Many natural substances exhibit anti-inflammatory activity and considerable potential in prophylaxis and treatment of allergies. Knowing exact molecular targets, which is required for developing these as medicinal products, is often challenging for multicomponent compositions.

In the present study we examined novel polyphenolic substance, a water-soluble fraction of wood lignin (laboratory code BP-Cx-1). In our previous study, a number of polyphenolic components of BP-Cx-1 (flavonoids, sapogenins, phenanthrenes etc.) were identified as the major carriers of biological activity of BP-Cx drug family, and several molecular targets involved in cancer and/or inflammation signaling pathways were proposed based on the results of the in vitro and in silico screening studies.

In the present study, half maximal inhibitory concentration (IC50) of BP-Cx-1 was established with a radioligand method and a range of IC50 values between 22.8 and 40.3 μg/ml were obtained for adenosine receptors A1, A2A and prostaglandin receptors EP2, IP (PGI2). IC50 for serotonin 5-HT1 and for glucocorticoid GR receptors were 3.0 μg/ml and 12.6 μg/ml, respectively, both being within the range of BP-Cx-1 concentrations achievable in in vivo models.

Further, distribution of [³H] labelled BP-Cx-1 in NIH3T3 murine fibroblasts and MCF7/R carcinoma cells was studied with autoradiography. [³H]-BP-Cx-1 (visualized as silver grains produced by tritium beta particles) was mainly localized along the cell membrane, in the perinuclear region and in the nucleus, suggesting ability of BP-Cx-1 to enter cells and bind to membrane or cytosol receptors.

In our experiment, we observed the effect of BP-Cx-1 on maturation of dendritic cells (DCs): downregulation of expression of the lipid-presentation molecule CD1a, co-stimulatory molecules CD80, CD83 and CD 40, decreased production of pro-inflammatory cytokines IL-4 and TNF-α and increased production of anti-inflammatory cytokine IL-10. It is hypothesized that [³H]-BP-Cx-1 detectable in the nucleus is part of the activated GR complex, known to be involved in regulation of transcription of genes responsible for the anti-inflammatory response. Based on IC50, cell distribution data and results of the experiment with DCs it is suggested that the in vivo effects of BP-Cx-1 are mediated via GR and 5-HT1 receptors thus promoting development of tolerogenic effector function in dendritic cells.

许多天然物质具有抗炎活性，在预防和治疗过敏中具有相当大的潜力。对于多组分组合物而言，知道开发这些药物产品所需的确切分子靶标通常是具有挑战性的。

在本研究中，我们研究了新型多酚物质，一种木质素的水溶性部分（实验室代码BP-Cx-1）。在我们先前的研究中，BP-Cx-1的多种多酚成分（类黄酮，皂甙元，菲等）被确定为BP-Cx药物家族的生物学活性的主要载体，并且涉及癌症和/根据体外和计算机筛选研究的结果，提出了“炎症信号通路”或“炎症信号通路” 。

在本研究中，通过放射性配体方法建立了BP-Cx-1的最大半数抑制浓度（IC50），对于腺苷受体A1，A2A和前列腺素受体EP2，IC50值的范围介于22.8和40.3μg/ ml之间， IP（PGI2）。血清素5-HT1和糖皮质激素GR受体的IC50分别为3.0μg/ ml和12.6μg/ ml，均在体内模型可达到的BP-Cx-1浓度范围内。

此外，用放射自显影研究了[ ³ H]标记的BP-Cx-1在NIH3T3鼠成纤维细胞和MCF7 / R癌细胞中的分布。[ ³ H] -BP-Cx-1（可视为βparticles产生的银粒）主要位于细胞膜上，在核周区域和细胞核中，表明BP-Cx-1进入细胞的能力和结合膜或细胞溶胶受体。

在我们的实验中，我们观察到了BP-Cx-1对树突状细胞（DC）成熟的影响：下调脂类呈递分子CD1a，共刺激分子CD80，CD83和CD 40的表达，降低pro-炎症细胞因子IL-4和TNF-α以及抗炎细胞因子IL-10的产生增加。据推测，在细胞核中可检测到的[ ³ H] -BP-Cx-1是活化的GR复合物的一部分，已知该复合物与调节负责抗炎反应的基因的转录有关。基于IC50，细胞分布数据和DC实验结果，表明BP-Cx-1的体内作用是通过GR和5-HT1受体介导的，从而促进了树突状细胞中致耐受效应子功能的发展。