College of Chemical Engineering, Nanjing Forestry University, 159 Long Pan Road, Nanjing 210037, China.
College of Chemical Engineering, Nanjing Forestry University, 159 Long Pan Road, Nanjing 210037, China.
Fitoterapia. 2018 Sep;129:25-33. doi: 10.1016/j.fitote.2018.05.029. Epub 2018 May 28.
Chlorogenic acid (CGA) has been reported to exhibit potent anti-inflammatory activity. However, the development of anti-inflammatory agent based on CGA has not been investigated. In this paper, a series of caffeoyl salicylate compounds derived from CGA were designed, synthesized, and evaluated by LPS-induced nitric oxide synthase inhibition and QRT-PCR technique. Most compounds showed modest activity to inhibit production of nitric oxide (NO) in RAW 264.7 cells induced by lipopolysaccharides (LPS). Among these compounds, QRT-PCR and western blotting results indicated that compounds 6b, 6c, 6f, 6g and D104 that possess 5-member ring or 6-member ring caused a significant inhibition against expression of the iNOS2 in LPS-induced macrophages. In addition, cytotoxic assay displayed most derivatives have good safety in vitro. This new promising scaffold could be further exploited for the development of anti-inflammatory agent in the future.
绿原酸（CGA）已被报道具有很强的抗炎活性。然而，基于 CGA 的抗炎剂的开发尚未得到研究。在本文中，设计、合成了一系列源自 CGA 的咖啡酰水杨酸酯化合物，并通过 LPS 诱导的一氧化氮合酶抑制和 QRT-PCR 技术进行了评价。大多数化合物对脂多糖（LPS）诱导的 RAW 264.7 细胞中一氧化氮（NO）的产生表现出适度的抑制活性。在这些化合物中，QRT-PCR 和 Western blot 结果表明，具有 5 元环或 6 元环的化合物 6b、6c、6f、6g 和 D104 对 LPS 诱导的巨噬细胞中 iNOS2 的表达有显著抑制作用。此外，细胞毒性测定显示大多数衍生物在体外具有良好的安全性。这个新的有前途的骨架可以在未来进一步开发用于抗炎剂。
