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Kaempferol-3-O-rutinoside (also known as nicotiflorin) is a natural flavonol glycoside found in various plants, including Solidago virgaurea (goldenrod) and Tetrastigma hemsleyanum. It exhibits a range of pharmacological activities, including anti-inflammatory, antioxidant, neuroprotective, and antineoplastic properties. In preclinical studies, kaempferol-3-O-rutinoside has been shown to inhibit the growth of human breast cancer cell lines (such as MCF-7 and MDA-MB-231) and lung adenocarcinoma cells (such as A549). Its mechanism of action in breast cancer involves the activation of AMPK (5' AMP-activated protein kinase) and the upregulation of FOXO3a, which subsequently induces the expression of the pro-apoptotic protein Bim, leading to G0/G1 cell cycle arrest and apoptosis. In lung cancer models, it has been shown to trigger cytoskeleton collapse, mitochondrial dysfunction, and calcium overload. Additionally, kaempferol-3-O-rutinoside binds to vascular endothelial growth factor C (VEGF-C), potentiating its anti-inflammatory effects in macrophages.
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