| 不同企业雷公藤多苷片及其主要单体成分药效作用评价 |
| 投稿时间：2020-08-26 点此下载全文
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| 引用本文：汪祺,王曼虹,王亚丹,张乐帅,马双成,文海若.不同企业雷公藤多苷片及其主要单体成分药效作用评价[J].中国现代中药,2021,23(8):1335-1343 |
| DOI：10.13313/j.issn.1673-4890.20200826003 |
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| 作者中文名 | 作者英文名 | 单位中文名 | 单位英文名 | E-Mail |
| 汪祺 |
WANG Qi |
中国食品药品检定研究院，北京 100050 |
National Institutes for Food and Drug Control, Beijing 100050, China |
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| 王曼虹 |
WANG Man-hong |
中国食品药品检定研究院，北京 100050 |
National Institutes for Food and Drug Control, Beijing 100050, China |
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| 王亚丹 |
WANG Ya-dan |
中国食品药品检定研究院，北京 100050 |
National Institutes for Food and Drug Control, Beijing 100050, China |
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| 张乐帅 |
ZHANG Le-shuai |
苏州大学，江苏 苏州 215123 |
Soochow University, Suzhou 215123, China |
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| 马双成 |
MA Shuang-cheng |
中国食品药品检定研究院，北京 100050 |
National Institutes for Food and Drug Control, Beijing 100050, China |
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| 文海若 |
WEN Hai-ruo |
中国食品药品检定研究院，北京 100050 |
National Institutes for Food and Drug Control, Beijing 100050, China |
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| 基金项目:国家自然科学基金项目 （81503347， 81503068）；国家“重大新药创制”科技重大专项（2018ZX09201017-001） |
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| 中文摘要: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。 |
| 中文关键词:雷公藤多苷片 抗炎 一氧化氮 分化抗原簇86 雷公藤甲素 雷公藤红素 雷公藤内酯甲 |
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| Pharmacodynamic Effects of Different Manufacturers' Tripterygium Glycoside Tablets and the Main Monomer Components |
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| Abstract: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. |
| keywords:Tripterygium Glycoside Tablets anti-inflammation NO CD86 triptolide tripterine wilforlide A |
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