ABSTRACT
Supplement-drug interaction on CYP enzyme activity is occasionally found to cause clinically adverse events, and no report on interactions of propolis is available either in vitro or clinical. In this study, we tried to estimate the risk of an interaction between an ethanol extract of Brazilian green propolis (EEP-B55) and drugs in vitro and in vivo. The activities of CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 were attenuated by EEP-B55 in a concentration-dependent manner, and artepillin C, kaempferide, dihydrokaempferide, isosakuranetin, and kaempferol were estimated to have potential for CYP inhibition. The IC50 values of artepillin C for each CYP were approximately 33-fold higher than its Cmax in the blood of rats after dosing with 5-fold the recommended daily intake of EEP-B55. These findings suggest that liver CYP enzyme activities are not markedly affected by artepillin C at the recommended daily intake of EEP-B55.
Subject(s)
Cytochrome P-450 Enzyme Inhibitors/chemistry , Cytochrome P-450 Enzyme System/chemistry , Food-Drug Interactions , Propolis/chemistry , Animals , Brazil , Cytochrome P-450 Enzyme Inhibitors/metabolism , Cytochrome P-450 Enzyme System/metabolism , Humans , Kinetics , Male , Propolis/metabolism , Rats , Rats, WistarABSTRACT
Buckwheat (Fagopyrum esculentum) is rich in antihypertensive compounds. This study investigated the effect of lactic-fermented buckwheat sprouts (neo-FBS) on level, identification, and potency of blood pressure-lowering (BPL) compounds. A single oral dose of 1.0 mg/kg body weight buckwheat sprouts (BS) in spontaneously hypertensive rats did not show significant BPL activity, whereas neo-FBS significantly decreased blood pressure. HPLC of neo-FBS identified two peaks absent in the profile of BS. The peak exhibiting potent BPL activity was fractionated, and six peptides (DVWY, FDART, FQ, VAE, VVG, and WTFR) and tyrosine were identified by LC-MS/MS and Edman degradation. Single oral dose administration of the peptides revealed significant BPL effect of all the peptides, with the most potent being DVWY, FQ, and VVG. DVWY, VAE, and WTFR are novel. This study demonstrates that lactic fermentation of BS produces new, highly potent antihypertensive peptides and increases active compounds GABA and tyrosine already present in BS.
