Anti-HIV cyclotides from the Chinese medicinal herb Viola yedoensis.
Anti-HIV cyclotides from the Chinese medicinal herb Viola yedoensis.
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DOI：
10.1021/np070393g
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发表时间：
2008
影响因子：
5.1
通讯作者：
Conan K. Wang;M. Colgrave;K. Gustafson;D. Ireland;U. Goransson;D. Craik
中科院分区：
文献类型：
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作者：
Conan K. Wang;M. Colgrave;K. Gustafson;D. Ireland;U. Goransson;D. Craik
环肽是一种以三个二硫键的结状排列为特征的大环植物肽。它们显示出一系列有趣的生物活性，包括抗艾滋病毒和杀虫活性。从两个系统发育较远的植物科，茜草科和堇菜科中分离出100多种不同的环核苷酸。在本研究中，我们对紫堇（Viola yedoensis）中的环核苷酸进行了表征，紫堇是堇菜科的一种重要中草药，据报道含有潜在的抗hiv药物。从紫杉中鉴定出5个新的和3个已知的环核苷酸，并显示出抗hiv活性。其中最活跃的是环violacin Y5，这是迄今为止使用体外xtt抗艾滋病毒测定法检测的所有环肽类药物中最有效的一种。环堇菜酸Y5是紫菜中最疏水的环核苷酸。我们表明，疏水性和抗hiv活性之间存在正相关的新环核苷酸，这种趋势与他们的能力破坏膜，判断从溶血试验对人红细胞。
Cyclotides are macrocyclic plant peptides characterized by a knotted arrangement of three disulfide bonds. They display a range of interesting bioactivities, including anti-HIV and insecticidal activities. More than 100 different cyclotides have been isolated from two phylogenetically distant plant families, the Rubiaceae and Violaceae. In this study we have characterized the cyclotides from Viola yedoensis, an important Chinese herb from the Violaceae family that has been reported to contain potential anti-HIV agents. From V. yedoensis five new and three known cyclotides were identified and shown to have anti-HIV activity. The most active of these is cycloviolacin Y5, which is one of the most potent of all cyclotides tested so far using in vitro XTT-based anti-HIV assays. Cycloviolacin Y5 is the most hydrophobic of the cyclotides from V. yedoensis. We show that there is a positive correlation between the hydrophobicity and the anti-HIV activity of the new cyclotides and that this trend tracks with their ability to disrupt membranes, as judged from hemolytic assays on human erythrocytes.