不同企业雷公藤多苷片及其主要单体成分药效作用评价

Pharmacodynamic Effects of Different Manufacturers’ Tripterygium Glycoside Tablets and the Main Monomer Components

目的:依托国家药品评价抽验项目,考察不同生产企业雷公藤多苷片及其中主要单体成分的抗炎及免疫抑制活性,为阐释该制剂的药效物质基础提供实验依据。方法:以脂多糖(LPS)诱导小鼠巨噬细胞RAW264.7为体外炎症模型,并以一氧化氮(NO)分泌水平和分化抗原簇86(CD86)表达水平为指标,明确雷公藤多苷片及其主要成分的药效作用。结果:实验发现,不同企业雷公藤多苷片均可拮抗LPS诱导的RAW264.7细胞中NO和CD86水平升高,具有不同程度的抗炎及免疫抑制活性,但其药理活性与制剂中所含雷公藤甲素、雷公藤内酯甲不完全呈正相关,提示存在其他药效成分;单体实验发现,标准中含量测定项雷公藤内酯甲并无明显药理活性,而雷公藤甲素、雷公藤红素和雷公藤对醌B对RAW264.7细胞活力有显著影响,且均可抑制LPS诱导的NO和CD86水平增加,提示三者可能为雷公藤多苷片中主要药效成分。结论:雷公藤多苷片中的雷公藤甲素、雷公藤红素和雷公藤对醌B等成分具有一定药理活性,而质量控制成分雷公藤内酯甲活性较弱,建议进一步研究明确主要单体成分的量效关系,科学合理地规范该制剂的产品质量,保证临床用药的有效性、安全性。

Objective:To investigate the anti-inflammatory and immunosuppressive activities of Tripterygium Glycoside Tablets(TPT)from different manufacturers and the main monomer components,so as to provide experimental basis for the interpretation of the therapeutic material basis of the preparation based on the national drug sampling and testing project.Methods:With the lipopolysaccharide(LPS)-induced in vitro inflammatory mouse RAW264.7 macrophage model and the indexes of nitric oxide(NO)and cluster differentiation 86(CD86),the pharmacological effects of TPT and the main components were elucidated.Results:TPT from different manufacturers could antagonize LPS-induced rise of NO and CD86 and had anti-inflammatory and immunosuppressive activities to varying degrees.However,their pharmacological activities were not completely positively correlated with triptolide and wilforlide A in the preparation,suggesting the existence of other active ingredients.The monomer experiment found that wilforlide A had no obvious activity,while triptolide,tripterine,and triptoquinone B had significant effects on RAW264.7 viability and all of them inhibited the LPS-induced increase of NO and CD86,suggesting that the threy were the main active components of TPT.Conclusion:This study preliminarily proves that triptolide,wilforlide A,and triptoquinone B in TPT have certain pharmacological activities,while the quality control component wilforlide A has weak activity.The dose-effect relationship of the main monomer components should be further clarified in an attempt to scientifically and reasonably regulate the quality of this preparation and ensure the efficacy and safety of it in clinical application.