Department of Pharmacognosy and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, China.
Department of Pharmacognosy and Utilization Key Laboratory of Northeast Plant Materials, School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, China.
Bioorg Chem. 2020 Jun;99:103764. doi: 10.1016/j.bioorg.2020.103764. Epub 2020 Mar 19.
The Syringae Folium (SF), noted in Chinese Pharmacopeia, has been used in herbal medicines to treat inflammatory diseases and its water extract of SF, Yanlixiao (YLX) which is commercial preparation traditional Chinese medicine has been widely used clinically against intestinal inflammations. To explore its therapeutic material basis of SF, an effective fraction from SF (ESF) was found out by bio-guided isolation and enrichment of active components. In this research, ESF was identified as the anti-inflammatory fraction by comparing the survival rate of LPS-induced inflammation mouse model. The in vivo anti-inflammation efficacy of ESF was further tested by mouse ear edema model. Fifteen main components of ESF were separated from ESF after identification by UPLC-TOF-MS, and their inhibition on lipopolysaccharide (LPS)-induced nitric oxide (NO) production was tested along with ESF in RAW 264.7 macrophages cell line. Aiming to search its anti-inflammation mechanisms, the network pharmacology study was performed based on the main active components. As results, ESF was found with better efficacy in inhibiting ear swelling (82.2 mg/kg, 43.7%) compared with YLX (293.3 mg/kg, 37.9%). Meanwhile, the main ESF components, luteolin and quercetin were found with significant efficacy in reducing NO production compared with aminoguanidine (positive control) (81.3%, 78.7% and 76.3%, respectively, 50 μg/ml). Analysis of network pharmacology also suggested that luteolin and quercetin could be the key components for the anti-inflammation activity of ESF, and NFKB1, RELA, AKT1, TNF and PIK3CG were identified as key targets and MAPK, NF-κB, TCR and TLRs signaling pathways could be involved in the anti-inflammation action of ESF. The results attained in this study indicated that ESF had the potential to be developed as an anti-inflammation agent applied in clinic.
《桑叶(SF)》在《中国药典》中有记载,已被用于草药治疗炎症性疾病,其水提取物 YLX 是一种商业制剂的传统中药,已广泛用于临床治疗肠道炎症。为了探索 SF 的治疗物质基础,通过生物导向的活性成分的分离和富集,发现了 SF 的有效部位(ESF)。在这项研究中,通过比较 LPS 诱导的炎症小鼠模型的存活率,将 ESF 鉴定为抗炎部位。通过小鼠耳肿胀模型进一步测试 ESF 的体内抗炎功效。通过 UPLC-TOF-MS 鉴定 ESF 后,从 ESF 中分离出 15 种主要成分,并在 RAW 264.7 巨噬细胞系中测试它们对脂多糖(LPS)诱导的一氧化氮(NO)产生的抑制作用以及 ESF 的抑制作用。为了寻找其抗炎机制,基于主要活性成分进行了网络药理学研究。结果表明,与 YLX(293.3mg/kg,37.9%)相比,ESF 在抑制耳肿胀方面(82.2mg/kg,43.7%)具有更好的疗效。同时,主要 ESF 成分木犀草素和槲皮素在降低 NO 产生方面与氨基胍(阳性对照)相比具有显著疗效(分别为 81.3%、78.7%和 76.3%,50μg/ml)。网络药理学分析还表明,木犀草素和槲皮素可能是 ESF 抗炎活性的关键成分,NFKB1、RELA、AKT1、TNF 和 PIK3CG 被鉴定为关键靶点,MAPK、NF-κB、TCR 和 TLRs 信号通路可能参与 ESF 的抗炎作用。本研究结果表明,ESF 具有开发为临床应用的抗炎药物的潜力。