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kratom生物碱:与酶、受体和细胞屏障的相互作用。

Kratom Alkaloids: Interactions With Enzymes, Receptors, and Cellular Barriers.

作者信息

Hanapi Nur Aziah, Chear Nelson Jeng-Yeou, Azizi Juzaili, Yusof Siti R

机构信息

Centre for Drug Research, Universiti Sains Malaysia, Minden, Malaysia.

出版信息

Front Pharmacol. 2021 Nov 17;12:751656. doi: 10.3389/fphar.2021.751656. eCollection 2021.

Abstract

Parallel to the growing use of kratom, there is a wealth of evidence from self-report, preclinical, and early clinical studies on therapeutic benefits of its alkaloids in particular for treating pain, managing substance use disorder, and coping with emotional or mental health conditions. On the other hand, there are also reports on potential health risks concerning kratom use. These two aspects are often discussed in reviews on kratom. Here, we aim to highlight specific areas that are of importance to give insights into the mechanistic of kratom alkaloids pharmacological actions. This includes their interactions with drug-metabolizing enzymes and predictions of clinical drug-drug interactions, receptor-binding properties, interactions with cellular barriers in regards to barrier permeability, involvement of membrane transporters, and alteration of barrier function when exposed to the alkaloids.

摘要

与 kratom 使用的日益增加并行的是,来自自我报告、临床前和早期临床研究的大量证据表明,其生物碱具有治疗益处,特别是在治疗疼痛、管理物质使用障碍以及应对情绪或心理健康状况方面。另一方面,也有关于使用 kratom 的潜在健康风险的报告。这两个方面在关于 kratom 的综述中经常被讨论。在这里,我们旨在突出特定的重要领域,以深入了解 kratom 生物碱药理作用的机制。这包括它们与药物代谢酶的相互作用以及临床药物 - 药物相互作用的预测、受体结合特性、与细胞屏障在屏障通透性方面的相互作用、膜转运蛋白的参与以及暴露于生物碱时屏障功能的改变。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ed5f/8637859/f740cb5531ce/fphar-12-751656-g001.jpg

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