Study on the metabolism profile of flavanomarein in Coreopsis tinctoria Nutt

Coreopsis tinctoria Nutt. (family Asteraceae) is a popular medicine-food plant, which improves chronic diseases such as hyperlipemia, hypertension, and diabetes. Flavanomarein is the main active component of Coreopsis tinctoria Nutt, in which the blood concentration of volunteers is low and bioavailability is poor. Thus, the understanding of flavanomarein metabolites and metabolic pathways is significant to clarify its effectiveness. This study systematically studied the metabolites of flavanomarein by oral and injection. The biological samples (feces, urine, and plasma) were analyzed by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry in negative ion mode. The metabolic law of flavanomarein in the liver was further verified by a liver microsomal incubation experiment in vitro. A total of 12 metabolites were identified by oral administration while 15 metabolites were detected by injection. It was shown that metabolic pathways include acetylation, hydroxylation, glucuronidation, methylation, dehydrogenation, and so forth. The liver extraction rate of flavanomarein was 0.08, which means the metabolic stability of flavanomarein is well in rats' liver microsomes. It is a systematic study on the metabolism of flavanomarein and provides a metabolic rationale for further in-depth in vivo biotransformation.