Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats

BMC Complementary and Alternative Medicine

Phisit Khemawoot¹  Kittisak Likhitwitayawuid²  Boonchoo Sritularak²  Dhirarin Junsaeng³  Tosapol Anukunwithaya³  Phanit Songvut³ 

[1]Department of Biochemistry and Microbiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University

[2]Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University

[3]Department of Pharmacology and Physiology, Faculty of Pharmaceutical Sciences, Chulalongkorn University

关键词: Artocarpus lacucha;    Moraceae;    Oxyresveratrol;    Piperine;    Bioenhancer;    Pharmacokinetics;   

DOI  :  10.1186/s12906-019-2653-y

来源: DOAJ

【 摘 要 】

Abstract Background 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. 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. Methods Male 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. Results The 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. Conclusion The 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.

【 授权许可】

Unknown