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姜黄素作为一种具有临床应用前景的抗癌药物:药代动力学与药物相互作用。

Curcumin as a clinically-promising anti-cancer agent: pharmacokinetics and drug interactions.

作者信息

Adiwidjaja Jeffry, McLachlan Andrew J, Boddy Alan V

机构信息

a Faculty of Pharmacy , The University of Sydney , Sydney , Australia.

b Centre for Education and Research on Ageing , Concord Repatriation General Hospital , Concord , Australia.

出版信息

Expert Opin Drug Metab Toxicol. 2017 Sep;13(9):953-972. doi: 10.1080/17425255.2017.1360279. Epub 2017 Aug 10.

DOI:10.1080/17425255.2017.1360279
PMID:28776444
Abstract

Curcumin has been extensively studied for its anti-cancer properties. While a diverse array of in vitro and preclinical research support the prospect of curcumin use as an anti-cancer therapeutic, most human studies have failed to meet the intended clinical expectation. Poor systemic availability of orally-administered curcumin may account for this disparity. Areas covered: This descriptive review aims to concisely summarise available clinical studies investigating curcumin pharmacokinetics when administered in different formulations. A critical analysis of pharmacokinetic- and pharmacodynamic-based interactions of curcumin with concomitantly administered drugs is also provided. Expert opinion: The encouraging clinical results of curcumin administration are currently limited to people with colorectal cancer, given that sufficient curcumin concentrations persist in colonic mucosa. Higher parent curcumin systemic exposure, which can be achieved by several newer formulations, has important implications for optimal treatment of cancers other than those in gastrointestinal tract. Curcumin-drug pharmacokinetic interactions are also almost exclusively in the enterocytes, owing to extensive first pass metabolism and poor curcumin bioavailability. Greater scope of these interactions, i.e. modulation of the systemic elimination of co-administered drugs, may be expected from more-bioavailable curcumin formulations. Further studies are still warranted, especially with newer formulations to support the inclusion of curcumin in cancer therapy regimens.

摘要

姜黄素因其抗癌特性已得到广泛研究。尽管大量的体外和临床前研究支持将姜黄素用作抗癌治疗药物的前景,但大多数人体研究未能达到预期的临床效果。口服姜黄素的全身利用率低可能是造成这种差异的原因。涵盖领域:本描述性综述旨在简要总结研究不同剂型姜黄素药代动力学的现有临床研究。还对姜黄素与同时给药药物基于药代动力学和药效学的相互作用进行了批判性分析。专家意见:鉴于结肠黏膜中姜黄素浓度持续存在,目前姜黄素给药令人鼓舞的临床结果仅限于结直肠癌患者。通过几种新剂型可实现更高的母体姜黄素全身暴露,这对于胃肠道以外癌症的最佳治疗具有重要意义。由于广泛的首过代谢和姜黄素生物利用度低,姜黄素与药物的药代动力学相互作用几乎完全发生在肠细胞中。从生物利用度更高的姜黄素制剂中,可能会预期到这些相互作用的更大范围,即对同时给药药物全身消除的调节。仍有必要进行进一步研究,特别是使用新剂型来支持将姜黄素纳入癌症治疗方案。

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