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目的:研究NSAID-贝母素乙酯的合成方法,评价其镇咳、抗炎、平喘的药理活性。方法:分别用4种NSAID药物与贝母素乙通过酯化反应得到目标化合物。通过小鼠镇咳实验、小鼠耳肿胀实验以及豚鼠平喘实验,考察其镇咳、抗炎、平喘活性。结果:成功合成4种化合物,并完成其结构鉴定。化合物3,4,5呈现出较好的镇咳活性,并能显著延长咳嗽潜伏期;化合物2,3,5的抗炎效果显著;4种化合物均有一定的平喘活性。结论:4种NSAID-贝母素乙酯都在不同程度上保留或增强了其原料药物的镇咳、抗炎、平喘药理活性,为进行进一步研究奠定了基础。
Objective: To study the synthetic method of NSAID-Fritillaria ethyl ester to evaluate the pharmacological activities of antitussive, anti-inflammatory and anti-asthmatic. Methods: The target compounds were obtained by esterification with four NSAID drugs and peiminine respectively. Antitussive, anti-inflammatory and anti-asthmatic activity were investigated by antitussive test in mice, ear swelling in mice and asthma in guinea pigs. Results: Four compounds were successfully synthesized and their structures were identified. Compounds 3, 4 and 5 showed better antitussive activity and prolonged cough latency significantly. The anti-inflammatory effects of compounds 2, 3 and 5 were significant. All four compounds had some antiasthmatic activity. CONCLUSION: Four kinds of NSAID-peimin ethyl ester all retain or enhance the antitussive, anti-inflammatory and anti-asthmatic pharmacological activity of their raw drug to varying degrees, which lays the foundation for further research.