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Galanthamine and other Amaryllidaceae related alkaloids are inhibitors of α7, α4β2 and α3β4 nicotinic acetylcholine receptors
Moraga-Nicolás, Felipe; Iturriaga-Vásquez, Patricio; Mutis, Ana; Hormazábal, Emilio; Bermúdez-Díaz, Isabel.
  • Moraga-Nicolás, Felipe; Universidad de La Frontera. Facultad de Ingeniería y Ciencias. Doctorado en Ciencias de Recursos Naturales. Temuco. CL
  • Iturriaga-Vásquez, Patricio; Universidad de La Frontera. Facultad de Ingeniería y Ciencias. Departamento de Ciencias Químicas y Recursos Naturales. Temuco. CL
  • Mutis, Ana; Universidad de La Frontera. Facultad de Ingeniería y Ciencias. Departamento de Ciencias Químicas y Recursos Naturales. Temuco. CL
  • Hormazábal, Emilio; Universidad de La Frontera. Facultad de Ingeniería y Ciencias. Departamento de Ciencias Químicas y Recursos Naturales. Temuco. CL
  • Bermúdez-Díaz, Isabel; Oxford Brookes University. Department of Biological and Medical Sciences. Oxford. GB
Rev. bras. farmacogn ; 29(4): 495-499, July-Aug. 2019. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1042280
Responsible library: BR1.1
ABSTRACT
Abstract Galanthamine is an Amaryllidaceae-derived acetylcholinesterase inhibitor used to treat memory impairment in Alzheimer's disease and vascular dementia. There is evidence that galanthamine, in addition to its effects on acetylcholinesterase, may enhance or inhibit brain nicotinic acetylcholine receptors, which could increase or decrease the therapeutic efficacy of galanthamine, respectively. Here, we evaluated the effects of galanthamine and two others Amaryllidaceae acetylcholinesterase inhibitors (haemanthamine and tazettine) analyzed by gas chromatography-mass spectrometry and identified by comparing their mass fragmentation patterns with literature and database NIST vs.2.0 on the agonist responses of brain nicotinic acetylcholine receptors α7, α3β4, (α4)2(β2)3 and (α4)3(β2)2. Using nicotinic acetylcholine receptors expressed heterologously in Xenopus oocytes, in conjunction with two-electrode voltage clamping, we found that galanthamine inhibits the function of nicotinic acetylcholine receptors assayed through a mix competitive and non-competitevely. Nicotinic acetylcholine receptor α7 were significantly more sensitive to inhibition (17 ± 0.6 µM) than the heteromeric receptor, α3β4 (90 ± 3.4 µM). Neither haemanthamine nor tazettine were more potent than galanthamine.

Full text: Available Index: LILACS (Americas) Language: English Journal: Rev. bras. farmacogn Journal subject: Pharmacy Year: 2019 Type: Article / Project document Affiliation country: Chile / United kingdom Institution/Affiliation country: Oxford Brookes University/GB / Universidad de La Frontera/CL

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Full text: Available Index: LILACS (Americas) Language: English Journal: Rev. bras. farmacogn Journal subject: Pharmacy Year: 2019 Type: Article / Project document Affiliation country: Chile / United kingdom Institution/Affiliation country: Oxford Brookes University/GB / Universidad de La Frontera/CL