Takada H, Tsujimoto M, Kato K, Kotani S, Kusumoto S, Inage M, Shiba T, Yano I, Kawata S, Yokogawa K
Infect Immun. 1979 Jul;25(1):48-53. doi: 10.1128/iai.25.1.48-53.1979.
Activation of peritoneal macrophages from guinea pigs by various bacterial cell walls, M-1 endo-N-acetylmuramidase enzymatically digested bacterial cell walls and synthetic muramyl dipeptides was studied in terms of stimulation of [14C] glucosamine incorporation. All test bacterial cell wall preparations significantly increased a [14C]glucosamine uptake by the macrophages. Some of the water-soluble M-1 enzyme digests also exerted stimulating effects on macrophages, although the activity of the digests was found to be weaker than those of original cell walls. Furthermore, an adjuvant-active synthetic MurNAc-L-Ala-D-isoGln (MDP) showed a weak but significant activity, whereas an adjuvant-inactive analog, MurNAc-L-Ala-L-iso-Gln, did not show a significant activity, at least with the dose of 100 microgram. Additional studies with 6-O-acyl derivatives of MDP revealed that 6-O-(2-tetradecylhexadecanoyl)-MDP and 6-O-(3-hydroxy-2-tetradecyl-octadecanoyl)-MDP exhibit stronger macrophage-stimulating effects than MDP. It can be concluded from the above findings that MDP is the essential structure responsible for stimulating the activity of cell walls on guinea pig peritoneal macrophages, but it requires a particle state, which results from an additive character of lipophilicity, to exert the activity fully and effectively.
研究了各种细菌细胞壁、M-1 内切-N-乙酰胞壁酸酶酶解细菌细胞壁和合成的胞壁酰二肽对豚鼠腹腔巨噬细胞的激活作用，采用刺激 [14C] 葡萄糖胺掺入法进行检测。所有受试细菌细胞壁制剂均显著增加了巨噬细胞对 [14C] 葡萄糖胺的摄取。一些水溶性 M-1 酶解产物也对巨噬细胞有刺激作用，尽管发现这些酶解产物的活性比原始细胞壁的活性弱。此外，具有佐剂活性的合成 MurNAc-L-Ala-D-异谷氨酰胺（MDP）表现出较弱但显著的活性，而无佐剂活性的类似物 MurNAc-L-Ala-L-异谷氨酰胺至少在 100 微克剂量下未表现出显著活性。对 MDP 的 6-O-酰基衍生物的进一步研究表明，6-O-(2-十四烷基十六烷酰基)-MDP 和 6-O-(3-羟基-2-十四烷基十八烷酰基)-MDP 对巨噬细胞的刺激作用比 MDP 更强。从上述研究结果可以得出结论，MDP 是刺激豚鼠腹腔巨噬细胞细胞壁活性的关键结构，但它需要一种由亲脂性加成特性导致的颗粒状态，才能充分有效地发挥活性。
