Screening of Indonesian medicinal plant extracts for antibabesial activity and isolation of new quassinoids from Brucea javanica.
Boiled extracts derived from 28 Indonesian medicinal plants were screened for their antibabesial activity against Babesia gibsoni in vitro. Of these extracts, the fruit of Brucea javanica was the most active in inhibiting parasite growth at a concentration of 10 microg/mL. Bioassay-guided fractionation of the fruit extract of Br. javanica led to the isolation of two new quassinoids, bruceantinol B and bruceine J, and the structures of these compounds were elucidated on the basis of their spectroscopic data and by chemical transformation to known compounds. In addition, the known quassinoids bruceines A-D, bruceantinol, and yadanziolide A were isolated. Antibabesial activities were also examined in vitro, and bruceine A and bruceantinol were shown to be more potent than diminazene aceturate, a drug (IC50 = 103 ng/mL) used clinically against B. gibsoni, with IC50 values of 4 and 12 ng/mL, respectively.
Subeki
Laboratory of Parasitology, Department of Disease Control, Graduate School of Veterinary Medicine, Hokkaido University, Sapporo 060-0818, Japan.
Matsuura
Hideyuki
H
Takahashi
Kosaku
K
Nabeta
Kensuke
K
Yamasaki
Masahiro
M
Maede
Yoshimitsu
Y
Katakura
Ken
K
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001403:Babesia / Q000187:drug effects*; D032269:Brucea / Q000737:chemistry*; D004133:Diminazene / Q000031:analogs & derivatives* / Q000494:pharmacology; D007214:Indonesia; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010946:Plants, Medicinal / Q000737:chemistry*; D036702:Quassins / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*
D000981:Antiprotozoal Agents; D036702:Quassins; C524985:bruceantinol B; C524984:bruceine J; C003915:diminazene aceturate; D004133:Diminazene