中文摘要
黄芪质量评价法尚不完善。我们前期发现黄芪每种成分进入体内均可产生数十种代谢产物,其中一些代谢产物具有生物活性,而其余代谢产物经活性筛选亦有可能被发现具有活性。本项目旨在研究构建黄芪质量评价新模式和新策略。在已有研究基础上,拟对黄芪总黄酮及15种黄酮成分分别进行大鼠体内代谢研究,鉴定代谢产物300种以上;给小型猪灌胃黄芪总黄酮,从含药尿或粪中分离制备代谢产物60种以上。用体内外实验筛选代谢产物中具有心血管活性的显效形式(活性代谢产物)明确各个显效形式都来源于哪些原形成分。用液质仪测定黄芪总黄酮和15种黄酮类成分分别灌胃给药后发挥心血管药效时相应各种显效形式的血药浓度;用体外实验比较各个显效形式药效强弱。在明确显效形式的种类、成分来源、血药浓度和药效贡献的基础上,以有意义的显效形式及其原形成分为基础构建黄芪质量评价新模式。
英文摘要
The quality evalution method of Astragali Radix has not been perfect. In previous research, we found that each constituent of Astragali Radix can produce dozens of metabolites in vivo. We confirmed that some of them have bioactivity and the rest of them may have the bioactivity through bioactivity screening. This research aims to study the establishment of new pattern and new strategy of the quality evalution Astragali Radix. Based on the previous research work, we plan to study the metabolism of total flavonoids and 15 flavonoids constituents respectively in rat in vivo and identify more than 300 kinds of metabolites. And then, we will separate and prepare more than 60 kinds of drug metabolites from urine or feces of minipigs after total flavonoids oral administration. We identify the effective forms (active metabolites) with cardiovascular activity from the metabolites by pharmacological experiments both in vivo and in vitro, and to confirm the original constituents of each effective forms. After oral administration of total flavonoids and 15 flavonoid constituents to animals separately, and we will use LC-QQQ-MS to measure the blood concentration of their effective forms when their cardiovascular effect is exerted. We will compare the intensity of their effect of each effective form in vitro . On the basis of confirming the species number, origins, blood concentration and efficacy contribution of effective forms, we will build the new model to evaluate the quality for Astragali Radix ,which is on the base of the important effective forms and their original constituents.
