Potent in vivo antimalarial activity of 3,15-di-O-acetylbruceolide against Plasmodium berghei infection in mice.
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.
Faculty of Pharmaceutical Sciences, Okayama University, Tsushima, Okayama 700-8530, Japan.
H S
HS
Kim
Y
Y
Shibata
N
N
Ko
N
N
Ikemoto
Y
Y
Ishizuka
N
N
Murakami
M
M
Sugimoto
M
M
Kobayashi
Y
Y
Wataya
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D037621:Artemisinins; D002243:Carbolines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002738:Chloroquine / Q000494:pharmacology / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D008288:Malaria / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010962:Plasmodium berghei / Q000187:drug effects*; D011728:Pyridones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011897:Random Allocation; D012717:Sesquiterpenes / Q000494:pharmacology / Q000627:therapeutic use
C423227:3,15-di-O-acetylbruceolide; D000962:Antimalarials; D037621:Artemisinins; D002243:Carbolines; D011728:Pyridones; D012717:Sesquiterpenes; D002738:Chloroquine; C031327:artemisinin