玛咖不同提取部位对磷酸二酯酶5抑制作用的谱-效关系研究

Spectrum-effect relationship of inhibition of different extracted parts from Lepdium meyenii on PDE5 activity

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 clarify the contribution of inhibitory effect of the chemical composition of fingerprint characteristic peaks from different parts of Lepdium meyenii （Maca） on PDE5, and to elucidate the material basis. Methods The HPLC fingerprints of different parts from L. meyenii were established. The isotope labelling method was adopted to test the inhibitory rate of different extracted parts on PDE5. The gray relative analysis and partial least-squares method were used to make correspond analysis of the spectrum-effect relationship. Results The fingerprints of different extracts were established and five peaks of the total 21 characteristic common peaks were identified by HPLC spectrum of standards and LCMS-IT-TOF. The strong relevance elements including macamide alkaloids represented by peaks 22-24 were verified as the potential PDE5 inhibitors. Conclusion A sensitive and convenient screening system for the PDE5 inhibitors via liquid scintillation counting is established. Macamides as liposoluble alkaloids could be material basis components to inhibit the activity of PDE5. This paper provides certain theory basis for resource utilization and the quality control of L. meyenii.