Abstract
BackgroundOxyresveratrol is a major bioactive component derived from the heartwood of Artocarpus lacucha. This compound exerts several biological activities, including neuroprotective effects in vitro and in vivo. However, there is limited pharmacokinetic information on this compound, especially its distribution in neuronal tissue and its route of excretion. The aim of this study was to investigate the pharmacokinetic profiles of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.MethodsMale Wistar rats were administered with oxyresveratrol 10 mg/kg, oxyresveratrol 10 mg/kg plus piperine 1 mg/kg via intravenous or oxyresveratrol 100 mg/kg, oxyresveratrol 100 mg/kg plus piperine 10 mg/kg via oral gavage. Plasma, internal organs, urine, and feces were collected. Determination of the oxyresveratrol concentration in biological samples was performed by liquid chromatography tandem mass spectrometry.ResultsThe combination with piperine had shown a significantly higher maximum concentration in plasma approximately 1500 μg/L within 1–2 h after oral dosing, and could increase oral bioavailability of oxyresveratrol approximately 2–fold. Oxyresveratrol could widely distributed most of the internal organs with a tissue to plasma ratio of 10–100 fold within 5 min after dosing. Urinary excretion of oxyresveratrol glucuronide was the major route of excretion after administration of oxyresveratrol alone and in combination with piperine.ConclusionThe addition of piperine could enhance some of the pharmacokinetic properties of oxyresveratrol via both intravenous and oral administration. This pharmacokinetic information will be useful for appropriate strategies to develop oxyresveratrol as a phytopharmaceutical product.
Highlights
Oxyresveratrol is a major bioactive component derived from the heartwood of Artocarpus lacucha
In relation to kidney markers, there were no significant changes between pre–dose and post–dose levels for all experimental groups, and all values were within the normal range for healthy rats (Table 1)
In conclusion, the addition of piperine enhanced some of the pharmacokinetic properties of oxyresveratrol via both intravenous and oral administration methods
Summary
Oxyresveratrol is a major bioactive component derived from the heartwood of Artocarpus lacucha. This compound exerts several biological activities, including neuroprotective effects in vitro and in vivo. The aim of this study was to investigate the pharmacokinetic profiles of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats. Artocarpus lacucha Buch.–Ham. has several pharmacological activities, and its major bioactive component is oxyresveratrol (2,4,3′,5′–tetrahydroxystilbene, Fig. 1). This compound can inhibit tyrosinase, the major enzyme involved in melanin production in humans, which can have a skin whitening effect [1,2,3]. The pharmacokinetic information obtained from this study will be useful for appropriate strategies to develop oxyresveratrol as a phytopharmaceutical product
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