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荒漠沙鼠中 20-羟基蜕皮甾酮的生物利用度和药代动力学:用于代谢综合征研究的沙鼠模型。

20-Hydroxyecdysone bioavailability and pharmacokinetics in Gerbillus tarabuli, a gerbil model for metabolic syndrome studies.

机构信息

LBPO/Nutrition & Metabolism, Department of Biology and Physiology of Organisms, Faculty of Biological Sciences, University of Sciences and Technology Houari Boumediene (USTHB), BP 32, El Alia, Bab Ezzouar 16111, Algiers, Algeria.

LBPO/Nutrition & Metabolism, Department of Biology and Physiology of Organisms, Faculty of Biological Sciences, University of Sciences and Technology Houari Boumediene (USTHB), BP 32, El Alia, Bab Ezzouar 16111, Algiers, Algeria.

出版信息

Steroids. 2023 Oct;198:109262. doi: 10.1016/j.steroids.2023.109262. Epub 2023 Jun 23.

DOI:10.1016/j.steroids.2023.109262
PMID:37355000
Abstract

Phytoecdysteroids are active natural compounds that have demonstrated many beneficial pharmacological effects on mammals, including Humans. 20-Hydroxyecdysone (20E) is the major phytoecdysteroid present in plants, and gerbils are particularly good responders to the addition of 20E to their diet. We have examined the oral bioavailability of 20E in the desert gerbil, Gerbillus tarabuli. 20E (5 and 50 mg.kg body weight) was administered to gerbils by intra-peritoneal injection and oral gavage, respectively. Plasma samples were collected over 8 h and analyzed by HPLC-MS/MS to determine the 20E concentrations. The calculated oral bioavailability of 20E is approx. 12%, with a half-life of 30.6 and 33 min after per os administration or intra-peritoneal injection, respectively. This bioavailabilitty is much higher than that observed in laboratory rodents (ca. 1%). It is proposed that this unexpectedly high oral bioavailability of 20E in gerbils contributes to its high efficacy in this animal.

摘要

植物甾醇是具有多种有益的哺乳动物(包括人类)药理作用的活性天然化合物。20-羟基蜕皮甾酮(20E)是植物中主要的植物甾醇,沙鼠对 20E 加入饮食中特别有反应。我们已经研究了沙漠沙鼠(Gerbillus tarabuli)中 20E 的口服生物利用度。通过腹腔内注射和口服灌胃分别给予沙鼠 20E(5 和 50 mg.kg 体重)。采集 8 小时的血浆样本,并通过 HPLC-MS/MS 分析以确定 20E 浓度。口服给予或腹腔内注射后,20E 的计算口服生物利用度分别约为 12%,半衰期分别为 30.6 和 33 分钟。与实验室啮齿动物(约 1%)相比,这种生物利用度要高得多。据推测,沙鼠中 20E 的这种出乎意料的高口服生物利用度有助于其在该动物中的高疗效。

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