ABSTRACT
Anti-babesial ingredients, (12R)- and (12S)-12,13-dihydro-12,13-dihydroxyxanthorrhizols, were isolated from Curcuma xanthorrhiza. The structures were established by the extensive NMR techniques. The assignments of (1)H NMR data of (12R)-12,13-dihydro-12,13-dihydroxyxanthorrhizol was revised, and (12S)-12,13-dihydro-12,13-dihydroxyxanthorrhizol was isolated as a pure form for the first time. The IC(50) of the active compounds were compared with that of commercial drug, diminazene aceturate (Ganaseg). IC(50) values of Ganaseg, (12R)-, and (12S)-12,13-dihydro-12,13-dihydroxyxanthorrhizols were 0.6 microg mL(-1), 8.3 microg mL(-1) and 11.6 microg mL(-1), respectively.
Subject(s)
Antiprotozoal Agents/isolation & purification , Antiprotozoal Agents/pharmacology , Babesia/drug effects , Curcuma/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Animals , Antiprotozoal Agents/chemistry , Babesia/growth & development , Indonesia , Inhibitory Concentration 50 , Mass Spectrometry , Nuclear Magnetic Resonance, Biomolecular , Optical Rotation , Phenols/chemistry , Spectrophotometry, Infrared , Spectrophotometry, UltravioletABSTRACT
Anti-babesial activity was confirmed in an extract of the bark of Curcuma zedoaria. The active ingredients were isolated, and their chemical structures were determined to be zedoalactones A, B, and C based on spectral data. Zedoalactone C is a hitherto unreported compound. The IC50 vales of these active compounds against Babesia gibsoni were compared with a standard drug, diminazene aceturate. The IC50 value of diminazene aceturate was 0.6 microg/mL, while those of zedoalactones A, B, and C were 16.5, 1.6 and 4.2 microg/mL, respectively.
Subject(s)
Antiprotozoal Agents/pharmacology , Babesia/drug effects , Curcuma , Phytotherapy , Plant Extracts/pharmacology , Animals , Antiprotozoal Agents/administration & dosage , Antiprotozoal Agents/therapeutic use , Babesiosis/drug therapy , Humans , Parasitic Sensitivity Tests , Plant Bark , Plant Extracts/administration & dosage , Plant Extracts/therapeutic useABSTRACT
Bark extracts from a total of 22 species of Central Kalimantan plants were evaluated for their anti-babesial activity against Babesia gibsoni in vitro. Of these plant species, extracts of Calophyllum tetrapterum, Garcinia rigida, Lithocarpus sp., Sandoricum emarginatum, and Shorea balangeran showed more than 90% inhibition of the parasite growth at a test concentration of 1000 microg/mL. Activity-guided fractionation of the bark of S. balangeran (Dipterocarpaceae) led to the reisolation of oligostilbenoids, vaticanol A(1), B(2), and G(3). The structures were determined on the basis of spectral evidence. Compounds 1 and 3 showed complete inhibition on the growth of Babesia gibsoni in vitro at a concentration of 25 microg/mL, and compound 2 at concentration of 50 microg/mL.
