Chu C, Schneerson R, Robbins J B, Rastogi S C
Infect Immun. 1983 Apr;40(1):245-56. doi: 10.1128/iai.40.1.245-256.1983.
Conjugates were prepared by carbodiimide-mediated coupling of adipic acid hydrazide derivatives of Haemophilus influenzae type b (Hib), Escherichia coli K100, and pneumococcal 6A (Pn6A) polysaccharides with tetanus toxoid (TT), as an example of a "useful" carrier, and horseshoe crab hemocyanin (HCH), as an example of a "nonsense" carrier. These conjugates were injected into NIH mice, and their serum antibody responses to the polysaccharides and proteins were characterized. As originally reported, Hib conjugates increased the immunogenicity of the capsular polysaccharide and elicited greater than the estimated protective levels of anti-Hib antibodies in most recipients after one injection and in all after the third injection (Schneerson et al., J. Exp. Med. 152:361-376, 1980). Both Hib conjugates induced similar anti-Hib responses. The K100-HCH conjugate was more immunogenic than the K100-TT conjugate and elicited anti-Hib responses similar to the Hib conjugates after the third injection. Simultaneous injection of the K100 and the Hib conjugates did not enhance the anti-Hib response. The Pn6A-TT conjugate induced low levels of anti-Hib antibodies; when injected simultaneously with the Hib conjugates, the anti-Hib response was enhanced, as all mice responded after the first injection and with higher levels of anti-Hib than observed with the Hib conjugates alone (P < 0.05). The Pn6A conjugates were not as immunogenic as the Hib conjugates. Pn6A-TT was more effective than was Pn6A-HCH; it elicited anti-Pn6A (>100 ng of antibody nitrogen per ml) in 6 of 10 mice after the third injection. The addition of the Hib-HCH conjugate to the Pn6A-TT conjugate increased the anti-Pn6A response with a higher geometric mean antibody titer, and 9 of 10 mice responded after the third injection. A preparation of diphtheria toxoid, TT, and pertussis vaccine increased the anti-Hib antibody levels after the first injection only in mice receiving Hib-TT, but not in mice receiving Hib-HCH, suggesting that additional carrier protein (TT) enhanced the anti-polysaccharide response. Simultaneous injection of Hib and Pn6A conjugates with the same or different carriers resulted in an enhanced serum antibody response to each polysaccharide. The anti-tetanus toxin response reached protective levels (>0.01 U/ml) in most mice after the first injection and in all mice after the second and third injections of TT conjugates. A progressive increase in the anti-HCH response with each additional injection was noted in animals receiving HCH conjugates. Animals receiving the diphtheria toxoid-TT-pertussis vaccine preparation responded with a greater increase in anti-carrier antibody than those receiving the conjugates alone. This method of synthesis provided conjugates capable of inducing protective levels of antibodies to both the polysaccharides and carrier proteins.
通过碳二亚胺介导,将b型流感嗜血杆菌(Hib)、大肠杆菌K100和肺炎球菌6A(Pn6A)多糖的己二酸酰肼衍生物与破伤风类毒素(TT,作为“有效”载体的示例)和鲎血蓝蛋白(HCH,作为“无意义”载体的示例)偶联,制备缀合物。将这些缀合物注射到NIH小鼠体内,并对它们针对多糖和蛋白质的血清抗体反应进行表征。如最初报道的那样,Hib缀合物提高了荚膜多糖的免疫原性,并且在大多数接受者中,一次注射后诱导的抗Hib抗体水平高于估计的保护水平,第三次注射后所有接受者均如此(施内尔森等人,《实验医学杂志》152:361 - 376,1980年)。两种Hib缀合物诱导了相似的抗Hib反应。K100 - HCH缀合物比K100 - TT缀合物更具免疫原性,并且在第三次注射后诱导出与Hib缀合物相似的抗Hib反应。同时注射K100和Hib缀合物并未增强抗Hib反应。Pn6A - TT缀合物诱导出低水平的抗Hib抗体;当与Hib缀合物同时注射时,抗Hib反应增强,因为所有小鼠在第一次注射后均有反应,且抗Hib水平高于单独使用Hib缀合物时观察到的水平(P < 0.05)。Pn6A缀合物的免疫原性不如Hib缀合物。Pn6A - TT比Pn6A - HCH更有效;第三次注射后,10只小鼠中有6只产生了抗Pn6A(每毫升>100纳克抗体氮)。向Pn6A - TT缀合物中添加Hib - HCH缀合物可提高抗Pn6A反应,几何平均抗体滴度更高,第三次注射后10只小鼠中有9只产生反应。白喉类毒素、TT和百日咳疫苗制剂仅在接受Hib - TT的小鼠中,第一次注射后提高了抗Hib抗体水平,而在接受Hib - HCH的小鼠中未提高,这表明额外的载体蛋白(TT)增强了抗多糖反应。同时注射具有相同或不同载体的Hib和Pn6A缀合物导致对每种多糖的血清抗体反应增强。在第一次注射TT缀合物后,大多数小鼠的抗破伤风毒素反应达到保护水平(>0.01 U/ml),第二次和第三次注射后所有小鼠均如此。在接受HCH缀合物的动物中,每次额外注射后抗HCH反应都有逐渐增加。接受白喉类毒素 - TT - 百日咳疫苗制剂的动物比单独接受缀合物的动物产生的抗载体抗体增加幅度更大。这种合成方法提供了能够诱导针对多糖和载体蛋白的保护性抗体水平的缀合物。