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高生物利用度的姜黄素形式及基于姜黄素的研究与应用的有前景途径:综述。

Highly Bioavailable Forms of Curcumin and Promising Avenues for Curcumin-Based Research and Application: A Review.

机构信息

School of Pharmacy and Health Professions, Creighton University Medical Center, Omaha, NE 68178, USA.

Biofortis Research, Addison, IL 60101, USA.

出版信息

Molecules. 2020 Mar 19;25(6):1397. doi: 10.3390/molecules25061397.

Abstract

Curcumin exerts a wide range of beneficial physiological and pharmacological activities, including antioxidant, anti-amyloid, anti-inflammatory, anti-microbial, anti-neoplastic, immune-modulating, metabolism regulating, anti-depressant, neuroprotective and tissue protective effects. However, its poor solubility and poor absorption in the free form in the gastrointestinal tract and its rapid biotransformation to inactive metabolites greatly limit its utility as a health-promoting agent and dietary supplement. Recent advances in micro- and nano-formulations of curcumin with greatly enhanced absorption resulting in desirable blood levels of the active forms of curcumin now make it possible to address a wide range of potential applications, including pain management, and as tissue protective. Using these forms of highly bioavailable curcumin now enable a broad spectrum of appropriate studies to be conducted. This review discusses the formulations designed to enhance bioavailability, metabolism of curcumin, relationships between solubility and particle size relative to bioavailability, human pharmacokinetic studies involving formulated curcumin products, the widely used but inappropriate practice of hydrolyzing plasma samples for quantification of blood curcumin, current applications of curcumin and its metabolites and promising directions for health maintenance and applications.

摘要

姜黄素具有广泛的有益的生理和药理活性,包括抗氧化、抗淀粉样蛋白、抗炎、抗菌、抗肿瘤、免疫调节、代谢调节、抗抑郁、神经保护和组织保护作用。然而,其在胃肠道中游离形式的溶解度差和吸收不良,以及其快速生物转化为无活性代谢物,极大地限制了它作为促进健康的药物和膳食补充剂的应用。最近,姜黄素的微纳米制剂的进展极大地提高了吸收度,从而使姜黄素的活性形式达到了理想的血液水平,现在使得解决广泛的潜在应用成为可能,包括疼痛管理和组织保护。使用这些高生物利用度的姜黄素形式,现在可以进行广泛的适当研究。本文综述了旨在提高生物利用度、姜黄素代谢的制剂,讨论了溶解度和粒径与生物利用度的关系,涉及姜黄素制剂产品的人体药代动力学研究,广泛使用但不适当的水解血浆样品进行血姜黄素定量的方法,姜黄素及其代谢物的当前应用,以及健康维护和应用的有希望的方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f171/7144558/b2716b71223c/molecules-25-01397-g001.jpg

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