Kessler H, Haupt A, Frimmer M, Ziegler K
Int J Pept Protein Res. 1987 May;29(5):621-8. doi: 10.1111/j.1399-3011.1987.tb02292.x.
Cyclic somatostatin analogues containing the modified retro sequence of the amino acids Phe7 to Phe11 of the natural compound have been found to exhibit high activity for cytoprotection of rat hepatocytes against cell poisons such as phallotoxins and galactosamine. Cyclo(-Phe(p-NH(1-14C)Ac)-Thr-Lys(CO(p-N3)C6H4)-Trp-Phe-D-Pro), a photoreactive and radioactive analogue of one of the most active cyclohexapeptides, was synthesized by a combination of solid phase technique and classical solution peptide synthesis. This peptide labels the same proteins in rat liver cell membrane that are modified by photolysable derivatives of bile acids, phalloidin and antamanide.
已发现含有天然化合物氨基酸Phe7至Phe11修饰反向序列的环状生长抑素类似物对大鼠肝细胞具有高度的细胞保护活性，可抵御诸如鬼笔毒素和半乳糖胺等细胞毒素。通过固相技术和经典溶液肽合成相结合的方法，合成了一种光反应性和放射性类似物——环（-Phe（p-NH（1-14C）Ac）-Thr-Lys（CO（p-N3）C6H4）-Trp-Phe-D-Pro），它是活性最高的环己肽之一。该肽标记大鼠肝细胞膜中与被胆汁酸、鬼笔环肽和鹅膏蕈碱的光裂解衍生物修饰的相同蛋白质。
