Polymethoxylated flavones (PMF) are associated with biological effects on human health including cardiovascular protection and improved endothelial function. This current study examined whether the mammalian metabolites of these compounds were also able to interact with human cells and exert potentially beneficial effects. Seven metabolites of the main PMFs were isolated and structurally characterized, including metabolites labeled: TAG-G, TAN-OH, SIN-G, SIN-OH, NOB-G, NOB-OH and HMF-OH.  With confocal microscopy cells treated with PMFs and PMF metabolites showed higher natural fluorescence emission compared to untreated control cells and demonstrated complex binding interactions between these compounds and human cells. To examine biological activity, the PMFs and PMF metabolites were incubated 24h with Huh7.5 cells at 5, 10, 25 and 50µM. Microsomal triglyceride transfer protein (MTP) activity and apolipoprotein B (ApoB) secretion were evaluated. TAN and HMF were able to reduce ApoB secretion at all concentrations, as well as TAN-OH at 5 and 25µM. NOB-OH at 5µM showed the lower ApoB secretion compared to other doses of NOB or NOB metabolites. Among the different doses, SIN-OH at 5 and 10µM, and HMF at 10 and 50µM were also able to reduce ApoB secretion, but had no effect on MTP activity. From this study, PMFs and their metabolites are shown to incorporate into Huh7.5 cells, and reduce ApoB liver secretion and in some cases MTP activity.

Isolation and identification of polymethoxylated flavones metabolites in rat urine and its evaluation on hepatic lipoprotein secretion

2019 Spring National Meeting

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.