Lee Tae Yeon, Yang Wooin, Cha Dong Seok, Han Young Taek
College of Pharmacy, Dankook University, Cheonan 31116, South Korea.
College of Pharmacy, Woosuk University, Wanju-gun 55338, South Korea.
J Asian Nat Prod Res. 2023 May;25(5):446-455. doi: 10.1080/10286020.2022.2104259. Epub 2022 Aug 18.
2-(Quinoline-8-carboxamido)benzoic acid (2-QBA; ) is a natural quinoline alkaloid isolated from the deep-sea-derived fungus sp. SCSIO06786. Alkaloid was synthesized by an amidation reaction of 8-quinolinecaroxylic acid with methyl anthranilate, followed by hydrolysis. The neuroprotective properties of 1 were evaluated using a Parkinson's disease model, which revealed that significantly ameliorated 1-methyl-4-phenylpyridinium (MPP)-induced dopaminergic neurodegeneration in a dose-dependent manner. MPP-induced behavioral defects in worms, including impaired locomotion and basal slowing ability, were restored by treatment with . We further demonstrated that treatment with modulates the formation of neurotoxic α-synuclein oligomers by suppressing α-synuclein expressions and enhancing proteasome activity. These results suggest that is a promising therapeutic candidate for the treatment of Parkinson's disease.
2-(喹啉-8-甲酰胺基)苯甲酸(2-QBA; )是从深海来源的真菌 sp. SCSIO06786中分离得到的一种天然喹啉生物碱。生物碱 通过8-喹啉羧酸与邻氨基苯甲酸甲酯的酰胺化反应合成,随后进行水解。使用帕金森病模型评估了1的神经保护特性,结果表明 以剂量依赖性方式显著改善了1-甲基-4-苯基吡啶鎓(MPP)诱导的多巴胺能神经变性。通过用 处理,恢复了MPP诱导的蠕虫行为缺陷,包括运动受损和基础减慢能力。我们进一步证明,用 处理通过抑制α-突触核蛋白表达和增强蛋白酶体活性来调节神经毒性α-突触核蛋白寡聚体的形成。这些结果表明, 是治疗帕金森病的有前景的治疗候选物。