基于谱效关系和成分敲除探讨独一味总黄酮抗类风湿关节炎的关键成分  

Study on the key components of total flavonoids from Lamiophlomis Herba in the treatment of rheumatoid arthritis based on spectrum-effect relationship and component knockout

作　　者：陈瑞鑫 康点点 詹琥珀 蒋桂华[1,3] 蒋运斌 CHEN Rui-xin;KANG Dian-dian;ZHAN HU-po;JIANG Gui-hua;JIANG Yun-bin(State Key Laboratory of Southwestern Chinese Medicine Resources,School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;College of Pharmaceutical Sciences,Southwest University,Chongqing 400000,China;School of Ethnic Medicine,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院,西南特色中药资源国家重点实验室,成都611137 [2]西南大学药学院中医药学院,重庆400000 [3]成都中医药大学民族医药学院,成都611137

出　　处：《天然产物研究与开发》2023年第11期1833-1841,共9页Natural Product Research and Development

基　　金：国家自然科学基金青年科学基金(82104528);重庆市自然科学基金面上项目(cstc2020jcyj-msxmX0146);国家重点研发计划(2019YFC1712302)。

摘　　要：为探讨独一味总黄酮抗类风湿关节炎(rheumatoid arthritis,RA)的关键成分,阐明独一味治疗RA的药效物质基础,本研究建立了独一味总黄酮的指纹图谱,13批独一味总黄酮指纹图谱共标示了8个共有峰,指认了其中3个共有峰。同时基于13批独一味总黄酮样品对成纤维样滑膜细胞(fibroblast-like synoviocytes,FLS)活力的影响,建立了独一味总黄酮抗RA的谱效关系,结果表明木犀草苷和木犀草素为独一味总黄酮抗RA的关键成分。采用成分敲除技术探讨独一味总黄酮中木犀草苷成分抗RA的药效,并比较了等摩尔量木犀草苷和木犀草素对照品分别对FLS细胞活力的影响,结果表明木犀草苷和木犀草素成分均能显著抑制FLS细胞活力(P<0.01),且二者抑制率无显著性差异。结合独一味总黄酮HPLC图谱中木犀草苷含量明显高于木犀草素,表明木犀草苷为独一味总黄酮抗RA的关键成分之一,可为临床运用独一味治疗RA提供一定的参考。This study aimed to explore the key components of total flavonoids from Lamiophlomis Herba(LH)against rheumatoid arthritis(RA),which can elucidate the active components of LH against RA.In this work,the fingerprint of 13 batches of the total flavonoids from LH was established,including eight common peaks,of which three were identified.Based on the effect of 13 batches of total flavonoids from LH on the activity of fibroblast-like synoviocytes(FLS),the spectrum-effect relationship was established for the anti-RA effect of total flavonoids from LH.The results showed that luteoloside and luteolin were key components of total flavonoids from LH against RA.Then,the component knockout technique was used to investigate the anti-RA efficacy of the luteoloside component in the total flavonoids from LH,and the effects of luteoloside and luteolin on FLS cell viability were compared.The results showed that luteoloside and luteolin could significantly inhibit FLS cell viability(P<0.01),and there was no significant difference between their inhibition rates.Because the HPLC spectrum of total flavonoids form LH showed that the content of luteoloside was higher than that of luteolin,luteoloside is a key component of total flavonoids from LH against RA.This work can provide a certain reference for the clinical application of LH in the treatment of RA.

关 键 词：独一味 总黄酮 类风湿关节炎 药效物质基础 

分 类 号：R932[医药卫生—生药学]