Abstract:
Despite the very large number of phytocannabinoids isolated from Cannabis (Cannabis sativa L.), bioactivity studies have long remained focused on the so called \"Big Four\" [Δ9-THC (1), CBD (2), CBG (3) and CBC (4)] because of their earlier characterization and relatively easy availability via isolation and/or synthesis. Bioactivity information on the chemical space associated with the remaining part of the cannabinome, a set of ca 150 compounds traditionally referred to as \"minor phytocannabinoids\", is scarce and patchy, yet promising in terms of pharmacological potential. According to their advancement stage, we sorted the bioactivity data available on these compounds, better referred to as the \"dark cannabinome\", into categories: discovery (in vitro phenotypical and biochemical assays), preclinical (animal models), and clinical. Strategies to overcome the availability issues associated with minor phytocannabinoids are discussed, as well as the still unmet challenges facing their development as mainstream drugs.
摘要:
尽管从大麻(CannabissativaL.)中分离出了大量的植物大麻素,生物活性研究长期以来一直集中在所谓的“四大”[Δ9-THC(1),CBD(2),CBG(3)和CBC(4)],因为它们的早期表征和通过分离和/或合成相对容易获得。与大麻素剩余部分相关的化学空间的生物活性信息,一组约150种化合物,传统上称为“次要植物大麻素”,稀缺而零散,但在药理潜力方面很有希望。根据他们的进步阶段,我们对这些化合物的生物活性数据进行了分类,更好地称为“深色大麻组”,分类:发现(体外表型和生化测定),临床前(动物模型),和临床。讨论了克服与次要植物大麻素相关的可用性问题的策略,以及它们作为主流药物发展面临的仍未解决的挑战。