Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids

Autor: Norberto Peporine Lopes, Luís Guilherme Pereira Feitosa, João Luis Callegari Lopes, Daniel R. Callejon, Thalita B. Riul, Achyut Adhikari, Lucas Miranda Marques, Denise Brentan Silva, Marcelo Dias Baruffi, Ram Lal Shrestha, Thais Guaratini
Rok vydání: 2014
Předmět:
Zdroj: Molecules; Volume 19; Issue 5; Pages: 5692-5703
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP
Molecules
Molecules, Vol 19, Iss 5, Pp 5692-5703 (2014)
ISSN: 1420-3049
Popis: 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.
Databáze: OpenAIRE