ANTIMALARIAL ACTIVITY OF CEDRONIN

被引:30
作者
MORETTI, C
DEHARO, E
SAUVAIN, M
JARDEL, C
DAVID, PT
GASQUET, M
机构
[1] IBBA, ORSTOM, FARMACOGNOSIA LAB, LA PAZ, BOLIVIA
[2] ORSTOM, NOUMEA, NEW CALEDONIA
[3] CHU TIMONE, PARASITOL LAB, F-13385 MARSEILLE, FRANCE
关键词
CEDRONIN; QUASSINOIDS; ANTIMALARIAL ACTIVITY; SIMABA CEDRON; SIMAROUBACEAE;
D O I
10.1016/0378-8741(94)90117-1
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Cedronin was isolated from Simaba cedron Planchon (Simaroubaceae), a species popularly believed in South America to have antimalarial properties. It was examined for in vitro and in vivo antimalarial activities and for cytotoxicity against KB cells. Experimental results showed that cedronin was active against chloroquine-sensitive and resistant strain, with an IC50 of 0.25 mu g/ml (0.65 mu mol/ml). It was also found to be active in vivo against Plasmodium vinkei with an IC50 of 1.8 mg/kg (4.7 nM/kg) in the classic 4-day test. Cedronin belongs to the small group of quassinoids with a C-19 basic skeleton and shows a rather low cytotoxicity against KB cells (IC50 = 4 mu g/ml, 10.4 mu M) as compared with C-20 biologically active quassinoids; however its toxic/therapeutic ratio (10/1.8) remains lower than chloroquine (10/0.5).
引用
收藏
页码:57 / 61
页数:5
相关论文
共 18 条
[1]  
ANDERSON M M, 1990, Planta Medica, V56, P649, DOI 10.1055/s-2006-961301
[2]   NEW OBSERVATIONS ON MALARIA PARASITES OF RODENTS OF CENTRAL AFRICAN REPUBLIC - PLASMODIUM-VINCKEI PETTERI SUBSP NOV AND PLASMODIUM-CHABAUDI LANDAU, 1965 [J].
CARTER, R ;
WALLIKER, D .
ANNALS OF TROPICAL MEDICINE AND PARASITOLOGY, 1975, 69 (02) :187-+
[3]  
CHAN KL, 1986, PLANTA MED, P105, DOI 10.1055/s-2007-969091
[4]   INVITRO AND INVIVO ASSESSMENT OF THE ANTIMALARIAL ACTIVITY OF SERGEOLIDE [J].
FANDEUR, T ;
MORETTI, C ;
POLONSKY, J .
PLANTA MEDICA, 1985, 51 (01) :20-23
[5]  
FEUILLET C, 1983, CNDOLLEA, V38, P746
[6]  
Grenand P.C., 1987, PHARMACOPEES TRADITI
[7]   CEDRONIN AND 7-EPI-CEDRONIN - X-RAY CRYSTAL-STRUCTURE ANALYSIS [J].
JACOBS, H ;
LEWIS, DE ;
SAWYER, JF ;
MCLEAN, S .
JOURNAL OF NATURAL PRODUCTS, 1987, 50 (04) :700-705
[8]   INVITRO STUDIES ON THE MODE OF ACTION OF QUASSINOIDS WITH ACTIVITY AGAINST CHLOROQUINE-RESISTANT PLASMODIUM-FALCIPARUM [J].
KIRBY, GC ;
ONEILL, MJ ;
PHILLIPSON, JD ;
WARHURST, DC .
BIOCHEMICAL PHARMACOLOGY, 1989, 38 (24) :4367-4374
[9]  
LECOINTE P, 1922, AMAZONIE BRESILIENNE, P513
[10]   2 NEW QUASSINOIDS FROM SIMABA-MULTIFLORA FRUITS [J].
MORETTI, C ;
BHATNAGAR, S ;
BELOEIL, JC ;
POLONSKY, J .
JOURNAL OF NATURAL PRODUCTS, 1986, 49 (03) :440-444