| 摘要: |
| 环肽是植物来源的超稳定肽，由头至尾环化骨架和形成胱氨酸结的3个二硫键非常稳定。与其他类似大小的肽相比，环肽的这种独特的拓扑学结构使它们对化学、热和生物降解异常稳定，它们出色的稳定性和对序列替换的耐受性可使它们用作药物设计的框架。本文主要介绍了环肽在药学研究领域3个方面的应用，特别是近年来在将生物活性肽序列嫁接到环肽的框架上，以产生新的生物学活性方面的研究进展。 |
| 关键词: 生物活性 环肽 嫁接 药学研究 |
| DOI：10.13748/j.cnki.issn1007-7693.2019.05.024 |
| 分类号:R915 |
| 基金项目:广西中医基础研究重点实验室系统课题（16-380-58-03）；广西中医药大学校级课题面上项目（2018MS010） |
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| Biologically Active Cyclotides and Their Pharmaceutical Progress |
|
DUAN Huiming
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Guangxi University of Chinese Medicine, Guangxi Scientific Experimental Center of Traditional Chinese Medicine, Guangxi Key Laboratory of Chinese Medicine Foundation Research, Nanning 530200, China
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| Abstract: |
| Cyclotides are plant-derived ultrastable peptides that are stabilized by head-to-tail cyclization backbone and three disulfide bonds that form cystine knots. This unique topology allows them to be exceptionally stable against chemical, thermal and biodegradability compared to other similarly sized peptides. Their excellent stability and tolerance to sequence substitution enable them to be used as frameworks for drug design. This article mainly introduces the application of cyclotides in three areas of pharmaceutical research, especially the recent progress in grafting bioactive peptide sequences onto the framework of cyclotides to generate new biological activities. |
| Key words: biological activity cyclotides grafting pharmaceutical research |
