In vitro and in vivo activity of meglumine antimoniate produced at Farmanguinhos-Fiocruz, Brazil, against Leishmania (Leishmania) amazonensis, L (L.) chagasi and L (Viannia) braziliensis.
The leishmanicidal activity of four batches of meglumine antimoniate, produced in Farmanguinhos-Fiocruz, Brazil (TAMs), was assessed and compared to Glucantime-Aventis Pharma Ltda. Using the amastigote-like in vitro model, the active concentrations of Sb v varied from 10microg/ml to 300microg/ml for L. (L.) chagasi and from 50microg/ml to 300microg/ml for L. (L.) amazonensis, with no statistically significant differences among the four batches of TAMs and Glucantime. The inhibitory concentrations (IC50) determined by the amastigote-infected macrophage model for TAM01/03 and Glucantime were, respectively: 26.3microg/ml and 127.6microg/ml for L. chagasi, 15.4microg /ml and 22.9microg/ml for L. amazonensis, and 12.1 microg/ml and 24.2microg/ml for L. (V.) braziliensis. The activities of the four batches of TAMs were confirmed in an in vivo model by assessing, during eight weeks skin lesions caused by L. braziliensis in hamster that were treated with 20mg Sb v/Kg/day for 30 consecutive days. The meglumine antimoniate produced by Farmanguinhos was as effective as the reference drug, Glucantime-Aventis, against three species of Leishmania that are of medical importance in Brazil.
Morais-Teixeira
Eliane de
Ed
Laboratório de Pesquisa Clínica, Centro de Pesquisas René Rachou-Fiocruz, Belo Horizonte, MG, Brasil.
Carvalho
Alcione S de
AS
Costa
Jorge C S da
JC
Duarte
Silvio L
SL
Mendonça
Jorge S
JS
Boechat
Núbia
N
Rabello
Ana
A
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D006224:Cricetinae; D020128:Inhibitory Concentration 50; D007892:Leishmania braziliensis / Q000187:drug effects*; D018314:Leishmania infantum / Q000187:drug effects*; D007894:Leishmania mexicana / Q000187:drug effects*; D008536:Meglumine / Q000494:pharmacology*; D000077485:Meglumine Antimoniate; D009942:Organometallic Compounds / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests
D000981:Antiprotozoal Agents; D009942:Organometallic Compounds; D008536:Meglumine; D000077485:Meglumine Antimoniate