Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, United Arab Emirates University, P.O. Box 17666, Al Ain, United Arab Emirates.
Department of Internal Medicine, College of Medicine and Health Sciences, United Arab Emirates University, P.O. Box 17666, Al Ain, United Arab Emirates.
Biomed Pharmacother. 2021 Aug;140:111639. doi: 10.1016/j.biopha.2021.111639. Epub 2021 Jun 3.
The endocannabinoid system (ECS), a conserved physiological system emerged as a novel pharmacological target for its significant role and potential therapeutic benefits ranging from neurological diseases to cancer. Among both, CB1 and CB2R types, CB2R have received attention for its pharmacological effects as antioxidant, anti-inflammatory, immunomodulatory and antiapoptotic that can be achieved without causing psychotropic adverse effects through CB1R. The ligands activate CB2R are of endogenous, synthetic and plant origin. In recent years, β-caryophyllene (BCP), a natural bicyclic sesquiterpene in cannabis as well as non-cannabis plants, has received attention due to its selective agonist property on CB2R. BCP has been well studied in a variety of pathological conditions mediating CB2R selective agonist property. The focus of the present manuscript is to represent the CB2R selective agonist mediated pharmacological mechanisms and therapeutic potential of BCP. The present narrative review summarizes insights into the CB2R-selective pharmacological properties and therapeutic potential of BCP such as cardioprotective, hepatoprotective, neuroprotective, nephroprotective, gastroprotective, chemopreventive, antioxidant, anti-inflammatory, and immunomodulator. The available evidences suggest that BCP, can be an important candidate of plant origin endowed with CB2R selective properties that may provide a pharmacological rationale for its pharmacotherapeutic application and pharmaceutical development like a drug. Additionally, given the wide availability in edible plants and dietary use, with safety, and no toxicity, BCP can be promoted as a nutraceutical and functional food for general health and well-being. Further, studies are needed to explore pharmacological and pharmaceutical opportunities for therapeutic and preventive applications of use of BCP in human diseases.
内源性大麻素系统（ECS）是一种保守的生理系统，作为一种新型的药理学靶点，因其在神经退行性疾病到癌症等多种疾病中的重要作用和潜在治疗益处而受到关注。在 CB1 和 CB2R 两种受体中，CB2R 因其具有抗氧化、抗炎、免疫调节和抗细胞凋亡的药理学作用而受到关注，这种作用不会通过 CB1R 引起精神不良反应。激活 CB2R 的配体有内源性、合成和植物来源。近年来，β-石竹烯（BCP）作为大麻和非大麻植物中的一种天然双环倍半萜烯，因其对 CB2R 的选择性激动剂特性而受到关注。BCP 已在多种病理条件下得到了广泛研究，介导 CB2R 选择性激动剂特性。本文的重点是代表 CB2R 选择性激动剂介导的药理学机制和 BCP 的治疗潜力。本综述总结了 BCP 对 CB2R 选择性药理学特性和治疗潜力的见解，如心脏保护、肝脏保护、神经保护、肾脏保护、胃保护、化学预防、抗氧化、抗炎和免疫调节剂。现有证据表明，BCP 作为一种具有 CB2R 选择性的植物来源化合物，可能是一种重要的候选药物，为其药理学应用和药物开发提供了药理学依据。此外，鉴于其在食用植物中的广泛存在和饮食用途、安全性和无毒性，BCP 可以作为一种营养保健品和功能性食品，促进一般健康和福祉。此外，还需要进一步研究以探索 BCP 在人类疾病中的治疗和预防应用的药理学和药物学机会。
