alpha-Asarone (α-Asarone)

α-Asarone is a component of certain essential oils used in traditional Chinese herbal medicine. Although carcinogenic, α-asarone has been shown to be neuroprotective and radioprotective in mice when given at 50 mg/kg.^1,2,3 It also lowers serum cholesterol in rats, specifically reducing LDL-cholesterol levels and cholesterol saturation index, by directly inhibiting HMG-CoA reductase (IC₅₀ = 3 mM).^4,5 α-Asarone also directly interacts with and inhibits certain isoforms of cytochrome P450 (IC₅₀ = 55.2 and 65.2 μg/ml for CYP2D6 and CYP3A4, respectively).⁶

1.Limón, I.D., Mendieta, L., Díaz, A., et al.Neuroprotective effect of alpha-asarone on spatial memory and nitric oxide levels in rats injected with amyloid-β(25-35)Neurosci. Lett.453(2)98-103(2009) 2.Sandeep, D., and Nair, C.K.Radioprotection by α-asarone: Prevention of genotoxicity and hematopoietic injury in mammalian organismMutat. Res.722(1)62-68(2011) 3.Zuo, H.L., Yang, F.Q., Zhang, X.M., et al.Separation of cis- and trans-Asarone from Acorus tatarinowii by preparative gas chromatographyJ. Anal. Methods Chem.402081(2012) 4.Rodríguez-Páez, L., Juárez-Sanchez, M., Antúnez-Solís, J., et al.α-Asarone inhibits HMG-CoA reductase, lowers serum LDL-cholesterol levels and reduces biliary CSI in hypercholesterolemic ratsPhytomedicine10(5)397-404(2003) 5.Antunez-Solis, J., Hernández-Derramadero, F., Aquino-Vega, M., et al.2,4,5-trimethoxycinnamic acid: The major metabolite of α-asarone, retains most of the pharmacological properties of α-asaroneJ. Enzyme Inhib. Med. Chem.24(3)903-909(2009) 6.Pandit, S., Mukherjee, P.K., Ponnusankar, S., et al.Metabolism mediated interaction of α-asarone and Acorus calamus with CYP3A4 and CYP2D6Fitoterapia82(3)369-374(2011)