基于视网膜Müller细胞的人参皂苷类成分调节糖基化终末产物干预下HIF-1α表达的谱效关系研究

Study on the spectrum-effect relationship of ginsenoside regulating expression of HIF-1α under AGEs based on retinal Müller cells

目的:研究人参须根皂苷HPLC指纹图谱与调节糖基化终末产物干预下视网膜Müller细胞HIF-1α活性表达之间的关系,筛选人参防治糖尿病性视网膜病变的活性成分。方法:采用HPLC建立10批人参须根皂苷指纹图谱,测定人参皂苷类成分抑制糖基化终末产物干预下视网膜Müller细胞HIF-1α的表达活性,运用偏最小二乘法研究特征峰面积与药效值之间的谱效相关性。结果:10批人参须根皂苷提取物(剂量:400mg/L)对HIF-1α的活性表达均有不同程度的抑制作用,其中人参皂苷Re、人参皂苷Rh1、人参皂苷Rd及4个尚未确定结构的成分可能是人参防治糖尿病性视网膜病变的主要活性成分。结论:谱效关系研究为筛选人参防治糖尿病性视网膜病变活性成分提供了一个有效途径。

Objective： This work investigated the spectrum-effect relationship between HPLC fingerprint of ginsenoside extractions and inhibition effect of the hypoxia-inducible factor-let （HIF-let） in retinal MUller cell under the condition of AGEs, and screened active components of Pa- nax ginseng C.A. Mayer in the prevention and treatment of DR. Methods ： Fingerprint of ginsenoside extractions from various sources were established by HPLC, while the inhibition effect of the HIF-let in retinal Mailer cell was evaluated by measuring the content of HIF-1α. The spectrum-effect relationship between the HPLC fingerprint and pharmacological activity was analyzed using Partial least square regression anal- ysis. Results： Ten samples all had the capacity to inhibit the expression of HIF-1α and the inhibitory extent varied with various sources of ex- tracts. Dose of each batch of samples is 400mg/L. Ginsenoside Re, ginsenoside Rhl, ginsenoside Rd and other four unknown ingredients （peak numbers 1, 2, 11 and 13） in HPLC fingerprint might be the active components. Conclusion： The spectrum-effect relationship pro- vides an effective approach to screen the active substance of Ginseng for curing DR.