Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids

Molecules

Daniel R. Callejon¹  Thalita B. Riul³  Luis G. P. Feitosa¹  Thais Guaratini¹  Denise B. Silva¹  Achyut Adhikari¹  Ram L. (S.) Shrestha²  Lucas M. M. Marques¹  Marcelo D. Baruffi³  João L. C. Lopes¹ 

[1] Núcleo de 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; E-Mails:;Amrit Science Campus, Tribhuvan University, Kathmandu, Nepal; E-Mail:;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; E-Mails:

关键词: Leishmania amazonensis;    spirocyclic erythrina-alkaloids;    tetrahydro-protoberberine-type alkaloids;    Corydalis govaniana;    Erythrina verna;   

DOI  :  10.3390/molecules19055692

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.