应用体外模型从植物提取物中筛选治疗雄激素源性脱发的5a-还原酶抑制剂

Screening 5a-reductase Inhibitors from Plant Extraction for Treatment of Androgenic Alopecia in vitro

目的应用5a-还原酶抑制剂体外筛选模型,寻找植物提取物中天然5a-还原酶抑制剂,用于雄激素源性脱发的治疗。方法通过HPLC测定底物睾酮(T)在酶促反应中的下降速率计算酶活力,建立5a-还原酶抑制剂体外筛选模型。采用此体外模型对多种植物提取物进行酶抑制作用筛选,继而对筛出的植物提取物采用制备液相进行组分分离制备,测定各段组分酶抑制活性,最终找出具有酶抑制作用的活性成分。结果通过体外模型筛选发现有酶抑制活性的咖啡提取物,并找到其活性成分咖啡鞣酸。结论通过体外模型筛选5a-还原酶抑制剂,结合制备液相分离植物提取物组分。

Objective To apply an in vitro model to screen steroid 5a- reductase inhibitors from plant extractions for treatment of androgenic alopecia. Methods The activity of the enzyme was determined by calculating the descending rate of the concentration of substrate testosterone by HPLC. Many kinds of herb extractions were screened by the in vitro model, then the ingredients partitions of the screen out herb extraction were separated by preparation HPLC and the enzyme inhibition activity of each partition was tested. At last the active compound was discovered. Results Coffee extraction and its active compound caffeotannic acid was found out with high enzyme inhibition activity by in vitro model screening. Conclusions Screening 5a- reductase inhibitors by in vitro model, combining with preparation HPLC to separate herb extractions ingredients partitions, is a good way to find new active compound.