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抗疟药,2. 青蒿琥酯,伯氏疟原虫细胞色素氧化酶活性的抑制剂。

Antimalarial agents, 2. Artesunate, an inhibitor of cytochrome oxidase activity in Plasmodium berghei.

作者信息

Zhao Y, Hanton W K, Lee K H

出版信息

J Nat Prod. 1986 Jan-Feb;49(1):139-42. doi: 10.1021/np50043a018.

DOI:10.1021/np50043a018
PMID:3009719
Abstract

The activity of the cytochrome oxidase, which is located in the plasma and the nuclear and the food-vacuole-limiting membranes as well as in the mitochondria of the trophozoites of Plasmodium berghei, was inhibited completely by sodium artesunate, an antimalarial drug, in vitro at 1 mM and in vivo at 100 mg/kg iv. This enzyme appears to be a target for the antimalarial mechanism of action of artesunate and qinghaosu.

摘要

疟原虫滋养体的血浆、细胞核、食物泡限制膜以及线粒体中所含的细胞色素氧化酶的活性,在体外1 mM时可被抗疟药青蒿琥酯完全抑制,在体内静脉注射100 mg/kg时也被完全抑制。这种酶似乎是青蒿琥酯和青蒿素抗疟作用机制的靶点。

相似文献

1
Antimalarial agents, 2. Artesunate, an inhibitor of cytochrome oxidase activity in Plasmodium berghei.抗疟药,2. 青蒿琥酯,伯氏疟原虫细胞色素氧化酶活性的抑制剂。
J Nat Prod. 1986 Jan-Feb;49(1):139-42. doi: 10.1021/np50043a018.
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Comparison of in vivo and in vitro antimalarial activity of artemisinin, dihydroartemisinin and sodium artesunate in the Plasmodium berghei-rodent model.青蒿素、双氢青蒿素和青蒿琥酯钠在伯氏疟原虫-啮齿动物模型中的体内和体外抗疟活性比较。
Int J Parasitol. 1994 Jul;24(4):589-94. doi: 10.1016/0020-7519(94)90150-3.
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Antimalarial agents. III. Mechanism of action of artesunate against Plasmodium berghei infection.
Chem Pharm Bull (Tokyo). 1987 May;35(5):2052-61. doi: 10.1248/cpb.35.2052.
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The antimalarial action on Plasmodium falciparum of qinghaosu and artesunate in combination with agents which modulate oxidant stress.青蒿素和青蒿琥酯与调节氧化应激的药物联合对恶性疟原虫的抗疟作用。
Trans R Soc Trop Med Hyg. 1987;81(5):710-4. doi: 10.1016/0035-9203(87)90003-4.
5
[Development of a qinghaosu-resistant line of Plasmodium berghei ANKA and N strain].[伯氏疟原虫ANKA株和N株青蒿素抗性品系的培育]
Yao Xue Xue Bao. 1986 Nov;21(11):811-5.
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Qinghaosu-induced changes in the morphology of Plasmodium inui.青蒿素诱导的约氏疟原虫形态变化。
Am J Trop Med Hyg. 1985 May;34(3):424-8. doi: 10.4269/ajtmh.1985.34.424.
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[Development of a line of Plasmodium berghei resistant to sodium artesunate].[对青蒿琥酯耐药的伯氏疟原虫品系的培育]
Zhongguo Yao Li Xue Bao. 1987 Mar;8(2):149-52.
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[Effects of qinghaosu on the surface structure of erythrocytes infected with Plasmodium berghei and the erythrocyte-free parasites].[青蒿素对感染伯氏疟原虫的红细胞及游离疟原虫表面结构的影响]
Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1986;4(4):260-2.
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Activated oxygen mediates the antimalarial activity of qinghaosu.活性氧介导青蒿素的抗疟活性。
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Effects of dihydroartemisinin on fine structure of erythrocytic stages of Plasmodium berghei ANKA strain.双氢青蒿素对伯氏疟原虫ANKA株红细胞内期超微结构的影响。
Acta Pharmacol Sin. 2000 Mar;21(3):234-8.

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