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[氯喹在氯喹敏感及氯喹耐药伯氏疟原虫中的蓄积与外排]

[Accumulation and effluxion of chloroquine in chloroquine-sensitive and chloroquine-resistant Plasmodium berghei].

作者信息

Wang Q, Wang M, Chang H, Yang B

机构信息

Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai 200025.

出版信息

Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1998;16(3):189-92.

PMID:12078239
Abstract

AIM

To explore whether the difference in the amount of chloroquine (CQ) accumulated in CQ-resistant (CR) and in CQ-sensitive (CS) P. berghei is involved in the infected erythrocytes (RBC) or in the parasites.

METHODS

The concentration of CQ in infected RBC and parasites following ig administration of CQ to CS and CR infected mice was determined by HPLC method (extra standard).

RESULTS

3 h after 4.06 mg/kg and 400 mg/kg administration, the accumulation of CQ in both infected RBC was similar, but in CR was 54.0% and 42.1% less than in CS (P < 0.001) respectively. The CQ accumulation in CS 3 h and 7 h after ig administration of CQ 400 mg/kg was similar (0.780 +/- 0.128 nmol/protein and 0.760 +/- 0.180 nmol/mg protein), while in CR the CQ-accumulation was higher at 7 h than that at 3 h after CQ administration (0.452 +/- 0.079 nmol/mg protein and 0.559 +/- 0.124 nmol/mg protein P < 0.02).

CONCLUSION

The low CQ accumulation in CR is attributable to the parasite rather than to the infected RBC, and CR was not found to excrete CQ more rapidly than CS.

摘要

目的

探讨氯喹(CQ)抗性(CR)和敏感性(CS)伯氏疟原虫中积累的氯喹量的差异是与被感染红细胞(RBC)还是与疟原虫有关。

方法

通过高效液相色谱法(外标法)测定对CS和CR感染小鼠经口给予CQ后,被感染红细胞和疟原虫中CQ的浓度。

结果

给予4.06mg/kg和400mg/kg后3小时,两种感染红细胞中CQ的积累相似,但CR中的积累分别比CS中的少54.0%和42.1%(P<0.001)。给予400mg/kg CQ经口给药后3小时和7小时,CS中CQ的积累相似(0.780±0.128nmol/蛋白和0.760±0.180nmol/mg蛋白),而在CR中,给药后7小时的CQ积累高于3小时(0.452±0.079nmol/mg蛋白和0.559±0.124nmol/mg蛋白,P<0.02)。

结论

CR中CQ积累较低归因于疟原虫而非被感染的红细胞,且未发现CR比CS更快地排泄CQ。

相似文献

1
[Accumulation and effluxion of chloroquine in chloroquine-sensitive and chloroquine-resistant Plasmodium berghei].[氯喹在氯喹敏感及氯喹耐药伯氏疟原虫中的蓄积与外排]
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1998;16(3):189-92.
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[Isolation and quantitation of chloroquine-binding proteins in Plasmodium berghei].[伯氏疟原虫中氯喹结合蛋白的分离与定量]
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Chloroquine resistance in malaria: variations of substrate-stimulated chloroquine accumulation.疟疾中的氯喹耐药性:底物刺激的氯喹蓄积变化
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Antagonism of serum of mice infected with chloroquine-resistant 'NS' line to the antimalarial action of chloroquine.感染氯喹抗性“NS”系的小鼠血清对氯喹抗疟作用的拮抗作用。
Zhongguo Yao Li Xue Bao. 1989 May;10(3):257-60.
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[Free amino acid and synthesis of polyamines in Plasmodium-berghei-infected RBC].
Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1990;8(1):13-7.
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Amodiaquin accumulation by mouse erythrocytes infected with Plasmodium berghei.
J Pharmacol Exp Ther. 1975 Dec;195(3):397-403.
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Zhongguo Yao Li Xue Bao. 1993 Jan;14(1):9-12.
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Plasmodium berghei: dehydroepiandrosterone sulfate reverses chloroquino-resistance in experimental malaria infection; correlation with glucose 6-phosphate dehydrogenase and glutathione synthesis pathway.伯氏疟原虫:硫酸脱氢表雄酮可逆转实验性疟疾感染中的氯喹抗性;与葡萄糖6-磷酸脱氢酶和谷胱甘肽合成途径的相关性
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Malagashanine potentiates chloroquine antimalarial activity in drug resistant Plasmodium malaria by modifying both its efflux and influx.马拉加沙宁通过改变氯喹的流出和流入,增强其对耐药疟原虫的抗疟活性。
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Plasmodium berghei: efficacy and safety of combinations of chloroquine and promethazine in chloroquine resistant infections in gravid mice.伯氏疟原虫:氯喹与异丙嗪联合用药对妊娠小鼠氯喹耐药感染的疗效与安全性
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