nan Subeki

In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica

The medicinal plant Brucea javanica (L.) Merr. (Simaroubaceae) is widely distributed throughout Asia where its bitter fruits have been used in traditional medicine for various ailments. Fifteen C-20 quassinoids were isolated from the fruits of B. javanica and examined for their in vitro antitrypanosomal activities against trypomastigotes of Trypanosoma evansi. Bruceine A, bruceantinol, bruceine C, brusatol, and bruceine B showed strong antitrypanosomal activities with IC(50) values in the range of 2.9-17.8nM, which compared well with the standard trypanocidal drugs diminazene aceturate (IC(50)=8.8nM) and suramin (IC(50)=43.2nM). However, dehydrobruceine A, dehydrobruceine B, and dehydrobrusatol were about 2100, 900, and 1200 times less active, respectively, than bruceine A, bruceine B, and brusatol. The relationship of the structure and antitrypanosomal activity of these quassinoid compounds suggested that the presence of a diosphenol moiety in ring A and the nature of the C-15 side chain are important for their activities against T. evansi. This is the first report on the antitrypanosomal activity of isolated quassinoids.

Isolation of antibabesial compounds from Brucea javanica, Curcuma xanthorrhiza, and Excoecaria cochinchinensis

One new curcuminoid, 3′-demethoxycyclocurcumin (1), was isolated from Curcuma xanthorrhiza as an antibabesial compound, together with p-hydroxybenzaldehyde (2) and cleomiscosin A (3) from Brucea javanica and (+)-epiloliolide (4) from Excoecaria cochinchinensis. The antibabesial activities were examined in vitro, and compounds 1–4, and diminazene aceturate were studied with IC50 values of 16.6, 7.6, 15.6, 10.0, and 0.6 μg/ml, respectively.

Anti-babesial compounds from Curcuma xanthorrhiza

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 1H 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 IC50 of the active compounds were compared with that of commercial drug, diminazene aceturate (Ganaseg). IC50 values of Ganaseg, (12R)-, and (12S)-12,13-dihydro-12,13-dihydroxyxanthorrhizols were 0.6 µg mL−1, 8.3 µg mL−1 and 11.6 µg mL−1, respectively.