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毛叶花椒(芸香科)茎皮中生物碱和酰胺类化合物的抗疟活性较低。

Low antiplasmodial activity of alkaloids and amides from the stem bark of Zanthoxylum rubescens (Rutaceae).

作者信息

Penali L, Mulholland D A, Tano K D, Cheplogoi P K, Randrianarivelojosia M

机构信息

Malariology Department, Institut Pasteur de Côte d'Ivoire, 01 BP 490 Abidjan 01, Ivory Coast.

出版信息

Parasite. 2007 Jun;14(2):161-4. doi: 10.1051/parasite/2007142161.

DOI:10.1051/parasite/2007142161
PMID:17645189
Abstract

The stem bark of Zanthoxylum rubescens (syn. Fagara rubescens) is used for treating fevers associated with malaria in the Ivory Coast. Three alkaloids: N-nornitidine, 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, and bis[6-5,6-dihydrochelerythrinyl)] ether; and two amides: zanthomamide and lemairamide, were isolated from the stem bark of this plant. These compounds were screened in vitro against the chloroquine-sensitive 3D7 strain and the chloroquine-resistant FCM29 strain of P. falciparum. N-nornitidine was found to be inactive. 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, lemairamide and zanthomamide showed weak activity with average IC50 values ranging from 45.6 microM to 149.9 microM. Bis[6-15,6-dihydrochelerythrinyl)] ether was the most active of the tested compounds with mean IC50s of 14.9 +/- 1.4 microM in FCM29 strain and 15.3 +/- 3.4 microM in 3D7 strain (approximately 58 to approximately 1130 times less active than chloroquine respectively). The anti-Plasmodium activities of the tested alkaloids of Z. rubescens were low; and do not encourage the use of this plant as antimalarial.

摘要

在科特迪瓦,刺花椒(学名:Zanthoxylum rubescens,异名:Fagara rubescens)的茎皮用于治疗与疟疾相关的发热。从该植物的茎皮中分离出了三种生物碱:N-去甲诺丁、7,9-二甲氧基-2,3-亚甲二氧基苯并菲啶和双[6-5,6-二氢白屈菜红碱基]醚;以及两种酰胺:花椒酰胺和勒迈酰胺。针对恶性疟原虫的氯喹敏感3D7株和氯喹耐药FCM29株对这些化合物进行了体外筛选。发现N-去甲诺丁无活性。7,9-二甲氧基-2,3-亚甲二氧基苯并菲啶、勒迈酰胺和花椒酰胺显示出较弱的活性,平均IC50值在45.6微摩尔至149.9微摩尔之间。双[6-15,6-二氢白屈菜红碱基]醚是测试化合物中活性最高的,在FCM29株中的平均IC50为14.9±1.4微摩尔,在3D7株中的平均IC50为15.3±3.4微摩尔(分别比氯喹活性低约58至约1130倍)。刺花椒中测试生物碱的抗疟活性较低;不鼓励将这种植物用作抗疟药。

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