Immunological Activity of Water-solubilized Lignins and its Action Mechanism

(1)研究了LEN衍生的EP3、木质素磺酸盐(LS)等水溶性木质素及其衍生物或分解产物之间的构效关系。为了激活再尿巨噬细胞和促进骨髓细胞的增殖，分子量大于10000的木质素及其衍生物的聚阴离子性质是产生这种活性的首要条件。木素中的羧基、磺酰基和硫基等解离基团之间的活性没有差异。(2)用~&lt；14&gt；C-甲醛对三种不同相对分子质量和解离基数的水溶性木质素进行了羟甲基化反应。衍生化后活性保持不变。给大鼠灌胃和静脉给药，通过放射自显影和常规组织分析两种方法测量放射性的时程分布。结果表明，木质素通过血液顺利吸收，并主要沉积在肝脏、骨髓、肾脏等组织中。大部分放射性物质迅速排入尿液中，但较小部分放射性物质在上述生殖器官中滞留的时间较长，这与活性测定结果具有良好的相关性。(3)EP3、LS、葡聚糖硫酸盐、聚苯乙烯磺酸等不仅引起巨噬细胞的形态变化，而且增加了葡萄糖的消耗。巨噬细胞的活化依赖于水溶木质素的聚阴离子性质。(4)水溶木质素比灭活内毒素更能促进~3H-胸腺嘧啶核苷掺入骨髓细胞。葡聚糖硫酸盐没有显示任何活性。在骨髓中。细胞，结果表明，水溶木质素对祖细胞巨噬细胞增殖作用最强。

(1)Structure and activity relationship has been studied among the water-soluble lignins such as LENderived EP3, lignosulfonates(LS), and their derivatives or decomposition products. For both the activation of reurine macrophages and the proliferation of bone marrow cells, polyanionic nature of lignin and its derivatives having the molecular weight more than 10, 000 is the first requisite to emerge the activities. No difference in activities was observed between dissociation groups, such as carboxyl, solfonyl or sulfuryl group in lignins.(2)Three water-solubilized lignins with different molecular weight and number of dissociation groups were hydroxymethylated with ^<14>C-formaldehyde. The activities were maintained after derivatization. They were administered orally and intravenously to rats and time-course distribution of radio, activity was measured both by autoradiography using the imaging plate method and ordinally tissue analysis. As a result, the lignins were absorbed smoothly via blood and deposited in the tissues mainly in liver, bone marrow, kidney. The greater part of the radioactivity excreted rapidly into urine, the smaller part, however, remained in the above hislily productive organs for the longer period, suggesting that it revealed the good correlation with the results obtained from those of activity assays.(3)EP3, LS, dextran sulfate, polystyrene sulfonate, etc., induced not only the morphological changes of macrophages, but also augmented the glucose consumption. Activation of macrophages was found to depend on polyanionic nature of water-solubilized lignins.(4)Water-solubilized lignins enhanced more strongly the incorporation of ^3H-thymidine into bone marrow cells than imunoactive LPS. Dextran sulfate did not show any activity. Among the bone marrow. cells, it was shown that progenitor macrophage cells were most strongly proliferated by water-soluilized lignins.