Trypanosomiasis or trypanosomosis is the name of several diseases in vertebrates caused by parasitic protozoan trypanosomes of the genus Trypanosoma. A number of these diseases occur in animals. Trypanosomiasis in animals is caused by Trypanosoma congolense, Trypanosoma brucei brucei and Trypanosoma vivax. Among them, Trypanosoma congolense are extracellular and intravascular blood parasites that cause debilitating acute or chronic disease in cattle and other domestic animals. They remain in the bloodstream as extracellular parasites, thus destroying the host’s immune system.

Diminazene aceturate (also known as Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Due to its molecular structure, Diminazene aceturate has particular affinity for A-T base pairs in circular DNA and kinetoplast DNA. Plasma from Diminazene aceturate-treated cattle shows significant in vitro anti-trypanosome activity for up to 3 weeks after a single intramuscular injection. In addition, Diminazene aceturate also abolishes T. congolense-induced immunosuppression in vitro and in vivo. Furthermore, Diminazene aceturate administered during infection modulates the host immune response.

Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties. Moreover, Diminazene aceturate enhances the catalytic efficiency of ACE-2 and presumably increases angiotensin 1-7 generation.

To sum up, Diminazene aceturate is an anti-trypanosome agent for animals.

References:

[1] Shiby Kuriakose, et al. PLoS One. 2012;7(11):e48696.

[2] Carmen Castardeli, et al. Biomed Pharmacother. 2018 Nov;107:212-218.