Abstract：
Psoriasis is a chronic inflammatory disease and is difficult to cure. In this work, a series of novel chrysin derivatives have been designed and prepared while evaluating anti-inflammatory activities in vitro and in vivo. In vitro, RAW264.7 cells were used to detect the inflammatory activities at first, and compounds 4h, 4k, and 4o significantly decreased the levels of NO, TNF-α, and IL-6. In particular, compound 4o showed superior anti-inflammatory activities than other compounds. Moreover, compound 4o decreased the level of IL-17A in LPS-induced HaCaT cells in vitro. The effect and mechanism of anti-inflammatory activities on psoriasis were determined by imiquimod (IMQ)-induced psoriasis-like mice in vivo. Compound 4o deduced the level of IL-6, IL-17A, IL-22, IL-23, and TNF-α, and showed potent anti-psoriasis activity. Further mechanism study suggested that compound 4o could improve the skin inflammation of psoriasis by inhibiting the NF-κB and STAT3 signaling pathways.
摘要：
银屑病是一种慢性炎症性疾病，难以治愈。在这项工作中,在体外和体内评估抗炎活性的同时，设计并制备了一系列新型的chrysin衍生物。体外，首先用RAW264.7细胞检测炎症活性，和化合物4h，4k,并显著降低NO的水平，TNF-α,IL-6特别是,化合物4o显示出比其他化合物更好的抗炎活性。此外，化合物4o在体外降低LPS诱导的HaCaT细胞中IL-17A的水平。通过咪喹莫特（IMQ）诱导的银屑病样小鼠体内研究了抗炎活性对银屑病的作用和机制。化合物4o推导出IL-6、IL-17A、IL-22、IL-23和TNF-α，并显示出有效的抗牛皮癣活性。进一步的机制研究表明，化合物4o可通过抑制NF-κB和STAT3信号通路改善银屑病的皮肤炎症。
