Third Level Research Laboratory of State Administration of Traditional Chinese Medicine, School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.
2 Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangzhou 510515, China.
J Tradit Chin Med. 2022 Oct;42(5):749-757. doi: 10.19852/j.cnki.jtcm.2022.05.008.
To systematically evaluate the anti-inflammatory potential of diterpene lactones from Chuanxinlian () (AP).
We firstly adopted zebrafish, a novel and ideal animal model for high-throughput drug screening, to investigate the anti-inflammatory activities of 17 diterpene lactones isolated from AP.
The results showed that most of diterpene lactones displayed significant anti-inflammatory effects in lipopolysaccharide microinjection-, copper sulfate exposure- or tail transection-induced zebrafish inflammation models. Moreover, diterpene lactone 3-deoxy-andrographoside (AP-5) was firstly found to attenuate inflammatory responses, which was closely associated with the myeloid differentiation primary response 88/nuclear factor-kappa B and signal transducer and activator of transcription 3 pathways.
Our research sheds light on the inestimable roles of zebrafish in high-throughput drug screening, elucidates the potent inhibitory effects of diterpene lactones against inflammation and indicates that AP-5 may serve as a potential alternative agent for the treatment of inflammatory diseases.
系统评价穿心莲中的二萜内酯（AP）的抗炎潜力。
我们首先采用斑马鱼作为高通量药物筛选的新型理想动物模型，研究了从 AP 中分离得到的 17 种二萜内酯的抗炎活性。
结果表明，大多数二萜内酯在脂多糖微量注射、硫酸铜暴露或尾部横断诱导的斑马鱼炎症模型中均表现出显著的抗炎作用。此外，首次发现二萜内酯 3-脱氧穿心莲内酯（AP-5）可减轻炎症反应，这与髓样分化原初反应 88/核因子-κB 和信号转导子和转录激活子 3 途径密切相关。
本研究揭示了斑马鱼在高通量药物筛选中的不可估量作用，阐明了二萜内酯对炎症的强烈抑制作用，并表明 AP-5 可能作为治疗炎症性疾病的潜在替代药物。
