School of Pharmacy, Jiangsu University, Zhenjiang 212013, China.
School of Medicine, Jiangsu University, Zhenjiang 212013, China.
Mini Rev Med Chem. 2018;18(11):906-917. doi: 10.2174/1389557517666171123212557.
Sinomenine is one of the most widely known alkaloids owing to different therapeutic properties including anti-inflammatory and immunosuppressive activities, as well as the potency in neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease. Sinomenine has been studied as a potential anti-inflammatory agent through appropriate structural modifications. Recently, a number of such approaches have been attempted in various laboratories with great success. Several series of derivatives have been synthesized with changes at rings A, B, C and D. Herein, we present an up to date review of modifications and bioactivities of important modified derivatives. These studies offer interesting knowledge on the bioactivity and structural specificity of sinomenine, providing better understanding of the structure-activity relationships (SAR) between designing and development of sinomenine derivative with better therapeutic and lower side effects.
青藤碱是最广为人知的生物碱之一,具有多种治疗特性,包括抗炎和免疫抑制活性,以及在神经退行性疾病(如阿尔茨海默病和帕金森病)中的功效。通过适当的结构修饰,青藤碱已被研究作为一种潜在的抗炎药物。最近,许多实验室都在尝试这种方法,并取得了巨大的成功。已经合成了一系列在环 A、B、C 和 D 上发生变化的衍生物。在此,我们对重要修饰衍生物的修饰和生物活性进行了最新综述。这些研究为青藤碱的生物活性和结构特异性提供了有趣的知识,为设计和开发具有更好治疗效果和更低副作用的青藤碱衍生物的构效关系(SAR)提供了更好的理解。