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Author Report for: das Neves SC

Title: l-Hypaphorine and d-hypaphorine: Specific antiacetylcholinesterase activity in rat brain tissue
Yonekawa MKA, Penteado BB, Dal'Ongaro Rodrigues A, Lourenco EMG, Barbosa EG, das Neves SC, de Oliveira RJ, Marques MR, Silva DB and Santos E <4 more author(s)> Yonekawa MKA, Penteado BB, Dal'Ongaro Rodrigues A, Lourenco EMG, Barbosa EG, das Neves SC, de Oliveira RJ, Marques MR, Silva DB, de Lima DP, Beatriz A, Oses JP, Dos SJJA, Santos E (- 4)
Ref: Bioorganic & Medicinal Chemistry Lett, 47:128206, 2021 : PubMed
Abstract


ESTHER: Yonekawa_2021_Bioorg.Med.Chem.Lett_47_128206
PubMedSearch: Yonekawa 2021 Bioorg.Med.Chem.Lett 47 128206
PubMedID: 34146704
Inhibitor(s) related to this paper: Hypaphorine

Abstract

Acetylcholinesterase (AChEis) inhibitors are used to treat neurodegenerative diseases like Alzheimer's disease (AD). l-Hypaphorine (l-HYP) is a natural indole alkaloid that has been shown to have effects on the central nervous system (CNS). The goal of this research was to synthesize l-HYP and d-HYP and test their anticholinesterasic properties in rat brain regions. l-HYP suppressed acetylcholinesterase (AChE) activity only in the cerebellum, whereas d-HYP inhibited AChE activity in all CNS regions studied. No cytotoxic effect on normal human cells (HaCaT) was observed in the case of l-HYP and d-HYP although an increase in cell proliferation. Molecular modeling studies revealed that d-HYP and l-HYP have significant differences in their binding mode positions and interact stereospecifically with AChE's amino acid residues.