Neuroactivity of the naturally occurring aporphine alkaloid, roemerine

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.

Graphical Abstract

Keywords:

• Metabolomics
• alkaloid
• BDNF
• in silico
• Papaver

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by TÜBİTAK Ph.D. fellowship (2215) and Hacettepe University Scientific Researches Coordination Unit (Project Number: 014 D11 301 003-734). The author would like to thank OpenEye scientific for providing free academic licenses of their software packages.