Isoscopoletin is a coumarin that has been found in D. fragrans and has diverse biological activities and is an active metabolite of scoparone .1,2,3,4,5 It is formed from scoparone by the cytochrome P450 (CYP) isoform Cyp2c29 in mouse liver microsomes.5 Isoscopoletin is cytotoxic to A549 lung, MCF-7 breast, and HepG2 liver cancer cells (IC50s = 5.25, 8.58, and 4.76 ?M, respectively).1 It is active against Gram-positive and Gram-negative bacteria, including S. aureus and E. coli, respectively, as well as the plant pathogenic fungus A. niger, in agar diffusion assays.2 Isoscopoletin inhibits 15-lipoxygenase (15-LO; IC50 = 15.1 ?M) and reduces paw thickness in a rat model of carrageenan-induced paw edema when administered at a dose of 0.1 mg/kg.3,4
1.Zhao, D.-D., Zhao, Q.-S., Liu, L., et al.Compounds from Dryopteris fragrans (L.) Schott with cytotoxic activityMolecules19(3)3345-3355(2014) 2.Nazir, S., Li, B., Tahir, K., et al.Antimicrobial activity of five constituents isolated from Ranunculus muricatusJ. Med. Plants Res.7(47)3438-3443(2013) 3.Deng, S., Palu, A.K., West, B.J., et al.Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in TahitiJ. Nat. Prod.70(5)859-862(2007) 4.Selim, Y.A., and Ouf, N.H.Anti-inflammatory new coumarin from the Ammi majus LOrg. Med. Chem. Lett.2(1)1(2012) 5.Meyer, R.P., Hagemeyer, C.E., Knoth, R., et al.Oxidative hydrolysis of scoparone by cytochrome P450 CYP2C29 reveals a novel metaboliteBiochem. Biophys. Res. Commun.285(1)32-39(2001)