Titov V M, Meshcheryakova E A, Balashova T A, Andronova T M, Ivanov V T
Laboratory of Peptide Chemistry, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Moscow, Russia.
Int J Pept Protein Res. 1995 Apr;45(4):348-55. doi: 10.1111/j.1399-3011.1995.tb01048.x.
The conjugates of a muramyl dipeptide analog GMDP (N-acetylglucosaminyl beta 1-->4 N-acetylmuramyl-L-alanyl-D-isoglutamine) and tuftsin (Thr-Lys-Pro-Arg) were synthesized from unprotected GMDP by mixed anhydride procedure. The identity of the conjugates was confirmed by high resolution NMR and their immunomodulating properties were determined in various tests. It was found that the conjugate in which the GMDP carboxyl group forms an amide bond with the epsilon-amino group of tuftsin lysyl residue exceeds GMDP in all the activities determined. Synergism of GMDP and tuftsin was found in phagocytosis stimulation assay.
通过混合酸酐法由未保护的胞壁酰二肽类似物GMDP(N-乙酰葡糖胺基β1→4 N-乙酰胞壁酰-L-丙氨酰-D-异谷氨酰胺)和促吞噬素(苏氨酸-赖氨酸-脯氨酸-精氨酸)合成缀合物。通过高分辨率核磁共振确认了缀合物的结构,并在各种测试中测定了它们的免疫调节特性。结果发现,在所有测定的活性中,GMDP羧基与促吞噬素赖氨酰残基的ε-氨基形成酰胺键的缀合物超过了GMDP。在吞噬作用刺激试验中发现GMDP和促吞噬素有协同作用。