Studies On In Vivo And In Vitro Metabolism And Pharmacokinetics Of 1, 5-Dicaffeoylquinic Acid

Dicaffeoylquinic acids (DCQAs) are plant-derived compounds isolated from a variety of sources and which possess a broad spectrum of pharmacological properties, including antioxidant, antibacterial, antihistaminic, hepatoprotectant, and other biological effects. In the past 10 years, DCQAs have drawn more and more attention for their anti-HIV (human immunodeficiency virus) activity. However, by far most of the investigations are limited in their pharmacological effects and plant extraction methods, little is known regarding their metabolism and pharmacokinetics. 1,5-Dicaffeoylquinic acid (1,5-DCQA) will be applied for clinical investigation for new drug, which has been successfully synthesized by our country for the first time. In order to early look insight into its metabolic and pharmacokinetic properties to help to forecast its clinical application value, to direct the dosage regimen designation, to edify the structure and dose type, the present dissertation studied the metabolism and pharmacokinetics of 1,5-DCQA by using several advanced methods for the first time.1. The in vivo and in vitro metabolism of 1,5-DCQA by LC/MS~n analysisThe present study characterized the metabolic profile of 1,5-DCQA in vivo and in vitro by using liquid chromatography-mass spectrometry (LC/MS) in parallel to DAD (diode-array detection). A total of 22 metabolites were identified, including methylated,...