anti-trypanosomal

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor (IC50: 3.3 μM) that also inhibits glutathione reductase (IC50: 64.8 μM) and T. brucei (EC50: 1 μM).

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Fexinidazole (HOE 239) is an antiparasitic agent with activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.

Alazopeptin monohydrate is a microbial metabolite. Alazopeptin is an antibiotic, with moderate anti-trypanosomal.

1. Columbin has anti-inflammatory activity. 2. Columbin has chemopreventive ability against human colon cancer. 3. Columbin inhibits PLA2 hydrolysis of ghost RBC in a dose-dependent fashion.

Antitrypanosal agent 5 is a selective anti-trypanosomal agent that acts on T. brucei (IC50: 1 nM) and HEK293 cells (IC50: 483.3 μM).

MDL-73811 is a potent AdoMetDC (S-adenosylmethionine decarboxylease) inhibitor and anti-trypanosomal compound that cures Brucella infections in mice. However despite the good activity of MDL 73811, rapid plasma clearance and poor brain penetration hindered its further development.

N-p-trans-Coumaroyltyramine is a natural product and an acetylcholinesterase (AChE) inhibitor with an IC50 of 122 μM. It also exhibits anti-trypanosomal activity with an IC50 of 13.3 μM for T. brucei rhodesiense.

Eupatoriopicrin shows anti-trypanosomal activity and cytotoxicity against Trypanosoma brucei rhodesiense. Eupatoriopicrin-induced DNA damage may play a role in the observed cytotoxicity, it shows a weak sensitizing capacity in guinea pigs.