超短肽的抗疟活性。
Antimalarial activity of ultra-short peptides.
机构信息
Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Avenida Universidad 1001, Col. Chamilpa, 62209 Cuernavaca, Morelos, México.
出版信息
Molecules. 2009 Dec 8;14(12):5103-14. doi: 10.3390/molecules14125103.
Abstract
Ultra-short peptides 1-9 were designed and synthesized with phenylalanine, ornithine and proline amino acid residues and their effect on antimalarial activity was analyzed. On the basis of the IC(50) data for these compounds, the effects of nature, polarity, and amino acid sequence on Plasmodium berghei schizont cultures were analyzed too. Tetrapeptides Phe-Orn-Phe-Orn (4) and Lys-Phe-Phe-Orn (5) showed a very important activity with IC(50) values of 3.31 and 2.57 microM, respectively. These two tetrapeptides are candidates for subsequent in vivo assays and SARS investigations.
摘要
设计并合成了由苯丙氨酸、精氨酸和脯氨酸残基组成的超短肽 1-9，并分析了它们对抗疟活性的影响。基于这些化合物的 IC(50)数据，还分析了性质、极性和氨基酸序列对伯氏疟原虫裂殖体培养的影响。四肽 Phe-Orn-Phe-Orn（4）和 Lys-Phe-Phe-Orn（5）表现出非常重要的活性，IC(50)值分别为 3.31 和 2.57 μM。这两种四肽是后续体内试验和 SARS 研究的候选物。
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