Gao F, Shi P T, Zang Y M, Niu G B
Department of Physiology, Fourth Military Medical University, Xi' an.
Yao Xue Xue Bao. 1994;29(6):417-26.
Atriopeptin III (AP III) and its small molecular analog were synthesized manually by stepwise solid-phase method. The peptides were oxidized with iodine in 30% acetic acid at very high dilution to form intramolecular disulfide bridge and purified to homogeneity by conventional means, including Sephadex G15, dialysis and reversed-phase HPLC. Bioassay study demonstrated that the synthetic AP III possesses potent bioactivities identical to those of the same product of Peninsula Lab both in vitro and in vivo; whereas the linear peptide, having the same primary structure as AP III, showed very limited bioactivity. The small analog, with Ser-Ser-residue deleted from the N-terminal of AP III, was equipotent as AP III while exhibiting a longer half-life in vivo resulting from the peptide modification.
心房肽III（AP III）及其小分子类似物通过逐步固相法人工合成。肽在30%乙酸中用碘在非常高的稀释度下氧化以形成分子内二硫键，并通过常规方法纯化至均一性，包括葡聚糖凝胶G15、透析和反相高效液相色谱。生物活性测定研究表明，合成的AP III在体外和体内均具有与半岛实验室相同产品相同的强大生物活性；而具有与AP III相同一级结构的线性肽显示出非常有限的生物活性。从小分子类似物的AP III N端缺失Ser-Ser-残基，其活性与AP III相当，同时由于肽修饰在体内表现出更长的半衰期。
