Azuma I, Sugimura K, Yamawaki M, Uemiya M, Kusumoto S, Okada S, Shiba T, Yamamura Y
Infect Immun. 1978 Jun;20(3):600-7. doi: 10.1128/iai.20.3.600-607.1978.
Adjuvant and antitumor activities of synthetic 6-O-"mycoloyl"-N-acetylmuramyl-L-alanyl-D-isoglutamine were examined. All the synthetic 6-O-corynomycoloyl-, 6-O-mocardomycoloyl-, and 6-O-mycoloyl-N-acetylmuramyl-L-alanyl-D-isoglutamine were active as adjuvants for cell-mediated immune responses. However, 6-O-mycoloyl-N-acetylmuramyl-L-alanyl-D-isoglutamine was less active as an adjuvant on circulating antibody formation. It was shown that pyrogenic activity of N-acetylmuramyldipeptide was reduced by 6-O-acylation with mycolic acid, but not with nocardomycolic or corynomycolic acid. Tumor-suppression activity was observed by the synthetic 6-O-mycoloyl-N-acetylmuramyl-L-alanyl-D-isoglutamine by using transplantable tumor in syngenic mice.
对合成的6-O-“霉菌酰基”-N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺的佐剂活性和抗肿瘤活性进行了研究。所有合成的6-O-棒状霉菌酰基-、6-O-分枝杆菌酰基-和6-O-霉菌酰基-N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺作为细胞介导免疫反应的佐剂均具有活性。然而,6-O-霉菌酰基-N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺在循环抗体形成方面作为佐剂的活性较低。结果表明,N-乙酰胞壁酰二肽的致热活性通过用霉菌酸进行6-O-酰化而降低,但用诺卡氏霉菌酸或棒状霉菌酸进行酰化则不会降低。通过在同基因小鼠中使用可移植肿瘤,观察到合成的6-O-霉菌酰基-N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺具有肿瘤抑制活性。