- Screening of Indonesian medicinal plant extracts for antibabesial activity and isolation of new quassinoids from Brucea javanica
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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 μg/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,Matsuura, Hideyuki,Takahashi, Kosaku,Nabeta, Kensuke,Yamasaki, Masahiro,Maede, Yoshimitsu,Katakura, Ken
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p. 1654 - 1657
(2008/03/11)
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- Conversion of quassinoids for enhancement of inhibitory effect against Epstein-Barr virus early antigen activation. Introduction of lipophilic side chain and esterification of diosphenol
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Introduction of a senecioyl group into shinjulactones B and C, and esterification of the diosphenol moiety in brusatol and brucein A enhanced inhibitory effect against Epstein-Barr virus early antigen activation.
- Tamura, Sadaaki,Fukamiya, Narihiko,Mou, Xiao-Yang,Mukainaka, Teruo,Tokuda, Harukuni,Nishino, Hoyoku,Tagahara, Kiyoshi,Koike, Kazuo,Lee, Kuo-Hsiung,Okano, Masayoshi
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p. 876 - 878
(2007/10/03)
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