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大麻二酚及其合成衍生物的药理学特性与生物学效应

Pharmacological Aspects and Biological Effects of Cannabigerol and Its Synthetic Derivatives.

作者信息

Calapai Fabrizio, Cardia Luigi, Esposito Emanuela, Ammendolia Ilaria, Mondello Cristina, Lo Giudice Roberto, Gangemi Sebastiano, Calapai Gioacchino, Mannucci Carmen

机构信息

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina 98168, Italy.

Department of Human Pathology in Adulthood and Childhood "G. Barresi", University Hospital "G. Martino" of Messina, Via Consolare Valeria 1, Messina 98123, Italy.

出版信息

Evid Based Complement Alternat Med. 2022 Nov 8;2022:3336516. doi: 10.1155/2022/3336516. eCollection 2022.

Abstract

Cannabigerol (CBG) is a cannabinoid from the plant that lacks psychotomimetic effects. Its precursor is the acidic form, cannabigerolic acid (CBGA), which is, in turn, a biosynthetic precursor of the compounds cannabidiol (CBD) and Δ9-tetrahydrocannabinol (THC). CBGA decarboxylation leads to the formation of neutral cannabinoid CBG, through a chemical reaction catalyzed by heat. On the basis of the growing interest in CBG and with the aim of highlighting scientific information on this phytocannabinoid, we focused the content of this article on its pharmacokinetic and pharmacodynamic characteristics and on its principal pharmacological effects. CBG is metabolized in the liver by the enzyme CYP2J2 to produce hydroxyl and di-oxygenated products. CBG is considered a partial agonist at the CB1 receptor () and CB2R, as well as a regulator of endocannabinoid signaling. Potential pharmacological targets for CBG include transient receptor potential (TRP) channels, cyclooxygenase (COX-1 and COX-2) enzymes, cannabinoid, 5-HT1A, and alpha-2 receptors. Pre-clinical findings show that CBG reduces intraocular pressure, possesses antioxidant, anti-inflammatory, and anti-tumoral activities, and has anti-anxiety, neuroprotective, dermatological, and appetite-stimulating effects. Several findings suggest that research on CBG deserves to be deepened, as it could be used, alone or in association, for novel therapeutic approaches for several disorders.

摘要

大麻二酚(CBG)是一种来自植物的大麻素,没有拟精神病作用。它的前体是酸性形式的大麻二酚酸(CBGA),而CBGA又是大麻二酚(CBD)和Δ9-四氢大麻酚(THC)的生物合成前体。CBGA脱羧通过热催化的化学反应导致中性大麻素CBG的形成。基于对CBG的兴趣日益增加,并旨在突出关于这种植物大麻素的科学信息,我们将本文的内容聚焦于其药代动力学和药效学特征以及其主要药理作用。CBG在肝脏中由CYP2J2酶代谢,产生羟基化和双氧化产物。CBG被认为是CB1受体()和CB2R的部分激动剂,也是内源性大麻素信号传导的调节剂。CBG的潜在药理学靶点包括瞬时受体电位(TRP)通道、环氧化酶(COX-1和COX-2)、大麻素、5-HT1A和α-2受体。临床前研究结果表明,CBG可降低眼压,具有抗氧化、抗炎和抗肿瘤活性,并具有抗焦虑、神经保护、皮肤和刺激食欲的作用。一些研究结果表明,对CBG的研究值得深入开展,因为它可以单独或联合用于多种疾病的新型治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b181/9666035/a5e3e5c655d6/ECAM2022-3336516.001.jpg

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