State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China.
School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, Beijing 100191, China.
Phytochemistry. 2018 Dec;156:167-175. doi: 10.1016/j.phytochem.2018.10.001. Epub 2018 Oct 9.
Tripterygium hypoglaucum (H. Lév.) Hutch. has been used to remedy rheumatoid arthritis, however, it shows frequent toxicity to the body. In this study, liquid chromatograph-mass spectrometer (LC-MS) was guided to characterize abietanes diterpenoids with anti-inflammatory activity from the stem of T. hypoglaucum. Thirteen undescribed abietanes diterpenoids were isolated and purified, and their chemical structure was identified using various spectroscopic methods. These compounds belonged to abietanes with splitting C ring, abietanes with benzenoid rings, diterpene quinoids, diterpene quinoids with lactone rings, and abietanes with benzenoid and lactone rings, respectively. Lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 macrophages was used to evaluate anti-inflammatory activity of the compounds. The results indicated that hypoglicin B-G and hypoglicin J-M exhibited inhibitory activity of NO production with the IC values of 6.01, 25.21, 8.29, 3.63, 0.72, 0.89, 36.91, 0.82, 2.85, 11.92 μM, respectively. Among these compounds, compound hypoglicin L showed high anti-inflammatory activity and low toxicity (SI = 5.02 × 10). Further QPCR analysis revealed that hypoglicin D and hypoglicin L can inhibit the mRNA expression of iNOS in LPS-stimulated RAW264.7 cells at doses of 12.5 and 3.13 μM, respectively. Taken together, ten anti-inflammatory diterpenoids were found from T. hypoglaucum in this study.
昆明山海棠已被用于治疗类风湿关节炎，但它对人体有频繁的毒性。在这项研究中，液质联用（LC-MS）被用来从昆明山海棠的茎中鉴定具有抗炎活性的枞型二萜类化合物。分离并纯化了 13 种未描述的枞型二萜类化合物，通过各种光谱方法鉴定了它们的化学结构。这些化合物分别属于开裂 C 环枞型二萜、苯并环枞型二萜、二萜醌、内酯环二萜醌和苯并环及内酯环枞型二萜。采用脂多糖（LPS）诱导 RAW264.7 巨噬细胞产生一氧化氮（NO）的方法来评价化合物的抗炎活性。结果表明，hypoglicin B-G 和 hypoglicin J-M 对 NO 生成具有抑制作用，IC 值分别为 6.01、25.21、8.29、3.63、0.72、0.89、36.91、0.82、2.85、11.92 μM。在这些化合物中，化合物 hypoglicin L 表现出较高的抗炎活性和较低的毒性（SI = 5.02×10）。进一步的 QPCR 分析表明，hypoglicin D 和 hypoglicin L 可以分别在 12.5 和 3.13 μM 的剂量下抑制 LPS 刺激的 RAW264.7 细胞中 iNOS 的 mRNA 表达。总之，本研究从昆明山海棠中发现了 10 种具有抗炎活性的二萜类化合物。
