Wangchuk Phurpa, Sastraruji Thanapat, Taweechotipatr Malai, Keller Paul A, Pyne Stephen G
Nat Prod Commun. 2016 Dec;11(12):1801-1804.
Corydalis plants containing isoquinoline alkaloids are reported to possess promising phamacological properties for the treatment of important diseases including cancer, inflammation, Alzheimer's disease and microbial infections. As part of a wider program investigating Bhutanese medicinal plants,.we have previously identified eight isoquinoline alkaloids from C. dubia. Out of these, we report here on two of the major alkaloids, scoulerine (1) and cheilanthifoline (2) and their inhibitory activities against acetylcholinesterase (anti-AChE),-tumor necrosis factor alpha (anti TNF-α) and a bacteial strain, Helicobacterpylori. Both alkaloids showed weak anti TNF-α and antibacterial activities. However, the anti-AChE activity of scoulerine (1) was promising as it-significantly inhibited AChE with a minimum inhibitory requirement (MIR) value of 0.0015 nmol, which was two-fold better than the reference drug, galanthamine (MIR value of 0.003 nmol). As there are limited.anti-Alzheimer's chemotherapeutics, scoulerine (1) is worthy of further exploration, including lead optimization, structure-activity-relationship studies, analog development,.pharmacodynanics and in vivo animal studies.
据报道，含有异喹啉生物碱的紫堇属植物具有治疗包括癌症、炎症、阿尔茨海默病和微生物感染在内的重要疾病的潜在药理特性。作为一项更广泛的研究不丹药用植物项目的一部分，我们之前已从滇西紫堇中鉴定出8种异喹啉生物碱。在此，我们报告其中两种主要生物碱，scoulerine（1）和白屈菜红碱（2）及其对乙酰胆碱酯酶（抗AChE）、肿瘤坏死因子α（抗TNF-α）和一种细菌菌株幽门螺杆菌的抑制活性。两种生物碱均表现出较弱的抗TNF-α和抗菌活性。然而，scoulerine（1）的抗AChE活性很有前景，因为它以0.0015 nmol的最低抑制浓度（MIR）值显著抑制AChE，这比参考药物加兰他敏（MIR值为0.003 nmol）好两倍。由于抗阿尔茨海默病的化学治疗药物有限，scoulerine（1）值得进一步探索，包括先导化合物优化、构效关系研究、类似物开发、药效动力学和体内动物研究。
