Yuan Zhen, Liu Di, Zhang Bingyang, Cao Shijie, Yao Tie, Zhao Qiduo, Qiu Feng, Zhao Feng
School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai 264005, People's Republic of China.
School of Chinese Materia Medica, Tianjin University of Chinese Traditional Medicine, Tianjin 301617, People's Republic of China.
Fitoterapia. 2023 Apr;166:105460. doi: 10.1016/j.fitote.2023.105460. Epub 2023 Feb 16.
Two new verticillane-diterpenoids (1 and 2) were isolated from the gum resin Boswellia sacra. Their structures were elucidated by physiochemical and spectroscopic analysis, as well as ECD calculation. In addition, the in vitro anti-inflammatory activities of the isolated compounds were evaluated by determining the inhibitory effects on lipopolysaccharide (LPS)-induced NO production in RAW 264.7 mouse monocyte-macrophages. The results showed that compound 1 exhibited significant inhibitory effect on NO generation with an IC value of 23.3 ± 1.7 μM suggesting that it might be a candidate for an anti-inflammatory agent. Furthermore, 1 potently inhibited the release of inflammatory cytokines IL-6 and TNF-α induced by LPS in a dose-dependent manner. Using Western blot and Immunofluorescence methods, compound 1 was found to inhibit inflammation mainly by restraining the activation of NF-κB pathway. And in the MAPK signaling pathway, it was found to have inhibitory effects on the phosphorylation of JNK and ERK proteins and have no effect on the phosphorylation of p38 protein.
从乳香树的树胶脂中分离出两种新的环维黄杨烷二萜（1和2）。通过理化和光谱分析以及电子圆二色（ECD）计算对其结构进行了阐明。此外，通过测定对脂多糖（LPS）诱导的RAW 264.7小鼠单核巨噬细胞中NO产生的抑制作用，评估了分离出的化合物的体外抗炎活性。结果表明，化合物1对NO生成具有显著抑制作用，IC值为23.3±1.7μM，表明它可能是一种抗炎剂候选物。此外，1以剂量依赖性方式强烈抑制LPS诱导的炎性细胞因子IL-6和TNF-α的释放。使用蛋白质免疫印迹和免疫荧光方法，发现化合物1主要通过抑制NF-κB途径的激活来抑制炎症。并且在丝裂原活化蛋白激酶（MAPK）信号通路中，发现它对JNK和ERK蛋白的磷酸化有抑制作用，而对p38蛋白的磷酸化没有影响。
