5-Methoxycanthinone (Synonyms: 5-Methoxycanthin-6-one, NSC 88929)

5-Methoxycanthinone is an alkaloid that has been found in L. floridana and has anticancer properties.¹ It is cytotoxic to KB, A549, and HCT-8 cells (EC₅₀s = 2.9, 3.1, and 2.5 µg/ml, respectively). It is active against the P. falciparum mefloquine-resistant strain F32 and the multidrug and chloroquine-resistant strain K1 (IC₅₀s = 10.4 and 5.1 µg/ml, respectively).² However, it increases the parasite load by 68.4% in a mouse model of leishmaniasis when administered at a dose of 10 mg/kg per day.³

1.Xu, Z., Chang, F.R., Wang, H.-K., et al.Anti-HIV agents 45 and antitumor agents 205. Two new sesquiterpenes, leitneridanins A and B, and the cytotoxic and anti-HIV principles from Leitneria floridanaJ. Nat. Prod.63(12)1712-1715(2000) 2.CebriÁn-TorrejÓn, G., Spelman, K., Leblanc, K., et al.The antiplasmodium effects of a traditional South American remedy: Zanthoxylum chiloperone var. Angustifolium against chloroquine resistant and chloroquine sensitive strains of Plasmodium falciparumRevista Brasileira de Farmacognosia21(4)652-661(2011) 3.Ferreira, M.E., Rojas de Arias, A., Torres de Ortiz, S., et al.Leishmanicidal activity of two canthin-6-one alkaloids, two major constituents of Zanthoxylum chiloperone var. angustifoliumJ. Ethnopharmacol.80(2-3)199-202(2002)