Koyama Sachiko, Etkins Jumar, Jun Joshua, Miller Matthew, So Gerald C, Gisch Debora L, Eadon Michael T
Department of Medicine, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
College of Human Ecology, Cornell University, Ithaca, NY 14850, USA.
Int J Mol Sci. 2025 Jan 15;26(2):699. doi: 10.3390/ijms26020699.
Cannabidiol (CBD) is one of the major phytochemical constituents of cannabis, , widely recognized for its therapeutic potential. While cannabis has been utilized for medicinal purposes since ancient times, its psychoactive and addictive properties led to its prohibition in 1937, with only the medical use being reauthorized in 1998. Unlike tetrahydrocannabinol (THC), CBD lacks psychoactive and addictive properties, yet the name that suggests its association with cannabis has significantly contributed to its public visibility. CBD exhibits diverse pharmacological properties, most notably anti-inflammatory effects. Additionally, it interacts with key drug-metabolizing enzyme families, including cytochrome P450 (CYP) and uridine 5'-diphospho-glucuronosyltransferase (UGT), which mediate phase I and phase II metabolism, respectively. By binding to these enzymes, CBD can inhibit the metabolism of co-administered drugs, which can potentially enhance their toxicity or therapeutic effects. Mild to moderate adverse events associated with CBD use have been reported. Advances in chemical formulation techniques have recently enabled strategies to minimize these effects. This review provides an overview of CBD, covering its historical background, recent clinical trials, adverse event profiles, and interactions with molecular targets such as receptors, channels, and enzymes. We particularly emphasize the mechanisms underlying its anti-inflammatory effects and interaction with drugs relevant to organ transplantation. Finally, we explore recent progress in the chemical formulation of CBD in order to enhance its bioavailability, which will enable decreasing the dose to use and increase its safety and efficacy.
大麻二酚（CBD）是大麻的主要植物化学成分之一，因其治疗潜力而广受认可。虽然大麻自古以来就被用于医疗目的，但其精神活性和成瘾性导致其在1937年被禁止，直到1998年才重新授权其医疗用途。与四氢大麻酚（THC）不同，CBD缺乏精神活性和成瘾性，然而，其与大麻相关的名称显著提高了它的公众知名度。CBD具有多种药理特性，最显著的是抗炎作用。此外，它与关键的药物代谢酶家族相互作用，包括细胞色素P450（CYP）和尿苷5'-二磷酸葡萄糖醛酸转移酶（UGT），它们分别介导I相和II相代谢。通过与这些酶结合，CBD可以抑制共同给药药物的代谢，这可能会增强它们的毒性或治疗效果。已经报道了与使用CBD相关的轻度至中度不良事件。最近，化学制剂技术的进步使减少这些影响的策略成为可能。这篇综述概述了CBD，涵盖其历史背景、近期临床试验、不良事件概况以及与受体、通道和酶等分子靶点的相互作用。我们特别强调其抗炎作用的潜在机制以及与器官移植相关药物的相互作用。最后，我们探讨了CBD化学制剂的最新进展，以提高其生物利用度，这将有助于减少使用剂量并提高其安全性和有效性。
