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咖啡因及咖啡因衍生化合物在治疗中的前景。

The perspective of caffeine and caffeine derived compounds in therapy.

作者信息

Pohanka M

出版信息

Bratisl Lek Listy. 2015;116(9):520-30. doi: 10.4149/bll_2015_106.

DOI:10.4149/bll_2015_106
PMID:26435014
Abstract

Caffeine (1,3,7-trimethylxanthine) is a plant secondary metabolite with a significant impact on multiple processes and regulatory pathways in the body. Though major part of the population meets caffeine via coffee, tea or chocolate, it has also an important role in pharmacology and it is used as a supplementary substance in medicaments. Currently, the ability of caffeine to ameliorate some neurodegenerative disorders is proved in some studies. This review describes basic data about caffeine including toxicity, pharmacokinetics, biological mechanism of the action, and metabolism. Beside this, promising applications of caffeine, new medicaments and derivatives are discussed. Relevant papers and inventions are depicted in the manuscript. Caffeine is a pharmacologically promising substance that deserves big consideration in the current research and development. The compound has several reasons to be an object of scientific interest and to be used for pharmacology purposes. Despite an extensive research for a long time, no significantly negative effects on human health were proved hence caffeine can be considered as a completely safe compound. The recent data about amelioration of neurodegenerative and other disorders are promising and deserving more work on the issue. ARTICLE HIGHLIGHTS: Caffeine is a purine alkaloid from plants and it has a broad use in current pharmacology. Caffeine is a competitive antagonist of neurotransmitter adenosine on adenosine receptors. The substance is added as a supplementary to drugs and food.Besides interfering on adenosine receptors, caffeine interacts with acetylcholinesterase, monoamine oxidase, phosphodiesterase, ryanodine receptors and others.Current research is devoted to the role of caffeine in neurodegenerative diseases and immunity alteration. New chemical compounds based on caffeine moiety are prepared (Tab. 4, Fig. 6, Ref. 149).

摘要

咖啡因(1,3,7 - 三甲基黄嘌呤)是一种植物次生代谢产物,对人体的多种生理过程和调节途径有显著影响。虽然大多数人通过咖啡、茶或巧克力摄入咖啡因,但它在药理学中也具有重要作用,并且被用作药物中的辅助物质。目前,一些研究已证实咖啡因具有改善某些神经退行性疾病的能力。本综述描述了关于咖啡因的基础数据,包括毒性、药代动力学、作用的生物学机制和代谢。除此之外,还讨论了咖啡因、新药物及衍生物的潜在应用。手稿中描述了相关的论文和发明。咖啡因是一种在药理学上颇具潜力的物质,值得在当前的研发中给予充分考虑。该化合物有多个理由成为科学研究的对象并用于药理学目的。尽管经过了长期广泛的研究,但尚未证明其对人体健康有明显的负面影响,因此咖啡因可被视为一种完全安全的化合物。关于改善神经退行性疾病和其他疾病的最新数据很有前景,值得对该问题进行更多研究。文章亮点:咖啡因是一种来自植物的嘌呤生物碱,在当前药理学中有广泛应用。咖啡因是神经递质腺苷在腺苷受体上的竞争性拮抗剂。该物质被添加到药物和食品中作为补充剂。除了作用于腺苷受体外,咖啡因还与乙酰胆碱酯酶、单胺氧化酶、磷酸二酯酶、兰尼碱受体等相互作用。当前的研究致力于咖啡因在神经退行性疾病和免疫改变中的作用。基于咖啡因部分制备了新的化合物(表4、图6、参考文献149)。

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