Xu Wen-Yan, Zhao Si-Meng, Zeng Guang-Zhi, He Wen-Jun, Xu Hui-Min, Tan Ning-Hu
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
Yao Xue Xue Bao. 2012 Mar;47(3):271-9.
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.
天然环肽因其广泛分布的生物资源、复杂的分子结构和多样的生物活性,成为化学和制药领域的研究热点。环肽的生物生产者几乎分布于从细菌到动植物的各个生物界。许多环肽含有非编码氨基酸和非肽键。环肽最令人兴奋的特性是一系列有趣的生物活性,如抗生素短杆菌肽-S(2)、万古霉素(3)和达托霉素(4),免疫抑制剂环孢菌素-A(1)和阿斯汀-C(8),以及抗肿瘤药物阿利新(5)、RA-V(6)和RA-VII(7)。化合物1-4已在临床使用;化合物5-8正处于临床试验阶段或作为药物研究的候选物。在这篇综述中,介绍了这些重要的天然生物活性环肽1-8在化学和生物活性研究方面的进展,主要包括发现、生物活性、作用机制、定量构效关系和合成。