College of Chinese Medicine Material, Jilin Agricultural University, Changchun 130118, China.
Key Laboratory of Bioactive Substances and Resource Utilization of Chinese Herbal Medicine, Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100193, China.
Molecules. 2021 Sep 15;26(18):5603. doi: 10.3390/molecules26185603.
Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the aim of this study was to screen for compounds with anti-inflammatory activities in Benth. Using silica gel, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, 10 compounds were separated from Benth. extract, including four new diterpenoids (-), one amide alkaloid (), and five known diterpenoids (-). The structures of all the isolates were elucidated by HR-ESI-MS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, we investigated the anti-inflammatory activities of compounds -. It is worth noting that all were able to inhibit nitric oxide (NO) production with IC values < 50 μM and little effect on RAW 264.7 macrophage viability. Compounds and displayed remarkable inhibition with IC values of 19.2 and 18.8 μM, respectively. Meanwhile, screening on HCT-8 cells demonstrated that compounds and also had moderate cytotoxic activities with IC values of 36.3 and 41.4 μM, respectively, which is related to their anti-inflammatory effects.
Benth. 临床上用于治疗气管炎、咳嗽、哮喘、感冒、发热、小便不利等症状，具有清热祛湿的作用。然而，目前对其功效的物质基础的研究较少。因此，本研究旨在从 Benth. 中筛选具有抗炎活性的化合物。采用硅胶、ODS C18 和 Sephadex LH-20 柱层析以及半制备 HPLC 等方法，从 Benth. 提取物中分离得到 10 种化合物，包括 4 种新二萜（-）、1 种酰胺生物碱（）和 5 种已知二萜（-）。所有分离物的结构均通过 HR-ESI-MS、NMR 和 CD 分析确定。采用脂多糖（LPS）刺激 RAW 264.7 细胞，研究了化合物 - 的抗炎活性。值得注意的是，所有化合物均能抑制一氧化氮（NO）的产生，IC 值<50 μM，对 RAW 264.7 巨噬细胞活力影响较小。化合物和表现出显著的抑制作用，IC 值分别为 19.2 和 18.8 μM。同时，对 HCT-8 细胞的筛选表明，化合物和也具有中等的细胞毒性，IC 值分别为 36.3 和 41.4 μM，这与其抗炎作用有关。
