Reduced bioavailability of cyclosporine A in rats by mung bean seed coat extract

Abstract

Mung bean seed coat (MBSC) is a healthcare product in Asian countries. The aim of this study was to investigate the effect of an MBSC ethanol extract on the bioavailability of cyclosporine A (CsA) in rats. Rats were orally dosed with CsA alone or in combination with MBSC ethanol extracts (500 mg/kg, p.o.). The blood levels of CsA were assayed by liquid chromatography with an electrospray ionization source and tandem mass spectrometry (LC-MS/MS). The everted rat intestinal sac technique was used to determine the influence of MBSC on the absorption of CsA. The results reveal that combined CsA intake with MBSC decreased the Cmax, AUC0-t, t1/2z and MRT0-t values of CsA by 24.96%, 47.28%, 34.73% and 23.58%, respectively (P<0.05), and significantly raised the CL/F by 51.97% (P<0.01). The in vitro results demonstrated that significantly less CsA was absorbed (P<0.05). The overall results indicate that after being concomitantly ingested, MBSC reduced the bioavailability of CsA, at least partially, in the absorption phase.

Mung bean (Vigna radiata L.) soup decreases tacrolimus blood trough level

“…While, a preliminary study revealed that mung bean seed coat (MBSC) decreased the exposure of CsA by 47% in rats after one-week administration of MBSC extract. 18 It is known that both CYP3A enzymes and P-gp play very important roles in the oral bioavailabilities of CsA and tacrolimus. 1,19 As a result, some medicines, which are identified as inducers or inhibitors of CYP3A enzymes and/or P-gp, may influence serum concentrations of CsA and tacrolimus.…”

“…Thus, it was suspected that the marked change in blood concentration levels of the two CNIs might be due to the influence of mung bean food on the CYP3A enzymes, P-gp or both. [16][17][18] The mung bean is rich in bioactive phytochemicals, including polyphenols, polysaccharides, and peptides, and flavonoids, as a kind of polyphenols, are the most abundant secondary metabolites detected in the seed. 8,23,24 Besides a wide range of health benefits, flavonoid compounds can induce the expression and modulate the metabolic activity of CYPs, and increase P-gp levels in the small intestine.…”