In vitro and in vivo antimalarial activity of ferrochloroquine, a ferrocenyl analogue of chloroquine against chloroquine-resistant malaria parasites

被引：0

作者：

L. Delhaes

H. Abessolo

C. Biot

L. Berry

P. Delcourt

L. Maciejewski

J. Brocard

D. Camus

D. Dive

机构：

[1] INSERM Unité 167,

[2] Institut Pasteur,undefined

[3] 1 rue du Pr. Calmette,undefined

[4] B.P. 245,undefined

[5] 59019 Lille Cedex,undefined

[6] France e-mail: daniel.dive@pasteur-lille.fr Tel.: +33-3-20877896; Fax: +33-3-20877888,undefined

[7] INSERM Unité 42,undefined

[8] 369 rue Jules Guesde,undefined

[9] B.P. 39,undefined

[10] 59651 Villeneuve D'Ascq Cedex,undefined

[11] France,undefined

[12] Service de Parasitologie-Mycologie,undefined

[13] Faculté de Médecine,undefined

[14] 1 Place de Verdun,undefined

[15] 59045 Lille Cedex 2,undefined

[16] France,undefined

[17] Laboratoire de Catalyse-Synthèse Organométallique,undefined

[18] UPRESA CNRS 8010,undefined

[19] ENSCL,undefined

[20] Bâtiment C7,undefined

[21] Université des Sciences et Technologies,undefined

[22] B.P. 108,undefined

[23] 59652 Villeneuve D'Ascq Cedex,undefined

[24] France,undefined

来源：

Parasitology Research | 2001年 / 87卷

关键词：

Malaria; Growth Inhibition; Malaria Parasite; Acute Toxicity; Chloroquine;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Previous studies have shown that ferrochloroquine (FQ) exhibited an antimalarial activity against Plasmodium spp. The present work confirmed this activity, described the curative effect on P. vinckei and investigated the FQ toxicity in vitro and in vivo. The in vitro and in vivo growth inhibition of P. falciparum and P. berghei N, respectively, showed that FQ antimalarial activity was 1.5–10 times more potent than chloroquine. FQ completely inhibited the in vivo development of both chloroquine-susceptible and resistant P. vinckei strains and protected mice from lethal infection at a dose of 8.4 mg kg−1 day−1 given for 4 days subcutaneously or orally. This curative effect was 5–20 times more potent than chloroquine, according to the strains' resistance to chloroquine. At this curative dose, no clinical changes were observed in mice up to 14 days after the last administration. Nevertheless, the acute toxicity and lethality of ferrochloroquine seemed to be dependent on gastric surfeit. The FQ security index determined in vitro confirmed that it might be a promising compound.

引用

页码：239 / 244

页数：5