CYCLOSPORIN-A, A PEPTIDE METABOLITE FROM TRICHODERMA-POLYSPORUM (LINK EX PERS) RIFAI, WITH A REMARKABLE IMMUNOSUPPRESSIVE ACTIVITY
CYCLOSPORIN-A, A PEPTIDE METABOLITE FROM TRICHODERMA-POLYSPORUM (LINK EX PERS) RIFAI, WITH A REMARKABLE IMMUNOSUPPRESSIVE ACTIVITY
复制标题
DOI：
10.1002/hlca.19760590412
复制
发表时间：
1976-01-01
影响因子：
1.8
通讯作者：
WARTBURG, AV
中科院分区：
文献类型：
--
作者：
RUEGGER, A;KUHN, M;WARTBURG, AV
从 T. polysporum (Link ex Pers.) Rifai 菌株中分离出两种抗真菌代谢物，环孢菌素 A 和 C。主要成分环孢菌素A经NMR和质谱推导其分子式为C62H111N11O12。环孢菌素 A 的水解裂解提供了 11 个氨基酸片段，其中包括新的 C9 氨基酸的人工产物。通过异环孢菌素 A 的 Edman 降解确定氨基酸序列，异环孢菌素 A 是环孢菌素 A 通过 N,O-酰基迁移形成的基本重排产物。在一项独立调查中，对碘衍生物进行了 X 射线分析。根据化学、光谱和晶体学证据，阐明了环孢菌素 A 的完整结构。环孢素 A 和 C 在多种药理学模型中显示出显着的免疫抑制和抗炎活性。
Two antifungal metabolites, cyclosporins A and C, were isolated from a strain of T. polysporum (Link ex Pers.) Rifai. Cyclosporin A, the main component, has the molecular formula C62H111N11O12 as deduced by NMR and mass spectra. Hydrolytic cleavage of cyclosporin A furnished 11 amino acids as fragments, among them an artefact of a new C9-amino acid. The amino acid sequence was determined by Edman degradation of iso-cyclosporin A, a basic rearrangement product formed from cyclosporin A by N,O-acyl migration. In an independent investigation an X-ray analysis of the iodo derivative was perfromed. On the basis of the chemical, spectroscopic and crystallographic evidence the complete structure of cyclosporin A was elucidated. Cyclosporin A and C show remarkable immunosuppressive and antiphlogistic activities in several pharmacological models.