Ligustrazine (hydrochloride)

Ligustrazine is a compound that has been found in L. wallichii and has diverse biological activities, including antioxidant, anti-inflammatory, neuroprotective, and anticancer properties.^1,2,3 It inhibits hydrogen peroxide-induced decreases in cell viability and the levels of superoxide dismutase (SOD) and glutathione peroxidase (GPX) and increases in reactive oxygen species (ROS) and malondialdehyde (MDA) levels in human umbilical vein endothelial cells (HUVECs) when used at concentrations of 100 and 150 μg/ml.¹ Ligustrazine (50 and 100 μM) inhibits prostaglandin E₂ (PGE₂; Item No. 14010) production induced by LPS and IFN-γ in primary rat glia.² It reduces infarct volume, cortical edema, and cortical PGE₂ levels in a rat model of transient focal cerebral ischemia induced by common carotid artery and middle cerebral artery occlusion when administered at a dose of 20 mg/kg. Ligustrazine inhibits the proliferation of MG-63, Saos-2, and U2OS osteosarcoma cells (IC₅₀s = 10.3, 24.7, and 54.7 mg/ml, respectively) in vitro and reduces tumor growth in an MG-63 mouse xenograft model when administered at a dose of 100 mg/kg every other day.³

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1. Li , W.-M., Liu, H.-T., Li, X.-Y., et al. The effect of tetramethylpyrazine on hydrogen peroxide-induced oxidative damage in human umbilical vein endothelial cells. Basic Clin. Pharmacol. Toxicol. 106(1), 45-52 (2010).

2. Liao, S.-L., Kao, T.-K., Chen, W.-Y., et al. Tetramethylpyrazine reduces ischemic brain injury in rats. Neurosci. Lett. 372(1-2), 40-45 (2004).

3. Wang, Y., Fu, Q., and Zhao, W. Tetramethylpyrazine inhibits osteosarcoma cell proliferation via downregulation of NF-κB in vitro and in vivo. Mol. Med. Rep. 8(4), 984-988 (2013).