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梁格散抗炎成分的最佳组合。

Optimal combination of anti-inflammatory components from Chinese medicinal formula Liang-Ge-San.

机构信息

Third Level Research Laboratory of State Administration of Traditional Chinese Medicine, School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, 510515, PR China; Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Guangzhou, 510515, PR China.

出版信息

J Ethnopharmacol. 2021 Apr 6;269:113747. doi: 10.1016/j.jep.2020.113747. Epub 2020 Dec 24.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Liang-Ge-San (LGS), a traditional Chinese medicine (TCM) formula, is usually used in acute inflammatory diseases in China.

AIM OF THE STUDY

This study aims to detect the optimal combination of anti-inflammatory components from LGS.

MATERIALS AND METHODS

Four mainly representative components (phillyrin, emodin, baicalin, and liquiritin) from LGS were chosen. The optimal combination was investigated by orthogonal design study. Zebrafish inflammation model was established by lipopolysaccharide (LPS)-yolk microinjection, and then the anti-inflammatory activities of different combinations were determined by survival analysis, changes on inflammatory cells infiltration, the MyD88/NF-κB and MAPK pathways and inflammatory cytokines production.

RESULTS

The different combinations of bioactive ingredients from LGS significantly protected zebrafish from LPS-induced inflammation, as evidenced by decreased recruitment of macrophages and neutrophils, inhibition of the MyD88/NF-κB and MAPK pathways and down-regulation of TNF-α and IL-6. Among them, the combination group 8 most significantly protected against LPS. The combination of group 8 is: 0.1 μM of emodin, 2 μM of baicalin, 20 μM of phillyrin and 12.5 μM of liquiritin.

CONCLUSION

The optimized combination group 8 exerts the most significant anti-inflammatory activity by inhibiting the recruitment of inflammatory cells, activation of the MyD88/NF-κB and MAPK pathways and the secretion of pro-inflammatory cytokines. This present study provides pharmacological evidences for the further development of new modern Chinese drug from LGS to treat acute inflammatory diseases, but indicated the use of zebrafish in the screening of components from formulas.

摘要

民族药理学相关性

凉膈散(Liang-Ge-San,LGS)是一种中药方剂,常用于中国的急性炎症性疾病。

目的

本研究旨在从凉膈散中检测出最佳的抗炎成分组合。

材料和方法

选择凉膈散中的四种主要代表性成分(连翘苷、大黄素、黄芩苷和甘草苷)。通过正交设计研究来考察最佳组合。通过脂多糖(LPS)-卵黄微注射建立斑马鱼炎症模型,然后通过生存分析、炎症细胞浸润变化、MyD88/NF-κB 和 MAPK 通路以及炎症细胞因子产生来确定不同组合的抗炎活性。

结果

凉膈散生物活性成分的不同组合显著保护斑马鱼免受 LPS 诱导的炎症,表现为巨噬细胞和中性粒细胞浸润减少,MyD88/NF-κB 和 MAPK 通路受到抑制,TNF-α和 IL-6 表达下调。其中,组合 8 对 LPS 的保护作用最为显著。组合 8 为:0.1μM 大黄素、2μM 黄芩苷、20μM 连翘苷和 12.5μM 甘草苷。

结论

优化组合 8 通过抑制炎症细胞募集、MyD88/NF-κB 和 MAPK 通路激活以及促炎细胞因子分泌,发挥最显著的抗炎活性。本研究为进一步开发从凉膈散中治疗急性炎症性疾病的新型现代中药提供了药理学依据,但也表明在成分筛选中使用斑马鱼。

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