PUB - Publikationen an der Universität Bielefeld

The investigation of the CH2Cl2-MeOH (1:1) extract of Peperomia vulcanica which showed antileishmanial activity during preliminary screening led to the isolation of two previously unknown compounds named peperolignan (1) and peperotannin (2) along with 13 known compounds. Their structures were determined on the basis of their spectroscopic data. The isolated compounds were assessed in vitro for their antileishmanial and antiplasmodial activities against Leishmania donovani 1S (MHOM/SD/62/1S) promastigotes and the Plasmodium falciparum chloroquine-sensitive 3D7 strain (Pf3D7), respectively. They were also assessed for their cytotoxicity on Raw 264.7 macrophage cells. The mixture of 4-hydroxy-2[(3,4-methylenedioxyphenyl)nonanoyl)cyclo-hexan-1,3-dione and 4-hydroxy-2[(3,4-methylenedioxyphenyl) undecanoyl] cyclo-hexane-1,3-dione (10a and 10b) exhibited potent antiplasmodial activity (IC50 = 0.35 mu g/mL) with selectivity index higher than 10-fold (SI = 63.4) and moderate leishmanicidal activity (IC50 = 12.17 mu g/mL) with very low selectivity index (SI = 1.82). The obtained results could provide an extent of validation to the traditional uses of Peperomia vulcanica for the treatment of malaria in endemic areas.