Lupenone

Lupenone is a triterpenoid that has been found in L. eriocalyx and has diverse biological activities.^1,2,3,4 It inhibits HIV-1 reverse transcriptase (IC₅₀ = 2.1 μM).¹ Lupenone is active against the W2 and D6 strains of P. falciparum (IC₅₀s = 208.1 and 394.7 ng/ml, respectively).² It induces melanogenesis in (EC₅₀ = 0.35 ?M), and inhibits the growth of, B16 2F2 melanoma cells in vitro (IC₅₀ = 25.4 ?M).³ Topical application of lupenone (1 mg/ear) reduces ear edema induced by phorbol 12-myristate 13-acetate in mice.⁴ It also inhibits acetic acid-induced writhing in mice when administered at a dose of 100 mg/kg.²

1.Akihisa, T., Ogihara, J., Kato, J., et al.Inhibitory effects of triterpenoids and sterols on human immunodeficiency virus-1 reverse transcriptaseLipids36(5)507-512(2001) 2.Manguro, L.O.A., Owuor, P.O., and Ochung, A.A.Isolation, characterization and biological activities of phytoconstituents from Lonchocarpus eriocalyx harms leavesTrends Phytochem. Res.2(3)135-146(2018) 3.Hata, K., Hori, K., and Takahashi, S.Differentiation- and apoptosis-inducing activities by pentacyclic triterpenes on a mouse melanoma cell lineJ. Nat. Prod.65(5)645-648(2002) 4.Yasukawa, K., Yu, S., Yamanouchi, S., et al.Some lupane-type triterpenes inhibit tumor promotion by 12-O-tetradecanoylphorbol-13-acetate in two-stage carcinogenesis in mouse skinPhytomedicine1(4)309-313(1995)