could also be act as an apoptosia inducer with antitumor activities.
Isorhamnetin, a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L., is well known for its anti-inflammatory, anti-oxidative, anti-adipogenic, anti-proliferative, and anti-tumor activities. Isorhamnetin could inhibit cardiac hypertrophy and fibrosis 8 weeks after aortic banding. In vitro studies performed in neonatal rat cardiomyocytes confirmed that isorhamnetin could attenuate cardiomyocyte hypertrophy induced by angiotensin II, which was associated with phosphatidylinositol 3-kinase-AKT signaling pathway[3]. Isorhamnetin inhibited epidermal growth factor (EGF)-induced neoplastic cell transformation. Isorhamnetin attenuated EGF-induced COX-2 expression in JB6 and A431 cells. In an in vivo mouse xenograft using A431 cells, isorhamnetin reduced tumor growth and COX-2 expression[4]. Isorhamnetin inhibits the proliferation of numerous breast cancer cells (IC50, ~10 µM), including MCF7, T47D, BT474, BT-549, MDA-MB-231 and MDA-MB-468, whereas less inhibitory activity is observed in the MCF10A normal breast epithelial cell line (IC50, 38 µM) [5]. Isorhamnetin inhibits the TGF-β/Smad signaling pathway and relieves oxidative stress, thus inhibiting HSC (hepatic stellate cells) activation and preventing liver fibrosis[6].
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