Fridkin M, Stabinsky Y, Zakuth V, Spirer Z
Biochim Biophys Acta. 1977 Jan 24;496(1):203-11. doi: 10.1016/0304-4165(77)90129-5.
The phagocytosis-stimulating tetrapeptide tuftsin, L-threonyl-L-lysyl-L-prolyl-L-arginine, was synthesized by both conventional and polymeric-reagent approaches. Using a combination of the two methods several analogs were prepared, including: [Ala1]tuftsin, [Lys1]tuftsin, [Ser1]tuftsin, [Val1]tuftsin, acetyl-tuftsin, p-aminophenylacetyl-tuftsin and tyrosyl-tuftsin. [Des-Thr1]tuftsin and [omega-NO2(4)]tuftsin were synthesized using a conventional procedure. The effects of synthetic peptides on the phagocytosis of heat-killed yeasts and on the reduction of the dye nitroblue tetrazolium by normal human polymorphonuclear leukocytes were investigated. Tuftsin and to a lesser extent [Lys1]tuftsin and [Ser1]tuftsin were found to stimulate phagocytosis, whereas the other analogs synthesized as well as [Ser1]tuftsin exhibited inhibitory effects to tuftsin's action. Tuftsin alone has stimulated nitroblue tetrazolium reduction; [Des-Thr1]tuftsin and [Ala1]tuftsin repressed this stimulation, while the other peptides showed no effect.
具有促吞噬作用的四肽促吞噬素，即L-苏氨酰-L-赖氨酰-L-脯氨酰-L-精氨酸，通过传统方法和聚合物试剂法合成。结合这两种方法制备了几种类似物，包括：[丙氨酸1]促吞噬素、[赖氨酸1]促吞噬素、[丝氨酸1]促吞噬素、[缬氨酸1]促吞噬素、乙酰基促吞噬素、对氨基苯乙酰基促吞噬素和酪氨酰促吞噬素。[去苏氨酸1]促吞噬素和[ω-硝基（4）]促吞噬素采用传统方法合成。研究了合成肽对热灭活酵母吞噬作用以及对正常人多形核白细胞还原染料硝基蓝四唑的影响。发现促吞噬素以及在较小程度上的[赖氨酸1]促吞噬素和[丝氨酸1]促吞噬素能刺激吞噬作用，而合成的其他类似物以及[丝氨酸1]促吞噬素对促吞噬素的作用表现出抑制作用。单独的促吞噬素能刺激硝基蓝四唑的还原；[去苏氨酸1]促吞噬素和[丙氨酸1]促吞噬素抑制这种刺激作用，而其他肽则无作用。
