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缬草型、次要型和酸性植物大麻素的药理潜力。

Pharmacological potential of varinic-, minor-, and acidic phytocannabinoids.

作者信息

Franco Rafael, Rivas-Santisteban Rafael, Reyes-Resina Irene, Casanovas Mireia, Pérez-Olives Catalina, Ferreiro-Vera Carlos, Navarro Gemma, Sánchez de Medina Verónica, Nadal Xavier

机构信息

Department of Biochemistry and Molecular Biomedicine, Universitat de Barcelona, Spain; Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas (CiberNed), Spain.

Department of Biochemistry and Molecular Biomedicine, Universitat de Barcelona, Spain; Centro de Investigación Biomédica en Red sobre Enfermedades Neurodegenerativas (CiberNed), Spain.

出版信息

Pharmacol Res. 2020 May 13;158:104801. doi: 10.1016/j.phrs.2020.104801.

Abstract

While natural Δ-tetrahidrocannabinol (ΔTHC), cannabidiol (CBD), and their therapeutic potential have been extensively researched, some cannabinoids have been less extensively investigated. The present article compiles data from the literature that highlight the health benefits and therapeutic potential of lesser known phytocannabinoids, which we have divided into varinic, acidic, and "minor" (i.e., cannabinoids that are not present in high quantities in common varieties of Cannabis sativa L). A growing interest in these compounds, which are enriched in some cannabis varieties, has already resulted in enough preclinical information to show that they are promising therapeutic agents for a variety of diseases. Every phytocannabinoid has a "preferential" mechanism of action, and often targets the cannabinoid receptors, CB and/or CB. The recent resolution of the structure of cannabinoid receptors demonstrates the atypical nature of cannabinoid binding, and that different binding modes depend on the agonist or partial agonist/inverse agonist, which allows for differential signaling, even acting on the same cannabinoid receptor. In addition, other players and multiple signaling pathways may be targeted/engaged by phytocannabinoids, thereby expanding the mechanistic possibilities for therapeutic use.

摘要

虽然天然的Δ-四氢大麻酚(ΔTHC)、大麻二酚(CBD)及其治疗潜力已得到广泛研究,但一些大麻素的研究尚不充分。本文汇编了文献中的数据,这些数据突出了鲜为人知的植物大麻素的健康益处和治疗潜力,我们将其分为戊酸类、酸性类和“次要”类(即普通大麻品种中含量不高的大麻素)。对这些在某些大麻品种中含量丰富的化合物的兴趣日益浓厚,已经产生了足够的临床前信息,表明它们是治疗多种疾病的有前景的治疗剂。每种植物大麻素都有“优先”作用机制,且通常靶向大麻素受体CB1和/或CB2。大麻素受体结构的最新解析揭示了大麻素结合的非典型性质,不同的结合模式取决于激动剂或部分激动剂/反向激动剂,这使得即使作用于同一大麻素受体也能产生不同的信号传导。此外,植物大麻素可能靶向/参与其他作用因子和多种信号通路,从而扩大了治疗用途的作用机制可能性。

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