Takeda Shuso
Department of Molecular Biology, Daiichi University of Pharmacy.
Yakugaku Zasshi. 2013;133(10):1093-101. doi: 10.1248/yakushi.13-00196.
Considerable attention has focused on cannabidiol (CBD), a major non-psychotropic constituent of fiber-type cannabis plant, and it has been reported to possess diverse biological activities. Although CBD is obtained from non-enzymatic decarboxylation of its parent molecule, cannabidiolic acid (CBDA), several studies have investigated whether CBDA itself is biologically active. In the present report, the author summarizes findings indicating that; 1) CBDA is a selective cyclooxygenase-2 (COX-2) inhibitor, and ii) CBDA possesses an anti-migrative potential for highly invasive cancer cells, apparently through a mechanism involving inhibition of cAMP-dependent protein kinase A, coupled with an activation of the small GTPase, RhoA. Further, the author introduces recent findings on the medicinal chemistry and pharmacology of the CBD derivative, CBD-2',6'-dimethyl ether (CBDD), that exhibits inhibitory activity toward 15-lipoxygenase (15-LOX), an enzyme responsible for the production of oxidized low-density lipoprotein (LDL). These studies establish CBD as both an important experimental tool and as a lead compound for pharmaceutical development. In this review, the author further discusses the potential uses of CBD and its derivatives in future medicines.
大麻二酚（CBD），一种纤维型大麻植物的主要非精神活性成分，已受到广泛关注，据报道它具有多种生物活性。尽管CBD是由其母体分子大麻二酚酸（CBDA）经非酶脱羧作用获得的，但已有多项研究探讨了CBDA本身是否具有生物活性。在本报告中，作者总结了以下研究结果：1）CBDA是一种选择性环氧合酶-2（COX-2）抑制剂；2）CBDA对高侵袭性癌细胞具有抗迁移潜力，显然是通过一种涉及抑制环磷酸腺苷（cAMP）依赖性蛋白激酶A并激活小GTP酶RhoA的机制实现的。此外，作者介绍了大麻二酚衍生物CBD-2'，6'-二甲醚（CBDD）的药物化学和药理学方面的最新研究结果，该衍生物对15-脂氧合酶（15-LOX）具有抑制活性，15-脂氧合酶是一种负责产生氧化型低密度脂蛋白（LDL）的酶。这些研究确立了CBD作为重要实验工具和药物开发先导化合物的地位。在这篇综述中，作者进一步讨论了CBD及其衍生物在未来药物中的潜在用途。
