Scutellarin is cytotoxic to cancer cells and could induce DNA damage, metabolic suppression and mitochondrial reactive oxygen species. It has has antioxidant, anti-inflammatory, and antiproliferative biological activities that can be can be found in scutellaria lateriflora.
Scutellarein is a flavonoid monomer found in traditional Chinese medicine such as Scutellaria barbata. Scutellarein treatment showed potent cytotoxicity on MM (multiple myeloma) cells but not on viable CBL(circulating B lymphocytes), and intravenous injection of scutellarein significantly reduced MM xenograft tumor burden in nude mice. Scutellarein treatment in MM cells activated the mitochondrial-mediated intrinsic apoptosis pathway by increasing the production of mitochondrial superoxide, which was reduced to ROS by NADPH, but this effect was weakened in healthy CBL. Co-treatment with scutellarein synergized with bortezomib in inducing apoptosis in MM cells in vitro and in reducing tumor volume in MM xenografted nude mice[3]. Scutellarein can induce apoptosis of HCT116 cells. Scutellarein can increase the production of intracellular ROS and lead to the collapse of mitochondrial membrane potential. Meanwhile, the activity of caspase-3 in HCT116 cells was elevated by scutellarein. Moreover, down-regulated Bcl-2 and up-regulated Bax were observed. Additionaly, scutellarein resulted in cytochrome c release from mitochondria[4]. Scutellarein has antiproliferative index against multiple cancer cell lines and diminished the oxidative stress and tumor development of murine ascitic lymphoma & inflammatory hepatocellular carcinoma[5]. Scutellarein possesses important novel anti-obesity effects accompanying lipid lowering and anti-inflammation-based liver protective effects. The antagonistic effect of Scutellarein on hyperlipidemia was a result of the repression of the lipid synthesis pathway, de novo pathway, HMGCR, promoting fatty acid oxidation (PPARα, CPT-1a) and increased cholesterol output (PPARγ-LXRα-ABCA1)[6].
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