title: Leishmanicidal evaluation of tetrahydroprotoberberine and spirocyclic erythrina-alkaloids.
abstract: Leishmaniasis is one of the World's most problematic diseases in developing countries. Traditional medicines to treat leishmaniasis have serious side effects, as well as significant parasite resistance problems. In this work, two alkaloids 1 and 2 were obtained from Corydalis govaniana Wall and seven alkaloids 3-9, were obtained from Erythrina verna. The structures of the compounds were confirmed by mass spectrometry and 1D- and 2D-NMR spectroscopy. The leishmanicidal activity of compounds 1-9 against Leishmania amazonensis was tested on promastigote forms and cytotoxicity against J774 (macrophage cell line) was assessed in vitro. Compound 1 showed potent activity (IC50 = 0.18 µg/mL), compared with the standard amphotericin B (IC50 = 0.20 µg/mL). The spirocyclic erythrina-alkaloids showed lower leishmanicidal activity than dibenzoquinolizine type alkaloids.
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. daniel_callejon@yahoo.com.br.
authors.forename: Daniel R
authors.initials: DR
authors.lastname: Callejon
authors.affiliation: Departamento de Análises Clínicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil. tbriul@hotmail.com.
authors.forename: Thalita B
authors.initials: TB
authors.lastname: Riul
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. luis@lychnoflora.com.br.
authors.forename: Luis G P
authors.initials: LG
authors.lastname: Feitosa
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. thaisguaratini@yahoo.com.br.
authors.forename: Thais
authors.initials: T
authors.lastname: Guaratini
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. denisebrentan@gmail.com.
authors.forename: Denise B
authors.initials: DB
authors.lastname: Silva
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. adhikarimine@yahoo.com.
authors.forename: Achyut
authors.initials: A
authors.lastname: Adhikari
authors.affiliation: Amrit Science Campus, Tribhuvan University, Kathmandu, Nepal. Swagatstha@hotmail.com.
authors.forename: Ram L S
authors.initials: RL
authors.lastname: Shrestha
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. lucasmauriz@yahoo.com.br.
authors.forename: Lucas M M
authors.initials: LM
authors.lastname: Marques
authors.affiliation: Departamento de Análises Clínicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil. mdbaruff@fcfrp.usp.br.
authors.forename: Marcelo D
authors.initials: MD
authors.lastname: Baruffi
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. joaoluis@usp.br.
authors.forename: João L C
authors.initials: JL
authors.lastname: Lopes
authors.affiliation: Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil. nplopes@fcfrp.usp.br.
authors.forename: Norberto P
authors.initials: NP
authors.lastname: Lopes
mesh_terms: D000470:Alkaloids / Q000737:chemistry; D001600:Berberine Alkaloids / Q000008:administration & dosage* / Q000737:chemistry; D002460:Cell Line; D004895:Erythrina / Q000737:chemistry*; D006801:Humans; D007891:Leishmania / Q000187:drug effects / Q000469:parasitology*; D007896:Leishmaniasis / Q000188:drug therapy* / Q000469:parasitology; D008264:Macrophages / Q000187:drug effects / Q000473:pathology; D021261:Parasitic Sensitivity Tests; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000470:Alkaloids; D001600:Berberine Alkaloids; D010936:Plant Extracts; C014845:berbine