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健康受试者口服蜂王浆后中链脂肪酸的代谢和药代动力学

Metabolism and pharmacokinetics of medium chain fatty acids after oral administration of royal jelly to healthy subjects.

作者信息

Yamaga Masayuki, Tani Hiroko, Yamaki Ayanori, Tatefuji Tomoki, Hashimoto Ken

机构信息

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

出版信息

RSC Adv. 2019 May 17;9(27):15392-15401. doi: 10.1039/c9ra02991e. eCollection 2019 May 14.

Abstract

The unique fatty acids in royal jelly (RJ), 10-hydroxy-2-decenoic acid and 10-hydroxydecanoic acid are expected to be associated with many health benefits, but little is known on the pharmacokinetics and metabolism. The aim of this study is to confirm the metabolism and pharmacokinetics of RJ fatty acids in humans. Twelve volunteers received RJ capsules or enzyme treated RJ (ETRJ) capsules (800 mg). The other group received two doses of ETRJ tablets (800 mg and 1600 mg). Plasma samples were collected up to 12 h after the RJ intake and urine samples were collected within 24 h after ETRJ tablet consumption. The samples were analyzed by LC/MS/MS. A multivariate analysis of the RJ dose plasma samples detected 2-decenedioic acid (2-DA), sebacic acid (SA), and 3-hydroxysebacic acid (3-HSA) with significantly different intensities ( < 0.05) before and after RJ intake. The area under the concentration (AUC) of 2-DA, SA, and 3-HSA was 2500.05 ± 569.58, 322.57 ± 137.36, and 242.98 ± 58.36 ng h mL, respectively. By enzyme treatment, the AUC of 2-DA, SA, and 3-HSA was significantly increased ( < 0.05). The values of AUC and urinary excretion of these metabolites were dose-dependent. The major RJ fatty acids were metabolized to dicarboxylate, absorbed into the circulation and their absorption increased by enzyme treatment. This study provides useful information that will support studies aimed at clarifying the identity of bioactive RJ constituents and their biological effect, and further the development of RJ.

摘要

蜂王浆(RJ)中的独特脂肪酸,10-羟基-2-癸烯酸和10-羟基癸酸有望带来诸多健康益处,但对其药代动力学和代谢情况却知之甚少。本研究旨在确认RJ脂肪酸在人体中的代谢和药代动力学。12名志愿者服用了RJ胶囊或经酶处理的RJ(ETRJ)胶囊(800毫克)。另一组服用了两剂ETRJ片剂(800毫克和1600毫克)。在摄入RJ后长达12小时收集血浆样本,在服用ETRJ片剂后24小时内收集尿液样本。样本通过液相色谱-质谱/质谱联用仪进行分析。对RJ剂量血浆样本进行的多变量分析检测到,在摄入RJ前后,2-癸烯二酸(2-DA)、癸二酸(SA)和3-羟基癸二酸(3-HSA)的强度存在显著差异(<0.05)。2-DA、SA和3-HSA的浓度-时间曲线下面积(AUC)分别为2500.05±569.58、322.57±137.36和242.98±58.36纳克·小时/毫升。经酶处理后,2-DA、SA和3-HSA的AUC显著增加(<0.05)。这些代谢物的AUC值和尿排泄量呈剂量依赖性。主要的RJ脂肪酸被代谢为二羧酸,吸收进入循环系统,并且酶处理可增加其吸收。本研究提供了有用信息,将支持旨在阐明具有生物活性的RJ成分及其生物学效应的研究,进而推动RJ的进一步开发。

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