| In Vitro | In vitro activity: Alizarin weakly inhibits CYP2A6 and CYP2E1. Alizarin shows competitive inhibition against CYP1B1 with Ki of 0.5 μM. Alizarin reduces the mutagenicity of MeIQx, which induced by each CYP1A2 or CYP1B1, while does not effectively reduce the mutation induced by B[a]P. Alizarin exhibits antioxidants against iodophenol-derived phenoxyl radicals, superoxide anion radicals and lipid peroxidation in rat liver microsomes.
Cell Assay: Alizarin is proved to have anti-tumor efficacy. It suppresses the cell growth of the prostate cancer, breast cancer and osteosarcoma cell lines in vitro. Among these, the osteosarcoma cells appear to be most sensitive. The IC50 values of Alizarin against three osteosarcoma cell lines Saos-2, MG-63 and U-2 OS are 27.5, 29 and 69.9μg/ml, respectively. Alizarin inhibits the cell growth through cell proliferation blockade rather than induction of apoptosis. It inhibits the phosphorylation of ERK. In addition, Alizarin is also found to induce S-phase arrest as well as a decrease of the G0/G1 and G2/M phases. |
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