Johnson R B, Köhl S, Wiesmüller K, Jung G, Bessler W G
Immunobiology. 1983 Jul;165(1):27-35. doi: 10.1016/S0171-2985(83)80044-8.
Two analogues of the N-terminal part of bacterial lipoprotein, S-[2,3-bis(palmitoyloxy)-(2RS)propyl]-N-palmitoyl-(R)-cysteine methyl ester ("tripalmitoyl cysteine") and S [-2,3-bis(palmitoyloxy)-(2RS)-propyl]-N-palmitoyl-(R)-cysteinyl-(S)-seryl-(S)-seryl-(S)-asparaginyl-(S)-alanine ("tripalmitoyl pentapeptide") were synthesized and tested for mitogenic activity. The compounds were potent mitogens towards mouse spleen cell cultures, as measured by 3H-thymidine incorporation and by hemolytic plaque assays. This activity was not dependent on the presence of serum. Tripalmitoyl pentapeptide had little, if any, effect on thymocytes. When injected intravenously into Balb/c mice, the synthetic compounds induced splenomegaly and polyclonal B-cell activation, the latter was evident from an increase in the number of plaque-forming cells against trinitrophenylated sheep red blood cells. Thus, a synthetic fragment of a bacterial surface component was shown to exhibit marked biological activity in vitro as well as in vivo.
合成了细菌脂蛋白N端部分的两种类似物，即S-[2,3-双（棕榈酰氧基）-（2RS）丙基]-N-棕榈酰-（R）-半胱氨酸甲酯（“三棕榈酰半胱氨酸”）和S [-2,3-双（棕榈酰氧基）-（2RS）-丙基]-N-棕榈酰-（R）-半胱氨酰-（S）-丝氨酰-（S）-丝氨酰-（S）-天冬酰胺酰-（S）-丙氨酸（“三棕榈酰五肽”），并检测了它们的促有丝分裂活性。通过3H-胸腺嘧啶核苷掺入法和溶血空斑试验测定，这些化合物对小鼠脾细胞培养物是有效的促有丝分裂原。这种活性不依赖于血清的存在。三棕榈酰五肽对胸腺细胞几乎没有影响。当静脉注射到Balb/c小鼠体内时，这些合成化合物诱导脾肿大和多克隆B细胞活化，后者从针对三硝基苯基化绵羊红细胞的空斑形成细胞数量增加中明显看出。因此，细菌表面成分的一个合成片段在体外和体内均显示出显著的生物学活性。
