Li Xiaoyi, Lu Cheng, Du Wenxia, Zou Qiuping, Wang Ruirui, Hu Chunyan, Li Yanping, Zhang Yi, Mao Zewei
School of Chinese Materia Medica, Yunnan University of Chinese Medicine Kunming 650500 PR China
RSC Med Chem. 2024 Jun 27;15(8):2773-2784. doi: 10.1039/d4md00301b. eCollection 2024 Aug 14.
Atopic dermatitis (AD), a recurrent inflammatory systemic skin disease, is difficult to cure. In the present study, several ethylenediamine-derived dehydrocostuslactone (DHCL) derivatives were prepared to assess their and anti-inflammatory activities. The results indicated that DHCL derivatives inhibited NO generation with low cytotoxicity. In particular, compound 5d exhibited the best anti-inflammatory activity. Subsequent experiments revealed that 5d not only inhibited the LPS-induced inflammatory response in RAW264.7 cells the MAPK-NF-κB signaling pathway inhibition but also significantly decreased Th2-type cytokine levels and inhibited the NF-κB signaling pathway activation in mice with MC903-induced AD. Therefore, DHCL derivatives may be considered as new agents for the treatment of AD.
特应性皮炎（AD）是一种复发性炎症性全身性皮肤病，难以治愈。在本研究中，制备了几种乙二胺衍生的脱氢木香内酯（DHCL）衍生物，以评估它们的[具体内容缺失]和抗炎活性。结果表明，DHCL衍生物以低细胞毒性抑制一氧化氮生成。特别是，化合物5d表现出最佳的抗炎活性。后续实验表明，5d不仅通过抑制MAPK-NF-κB信号通路抑制RAW264.7细胞中脂多糖诱导的炎症反应，还显著降低了MC903诱导的AD小鼠中Th2型细胞因子水平并抑制了NF-κB信号通路的激活。因此，DHCL衍生物可被视为治疗AD的新型药物。
