Citrus aurantium (bitter orange) extracts have been used in products for weight management and sports performance. These extracts contain large amounts of p-synephrine and much smaller amounts of p-octopamine. Both protoalkaloids exert lipolytic and glycogenolytic activities at similar concentrations. The biotransformation of p-synephrine and p-octopamine is not as well-known as those of other adrenergic amines. For this reason transformation of these amines was investigated in the isolated perfused liver. Special attention was devoted to the single pass extraction of each compound as well as to the kinetics of uptake. The assay of the amines in the outflowing perfusate was done by means of high performance liquid chromatography (HPLC). The single pass extraction of p-synephrine was higher than 90% at a portal concentration of 10 μM. It declined with the concentration, but was still around 30% at the concentration of 500 μM. At low concentrations (10-50 μM) the decreasing sequence of single pass extractions was p-synephrine > p-octopamine ≈ epinephrine > norepinephrine. Rates of uptake versus p-synephrine concentration resulted in a Michaelis-Menten type of relationship, with a KM value of 290.7 ± 32.1 μM and a Vmax of 0.762 ± 0.042 μmol min(-1) g(-1). The rates of uptake of p-octopamine did not present clear saturation and could be approximated by a linear relationship with a first order rate constant of 1.5 min(-1). The rapid hepatic transformation of p-synephrine and p-octopamine means that their concentration in the portal vein exceeds that in the systemic circulation during absorption. Their metabolic effects will, thus, be exerted predominantly in the liver.
Abstractp-synephrine and p-octopamine were found to increase lipolysis in adipocytes. The present study approaches the question if these compounds, natural products of the bitter orange (Citrus aurantium fruit), increase lipolysis and fatty acid oxidation in the liver. Experiments were done in the perfused rat liver. Non-recirculating hemoglobin-free perfusion was done using the Krebs/ Henseleit-bicarbonate buffer (pH 7.4) as perfusion fluid. Both p-synephrine and p-octopamine, at the concentrations of 100 µM, were found to stimulate the hepatic triacylglycerol lipase by 40% and 51%, respectively. These seem to be the maximal stimulations possible in the liver. In the perfused liver, p-synephrine, when present at an initial concentration of 500 µM, was able to increase the non-esterified fatty acid release after one hour of recirculating perfusion. The effects of p-synephrine on the oxidation of exogenously sup-
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.