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Neuroactivity of the naturally occurring aporphine alkaloid, roemerine
Natural Product Research ( IF 2.2 ) Pub Date : 2020-10-07 , DOI: 10.1080/14786419.2020.1830395
Omer Bayazeid 1 , Emirhan Nemutlu 2 , Cemil Can Eylem 2 , Mert İlhan 3 , Esra Küpeli-Akkol 3 , Hande Karahan 4 , Pelin Kelicen-Uğur 4 , Tayfun Ersoz 5 , Funda N Yalçın 1
Affiliation  

Abstract

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 in vitro, 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 (P. lacerum and P. syriacum) — has a neuronal activity through increasing BDNF protein expression and affecting serotonergic and glutamatergic systems in SH-SY5Y cell line.



中文翻译:

天然存在的阿朴啡生物碱罗默林的神经活性

摘要

罗默林是一种天然存在的阿朴啡生物碱。在这项研究中,我们筛选了食品和药物管理局 (FDA) 批准的药物的构象库,以识别有助于识别罗默林生物靶点的类似药物。评估体外神经活性,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) 和血清素 (5-HT) 的水平。通过基于结构的虚拟筛选,我们确定了五种与罗默林相似的药物;米氮平、托莫西汀、依匹斯汀、苯海拉明和奥芬那君。GC-MS 代谢组学研究表明,roemerine 对细胞裂解液和培养基中的丙氨酸-天冬氨酸-谷氨酸途径具有高度影响。此外,roemerine 在 10 µM 时增加了细胞间 5-HT 水平和细胞内 BDNF 蛋白表达。总之,罗默林 - 一种具有抗抑郁样作用的主要生物碱,具有植物(P. lacerum 和 P. syriacum) — 通过增加 BDNF 蛋白表达和影响 SH-SY5Y 细胞系中的血清素能和谷氨酸能系统而具有神经元活性。

更新日期:2020-10-07
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