Isoquinoline alkaloids as prolyl oligopeptidase inhibitors

Fitoterapia. 2015 Jun:103:192-6. doi: 10.1016/j.fitote.2015.04.004. Epub 2015 Apr 9.

Abstract

Prolyl oligopeptidase is a cytosolic serine peptidase that hydrolyses proline-containing peptides at the carboxy terminus of proline residues. It has been associated with schizophrenia, bipolar affective disorder, and related neuropsychiatric disorders and therefore may have important clinical implications. Thirty-one isoquinoline alkaloids of various structural types, previously isolated in our laboratory, were screened for their ability to inhibit prolyl oligopeptidase. Promising results have been showed by alkaloids californidine (IC50=55.6±3.5 μM), dihydrosanquinarine (IC50=99.1±7.6 μM), corypalmine (IC50=128.0±10.5 μM) and N-methyllaurotetanine (IC50=135.0±11.7 μM).

Keywords: Argemonine (CID: 442168); Berberine (PubChem CID: 2353); Californidine; Californidine (PubChem CID: 45266443); Canadine (PubChem CID: 443422); Corynoline (PubChem CID: 177014); Corypalmine (PubChem CID: 185605); Dihydrosanquinarine; Dihydrosanquinarine (PubChem CID: 124069); Isoquinoline alkaloids; N-Methyllaurotetanine (PubChem CID: 16573); Prolyl oligopeptidase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemistry*
  • Aporphines / chemistry
  • Dioxoles / chemistry
  • Heterocyclic Compounds, 4 or More Rings / chemistry
  • Isoquinolines / chemistry*
  • Molecular Structure
  • Prolyl Oligopeptidases
  • Serine Endopeptidases / chemistry*
  • Serine Proteinase Inhibitors / chemistry*

Substances

  • Alkaloids
  • Aporphines
  • Dioxoles
  • Heterocyclic Compounds, 4 or More Rings
  • Isoquinolines
  • Serine Proteinase Inhibitors
  • californidine
  • N-methyllaurotetanine
  • corypalmine
  • Serine Endopeptidases
  • Prolyl Oligopeptidases