TY - JOUR
T1 - Potent in vivo antimalarial activity of 3,15-di-O-acetylbruceolide against Plasmodium berghei infection in mice
AU - Kim, Hye Sook
AU - Shibata, Yasuharu
AU - Ko, Naoko
AU - Ikemoto, Naomi
AU - Ishizuka, Yuki
AU - Murakami, Nobutoshi
AU - Sugimoto, Masanori
AU - Kobayashi, Motomasa
AU - Wataya, Yusuke
N1 - Funding Information:
This work was supported by a Grant-in-Aids for Scientific Research on Priority Areas (08281105 Y.W.) from the Ministry of Education, Science, Culture and Sports, and supported in part by the Japanese Society for the Promotion of Science (H.-S.K.). The research was financially supported by the Sasakawa Scientific Research Grant from the Japan Science Society (H.-S.K.).
PY - 2000/1/1
Y1 - 2000/1/1
N2 - The antimalarial activity of the O-acylated bruceolide derivative, 3,15-di-O-acetylbruceolide, was evaluated against Plasmodium berghei in vivo. The concentration of 3,15-di-O-acetylbruceolide required for 50% suppression (ED50) of P. berghei in mice was 0.46±0.06 mg/kg/day, whereas bruceolide was only half as effective as 3,15-di-O-acetylbruceolide. Two antimalarial drugs used clinically, chloroquine and artemisinin, demonstrated only low activity corresponding to 1/4 and 1/12 of the ED50 value of 3,15-di-O-acetylbruceolide, respectively. These results may be helpful in the design of better chemotherapeutic bruceolides against falciparum malaria. Copyright (C) 2000 Elsevier Science Ireland Ltd.
AB - The antimalarial activity of the O-acylated bruceolide derivative, 3,15-di-O-acetylbruceolide, was evaluated against Plasmodium berghei in vivo. The concentration of 3,15-di-O-acetylbruceolide required for 50% suppression (ED50) of P. berghei in mice was 0.46±0.06 mg/kg/day, whereas bruceolide was only half as effective as 3,15-di-O-acetylbruceolide. Two antimalarial drugs used clinically, chloroquine and artemisinin, demonstrated only low activity corresponding to 1/4 and 1/12 of the ED50 value of 3,15-di-O-acetylbruceolide, respectively. These results may be helpful in the design of better chemotherapeutic bruceolides against falciparum malaria. Copyright (C) 2000 Elsevier Science Ireland Ltd.
KW - 3,15-di-O-acetylbruceolide
KW - Antimalarial agent
KW - Brucea javanica
KW - P. berghei
KW - P. falciparum
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U2 - 10.1016/S1383-5769(99)00023-9
DO - 10.1016/S1383-5769(99)00023-9
M3 - Article
C2 - 11227768
AN - SCOPUS:0033991555
VL - 48
SP - 271
EP - 274
JO - Parasitology International
JF - Parasitology International
SN - 1383-5769
IS - 3
ER -
