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口服嘉兰种子提取物粉末后白藜芦醇衍生物在人体内的药代动力学和安全性。

Pharmacokinetics and safety of resveratrol derivatives in humans after oral administration of melinjo (Gnetum gnemon L.) seed extract powder.

机构信息

Institute for Bee Products and Health Science, Yamada Bee Company, Inc. , 194 Ichiba, Kagamino-cho, Tomata-gun 708-0393, Japan.

出版信息

J Agric Food Chem. 2014 Feb 26;62(8):1999-2007. doi: 10.1021/jf4048435. Epub 2014 Feb 12.

DOI:10.1021/jf4048435
PMID:24495149
Abstract

Fruits and seeds of melinjo (Gnetum gnemon L.) are resveratrol derivative-rich materials. Pharmacokinetics of resveratrol derivatives in healthy volunteers after oral administration of 1000 mg of melinjo seed extract (MSE) powder were assessed and compared with those after oral dosing of trans-resveratrol (tRV) powder containing 4.8 mg of tRV only, equivalent to the content in 1000 mg MSE powder. Plasma tRV concentrations with enzymatic hydrolysis were maintained over 24 h, with a tmax of 12 h and a mean residence time (MRT) of 14 h, 5 and 2 times higher than those for tRV powder intake, respectively. Gnetin C, a resveratrol dimer, with hydrolysis was maintained in plasma for >96 h with a 36 h MRT. With repeated doses once daily for 28 days, plasma tRV and gnetin C concentrations with hydrolysis were in good agreement with the theoretical curves. MSE powder was well tolerated up to the oral dosing of 5000 mg with no serious adverse events.

摘要

麻枥果的果实和种子是白藜芦醇衍生物含量丰富的物质。在健康志愿者中,评估了口服 1000 毫克麻枥果种仁提取物(MSE)粉末后,白藜芦醇衍生物的药代动力学,并与仅含 4.8 毫克反式白藜芦醇(tRV)的 tRV 粉末口服剂量进行了比较,相当于 1000 毫克 MSE 粉末中的含量。经酶水解后,血浆中 tRV 浓度可维持 24 小时,tmax 为 12 小时,平均驻留时间(MRT)分别为 tRV 粉末摄入的 5 倍和 2 倍。麻枥果二聚体白藜芦醇苷经水解后,在血浆中维持时间超过 96 小时,MRT 为 36 小时。每日重复一次口服 28 天,水解后的血浆 tRV 和 gnetin C 浓度与理论曲线吻合良好。MSE 粉末的口服剂量高达 5000 毫克时,耐受性良好,无严重不良事件。

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