Benznidazol (Benznidazole)e has an antiprotozoal activity by interfering with parasite protein biosynthesis, influencing cytokines production and stimulating host phagocytosis.

Antiparasite:20.35 μM

Benznidazole inhibits the proliferation of leukemic non-adherent cells by controlling cell cycle at G0/G1 cell phase through up-regulation of p27. Growth inhibition induced by Benznidazole is a reversible process, not accompanied by significant cell death. Benznidazole also has an immunomodulatory effect on macrophages by blocking the transcription of some pro-inflammatory mediators without altering interleukin 10 expression [1].

In Wistar rats treated orally, Tmaxs of Benznidazole are 2.0 and 1.1 h, respectively. Tmaxs of 15, 30, or 60 min, depending on the dose, in BALB/c mice following intraperitoneal treatment and Tmaxs of 1 to 5 h for dogs treated orally. In mice, Benznidazole (100 mg/kg, p.o.): Tmax in plasma, 0.83 h; Cmax in plasma: 41.61 μg/ml. The elimination half-life (t1/2) of Benznidazole was 2.03 h, and mean residence time (MRT) was 3.86 h. The volume of distribution (V) and clearance (CL), both as a function of Benznidazole bioavailability (F), were 38.81 ml and 13.29 ml/h, respectively. Benznidazole can cross the blood-brain barrier and exert its action in cases of central nervous system parasitism. However, other studies have indicated that BNZ has toxic effects in the central nervous system. Dogs orally treated with BNZ presented encephalopathy with multifocal characteristics and clinical, pathological, and neurological disorders that were dose-dependent and time-dependent. Benznidazole biodistribution occurs broadly, reaching the heart and colon, which are the most relevant organs for T. cruzi infection, and also the spleen, brain, liver, lungs, and kidneys [2].

20000 THP-1 cells in 200 mL of complete medium were incubated in quadruplicate in a 96-well plate in the presence of BZL (0.1, 0.5 and 1 mM) or vehicle (0.1% DMSO) for 24 or 48 h and then 20 mL of MTT solution (5 mg/mL in phosphate-buffered saline [PBS]) was added to each well. After 2 h at 37 °C, the MTT solution was removed and precipitated formazan was solubilized in 200 mL DMSO. Formazan production was then measured at OD545nm in a microplate spectrophotometer, with DMSO as blank.