Song Xinjie, Kirtipal Nikhil, Lee Sunjae, Malý Petr, Bharadwaj Shiv
Zhejiang Provincial Key Lab for Chemical and Biological Processing Technology of Farm Product, School of Biological and Chemical Engineering, Zhejiang University of Science and Technology, Hangzhou, China.
School of Life Sciences, Gwangju Institute of Science and Technology (GIST), Gwangju, Republic of Korea.
Phytother Res. 2023 Dec;37(12):5558-5598. doi: 10.1002/ptr.8000. Epub 2023 Sep 7.
Caffeine, which shares consubstantial structural similarity with purine adenosine, has been demonstrated as a nonselective adenosine receptor antagonist for eliciting most of the biological functions at physiologically relevant dosages. Accumulating evidence supports caffeine's beneficial effects against different disorders, such as total cardiovascular diseases and type 2 diabetes. Conversely, paradoxical effects are also linked to caffeine ingestion in humans including hypertension-hypotension and tachycardia-bradycardia. These observations suggest the association of caffeine action with its ingested concentration and/or concurrent interaction with preferential molecular targets to direct explicit events in the human body. Thus, a coherent analysis of the functional targets of caffeine, relevant to normal physiology, and disease pathophysiology, is required to understand the pharmacology of caffeine. This review provides a broad overview of the experimentally validated targets of caffeine, particularly those of therapeutic interest, and the impacts of caffeine on organ-specific physiology and pathophysiology. Overall, the available empirical and epidemiological evidence supports the dose-dependent functional activities of caffeine and advocates for further studies to get insights into the caffeine-induced changes under specific conditions, such as asthma, DNA repair, and cancer, in view of its therapeutic applications.
咖啡因与嘌呤腺苷在结构上有本质的相似性,已被证明是一种非选择性腺苷受体拮抗剂,在生理相关剂量下能引发大多数生物学功能。越来越多的证据支持咖啡因对不同疾病具有有益作用,如对所有心血管疾病和2型糖尿病。相反,矛盾的效应也与人类摄入咖啡因有关,包括高血压 - 低血压和心动过速 - 心动过缓。这些观察结果表明咖啡因的作用与其摄入浓度和/或与优先分子靶点的同时相互作用有关,从而在人体中引发明确的事件。因此,需要对咖啡因与正常生理学和疾病病理生理学相关的功能靶点进行连贯分析,以了解咖啡因的药理学。本综述广泛概述了经实验验证的咖啡因靶点,特别是那些具有治疗意义的靶点,以及咖啡因对器官特异性生理学和病理生理学的影响。总体而言,现有的实证和流行病学证据支持咖啡因的剂量依赖性功能活动,并主张进一步研究,以便鉴于其治疗应用,深入了解在特定条件下(如哮喘、DNA修复和癌症)咖啡因引起的变化。