In vitro evaluation of the schistosomicidal effect of the extracts, fractions and major 3-hydroxy-2,6-dialkyl-substituted piperidine alkaloids from the flowers of Senna spectabilis (Fabaceae)

被引:11
作者
de Castro, Andreisa Teixeira [1 ]
Castro, Aline Pereira [1 ]
Silva, Matheus Siqueira [1 ]
Monteiro de Souza, Isabella Maria [1 ]
Martins-Souza, Raquel Lopes [1 ]
Chagas-Paula, Daniela Aparecida [1 ]
Leomil Coelho, Luiz Felipe [1 ]
Bolzani, Vanderlan da Silva [2 ]
Pivatto, Marcos [3 ]
Viegas Junior, Claudio [1 ]
Marques, Marcos Jose [1 ]
机构
[1] Univ Fed Alfenas Minas Gerais, BR-37130000 Alfenas, Brazil
[2] Univ Estadual Paulista Sao Paulo, BR-14800060 Araraquara, Brazil
[3] Univ Fed Uberlandia Minas Gerais, BR-38408100 Uberlandia, MG, Brazil
关键词
Schistosomiasis; Senna spectabilis; Alkaloids; Fluorescent probes; PRAZIQUANTEL-RESISTANT; ANTIMICROBIAL ACTIVITY; MANSONI; COMBINATION; CERCARIAE; ACETYLCHOLINESTERASE; CONSTITUENTS; OXAMNIQUINE; TREMATODE; ANALOGS;
D O I
10.1016/j.bmcl.2016.07.058
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this work, we present the in vitro schistosomicidal activity evaluation of the most active dichloromethane fraction (FDm) (ED50 = 83.5 mu g/mL) and of a mixture of the major alkaloids ((-)-cassine/(-)-spectaline, C/E) (ED50 = 37.4 mu g/mL) from the flowers of Senna spectabilis against adult worms and cercariae. We also demonstrate other toxic effects including paralysis of the adult worms, inhibition of the secretory activity, tegument lesions and cercaricidal activity. In the association test of Praziquantel (PZQ)-C/E, we observed up to 80% mortality of Schistosoma mansoni in comparison to PZQ monotherapy. Due to the diversity of the toxic effects, the schistosomicidal activity of C/E is likely a result of a multitarget mechanism involving the tegument, secretory system and neuromotor action. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4197 / 4204
页数:8
相关论文
共 54 条
[1]   Therapeutic effect of alpha lipoic acid combined with praziquantel on liver fibrosis induced by Schistosoma mansoni challenged mice [J].
Abdel-Hafeez, Ekhlas H. ;
Ahmad, Azza K. ;
Abdulla, Ahlam M. ;
Aabdel-Wahab, Soha ;
Mosalem, Fadia A. .
PARASITOLOGY RESEARCH, 2012, 111 (02) :577-586
[2]  
Aldenir F., 2007, BIORESOURCE TECHNOL, V98, P135
[3]  
Alexandre-Moreira MS, 2003, PLANTA MED, V69, P795, DOI 10.1055/s-2003-43201
[4]  
[Anonymous], 2014, Schistosomiasis
[5]   A combination of benznidazole and ketoconazole enhances efficacy of chemotherapy of experimental Chagas' disease [J].
Araújo, MSS ;
Martins-Filho, OA ;
Pereira, MES ;
Brener, Z .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2000, 45 (06) :819-824
[6]   Association of oxamniquine praziquantel and clonazepam in experimental Schistosomiasis mansoni [J].
Araujo, Neusa ;
Alves de Mattos, Ana Carolina ;
Zech Coelho, Paulo Marcos ;
Katz, Naftale .
MEMORIAS DO INSTITUTO OSWALDO CRUZ, 2008, 103 (08) :781-785
[7]  
Arnon R, 1999, PROTEIN SCI, V8, P2553
[8]  
Carrara V. S., 2013, J HELMINTHOL, V5, P1
[9]   Potent Schistosomicidal Constituents from Garcinia brasiliensis [J].
Castro, Aline Pereira ;
Alves de Mattos, Ana Carolina ;
Pereira, Neusa Araujo ;
Anchieta, Naira Ferreira ;
Silva, Matheus Siqueira ;
Dias, Danielle Ferreira ;
Silva, Claudinei Alves ;
Barros, Giulliano Vilela ;
Martins Souza, Raquel Lopes ;
Dos Santos, Marcelo Henrique ;
Marques, Marcos Jose .
PLANTA MEDICA, 2015, 81 (09) :733-741
[10]  
Chai JY, 2013, INFECT CHEMOTHER, V45, P32