Kulkarni Roshan R, Lee Wonhwa, Jang Tae Su, Lee JungIn, Kwak Soyoung, Park Mi Seon, Lee Hyun-Shik, Bae Jong-Sup, Na MinKyun
College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 702-701, Republic of Korea; BK21 Plus KNU Biomedical Convergence Program, Department of Biochemistry and Cell Biology, School of Medicine, Kyungpook National University, Daegu 702-701, Republic of Korea.
Bioorg Med Chem Lett. 2015 Nov 15;25(22):5367-71. doi: 10.1016/j.bmcl.2015.09.031. Epub 2015 Sep 12.
Endothelial dysfunction is a key pathological feature of many inflammatory diseases, including sepsis. In the present study, a new caffeoyl glucoside (1) and two known caffeoylated compounds (2 and 3) were isolated from the fruits of Nandina domestica Thunb. (Berberidaceae). The compounds were investigated for their effects against lipopolysaccharide (LPS)-mediated endothelial inflammatory responses. At 20 μM, 1 and 2 inhibited LPS-induced hyperpermeability, adhesion, and migration of leukocytes across a human endothelial cell monolayer in a dose-dependent manner suggesting that 1 and 2 may serve as potential scaffolds for the development of therapeutic agents to treat vascular inflammatory disorders.
内皮功能障碍是包括脓毒症在内的多种炎症性疾病的关键病理特征。在本研究中，从南天竹（小檗科）果实中分离出一种新的咖啡酰葡萄糖苷（1）和两种已知的咖啡酰化化合物（2和3）。研究了这些化合物对脂多糖（LPS）介导的内皮炎症反应的影响。在20 μM浓度下，化合物1和2以剂量依赖的方式抑制LPS诱导的人内皮细胞单层的通透性增加、白细胞黏附和迁移，这表明化合物1和2可能作为开发治疗血管炎症性疾病治疗药物的潜在骨架。
