In vivo anti-malarial effect of the A-amino alcohol 1t on Plasmodium berghei

被引:3
作者
Bahamontes-Rosa, N. [1 ]
Bucher, K. [1 ]
Held, J. [1 ]
Robin, A. [2 ]
Hoffmann, W. H. [1 ]
Flitsch, S. L. [2 ]
Kremsner, P. G. [1 ,3 ]
Kun, J. F. J. [1 ]
机构
[1] Univ Tubingen, Dept Parasitol, Inst Trop Med, D-72074 Tubingen, Germany
[2] Univ Manchester, Manchester Interdisciplinary Bioctr, Manchester M1 7DN, Lancs, England
[3] Albert Schweitzer Hosp, Med Res Unit, Lambarene, Gabon
关键词
MALARIA PARASITES; CEREBRAL MALARIA; AQUAGLYCEROPORIN; DISEASE;
D O I
10.1007/s00436-009-1348-6
中图分类号
R38 [医学寄生虫学]; Q [生物科学];
学科分类号
07 ; 0710 ; 09 ; 100103 ;
摘要
Glycerol derivatives are a class of compounds, which are easy and inexpensive to produce with potent anti-malarial activities against blood stages of Plasmodium falciparum in vitro. In the present study, one of these compounds, termed 1t, which had the lowest IC50 values, was assessed in a murine malarial model. Nuclear magnetic resonance imaging and Balb/c mice infected with Plasmodium berghei ANKA strain were treated in a 4-day suppressive test. Mice received a once-daily intraperitoneal administration of 50 mg/Kg of the drug for 4 days. Although no parasitaemia clearance was reached, a slower parasite proliferation and a slightly longer survival time compared with the placebo group were observed.
引用
收藏
页码:1459 / 1464
页数:6
相关论文
共 12 条
[1]   PRESENT DEVELOPMENT CONCERNING ANTIMALARIAL ACTIVITY OF PHOSPHOLIPID-METABOLISM INHIBITORS WITH SPECIAL REFERENCE TO IN-VIVO ACTIVITY [J].
ANCELIN, ML ;
VIAL, HJ ;
CALAS, M ;
GIRAL, L ;
PIQUET, G ;
RUBI, E ;
THOMAS, A ;
PETERS, W ;
SLOMIANNY, C ;
HERRERA, S ;
LOUIS, F ;
MOUANDA, V .
MEMORIAS DO INSTITUTO OSWALDO CRUZ, 1994, 89 :85-90
[2]   Limited genetic diversity of the Plasmodium falciparum aquaglyceroporin gene [J].
Bahamontes-Rosa, Noemi ;
Wu, Binghua ;
Beitz, Eric ;
Kremsner, Peter G. ;
Kun, Juergen F. J. .
MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 2007, 156 (02) :255-257
[3]   RENAL-DISEASE IN ACUTE PLASMODIUM-FALCIPARUM INFECTION IN MAN [J].
BOONPUCKNAVIG, V ;
SITPRIJA, V .
KIDNEY INTERNATIONAL, 1979, 16 (01) :44-52
[4]   Antimalarial drug discovery: Efficacy models for compound screening [J].
Fidock, DA ;
Rosenthal, PJ ;
Croft, SL ;
Brun, R ;
Nwaka, S .
NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (06) :509-520
[5]   Malaria: Burden of disease [J].
Guinovart, C ;
Navia, MM ;
Tanner, M ;
Alonso, PL .
CURRENT MOLECULAR MEDICINE, 2006, 6 (02) :137-140
[6]   A single, bi-functional aquaglyceroporin in blood-stage Plasmodium falciparum malaria parasites [J].
Hansen, M ;
Kun, JFJ ;
Schultz, JE ;
Beitz, E .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (07) :4874-4882
[7]   Evidence for multiple pathologic and protective mechanisms of murine cerebral malaria [J].
Jennings, VM ;
Lal, AA ;
Hunter, RL .
INFECTION AND IMMUNITY, 1998, 66 (12) :5972-5979
[8]   Pathogenesis of cerebral malaria: Recent experimental data and possible applications for humans [J].
Lou, J ;
Lucas, R ;
Grau, GE .
CLINICAL MICROBIOLOGY REVIEWS, 2001, 14 (04) :810-820
[9]   Dihydroxyacetone and methylglyoxal as permeants of the Plasmodium aquaglyceroporin inhibit parasite proliferation [J].
Pavlovic-Djuranovic, Slavica ;
Kun, Juergen F. J. ;
Schultz, Joachim E. ;
Beitz, Eric .
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, 2006, 1758 (08) :1012-1017
[10]   Microwave-assisted ring opening of epoxides: A general route to the synthesis of 1-aminopropan-2-ols with anti malaria parasite activities [J].
Robin, Aelig ;
Brown, Fraser ;
Bahamontes-Rosa, Noemi ;
Wu, Binghua ;
Beitz, Eric ;
Kun, Jurgen F. J. ;
Flitsch, Sabine L. .
JOURNAL OF MEDICINAL CHEMISTRY, 2007, 50 (17) :4243-4249