diminazene

Summary

Summary: An effective trypanocidal agent.

Top Publications

  1. Olbrich C, Gessner A, Schröder W, Kayser O, Muller R. Lipid-drug conjugate nanoparticles of the hydrophilic drug diminazene-cytotoxicity testing and mouse serum adsorption. J Control Release. 2004;96:425-35 pubmed
    ..To potentially deliver the hydrophilic antitrypanosomal drug diminazene diaceturate to the brain of infected mice, the drug was formulated as lipid-drug conjugate (LDC) nanoparticles (..
  2. Mutiso J, Macharia J, Barasa M, Taracha E, Bourdichon A, Gicheru M. In vitro and in vivo antileishmanial efficacy of a combination therapy of diminazene and artesunate against Leishmania donovani in BALB/c mice. Rev Inst Med Trop Sao Paulo. 2011;53:129-32 pubmed
    The in vitro and in vivo activity of diminazene (Dim), artesunate (Art) and combination of Dim and Art (Dim-Art) against Leishmania donovani was compared to reference drug; amphotericin B. IC50 of Dim-Art was found to be 2.28 ± 0...
  3. Tuntasuvan D, Jarabrum W, Viseshakul N, Mohkaew K, Borisutsuwan S, Theeraphan A, et al. Chemotherapy of surra in horses and mules with diminazene aceturate. Vet Parasitol. 2003;110:227-33 pubmed
    ..All animals were treated with diminazene aceturate at 3.5 mg/kg body weight by intramuscular injection on days 0 and 41 of the study...
  4. Penzhorn B, Lewis B, De Waal D, Lopez Rebollar L. Sterilisation of Babesia canis infections by imidocarb alone or in combination with diminazene. J S Afr Vet Assoc. 1995;66:157-9 pubmed
    ..5 mg kg-1, as well as by a single dose of diminazene at 3.5 mg kg-1, followed by a single dose of imidocarb at 6 mg kg-1 the following day...
  5. Delespaux V, Chitanga S, Geysen D, Goethals A, van den Bossche P, Geerts S. SSCP analysis of the P2 purine transporter TcoAT1 gene of Trypanosoma congolense leads to a simple PCR-RFLP test allowing the rapid identification of diminazene resistant stocks. Acta Trop. 2006;100:96-102 pubmed
    ..brucei (Smallest Sum Probability 2.8e-136). To investigate a possible link between point mutations and diminazene aceturate (DA) resistance in mice, the TcoAT1 putative genes of 26 T...
  6. Qiu Y, Shil P, Zhu P, Yang H, Verma A, Lei B, et al. Angiotensin-converting enzyme 2 (ACE2) activator diminazene aceturate ameliorates endotoxin-induced uveitis in mice. Invest Ophthalmol Vis Sci. 2014;55:3809-18 pubmed publisher
    ..The purpose of this study was to investigate the effect of endogenous ACE2 activation in preventing endotoxin-induced uveitis (EIU) in mice...
  7. de Koning H, Anderson L, Stewart M, Burchmore R, Wallace L, Barrett M. The trypanocide diminazene aceturate is accumulated predominantly through the TbAT1 purine transporter: additional insights on diamidine resistance in african trypanosomes. Antimicrob Agents Chemother. 2004;48:1515-9 pubmed
    Resistance to diminazene aceturate (Berenil) is a severe problem in the control of African trypanosomiasis in domestic animals. It has been speculated that resistance may be the result of reduced diminazene uptake by the parasite...
  8. Witola W, Inoue N, Ohashi K, Onuma M. RNA-interference silencing of the adenosine transporter-1 gene in Trypanosoma evansi confers resistance to diminazene aceturate. Exp Parasitol. 2004;107:47-57 pubmed
    ..substrate specificity to the P2-nucleoside transporter, but could not transport diamidines (pentamidine and diminazene). We have cloned and sequenced a similar gene (TevAT1) from Trypanosoma evansi and found it to have 99...
  9. Mbaya A, Nwosu C, Kumshe H. Genital lesions in male red fronted gazelles (Gazella rufifrons) experimentally infected with Trypanosoma brucei and the effect of melarsamine hydrochloride (Cymelarsan®) and diminazene aceturate (Berenil®) in its treatment. Theriogenology. 2011;76:721-8 pubmed publisher
    ..genital lesions associated with trypanosomosis and the efficacy of melarsamine hydrochloride (Cymelarsan®) and diminazene aceturate (Berenil®) in the treatment of the condition. The animals were divided into 6 equal groups (A-F)...
  10. Delespaux V, Dinka H, Masumu J, Van den Bossche P, Geerts S. Five-fold increase in Trypanosoma congolense isolates resistant to diminazene aceturate over a seven-year period in Eastern Zambia. Drug Resist Updat. 2008;11:205-9 pubmed publisher
    ..and 2003 (n=38) in the Eastern Province of Zambia were analyzed by BclI-PCR-RFLP to assess the evolution of diminazene aceturate (DA) resistance over a period of seven years...

Detail Information

Publications62

  1. Olbrich C, Gessner A, Schröder W, Kayser O, Muller R. Lipid-drug conjugate nanoparticles of the hydrophilic drug diminazene-cytotoxicity testing and mouse serum adsorption. J Control Release. 2004;96:425-35 pubmed
    ..To potentially deliver the hydrophilic antitrypanosomal drug diminazene diaceturate to the brain of infected mice, the drug was formulated as lipid-drug conjugate (LDC) nanoparticles (..
  2. Mutiso J, Macharia J, Barasa M, Taracha E, Bourdichon A, Gicheru M. In vitro and in vivo antileishmanial efficacy of a combination therapy of diminazene and artesunate against Leishmania donovani in BALB/c mice. Rev Inst Med Trop Sao Paulo. 2011;53:129-32 pubmed
    The in vitro and in vivo activity of diminazene (Dim), artesunate (Art) and combination of Dim and Art (Dim-Art) against Leishmania donovani was compared to reference drug; amphotericin B. IC50 of Dim-Art was found to be 2.28 ± 0...
  3. Tuntasuvan D, Jarabrum W, Viseshakul N, Mohkaew K, Borisutsuwan S, Theeraphan A, et al. Chemotherapy of surra in horses and mules with diminazene aceturate. Vet Parasitol. 2003;110:227-33 pubmed
    ..All animals were treated with diminazene aceturate at 3.5 mg/kg body weight by intramuscular injection on days 0 and 41 of the study...
  4. Penzhorn B, Lewis B, De Waal D, Lopez Rebollar L. Sterilisation of Babesia canis infections by imidocarb alone or in combination with diminazene. J S Afr Vet Assoc. 1995;66:157-9 pubmed
    ..5 mg kg-1, as well as by a single dose of diminazene at 3.5 mg kg-1, followed by a single dose of imidocarb at 6 mg kg-1 the following day...
  5. Delespaux V, Chitanga S, Geysen D, Goethals A, van den Bossche P, Geerts S. SSCP analysis of the P2 purine transporter TcoAT1 gene of Trypanosoma congolense leads to a simple PCR-RFLP test allowing the rapid identification of diminazene resistant stocks. Acta Trop. 2006;100:96-102 pubmed
    ..brucei (Smallest Sum Probability 2.8e-136). To investigate a possible link between point mutations and diminazene aceturate (DA) resistance in mice, the TcoAT1 putative genes of 26 T...
  6. Qiu Y, Shil P, Zhu P, Yang H, Verma A, Lei B, et al. Angiotensin-converting enzyme 2 (ACE2) activator diminazene aceturate ameliorates endotoxin-induced uveitis in mice. Invest Ophthalmol Vis Sci. 2014;55:3809-18 pubmed publisher
    ..The purpose of this study was to investigate the effect of endogenous ACE2 activation in preventing endotoxin-induced uveitis (EIU) in mice...
  7. de Koning H, Anderson L, Stewart M, Burchmore R, Wallace L, Barrett M. The trypanocide diminazene aceturate is accumulated predominantly through the TbAT1 purine transporter: additional insights on diamidine resistance in african trypanosomes. Antimicrob Agents Chemother. 2004;48:1515-9 pubmed
    Resistance to diminazene aceturate (Berenil) is a severe problem in the control of African trypanosomiasis in domestic animals. It has been speculated that resistance may be the result of reduced diminazene uptake by the parasite...
  8. Witola W, Inoue N, Ohashi K, Onuma M. RNA-interference silencing of the adenosine transporter-1 gene in Trypanosoma evansi confers resistance to diminazene aceturate. Exp Parasitol. 2004;107:47-57 pubmed
    ..substrate specificity to the P2-nucleoside transporter, but could not transport diamidines (pentamidine and diminazene). We have cloned and sequenced a similar gene (TevAT1) from Trypanosoma evansi and found it to have 99...
  9. Mbaya A, Nwosu C, Kumshe H. Genital lesions in male red fronted gazelles (Gazella rufifrons) experimentally infected with Trypanosoma brucei and the effect of melarsamine hydrochloride (Cymelarsan®) and diminazene aceturate (Berenil®) in its treatment. Theriogenology. 2011;76:721-8 pubmed publisher
    ..genital lesions associated with trypanosomosis and the efficacy of melarsamine hydrochloride (Cymelarsan®) and diminazene aceturate (Berenil®) in the treatment of the condition. The animals were divided into 6 equal groups (A-F)...
  10. Delespaux V, Dinka H, Masumu J, Van den Bossche P, Geerts S. Five-fold increase in Trypanosoma congolense isolates resistant to diminazene aceturate over a seven-year period in Eastern Zambia. Drug Resist Updat. 2008;11:205-9 pubmed publisher
    ..and 2003 (n=38) in the Eastern Province of Zambia were analyzed by BclI-PCR-RFLP to assess the evolution of diminazene aceturate (DA) resistance over a period of seven years...
  11. Teka I, Kazibwe A, El Sabbagh N, Al Salabi M, Ward C, Eze A, et al. The diamidine diminazene aceturate is a substrate for the high-affinity pentamidine transporter: implications for the development of high resistance levels in trypanosomes. Mol Pharmacol. 2011;80:110-6 pubmed publisher
    ..impediment to the control of these diseases, and we investigated how resistance to the main veterinary drug diminazene aceturate correlates with changes in drug transport in resistant strains...
  12. Qi Y, Zhang J, Cole Jeffrey C, Shenoy V, Espejo A, Hanna M, et al. Diminazene aceturate enhances angiotensin-converting enzyme 2 activity and attenuates ischemia-induced cardiac pathophysiology. Hypertension. 2013;62:746-52 pubmed publisher
    ..b>Diminazene aceturate (DIZE), a small molecule ACE2 activator, has been used to evaluate this hypothesis...
  13. Eisler M, Brandt J, Bauer B, Clausen P, Delespaux V, Holmes P, et al. Standardised tests in mice and cattle for the detection of drug resistance in tsetse-transmitted trypanosomes of African domestic cattle. Vet Parasitol. 2001;97:171-82 pubmed
  14. da Silva A, Zanette R, Wolkmer P, Costa M, Garcia H, Lopes S, et al. Diminazene aceturate in the control of Trypanosoma evansi infection in cats. Vet Parasitol. 2009;165:47-50 pubmed publisher
    The aim of this study was to investigate the efficacy of diminazene aceturate in the control of the infection by Trypanosoma evansi in cats...
  15. Gall Y, Woitag T, Bauer B, Sidibe I, McDermott J, Mehlitz D, et al. Trypanocidal failure suggested by PCR results in cattle field samples. Acta Trop. 2004;92:7-16 pubmed
    ..treatment of 738 cattle from 10 villages in Kénédougou, Burkina Faso with isometamidium chloride and diminazene aceturate...
  16. Magona J, Mayende J, Okiria R, Okuna N. Protective efficacy of isometamidium chloride and diminazene aceturate against natural Trypanosoma brucei, Trypanosoma congolense and Trypanosoma vivax infections in cattle under a suppressed tsetse population in Uganda. Onderstepoort J Vet Res. 2004;71:231-7 pubmed
    The protective efficacy of isometamidium chloride (ISMM) and diminazene aceturate (DIM) against Trypanosoma brucei, Trypanosoma congolense and Trypanosoma vivax infections in cattle under a suppressed tsetse population was assessed in ..
  17. Mamoudou A, Delespaux V, Chepnda V, Hachimou Z, Andrikaye J, Zoli A, et al. Assessment of the occurrence of trypanocidal drug resistance in trypanosomes of naturally infected cattle in the Adamaoua region of Cameroon using the standard mouse test and molecular tools. Acta Trop. 2008;106:115-8 pubmed publisher
    ..The problem appears to be more serious in T. congolense than in T. brucei. Appropriate measures need to be taken in order to control bovine trypanosomosis in this area...
  18. Staroverov S, Sidorkin V, Fomin A, Shchyogolev S, Dykman L. Biodynamic parameters of micellar diminazene in sheep erythrocytes and blood plasma. J Vet Sci. 2011;12:303-7 pubmed
    In this work, we used a preparation of diminazene, which belongs to the group of aromatic diamidines...
  19. Delespaux V, Geysen D, Van den Bossche P, Geerts S. Molecular tools for the rapid detection of drug resistance in animal trypanosomes. Trends Parasitol. 2008;24:236-42 pubmed publisher
    ..In this review the mechanisms involved in resistance to isometamidium and diminazene will be discussed, together with some new molecular detection tools that have been developed recently enabling ..
  20. Campbell M, Prankerd R, Davie A, Charman W. Degradation of berenil (diminazene aceturate) in acidic aqueous solution. J Pharm Pharmacol. 2004;56:1327-32 pubmed
    ..It is recommended that berenil be enteric coated for formulations to be used in treating Third World parasitic diseases. ..
  21. Lin M, Huang H. Use of a doxycycline-enrofloxacin-metronidazole combination with/without diminazene diaceturate to treat naturally occurring canine babesiosis caused by Babesia gibsoni. Acta Vet Scand. 2010;52:27 pubmed publisher
    ..of oral administration of a doxycycline-enrofloxacin-metronidazole combination with and without injections of diminazene diaceturate in the management of naturally occurring canine babesiosis caused by B...
  22. Haber P, Ye M, Wysocki J, Maier C, Haque S, Batlle D. Angiotensin-converting enzyme 2-independent action of presumed angiotensin-converting enzyme 2 activators: studies in vivo, ex vivo, and in vitro. Hypertension. 2014;63:774-82 pubmed publisher
    ..XNT (1-[(2-dimethylamino)ethylamino]-4-(hydroxymethyl)-7-[(4-methylphenyl) sulfonyl oxy]-9H-xanthene-9-one) and diminazene have been reported to exert various organ-protective effects, which are attributed to the activation of ACE2...
  23. Kayode O, Huang Z, Soares A, Caulfield T, Dong Z, Bode A, et al. Small molecule inhibitors of mesotrypsin from a structure-based docking screen. PLoS ONE. 2017;12:e0176694 pubmed publisher
    ..b>Diminazene (CID22956468), along with two similar compounds presenting the bis-benzamidine substructure, was validated as a ..
  24. Qian W, Wang H, Shan D, Li B, Liu J, Liu Q. Activity of several kinds of drugs against Neospora caninum. Parasitol Int. 2015;64:597-602 pubmed publisher
    ..herbicides (atrazine, glyphosate), anticoccidiosis drugs (toltrazuril and ponazuril), cyclophosphamide, diminazene aceturate and praziquantel in vitro using parasite growth, replication and host cell invasion assays in human ..
  25. Torr S, Mangwiro T. Interactions between cattle and biting flies: effects on the feeding rate of tsetse. Med Vet Entomol. 2000;14:400-9 pubmed
    ..61%). The lower feeding rates in young animals were attributed to higher rates of defensive movements. The results suggest that higher rates of defensive activities by young cattle reduce the risk of them contracting trypanosomiasis. ..
  26. Zhou J, Shen J, He G, Wang Q. Studies on the comprehensive control of babesiasis in cattle and buffaloes. Trop Anim Health Prod. 1997;29:66S-71S pubmed
    ..3. Good results were obtained in another epidemic area using this control method. These results indicated that this technique of controlling babesiosis is highly effective...
  27. Haaf T, Feichtinger W, Guttenbach M, Sanchez L, Muller C, Schmid M. Berenil-induced undercondensation in human heterochromatin. Cytogenet Cell Genet. 1989;50:27-33 pubmed
    ..At the ultrastructural level, undercondensation is associated with loosely packed, mutliply folded chromatin fibers with a diameter of approximately 250 A and organized probably as loops. ..
  28. Olbrich C, Gessner A, Kayser O, Müller R. Lipid-drug-conjugate (LDC) nanoparticles as novel carrier system for the hydrophilic antitrypanosomal drug diminazenediaceturate. J Drug Target. 2002;10:387-96 pubmed
    ..IR and DSC data showed that the antitrypanosomal drug diminazene is able to react with fatty acids to form water-insoluble salts like diminazenedistearate and -dioleate...
  29. Chekwube A, Onyema E, Ikenna U, Ezeokonkwo R. Effect of diminazene aceturate, levamisole and vitamin C combination therapy in rats experimentally infected with Trypanosoma brucei brucei. Asian Pac J Trop Med. 2014;7:438-45 pubmed publisher
    To investigate the effect of diminazene aceturate (DA) alone or in combination with either levamisole and/or Vitamin C in albino rats experimentally infected with Trypanosoma brucei brucei...
  30. Marinho Prado J, Lourenção A, Guedes R, Pallini A, Oliveira J, Oliveira M. Enzymatic response of the eucalypt defoliator Thyrinteina arnobia (Stoll) (Lepidoptera: Geometridae) to a bis-benzamidine proteinase Inhibitor. i. Neotrop Entomol. 2012;41:420-5 pubmed publisher
    ..Berenil also prevented the increase of the cysteine proteinases activity in response to trypsin inhibition. ..
  31. Hao C, Zhou T, Liu S, Wang L, Huang B, Kuang N, et al. Dual-channel optical sensing platform for detection of diminazene aceturate based on thioglycolic acid-wrapped cadmium telluride/cadmium sulfide quantum dots. J Colloid Interface Sci. 2016;472:76-83 pubmed publisher
    ..overlapping resonance Rayleigh scattering (DWO-RRS) and fluorescence has been designed for the detection of diminazene aceturate (DA). It is based on the use of thioglycolic acid-wrapped CdTe/CdS quantum dots (Q-dots)...
  32. Eze A, Gould M, Munday J, Tagoe D, Stelmanis V, Schnaufer A, et al. Reduced Mitochondrial Membrane Potential Is a Late Adaptation of Trypanosoma brucei brucei to Isometamidium Preceded by Mutations in the ? Subunit of the F1Fo-ATPase. PLoS Negl Trop Dis. 2016;10:e0004791 pubmed publisher
    ..b. rhodesiense. Resistance to isometamidium is a growing concern, as is cross-resistance to the diamidine drugs diminazene and pentamidine...
  33. Yamasaki M, Watanabe N, Idaka N, Yamamori T, Otsuguro K, Uchida N, et al. Intracellular diminazene aceturate content and adenosine incorporation in diminazene aceturate-resistant Babesia gibsoni isolate in vitro. Exp Parasitol. 2017;183:92-98 pubmed publisher
    The mechanism of the development of diminazene aceturate (DA) resistance in Babesia gibsoni is still unknown even though DA-resistant B. gibsoni isolate was previously developed in vitro. To clarify the mechanisms of DA-resistance in B...
  34. Silva R, Ramirez L, Souza S, Ortiz A, Pereira S, Davila A. Hematology of natural bovine trypanosomosis in the Brazilian Pantanal and Bolivian wetlands. Vet Parasitol. 1999;85:87-93 pubmed
    ..The clinical signs were lachrymation, progressive weakness, marked weight loss, inappetence, diarrhea and abortions during the third trimester of pregnancy...
  35. Wiemuth D, Grunder S. The pharmacological profile of brain liver intestine Na+ channel: inhibition by diarylamidines and activation by fenamates. Mol Pharmacol. 2011;80:911-9 pubmed publisher
    ..Inhibition by diarylamidines and activation by fenamates define a unique pharmacological profile for BLINaC, which will be useful to unravel the physiological function of this ion channel. ..
  36. Rizk M, El Sayed S, Aboulaila M, Yokoyama N, Igarashi I. Evaluation of the inhibitory effect of N-acetyl-L-cysteine on Babesia and Theileria parasites. Exp Parasitol. 2017;179:43-48 pubmed publisher
    ..The inhibitory effect of N-acetyl-L-cysteine was synergistically potentiated when used in combination with diminazene aceturate on B. bovis and B. caballi cultures...
  37. Guswanto A, Nugraha A, Tuvshintulga B, Tayebwa D, Rizk M, Batiha G, et al. 17-DMAG inhibits the multiplication of several Babesia species and Theileria equi on in vitro cultures, and Babesia microti in mice. Int J Parasitol Drugs Drug Resist. 2018;8:104-111 pubmed publisher
    ..Furthermore, the two-drug combination of 17-DMAG with diminazene aceturate (DA) and atovaquone (AV) showed synergism or addition on in vitro cultures of Babesia and Theileria ..
  38. Wang L, Fan S, Li S, Wang X, Gao J, Yang X. Protective role of ACE2-Ang-(1-7)-Mas in myocardial fibrosis by downregulating KCa3.1 channel via ERK1/2 pathway. Pflugers Arch. 2016;468:2041-2051 pubmed
    ..As the activator of ACE2, diminazene aceturate (DIZE) inhibited increase of blood pressure, collagen deposition, and KCa3...
  39. Dhawale V, Amara V, Karpe P, Malek V, Patel D, Tikoo K. Activation of angiotensin-converting enzyme 2 (ACE2) attenuates allergic airway inflammation in rat asthma model. Toxicol Appl Pharmacol. 2016;306:17-26 pubmed publisher
    ..induced in male wistar rats by sensitization and challenge with ovalbumin and then treated with ACE2 activator, diminazene aceturate (DIZE) for 2weeks...
  40. Nguyen B, Wilson W. The effects of hairpin loops on ligand-DNA interactions. J Phys Chem B. 2009;113:14329-35 pubmed publisher
    ..The use of a non-nucleotide loop (with a reduced negative charge) not only enhances the thermal stability of the hairpin but also reduces the nonspecific binding at the loop without compromising the primary binding affinity on the stem. ..
  41. Krautbauer R, Pope L, Schrader T, Allen S, Gaub H. Discriminating small molecule DNA binding modes by single molecule force spectroscopy. FEBS Lett. 2002;510:154-8 pubmed
    ..The minor groove binder berenil, the crosslinker cisplatin and the intercalator ethidium bromide are compared. ..
  42. Edwards T, Sigurdsson S. Electron paramagnetic resonance dynamic signatures of TAR RNA-small molecule complexes provide insight into RNA structure and recognition. Biochemistry. 2002;41:14843-7 pubmed
    ..The data presented here show that the dynamic signatures provide strong insights into RNA structure and recognition and demonstrate the value of EPR spectroscopy for the investigation of small molecule binding to RNA. ..
  43. Sheader K, te Vruchte D, Rudenko G. Bloodstream form-specific up-regulation of silent vsg expression sites and procyclin in Trypanosoma brucei after inhibition of DNA synthesis or DNA damage. J Biol Chem. 2004;279:13363-74 pubmed
    ..brucei. We postulate that the redistribution of a limiting bloodstream form-specific factor involved in both silencing and DNA repair results in the derepression of normally silenced pol I transcription units after DNA damage. ..