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目的阐明玛咖不同提取部位的指纹图谱特征峰所代表的化学成分对磷酸二酯酶5(PDE5)抑制作用的影响,揭示药效物质基础。方法采用高效液相法建立玛咖不同提取部位的指纹图谱;采用同位素标记法测试不同提取部位对PDE5的抑制率;采用灰度关联分析法和偏最小二乘法分析谱-效关系。结果建立了玛咖不同提取部位的指纹图谱;指纹图谱中共有色谱峰21个,指认了其中5个成分。谱-效关系表明,玛咖对PDE5抑制作用的药效是多种成分共同作用的结果,脂溶性的玛咖酰胺类生物碱(峰22、23、24)对药效活性贡献较大。酶活性测试验证了3种玛咖酰胺具有较好的PDE5抑制作用。结论本实验建立的PDE5抑制剂筛选方法,采用液体闪烁计数,灵敏度高,简便易行;同时揭示了玛咖不同提取部位的指纹图谱与PDE5抑制作用具有相关性,玛咖酰胺类生物碱可能为PDE5抑制作用的药效物质基础,这为玛咖的资源利用和质量控制提供了理论依据。
Objective To elucidate the effects of the chemical components represented by the fingerprint peaks of different extracts on the inhibitory effect of phosphodiesterase 5 (PDE5), and to reveal the basis of pharmacodynamic substances. Methods The fingerprint of different parts of Maca extract was established by high performance liquid chromatography. The inhibition rate of PDE5 by different extraction sites was tested by isotope labeling method. The spectral-efficiency relationship was analyzed by gray relational analysis and partial least squares. Results The fingerprint of different parts of Maca was established. There were 21 peaks in the fingerprint and 5 of them were identified. The spectroscopic-efficacy relationship shows that the pharmacodynamic effect of maca on PDE5 inhibition is the result of the synergistic action of various components. Fat soluble macharamide alkaloids (peaks 22, 23, 24) contribute significantly to pharmacodynamic activity. Enzyme activity test showed that three kinds of maca amide have better PDE5 inhibitory effect. Conclusion The screening method of PDE5 inhibitor established in this experiment, using liquid scintillation counting, has high sensitivity and is simple and easy to perform. Meanwhile, it is revealed that the fingerprint of different parts of Maca has a correlation with the inhibitory effect of PDE5. Macaramides alkaloids may be PDE5 inhibitory effect of the material basis for the use of Maca resources and quality control provides a theoretical basis.