Uemiya M, Sugimura K, Kusama T, Saiki I, Yamawaki M, Azuma I, Yamamura Y
Infect Immun. 1979 Apr;24(1):83-9. doi: 10.1128/iai.24.1.83-89.1979.
Adjuvant and antitumor activities of synthetic-6-O-mycoloyl-N-acetylmuramyl-L-seryl-D-isoglutamine and 6-O-mycoloyl-N-acetylmuramyl-glycyl-D-isoglutamine were examined in comparison with those of 6-O-mycoloyl-N-acetylmuramyl-L-alanyl-D-isoglutamine. Synthetic 6-O-mycoloyl-N-acetylmuramyl-L-seryl-D-isoglutamine was active as an adjuvant for the induction of delayed-type hypersensitivity to m-[4-(4'-arsono-phenylazo)-phenyl]-N-acetyl-L-tyrosine in guinea pigs and for cell-mediated cytotoxicity in allogeneic mice. 6-O-mycoloyl-N-acetylmuramyl-glycyl-D-isoglutamine was inactive as an adjuvant for the induction of delayed-type hypersensitivity in guinea pigs; however, it was active for cell-mediated cytotoxicity in allogeneic mice. 6-O-mycoloyl-N-acetylmuramyl-L-seryl-D-isoglutamine and 6-O-mycoloyl-N-acetylmuramyl-glycyl-D-isoglutamine were not pyrogenic in rabbits. The antitumor activity of these 6-O-mycoloyl-N-acetylmuramyldipeptides was examined preliminarily by using transplantable syngeneic mouse tumors.
将合成的6-O-霉菌酰基-N-乙酰胞壁酰-L-丝氨酰-D-异谷氨酰胺和6-O-霉菌酰基-N-乙酰胞壁酰-甘氨酰-D-异谷氨酰胺的佐剂活性和抗肿瘤活性与6-O-霉菌酰基-N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺进行了比较。合成的6-O-霉菌酰基-N-乙酰胞壁酰-L-丝氨酰-D-异谷氨酰胺作为佐剂,可诱导豚鼠对间-[4-(4'-砷酸基-苯偶氮)-苯基]-N-乙酰-L-酪氨酸产生迟发型超敏反应,并在同种异体小鼠中诱导细胞介导的细胞毒性。6-O-霉菌酰基-N-乙酰胞壁酰-甘氨酰-D-异谷氨酰胺作为佐剂在豚鼠中诱导迟发型超敏反应时无活性;然而,它在同种异体小鼠中对细胞介导的细胞毒性具有活性。6-O-霉菌酰基-N-乙酰胞壁酰-L-丝氨酰-D-异谷氨酰胺和6-O-霉菌酰基-N-乙酰胞壁酰-甘氨酰-D-异谷氨酰胺在兔中不引起发热。通过使用可移植的同基因小鼠肿瘤初步检测了这些6-O-霉菌酰基-N-乙酰胞壁酰二肽的抗肿瘤活性。