scholarly journals Human African trypanosomiasis in endemic focus of Abraka, Nigeria

2010 ◽  
Vol 3 (6) ◽  
pp. 448-450 ◽  
Author(s):  
Onyebiguwa Patrick Goddey Nmorsi ◽  
Clement Isaac ◽  
Igho Benjamin Igbinosa ◽  
Duncan Ogheneocovo Umukoro ◽  
Dafe Palmer Aitaikuru
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Endemic Focus

The Inhibition of Cysteine Proteases Rhodesain and TbCatB: A Valuable Approach to Treat Human African Trypanosomiasis

2016 ◽  
Vol 16 (17) ◽  
pp. 1374-1391 ◽  
Author(s):  
Roberta Ettari ◽  
Santo Previti ◽  
Lucia Tamborini ◽  
Gregorio Cullia ◽  
Silvana Grasso ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
Cysteine Proteases ◽  
African Trypanosomiasis

Recent Updates on Development of Drug Molecules for Human African Trypanosomiasis

2016 ◽  
Vol 16 (20) ◽  
pp. 2245-2265 ◽  
Author(s):  
Ajmer Singh Grewal ◽  
Deepti Pandita ◽  
Shashikant Bhardwaj ◽  
Viney Lather
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Drug Molecules

New Pd-Fe ferrocenyl antiparasitic compounds with bioactive 8-hydroxyquinoline ligands: a comparative study with their Pt-Fe analogues

2021 ◽  
Author(s):  
Feriannys Rivas ◽  
Andrea Medeiros ◽  
Cristina Quiroga ◽  
Diego Benítez ◽  
Marcelo Comini ◽  
...  
Keyword(s):  
Comparative Study ◽  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
African Trypanosomiasis

In the search for a more effective chemotherapy for the treatment of Human African Trypanosomiasis, the disease caused by the parasite Trypanosoma brucei, the development of ferrocenyl compounds has arisen...

Human African trypanosomiasis: Potential therapeutic benefits of an alternative suramin and melarsoprol regimen

2002 ◽  
Vol 51 (4) ◽  
pp. 381-388 ◽  
Author(s):  
Frank W Jennings ◽  
Jean Rodgers ◽  
Barbara Bradley ◽  
George Gettinby ◽  
Peter G.E Kennedy ◽  
...  
Keyword(s):  
Human African Trypanosomiasis ◽  
African Trypanosomiasis ◽  
Therapeutic Benefits

scholarly journals Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

2010 ◽  
Vol 54 (7) ◽  
pp. 2893-2900 ◽  
Author(s):  
Antoaneta Y. Sokolova ◽  
Susan Wyllie ◽  
Stephen Patterson ◽  
Sandra L. Oza ◽  
Kevin D. Read ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
Human African Trypanosomiasis ◽  
Parent Drug ◽  
Cross Resistance ◽  
Pharmacokinetic Studies ◽  
African Trypanosomiasis ◽  
Trypanosoma Brucei Brucei ◽  
Resistant Lines

ABSTRACT The success of nifurtimox-eflornithine combination therapy (NECT) for the treatment of human African trypanosomiasis (HAT) has renewed interest in the potential of nitro drugs as chemotherapeutics. In order to study the implications of the more widespread use of nitro drugs against these parasites, we examined the in vivo and in vitro resistance potentials of nifurtimox and fexinidazole and its metabolites. Following selection in vitro by exposure to increasing concentrations of nifurtimox, Trypanosoma brucei brucei nifurtimox-resistant clones designated NfxR1 and NfxR2 were generated. Both cell lines were found to be 8-fold less sensitive to nifurtimox than parental cells and demonstrated cross-resistance to a number of other nitro drugs, most notably the clinical trial candidate fexinidazole (∼27-fold more resistant than parental cells). Studies of mice confirmed that the generation of nifurtimox resistance in these parasites did not compromise virulence, and NfxR1 remained resistant to both nifurtimox and fexinidazole in vivo. In the case of fexinidazole, drug metabolism and pharmacokinetic studies indicate that the parent drug is rapidly metabolized to the sulfoxide and sulfone form of this compound. These metabolites retained trypanocidal activity but were less effective in nifurtimox-resistant lines. Significantly, trypanosomes selected for resistance to fexinidazole were 10-fold more resistant to nifurtimox than parental cells. This reciprocal cross-resistance has important implications for the therapeutic use of nifurtimox in a clinical setting and highlights a potential danger in the use of fexinidazole as a monotherapy.

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