Klein Thomas W, Newton Catherine A
University of South Florida, Department of Molecular Medicine, Tampa, FL, USA.
Adv Exp Med Biol. 2007;601:395-413. doi: 10.1007/978-0-387-72005-0_43.
Cannabinoid-based drugs modeled on cannabinoids originally isolated from marijuana are now known to significantly impact the functioning of the endocannabinoid system of mammals. This system operates not only in the brain but also in organs and tissues in the periphery including the immune system. Natural and synthetic cannabinoids are tricyclic terpenes, whereas the endogenous physiological ligands are eicosanoids. Several receptors for these compounds have been extensively described, CB1 and CB2, and are G protein-coupled receptors; however, cannabinoid-based drugs are also demonstrated to function independently of these receptors. Cannabinoids regulate many physiological functions and their impact on immunity is generally antiinflammatory as powerful modulators of the cytokine cascade. This anti-inflammatory potency has led to the testing of these drugs in chronic inflammatory laboratory paradigms and even in some human diseases. Psychoactive and nonpsychoactive cannabinoid-based drugs such as Delta9-tetrahydrocannabinol, cannabidiol, HU-211, and ajulemic acid have been tested and found moderately effective in clinical trials of multiple sclerosis, traumatic brain injury, arthritis, and neuropathic pain. Furthermore, although clinical trials are not yet reported, preclinical data with cannabinoid-based drugs suggest efficacy in other inflammatory diseases such as inflammatory bowel disease, Alzheimer's disease, atherosclerosis, and osteoporosis.
以最初从大麻中分离出的大麻素为模型的基于大麻素的药物,如今已知会对哺乳动物的内源性大麻素系统的功能产生重大影响。该系统不仅在大脑中发挥作用,还在包括免疫系统在内的外周器官和组织中发挥作用。天然和合成大麻素是三环萜类化合物,而内源性生理配体是类花生酸。这些化合物的几种受体,即CB1和CB2,已被广泛描述,它们是G蛋白偶联受体;然而,基于大麻素的药物也被证明可独立于这些受体发挥作用。大麻素调节多种生理功能,并且它们对免疫的影响通常是抗炎的,作为细胞因子级联反应的强大调节剂。这种抗炎效力已促使人们在慢性炎症实验室模型甚至一些人类疾病中对这些药物进行测试。诸如Delta9-四氢大麻酚、大麻二酚、HU-211和阿居米酸等具有精神活性和非精神活性的基于大麻素的药物,已在多发性硬化症、创伤性脑损伤、关节炎和神经性疼痛的临床试验中进行了测试,并发现具有一定疗效。此外,尽管尚未报告临床试验情况,但基于大麻素的药物的临床前数据表明其在其他炎症性疾病如炎症性肠病、阿尔茨海默病、动脉粥样硬化和骨质疏松症中具有疗效。