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The fallacy of enzymatic hydrolysis for the determination of bioactive curcumin in plasma samples as an indication of bioavailability: a comparative study.
BMC Complementary and Alternative Medicine ( IF 4.782 ) Pub Date : 2019-11-04 , DOI: 10.1186/s12906-019-2699-x
Sidney J Stohs 1 , C Y O Chen 2 , Harry G Preuss 3 , Sidhartha D Ray 4 , Luke R Bucci 5 , Jin Ji 6 , Kevin J Ruff 7
Affiliation  

BACKGROUND Numerous health benefits have been demonstrated for curcumin which is extracted from turmeric (Curcuma longa L). However, due to its poor absorption in the free form in the gastrointestinal tract and rapid biotransformation, various formulations have been developed to enhance its bioavailability. Previous studies indicate that the free form of curcumin is more bioactive than its conjugated counterparts in target tissues. Most curcumin pharmacokinetics studies in humans designed to assess its absorption and bioavailability have measured and reported total (free plus conjugated) curcumin, but not free, bioactive curcumin in the plasma because enzymatic hydrolysis was employed prior to its extraction and analysis. Therefore, the bioavailability of free curcumin cannot be determined. METHODS Eight human subjects (4 male, 4 female) consumed a single dose of 400 mg curcumin in an enhanced absorption formulation, and blood samples were collected over 6 h. Plasma was treated either with or without glucuronidase/sulfatase prior to extraction. Curcumin and its major metabolites were analyzed using HPLC-tandem mass spectrometry. In addition, the literature was searched for pharmacokinetic studies involving curcumin using PubMed and Google Scholar, and the reported bioavailability data were compared based on whether hydrolysis of plasma samples was used prior to sample analysis. RESULTS Hydrolysis of blood plasma samples prior to extraction and reporting the results as "curcumin" obscures the amount of free, bioactive curcumin and total curcuminoids as compared to non-hydrolyzed samples. As a consequence, the data and biological effects reported by most pharmacokinetic studies are not a clear indication of enhanced plasma levels of free bioactive curcumin due to product formulations, leading to a misrepresentation of the results of the studies and the products when enzymatic hydrolysis is employed. CONCLUSIONS When enzymatic hydrolysis is employed as is the case with most studies involving curcumin products, the amount of free bioactive curcumin is unknown and cannot be determined. Therefore, extreme caution is warranted in interpreting published analytical results from biological samples involving ingestion of curcumin-containing products. TRIAL REGISTRATION ClinicalTrails.gov, trial identifying number NCT04103788 , September 24, 2019. Retrospectively registered.

中文翻译:

酶水解测定血浆样品中生物活性姜黄素作为生物利用度指标的谬误:一项比较研究。

背景技术从姜黄(Curcuma longa L)中提取的姜黄素已被证明具有多种健康益处。然而,由于其游离形式在胃肠道中吸收差且生物转化快,因此已开发出多种制剂来提高其生物利用度。先前的研究表明,在靶组织中,游离形式的姜黄素比其结合形式的姜黄素更具生物活性。大多数旨在评估其吸收和生物利用度的人体姜黄素药代动力学研究测量并报告了血浆中的总姜黄素(游离加结合),但不是游离的生物活性姜黄素,因为在提取和分析之前采用了酶水解。因此,无法确定游离姜黄素的生物利用度。方法 8 名人类受试者(4 名男性,4 名女性)服用单剂量的 400 毫克姜黄素增强吸收制剂,并在 6 小时内收集血液样本。提取前用或不用葡萄糖醛酸酶/硫酸酯酶处理血浆。使用 HPLC-串联质谱法分析姜黄素及其主要代谢物。此外,使用PubMed和Google Scholar检索涉及姜黄素的药代动力学研究文献,并根据样品分析前是否使用血浆样品水解来比较报道的生物利用度数据。结果 与未水解的样品相比,在提取之前对血浆样品进行水解并将结果报告为“姜黄素”,从而掩盖了游离的生物活性姜黄素和总姜黄素的含量。因此,大多数药代动力学研究报告的数据和生物效应并不能明确表明产品配方导致游离生物活性姜黄素的血浆水平升高,从而导致在采用酶水解时研究结果和产品的误传。结论 当像大多数涉及姜黄素产品的研究那样采用酶水解时,游离生物活性姜黄素的量是未知的并且无法确定。因此,在解释已发表的涉及摄入含姜黄素产品的生物样品的分析结果时,需要极其谨慎。试验注册 ClinicalTrails.gov,试验识别号 NCT04103788,2019 年 9 月 24 日。回顾性注册。
更新日期:2019-11-04
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