ChemInform Abstract: The in vitro Trypanocidal Activity of Organotin Compounds.

ChemInform ◽  
2010 ◽  
Vol 28 (25) ◽  
pp. no-no
Author(s):  
J. SUSPERREGUI ◽  
A. PETSOM ◽  
M. BAYLE ◽  
G. LAIN ◽  
C. GIROUD ◽  
...  
1997 ◽  
Vol 32 (2) ◽  
pp. 123-128 ◽  
Author(s):  
J Susperregui ◽  
A Petsom ◽  
M Bayle ◽  
G Lain ◽  
C Giroud ◽  
...  

Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
WR Cunha ◽  
FM Dos Santos ◽  
JA Peixoto ◽  
RCS Veneziani ◽  
AEM Crotti ◽  
...  

Author(s):  
Ngozi Nwodo ◽  
Festus Okoye ◽  
Daowan Lai ◽  
Abdesammed Debbab ◽  
Marcel Kaiser ◽  
...  

1995 ◽  
Vol 32 (2-3) ◽  
pp. 143-160 ◽  
Author(s):  
Beat J. Brüschweiler ◽  
Friedrich E. Würgler ◽  
Karl Fent

2008 ◽  
Vol 118 (4) ◽  
pp. 637-640 ◽  
Author(s):  
Karin Merschjohann ◽  
Dietmar Steverding

2004 ◽  
Vol 48 (5) ◽  
pp. 1733-1738 ◽  
Author(s):  
Mhairi L. Stewart ◽  
Gorka Jimenez Bueno ◽  
Alessandro Baliani ◽  
Burkhard Klenke ◽  
Reto Brun ◽  
...  

ABSTRACT A series of nitroheterocyclic compounds were designed with linkages to melamine or benzamidine groups that are known substrates of the P2 aminopurine and other transporters in African trypanosomes of the brucei group. Several compounds showed in vitro trypanotoxicity with 50% inhibitory concentrations in the submicromolar range. Although most compounds interacted with the P2 transporter, as judged by their ability to inhibit adenosine transport via this carrier, uptake through this route was not necessary for activity since TbAT1-null mutant parasites, deficient in this transporter, retained sensitivity to these drugs. One compound, a melamine-linked nitrofuran, also showed pronounced activity against parasites in mice. Studies into the mode of action of this compound indicated that neither reductive, nor oxidative, stress were related to its trypanocidal activity ruling out a genotoxic effect in T. brucei, distinguishing it from some other, mammalian cell toxic, trypanocidal nitroheterocycles.


1998 ◽  
Vol 17 (6) ◽  
pp. 1005-1012 ◽  
Author(s):  
Emanuele Argese ◽  
Cinzia Bettiol ◽  
Annamaria Volpi Ghirardini ◽  
Matteo Fasolo ◽  
Gianumberto Giurin ◽  
...  

2015 ◽  
Vol 61 (2) ◽  
pp. 50-62
Author(s):  
P.A. Onyeyili ◽  
K. Aliyoo

Summary The control of trypanosomosis in animals and humans based on chemotherapy is limited and not ideal, since the agents used are associated with severe side effects, and emergence of relapse and drug resistant parasites. The need for the development of new, cheap and safe compounds stimulated this study. Three concentrations (211, 21.1 and 2.11 mg per ml) of chloroform stem bark extract of Annona muricata were screened for trypanocidal activity against Trypanosoma brucei brucei in vitro. Also, two doses (200 mg per kg and 100 mg per kg) of the extract were evaluated for trypanocidal activity in rats infected with the parasite. Haematological parameters were determined on day 1 post infection and on days 1, 6 and 30-post extract treatment. The extracts inhibited parasite motility and totally eliminated the organisms at the concentrations used in vitro. The extract also showed promising in vivo trypanocidal activity. The observed in vitro and in vivo trypanocidal activities may be due to the presence of bioactive compounds present in the extracts as seen in this study. The extract also improved the observed decreases in haematological parameters of the treated rats, which may be due to their ability to decrease parasite load. The observed oral LD50 of 1,725.05 mg per kg of the chloroform A. muricata extract using up and down method is an indication of very low toxicity, implying that the extract could be administered with some degree of safety.


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