中文摘要：

天然环肽化合物以其广泛的分布、新奇的结构和丰富的活性成为化学家和药学家研究的热点。多年的天然产物化学及活性与药物研发已经从天然环肽化合物中发现一批药物,包括免疫抑制剂环孢菌素A（cyclosporin-A,1）、抗生素短杆菌肽S（gramicidin-S,2）、万古霉素（vancomycin,3）、达托霉素（daptomycin,4）等;多个环肽化合物正在进行临床试验研究,如具有抗肿瘤活性的海洋环肽aplidine（5）等;另有数个植物环肽化合物具有良好的成药前景,如具有抗肿瘤活性的茜草科类型环肽RA-V（6）和RA-Ⅶ（7）、免疫抑制活性的菊科类型环肽astin-C（8）等。本文将从分子及其重要活性发现、作用机制、构效关系或结构改造等方面简要介绍以上这些重要天然活性环肽的化学和生物活性研究进展,期望帮助读者了解天然活性环肽化合物的研究概况。

英文摘要：

Natural cyclopeptides are hot spots in chemical and pharmaceutical fields because of the wide spreading bio-resources,complex molecular structures and various bioactivities.Bio-producers of cyclopeptides distribute over almost every kingdom from bacteria to plants and animals.Many cyclopeptides contain non-coded amino acids and non-pepditic bonds.Most exciting characteristic of cyclopeptides is a range of interesting bioactivities such as antibiotics gramicidin-S（2）,vancomycin（3） and daptomycin（4）,immunosuppressive cyclosporin-A（1） and astin-C（8）,and anti-tumor aplidine（5）,RA-V（6） and RA-VII（7）.Compounds 1-4 are being used in clinics;compounds 5-8 are in the stages of clinical trial or as a candidate for drug research.In this review,the progress in chemical and bioactive studies on these important natural bioactive cyclopeptides 1？8 are introduced,mainly including discovery,bioactivity,mechanism,QSAR and synthesis.