Sipahi Hande, Gostner Johanna M, Becker Kathrin, Charehsaz Mohammad, Kirmizibekmez Hasan, Schennach Harald, Aydin Ahmet, Fuchs Dietmar
a Department of Toxicology , Faculty of Pharmacy, Yeditepe University , Kayisdagi , Istanbul , Turkey .
b Division of Biological Chemistry , Biocenter, Medical University , Innsbruck , Austria .
Pharm Biol. 2016;54(4):712-9. doi: 10.3109/13880209.2015.1072830. Epub 2015 Oct 1.
Natural products can present remarkable biological and pharmacological activities. In traditional medicine, plants have been used historically in treating cancer, infections, and other inflammatory conditions.
Verbascoside and catechin are widespread polyphenolic plant compounds that could play a role in the anti-inflammatory and health-promoting effects of plants and plant extracts.
This study compares the potential cytotoxic effects of polyphenols verbascoside and catechin (6.25-200 µM) on human peripheral blood mononuclear cells (PBMC) for 48 h and myelomonocytic THP-1 and THP-1 Blue cells for 24 h. The effects of the compounds on immune activation markers such as indoleamine 2,3-dioxygenase (IDO) activity as well as on neopterin formation and nuclear factor-κB (NF-κB) activation were investigated. Cytotoxicity of the compounds was tested using Cell-Titer Blue assay.
Verbascoside exhibited significant suppressive effects in mitogen-stimulated PBMC on tryptophan breakdown (>50 µM; IC50 value: 58.6 µM) and the production of neopterin (>6.25 µM; IC50 value: 217 µM). These effects correlated with a decline in cell viability, while THP-1 Blue cells were less sensitive. NF-κB activity was slightly enhanced at lower concentrations (<50 µM verbascoside) in stimulated cells and at the highest concentration used in unstimulated cells. Catechin had no relevant effects on cell viability and on the tested inflammation markers, except NF-κB activation in THP-1 Blue cells.
The results obtained show that verbascoside and catechin represent effective compounds which interfere with immunobiochemical pathways that are highly relevant for immunosurveillance and competing virus infections.
天然产物具有显著的生物学和药理活性。在传统医学中，植物长期以来一直被用于治疗癌症、感染和其他炎症性疾病。
毛蕊花糖苷和儿茶素是广泛存在的多酚类植物化合物，可能在植物和植物提取物的抗炎及促进健康作用中发挥作用。
本研究比较了多酚类化合物毛蕊花糖苷和儿茶素（6.25 - 200 μM）对人外周血单核细胞（PBMC）作用48小时以及对骨髓单核细胞THP - 1和THP - 1 Blue细胞作用24小时后的潜在细胞毒性作用。研究了这些化合物对免疫激活标志物如吲哚胺2,3 - 双加氧酶（IDO）活性、新蝶呤形成以及核因子 - κB（NF - κB）激活的影响。使用Cell - Titer Blue检测法测试化合物的细胞毒性。
毛蕊花糖苷对丝裂原刺激的PBMC中色氨酸分解（>50 μM；IC50值：58.6 μM）和新蝶呤产生（>6.25 μM；IC50值：217 μM）表现出显著抑制作用。这些作用与细胞活力下降相关，而THP - 1 Blue细胞对其敏感性较低。在刺激细胞中较低浓度（<50 μM毛蕊花糖苷）以及未刺激细胞中使用的最高浓度时，NF - κB活性略有增强。儿茶素对细胞活力以及所测试的炎症标志物无相关影响，但对THP - 1 Blue细胞中的NF - κB激活有影响。
所得结果表明，毛蕊花糖苷和儿茶素是有效的化合物，它们干扰了与免疫监视和对抗病毒感染高度相关的免疫生化途径。
