Metabolic Regularity of Bioactive Compounds in Epimedium in Rats Based on LC-MS Analysis Technology

Abstract

Background and Objective: Epimedium is an important traditional medicinal and edible plant in China. It is not only used as medicine but is often developed into health care products or functional food for long-term use. However, adverse reaction associated with its longterm use includes thirst or nosebleed. This study aimed to reveal the metabolic regularity of bioactive compounds in Epimedium, so as to explore the causes of its adverse reactions. Materials and Methods: In the current UPLC-QTOF-MS technique was adopted for qualitatively identifying the prototype components of Epimedium in the blood after multiple oral administrations in rats. Thereafter, a method for the simultaneous determination of eight components containing p-hydroxycinnamic acid, salidroside, brevicornin, lauric acid, liquiritigenin, sagittatosdie B, icariside I and icariside II in rat plasma was established by UPLC-QQQ-MS technology. Thereafter, this method was successfully used in the pharmacokinetic study of the eight analytes in rats after multiple oral administrations of Epimedium.Results: Totally 22 prototype components were determined in rat plasma, of which 16 were flavonoids and a small number of acids, phenols and triterpenes were also detected. The pharmacokinetic parameters of eight components were obtained, as a result, compared with a single administration, multiple administration induced the slow metabolic rate, prolonged Tmax, increased bioavailability and prolonged transformation time of chemical ingredient monomers. Conclusion: The relative increases of these ingredients in the whole body may be the reason for adverse reactions after long-term administration of Epimedium.