Medical Faculty, Institute for Drug Research, Hebrew University, Jerusalem 91120, Israel.
Kennedy Institute of Rheumatology, University of Oxford, Oxford OX3 7FY, UK.
Molecules. 2021 Sep 15;26(18):5601. doi: 10.3390/molecules26185601.
Interest in CBG (cannabigerol) has been growing in the past few years, due to its anti-inflammatory properties and other therapeutic benefits. Here we report the synthesis of three new CBG derivatives (HUM-223, HUM-233 and HUM-234) and show them to possess anti-inflammatory and analgesic properties. In addition, unlike CBG, HUM-234 also prevents obesity in mice fed a high-fat diet (HFD). The metabolic state of the treated mice on HFD is significantly better than that of vehicle-treated mice, and their liver slices show significantly less steatosis than untreated HFD or CBG-treated ones from HFD mice. We believe that HUM-223, HUM-233 and HUM-234 have the potential for development as novel drug candidates for the treatment of inflammatory conditions, and in the case of HUM-234, potentially for obesity where there is a huge unmet need.
在过去的几年中,由于其具有抗炎特性和其他治疗益处,人们对 CBG(大麻素二醇)的兴趣日益浓厚。在这里,我们报告了三种新型 CBG 衍生物(HUM-223、HUM-233 和 HUM-234)的合成,并证明它们具有抗炎和镇痛作用。此外,与 CBG 不同,HUM-234 还可以预防高脂肪饮食(HFD)喂养的小鼠肥胖。接受治疗的 HFD 小鼠的代谢状态明显好于接受载体治疗的小鼠,其肝切片的脂肪变性明显少于未经处理的 HFD 或来自 HFD 小鼠的 CBG 处理的肝切片。我们相信 HUM-223、HUM-233 和 HUM-234 有可能成为治疗炎症性疾病的新型候选药物,而对于 HUM-234,在肥胖症方面也有巨大的未满足的需求。