Callejon Daniel R, Riul Thalita B, Feitosa Luis G P, Guaratini Thais, Silva Denise B, Adhikari Achyut, Shrestha Ram L S, Marques Lucas M M, Baruffi Marcelo D, Lopes João L C, Lopes Norberto P
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.
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.
Molecules. 2014 May 5;19(5):5692-703. doi: 10.3390/molecules19055692.
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.
利什曼病是发展中国家面临的世界上最具问题的疾病之一。治疗利什曼病的传统药物有严重的副作用，以及显著的寄生虫耐药性问题。在这项工作中，从高氏紫堇中获得了两种生物碱1和2，从刺桐中获得了七种生物碱3 - 9。化合物的结构通过质谱以及一维和二维核磁共振光谱得以确认。在体外测试了化合物1 - 9对亚马逊利什曼原虫前鞭毛体形式的杀利什曼活性，并评估了其对J774（巨噬细胞系）的细胞毒性。与标准两性霉素B（IC50 = 0.20 µg/mL）相比，化合物1显示出强效活性（IC50 = 0.18 µg/mL）。螺环刺桐生物碱显示出比二苯并喹嗪类生物碱更低的杀利什曼活性。
