College of Pharmacy, Chosun University, Gwangju 61452, Korea.
Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan 54538, Korea.
Int J Mol Sci. 2021 Jul 12;22(14):7472. doi: 10.3390/ijms22147472.
The root bark of has been reported to have anti-sclerotic, anti-inflammatory, antioxidant, neuroprotective, hepatoprotective, and cytotoxic activities. In the present study, the effect of 16 compounds from on tumor necrosis factor-α+interferon-γ-treated HaCaT cells were investigated. Among these 16 compounds, 11 decreased IL-6 production and 15 decreased IL-8 production. The six most effective compounds, namely, steppogenin (), cudraflavone C (), macluraxanthone B (), 1,6,7-trihydroxy-2-(1,1-dimethyl-2-propenyl)-3- methoxyxanthone (), cudraflavanone B (), and cudratricusxanthone L (), were selected for further experiments. These six compounds decreased the expression levels of chemokines, such as regulated on activation, normal T cell expressed and secreted (RANTES) and thymus and activation-regulated chemokine (TARC), and downregulated the protein expression levels of intercellular adhesion molecule-1. Compounds , , , , and inhibited nuclear factor-kappa B p65 translocation to the nucleus; however, compound showed no significant effects. In addition, extracellular signal regulatory kinase-1/2 phosphorylation was only inhibited by compound , whereas p38 phosphorylation was inhibited by compounds and . Taken together, the compounds from showed potential to be further developed as therapeutic agents to suppress inflammation in skin cells.
的根皮已被报道具有抗硬化、抗炎、抗氧化、神经保护、肝保护和细胞毒性作用。在本研究中，研究了来自 的 16 种化合物对肿瘤坏死因子-α+干扰素-γ处理的 HaCaT 细胞的影响。在这 16 种化合物中，有 11 种降低了 IL-6 的产生，有 15 种降低了 IL-8 的产生。六种最有效的化合物，即，薯蓣皂苷元（）、库拉索黄酮 C（）、马陆烷酮 B（）、1,6,7-三羟基-2-(1,1-二甲基-2-丙烯基)-3-甲氧基黄烷酮（）、库拉索二氢黄酮 B（）和库拉索三醇 L（），被选为进一步实验的对象。这六种化合物降低了趋化因子的表达水平，如调节激活正常 T 细胞表达和分泌（RANTES）和胸腺激活调节趋化因子（TARC），并下调了细胞间黏附分子-1 的蛋白表达水平。化合物 、 、 、 、和 抑制核因子-κB p65 向核内易位；然而，化合物 没有显示出显著的效果。此外，细胞外信号调节激酶-1/2 的磷酸化仅被化合物 抑制，而 p38 的磷酸化被化合物 和 抑制。综上所述，来自 的化合物具有进一步开发为抑制皮肤细胞炎症的治疗剂的潜力。
