title: Huperzia quadrifariata and Huperzia reflexa alkaloids inhibit acetylcholinesterase activity in vivo in mice brain.
abstract: Huperzine A, a Lycopodium alkaloid produced by Chinese folk herb Huperzia serrata (Lycopodiaceae), has been shown to be a promising agent for the treatment of Alzheimer's disease due to its potent acetylcholinesterase (AChE) activity, as well its efficacy in the treatment of memory of aged patients. Thus, the effects of two Huperzia species of habitats in Brazil (H. quadrifariata and H. reflexa) with described in vitro AChE inhibition activities were studied and their effects on mice brain AChE inhibition were determined after a single intraperitoneal (i.p.) injection. The alkaloid extracts were administered to mice in various doses (10, 1 and 0.5mg/kg) and acetylcholinesterase activity was measured post mortem in two brain areas using the Ellman's colorimetric method. The AChE activity was found to be significantly reduced in both the cortex and hippocampus, although this activity was less potent than that of reference inhibitor huperzine A (0.5mg/kg). Thus, it appears that H. quadrifariata and H. reflexa alkaloid extracts, shown to inhibit acetylcholinesterase in vitro, also have very potent in vivo effects, suggesting that the Huperzia species may still constitute a promising source of compounds with pharmaceutical interest for Alzheimer's disease.
authors.affiliation: Programa de Pós Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil. edukonrath@yahoo.com.br
authors.forename: E L
authors.initials: EL
authors.lastname: Konrath
authors.forename: B M
authors.initials: BM
authors.lastname: Neves
authors.forename: C Dos S
authors.initials: Cdos S
authors.lastname: Passos
authors.forename: P S
authors.initials: PS
authors.lastname: Lunardi
authors.forename: M G
authors.initials: MG
authors.lastname: Ortega
authors.forename: J L
authors.initials: JL
authors.lastname: Cabrera
authors.forename: C A
authors.initials: CA
authors.lastname: Gonçalves
authors.forename: A T
authors.initials: AT
authors.lastname: Henriques
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D000470:Alkaloids / Q000494:pharmacology* / Q000627:therapeutic use; D000544:Alzheimer Disease / Q000188:drug therapy / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects; D002800:Cholinesterase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006624:Hippocampus / Q000187:drug effects; D032501:Huperzia / Q000737:chemistry*; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008517:Phytotherapy; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use; D012717:Sesquiterpenes / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000470:Alkaloids; D002800:Cholinesterase Inhibitors; D010936:Plant Extracts; D012717:Sesquiterpenes; C050426:huperzine A; D000110:Acetylcholinesterase