Faculty of Pharmacy, Department of Pharmacognosy, Hacettepe University, Sihhiye, Ankara, Turkey.
Faculty of Pharmacy, Department of Analytical Chemistry, Hacettepe University, Sihhiye, Ankara, Turkey.
Nat Prod Res. 2021 Dec;35(24):6147-6152. doi: 10.1080/14786419.2020.1830395. Epub 2020 Oct 7.
Roemerine is a naturally occurring aporphine alkaloid. In this study, we screened a conformer library of Food and Drug Administration (FDA)-approved drugs to identify similar drugs that can assist in identifying the biological targets of roemerine. To assess the neuroactivity , we measured the levels of cell metabolites, Brain-Derived Neurotrophic Factor (BDNF) and serotonin (5-HT) in SH-SY5Y cell line. By means of structure-based virtual screening, we identified five drugs that are similar to roemerine; mirtazapine, atomoxetine, epinastine, diphenhydramine and orphenadrine. GC-MS metabolomics study revealed that roemerine has a high impact on alanine-aspartate-glutamate pathway in cell lysate and cultured medium. Additionally, roemerine increased intercellular 5-HT level and intracellular BDNF protein expression at 10 µM. In conclusion, roemerine - a major alkaloid in antidepressant-like effect possessing plants () - has a neuronal activity through increasing BDNF protein expression and affecting serotonergic and glutamatergic systems in SH-SY5Y cell line.
罗梅灵是一种天然存在的阿朴啡生物碱。在这项研究中,我们筛选了美国食品和药物管理局 (FDA) 批准药物的构象文库,以确定类似的药物,以帮助识别罗梅灵的生物靶标。为了评估神经活性,我们测量了 SH-SY5Y 细胞系中细胞代谢物、脑源性神经营养因子 (BDNF) 和 5-羟色胺 (5-HT) 的水平。通过基于结构的虚拟筛选,我们鉴定了五种与罗梅灵相似的药物:米氮平、阿托西汀、依帕司他、苯海拉明和奥芬那君。GC-MS 代谢组学研究表明,罗梅灵对细胞裂解物和培养基中的丙氨酸-天冬氨酸-谷氨酸途径有很大影响。此外,罗梅灵在 10μM 时增加了细胞间 5-HT 水平和细胞内 BDNF 蛋白表达。总之,罗梅灵——一种存在于具有抗抑郁作用的植物中的主要生物碱——通过增加 BDNF 蛋白表达和影响 SH-SY5Y 细胞系中的 5-羟色胺能和谷氨酸能系统,具有神经元活性。