Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Guilin Medical University, Guilin, China.
School of Medicine, Shanghai University, Shanghai, China.
Planta Med. 2022 Aug;88(9-10):721-728. doi: 10.1055/a-1712-8209. Epub 2021 Dec 28.
Caulis Trachelospermi, the stems with leaves of , is a well-known herbal drug of the Apocynaceae family recorded in the Chinese pharmacopeia and used for the treatment of inflammation-related diseases by ethnic minorities of China. The mechanism of anti-inflammatory activity and responsible constituents of have not been well elucidated in previous studies. Preliminary investigation showed that both the water and the ethyl ester extracts of exhibited potent inhibitory activity on nitric oxide (NO) production using lipopolysaccharide (LPS)-stimulated murine macrophages. Phytochemical investigation on these extracts afforded 23 compounds, including three new compounds (1: -3: ) identified on the basis of spectroscopic and mass spectrometric data. Anti-inflammatory bioassay showed that compounds 17, 18, 22: , and 23: inhibited significantly the production of NO in a concentration-dependent manner. Further studies indicated that compound 23: inhibited significantly TNF- and IL-6 produced by LPS-stimulated RAW 264.7 cells with good selectivity, as well as protein expression of iNOS in RAW 264.7 cells. These chemical constituents may contribute to the anti-inflammatory potential of .
通光藤茎和叶,为夹竹桃科知名草药,在中国药典中有记载,中国少数民族用于治疗炎症相关疾病。其抗炎活性机制和有效成分在以前的研究中尚未得到很好的阐明。初步研究表明,通光藤的水提物和乙酸乙酯提取物对脂多糖(LPS)刺激的小鼠巨噬细胞产生的一氧化氮(NO)具有很强的抑制活性。对这些提取物的植物化学研究得到了 23 种化合物,其中包括基于光谱和质谱数据鉴定的三种新化合物(1: -3: )。抗炎生物测定表明,化合物 17、18、22: ,和 23:以浓度依赖的方式显著抑制了 NO 的产生。进一步的研究表明,化合物 23:显著抑制了 LPS 刺激的 RAW 264.7 细胞中 TNF-α和 IL-6 的产生,具有良好的选择性,以及 RAW 264.7 细胞中 iNOS 的蛋白表达。这些化学成分可能是通光藤具有抗炎潜力的原因。