Abstract
Moracin C from Morus alba fruits, also known as the mulberry, has been proven to exhibit inhibitory activities
against lipoxygenase enzymes, TNF-α and interleukin-1β secretion, and proprotein convertase subtilisin/kexin type 9 expression. Despite
the various pharmacological activities of moracin C, its pharmacokinetic characteristics
have yet to be reported. Here, the pharmacokinetic parameters and tissue distribution
of moracin C have been investigated in mice, and the plasma concentration of moracin
C with multiple dosage regimens was simulated via pharmacokinetic modeling. Our results
showed that moracin C was rapidly and well absorbed in the intestinal tract, and was
highly distributed in the gastrointestinal tract, liver, kidneys, and lungs. Moracin
C was distributed in the ileum, cecum, colon, and liver at a relatively high concentration
compared with its plasma concentration. It was extensively metabolized in the liver
and intestine, and its
glucuronidated metabolites were proposed. In addition, the simulated plasma concentrations
of moracin C upon multiple treatments (i.e., every 12 and 24 h) were suggested. We
suggest that the pharmacokinetic characteristics of moracin C would be helpful to
select a disease model for in vivo evaluation. The simulated moracin C concentrations under various dosage regimens
also provide helpful knowledge to support its pharmacological effect.
Key words
moracin C - mulberry -
Morus alba
- Moraceae - pharmacokinetics - tissue distribution - LC-MS/MS - simulation
