State Key Laboratory of Natural Medicines, School of Life Science and Technology, China Pharmaceutical University, Nanjing, 210009, China.
Key Laboratory of Universities in Hunan Province on Cardiovascular and Cerebrovascular Natural Drugs Research, Department of Pharmacology, Xiangnan University, Chenzhou, 423000, PR China.
Eur J Pharmacol. 2019 Aug 15;857:172453. doi: 10.1016/j.ejphar.2019.172453. Epub 2019 Jun 13.
Aesculin, a natural product from the traditional and widely-used Chinese medicine named Cortex fraxini, has attracted attention as a novel therapeutic modulator of inflammation. However, little is known about its effect on ulcerative colitis (UC). This study aimed to investigate the protective effects and mechanisms of aesculin on colitis. The results showed that, few cytotoxicity of aesculin were shown in vivo and in the RAW264.7 macrophages, while aesculin significantly relieved the symptoms of DSS-induced colitis and restrained the expression of inflammatory factors including iNOS, IL-1β, TNF-α in both peritoneal macrophages and colonic tissues from DSS-induced mice and RAW264.7 macrophages. Of note, aesculin attenuated the activity of NF-κB signaling while promoted the nuclear localization of PPAR-γ in both rectal tissues from DSS-induced mice and LPS-stimulated macrophages. These findings demonstrated that the protection of aesculin against ulcerative colitis might be due to its regulation on the PPAR-γ and NF-κB pathway. Thus, aesculin could serve as a potential therapeutic agent for the treatment of ulcerative colitis.
秦皮素是一种从传统的、广泛使用的中药秦皮中提取的天然产物，作为一种新型的炎症治疗调节剂引起了人们的关注。然而，关于它对溃疡性结肠炎（UC）的作用知之甚少。本研究旨在探讨秦皮素对结肠炎的保护作用及其机制。结果表明，秦皮素在体内和 RAW264.7 巨噬细胞中表现出很少的细胞毒性，而秦皮素显著缓解了 DSS 诱导的结肠炎的症状，并抑制了 DSS 诱导的小鼠腹膜巨噬细胞和结肠组织中包括 iNOS、IL-1β、TNF-α在内的炎症因子的表达和 RAW264.7 巨噬细胞。值得注意的是，秦皮素减弱了 NF-κB 信号通路的活性，同时促进了 DSS 诱导的小鼠直肠组织和 LPS 刺激的巨噬细胞中 PPAR-γ的核定位。这些发现表明，秦皮素对溃疡性结肠炎的保护作用可能是由于其对 PPAR-γ 和 NF-κB 通路的调节。因此，秦皮素可以作为治疗溃疡性结肠炎的潜在治疗剂。
