The mode of action of the antimalarial artemisinin and its derivatives

被引:67
作者
Kamchonwonggpaisan, S [1 ]
Meshnick, SR [1 ]
机构
[1] UNIV MICHIGAN, SCH PUBL HLTH, DEPT EPIDEMIOL, ANN ARBOR, MI 48109 USA
来源
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1996年 / 27卷 / 04期
关键词
areether; artemether; artesunate; oxidant; peroxide; plasmodium; trioxane;
D O I
10.1016/0306-3623(95)02047-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1. Artemisinin (qinghaosu) is a sesquiterpene endoperoxide derived from a plant which was used in Chinese herbal medicine for thousands of years. 2. Artemisinin and its derivatives have potent antimalarial activity, and are now being used clinically in much of the world. 3. The artemisinin derivatives have an unusual mode of action involving the iron catalyzed generation of a carbon-centered free radical followed by the alkylation of malaria specific proteins.
引用
收藏
页码:587 / 592
页数:6
相关论文
共 85 条
[1]  
Aboul-Enein H Y, 1989, Drug Des Deliv, V4, P129
[2]   CONCENTRATION AND TIME DEPENDENCY OF ARTEMISININ EFFICACY AGAINST PLASMODIUM-FALCIPARUM IN-VITRO [J].
ALIN, MH ;
BJORKMAN, A .
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 1994, 50 (06) :771-776
[3]  
[Anonymous], 1979, CHINESE MED J-PEKING, V92, P811
[4]  
[Anonymous], 1994, T R SOC TROP MED S1, DOI DOI 10.1016/0035-9203(94)90459-6
[5]  
ASAWAMAHASAKDA W, 1994, J LAB CLIN MED, V123, P757
[6]   REACTION OF ANTIMALARIAL ENDOPEROXIDES WITH SPECIFIC PARASITE PROTEINS [J].
ASAWAMAHASAKDA, W ;
ITTARAT, I ;
PU, YM ;
ZIFFER, H ;
MESHNICK, SR .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1994, 38 (08) :1854-1858
[7]   STRUCTURE-ACTIVITY-RELATIONSHIPS OF THE ANTIMALARIAL AGENT ARTEMISININ .1. SYNTHESIS AND COMPARATIVE MOLECULAR-FIELD ANALYSIS OF C-9 ANALOGS OF ARTEMISININ AND 10-DEOXOARTEMISININ [J].
AVERY, MA ;
GAO, FG ;
CHONG, WKM ;
MEHROTRA, S ;
MILHOUS, WK .
JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (26) :4264-4275
[8]   DECOMPOSITION OF ARTEETHER IN SIMULATED STOMACH ACID YIELDING COMPOUNDS RETAINING ANTIMALARIAL ACTIVITY [J].
BAKER, JK ;
MCCHESNEY, JD ;
CHI, HT .
PHARMACEUTICAL RESEARCH, 1993, 10 (05) :662-666
[9]   NEUROTOXICITY IN ANIMALS DUE TO ARTEETHER AND ARTEMETHER [J].
BREWER, TG ;
PEGGINS, JO ;
GRATE, SJ ;
PETRAS, JM ;
LEVINE, BS ;
WEINA, PJ ;
SWEARENGEN, J ;
HEIFFER, MH ;
SCHUSTER, BG .
TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE, 1994, 88 :33-36
[10]   FATAL NEUROTOXICITY OF ARTEETHER AND ARTEMETHER [J].
BREWER, TG ;
GRATE, SJ ;
PEGGINS, JO ;
WEINA, PJ ;
PETRAS, JM ;
LEVINE, BS ;
HEIFFER, MH ;
SCHUSTER, BG .
AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 1994, 51 (03) :251-259