scholarly journals Antileishmanial activity and tubulin polymerization inhibition of podophyllotoxin derivatives on Leishmania infantum

Author(s):  
José Miguel Escudero-Martínez ◽  
Yolanda Pérez-Pertejo ◽  
Rosa M. Reguera ◽  
María Ángeles Castro ◽  
María Victoria Rojo ◽  
...  
RSC Advances ◽  
2015 ◽  
Vol 5 (35) ◽  
pp. 27775-27784 ◽  
Author(s):  
Hong-Yan Lin ◽  
Li-Fei Bai ◽  
Fang Wang ◽  
Xun Wu ◽  
Lu-Jing Han ◽  
...  

S12, the best anticancer agent among the 17 podophyllotoxin derivatives, showed a proliferative inhibition effect via inhibiting tubulin polymerization.


2017 ◽  
Vol 95 ◽  
pp. 536-547 ◽  
Author(s):  
Letícia de Almeida ◽  
Thaís Gaban Passalacqua ◽  
Luiz Antonio Dutra ◽  
Jéssica N. Varonez da Fonseca ◽  
Rhayanne F. Queiroz Nascimento ◽  
...  

2015 ◽  
Vol 114 (12) ◽  
pp. 4625-4635 ◽  
Author(s):  
Paula S. Lage ◽  
Miguel A. Chávez-Fumagalli ◽  
Juliana T. Mesquita ◽  
Laís M. Mata ◽  
Simone O. A. Fernandes ◽  
...  

2003 ◽  
Vol 47 (1) ◽  
pp. 174-180 ◽  
Author(s):  
Carole Di Giorgio ◽  
Florence Delmas ◽  
Nathalie Filloux ◽  
Maxime Robin ◽  
Laetitia Seferian ◽  
...  

ABSTRACT 9-Chloro and 9-amino-2-methoxyacridines bearing different substituents in position 7, as well as their corresponding unsubstituted dimeric and tetrameric complexes, were investigated for in vitro antiproliferative properties against Leishmania infantum compared to toxicity towards human monocytes. The results clearly confirmed that several compounds of the 2-methoxyacridine series, together with their corresponding dimeric and tetrameric derivatives, had strong in vitro antiparasitic properties. Antileishmanial activity was shown to depend on the nature of both 7- and 9-substituted groups in monoacridines, while it varied according to the nature of the 9-substituted group and the length of the linker among bis- and tetra-acridines. The effects of acridine derivatives on DNA synthesis raised the hypothesis that DNA metabolism constituted their main target in Leishmania promastigotes; however, secondary effects on other biochemical pathways, including protein and lipid metabolism, were observed, suggesting that acridine compounds could be considered multitarget drugs.


2020 ◽  
Vol 119 (7) ◽  
pp. 2263-2274 ◽  
Author(s):  
Flávio Simas Moreira Neri ◽  
David Bacelar Costa Júnior ◽  
Thamires Quadros Froes ◽  
Priscila Brandão Gomes da Silva ◽  
Micalyne Soares do Egito ◽  
...  

2017 ◽  
Vol 117 (2) ◽  
pp. 391-403 ◽  
Author(s):  
Débora Vasconcelos Costa Mendonça ◽  
Daniela Pagliara Lage ◽  
Stephane Lima Calixto ◽  
Flaviano Melo Ottoni ◽  
Grasiele de Sousa Vieira Tavares ◽  
...  

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
João S. B. da Luz ◽  
Erwelly B. de Oliveira ◽  
Monica C. B. Martins ◽  
Nicácio H. da Silva ◽  
Luiz C. Alves ◽  
...  

Leishmaniasis is considered by the World Health Organization as one of the infectious parasitic diseases endemic of great relevance and a global public health problem. Pentavalent antimonials used for treatment of this disease are limited and new phytochemicals emerge as an alternative to existing treatments, due to the low toxicity and cost reduction. Usnic acid is uniquely found in lichens and is especially abundant in genera such asAlectoria,Cladonia,Evernia,Lecanora,Ramalina,andUsnea. Usnic acid has been shown to exhibit antiviral, antiprotozoal, antiproliferative, anti-inflammatory, and analgesic activity. The aim of this study was to evaluate the antileishmanial activity of usnic acid onLeishmania infantum chagasipromastigotes and the occurrence of drug-induced ultrastructural damage in the parasite. Usnic acid was effective against the promastigote forms (IC50= 18.30 ± 2.00 µg/mL). Structural and ultrastructural aspects of parasite were analyzed. Morphological alterations were observed as blebs in cell membrane and shapes given off, increasing the number of cytoplasmic vacuoles, and cellular and mitochondrial swelling, with loss of cell polarity. We concluded that the usnic acid presented antileishmanial activity against promastigote forms ofLeishmania infantum chagasiand structural and ultrastructural analysis reinforces its cytotoxicity. Further,in vitrostudies are warranted to further evaluate this potential.


2017 ◽  
Vol 135 ◽  
pp. 49-59 ◽  
Author(s):  
Marta Ruiz-Santaquiteria ◽  
Pedro A. Sánchez-Murcia ◽  
Miguel A. Toro ◽  
Héctor de Lucio ◽  
Kilian Jesús Gutiérrez ◽  
...  

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