State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China.
State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 730000, People's Republic of China; Research Institute, Lanzhou Jiaotong University, Lanzhou, 730070, People's Republic of China.
Phytochemistry. 2023 Aug;212:113723. doi: 10.1016/j.phytochem.2023.113723. Epub 2023 May 12.
A bioactivity-guided isolation from the aerial parts of Phyllanthus rheophyticus obtained 17 undescribed ent-cleistanthane-type diterpenoids, namely phyllarheophols A-Q, as well as 12 known analogs. Their structures were characterized by a combination of spectroscopic data interpretation, single-crystal X-ray diffraction and ECD analysis. The anti-inflammatory activities of these compounds were evaluated by measuring their inhibitory effects on NO production in LPS-stimulated RAW264.7 macrophages, and their preliminary structure-activity relationships were also discussed. Further study showed that promising compounds phyllarheophol D and phyacioid B significantly suppressed the expressions of cytokines and nitric oxide synthase through the NF-κB signaling pathway.
从显脉冷水花（Phyllanthus rheophyticus）的地上部分经生物活性导向分离得到 17 个新的未被描述的 ent-开环千里光菲烷型二萜类化合物，即 phyllarheophols A-Q，以及 12 个已知类似物。通过光谱数据分析、单晶 X 射线衍射和 ECD 分析等方法，确定了它们的结构。通过测定它们对 LPS 刺激的 RAW264.7 巨噬细胞中 NO 产生的抑制作用，评估了这些化合物的抗炎活性，并讨论了它们的初步结构-活性关系。进一步的研究表明，有前景的化合物 phyllarheophol D 和 phyacioid B 通过 NF-κB 信号通路显著抑制了细胞因子和一氧化氮合酶的表达。
