LEISHMANICIDAL ACTIVITY OF MESO COMPOUNDS

GALVEZ, CAROLINA ELIZABETH DEL VALLE; VILLECCO, MARGARITA; GIL, DIEGO; LOANDOS, MARÍA

Jornada; XXXVI Jornadas Científicas de la Asociación de Biología de Tucumán; 2019

Leishmaniasis is a serious disease that so far has no vaccine and the existing drugs are very expensive. Given these difficulties, there is an urgent need to develop new therapeutic alternatives. In previous work, we have designed and performed structural modifications of the 1,8- cineol monoterpenic ether, obtaining encouraging results. Therefore, three meso derivatives in C3 and C5 positions of cineol have been prepared in this work. In addition to this, the in vitro leishmanicidal activity on promastigotes and intracellular amastigotes of Leishmania infantum and L. donovani of the obtained meso compounds was studied. 500 μM of each synthesized compounds were added to a log-phase promastigote culture (106 parasites/mL). In addition, 5x103 J774 cells/well were placed in Labtek plates of culture to determine amastigote activity. Once the macrophages adhered, promastigotes in the stationary phase were incorporated (1:10) and it was kept overnight at 33ºC. Subsequently, the dilutions of the esters (100 μM) were added. The number of amastigotes/100 cells and the percentage of infection were determined after 48 h of incubation at 33ºC. Amphotericin B was used as the reference drug. All derivatives were able to reduce the multiplication of promastigotes between 50 and 60%. Against intracellular amastigotes, the compounds tested showed no difference in activity in the parasitic load and the infection rate, eliminating almost all of them. No significant differences in leishmanicidal activity were observed against L. donovani and L. infantum. These in vitro results show the potential utility of these compounds in vivo as antiparasitic agents against Leishmania disease.