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PubMed2005

Subcellular in vivo 1H MR spectroscopy of Xenopus laevis oocytes.

In vivo magnetic resonance (MR) spectra are typically obtained from voxels whose spatial dimensions far exceed those of the cells they contain. This study was designed to evaluate the potential of localized MR spectroscopy to investigate subcellular phenomena. Using a high magnetic field and a home-built microscopy probe with large gradient field strengths, we achieved voxel sizes of (180 microm)3. In the large oocytes of the frog Xenopus laevis, this was small enough to allow the recording of the first compartment-selective in vivo MR spectra from the animal and vegetal cytoplasm as well as the nucleus. The two cytoplasmic regions differed in their lipid contents and NMR lineshape characteristics-differences that are not detectable with whole-cell NMR techniques. In the nucleus, the signal appeared to be dominated by water, whereas other contributions were negligible. We also used localized spectroscopy to monitor the uptake of diminazene acturate, an antitrypanosomal agent, into compartments of a single living oocyte. The resulting spectra from the nucleus and cytoplasm revealed different uptake kinetics for the two components of the drug and demonstrate that MR technology is on the verge of becoming a tool for cell biology.

Animals↗
PubMed1998

Oral pharmacological treatments for parasitic diseases of rainbow trout oncorhynchus mykiss. III. Ichthyobodo necator.

A total of 32 drugs were evaluated as regards their efficacy for oral treatment of Ichthyobodo necator infestation of rainbow trout. In preliminary trials, all drugs were supplied to infected fish at 40 g per kg of feed for 10 d. The majority of the drugs tested (1,3-di-6-quinolylurea, aminosidine, amprolium, benznidazole, bithionol, chloroquine, diethylcarbamazine, dimetridazole, diminazene aceturate, febantel, flubendazole, ketoconazole, levamisole, mebendazole, netobimin, niclosamide, niridazole, nitroscanate, nitroxynil, oxibendazole, parbendazole, piperazine, praziquantel, ronidazole, sulphaquinoxaline, tetramisole, thiophanate, toltrazuril and trichlorfon) were ineffectdive. Metronidazole and secnidazole were 100% effective (unlike the other nitroimidazoles tested, namely dimetridazole, benznidazole and ronidazole). The non-carbamate benzimidazole triclabendazole was likewise 100% effective.

Administration, Oral↗
PubMed1981

Survey for trypanosomes in black rhinoceros (Diceros bicornis).

Blood samples were taken from 39 black rhinoceros (Diceros bicornis), usually soon after they were captured. The blood was examined microscopically for trypanosomes, and most samples were tested for trypanosome serum antibodies and inoculated into small laboratory animals. Serum antibodies were found in most animals and trypanosomes identified as Trypanosoma brucei were found in 7 of 39 (18%) of the rhinoceros. Berenil (diminazene aceturate) did not effect complete elimination of trypanosomes. In spite of treatment, one rhinoceros died of trypanosomiasis.

Animals↗
PubMed2001

Bioassay-guided studies on the cytotoxic and in vitro trypanocidal activities of a sesquiterpene (Muzigadial) derived from a Ugandan medicinal plant (Warburgia ugandensis).

Trypanosomosis is arguably the most important disease of man and his domesticated animals in the tropics. There are few compounds available for its treatment. This has exacerbated the development of drug resistance. There is therefore urgent need to search for newer compounds to treat this important disease. Medicinal plants represent a potential source of the drugs. This paper reports a bioassay-guided study to search for possible biological activity (cytotoxic and trypanocidal) in two Ugandan medicinal plants. The methodology adopted was the so-called 'ping-pong' approach, involving phytochemical purification (column chromatography and preparative thin layer chromatography), alongside biological studies (cytotoxicity, antibacterial, trypanocidal and antifungal studies). Phytochemical investigations of Zanthoxylum chalybeum (seed) yielded a pure crystalline compound, 27-135D, which was characterized by 'HNMR as the alkaloid skimmianine. Studies on stem bark yielded three alkaloids 27-165A, 27-173A and 27-173B. All the above pure isolates, and the crude extracts of Z. chalybeum had neither biological activity nor cytotoxicity in the brine shrimp assay. A cytotoxic sesquiterpine, characterized as muzigadial, was isolated from W. ugandensis. It was highly toxic in the brine shrimp assay and also had in vitro trypanocidal activity against IL 3338 as well as IL1180; reference drug-resistant and drug-sensitive trypanosome strains respectively, comparable to diminazene aceturate and Geneticin (G418). Muzigadial also had antifungal activity against Candida albicans. It was concluded that the brine shrimp assay might be a useful predictor of trypanocidal activity of plant extracts and that muzigadial may be potentially valuable in the treatment of drug-resistant trypanosomosis.

Animals↗
PubMed1992

Simultaneous control of ticks and tsetse flies in Satiri, Burkina Faso, by the use of flumethrin pour on for cattle.

Treatments of 2000 cattle at monthly intervals with flumethrin pour on (1 mg active ingredient/kg b.w.) resulted in a rapid decrease of African Animal Trypanosomosis (AAT). After an initial curative treatment of the sentinel herd with diminazene aceturate (7 mg/kg b.w.) only positive cases were treated. Three applications of flumethrin were sufficient to reduce the prevalence of AAT to below 5%. Apart from a slight increase at the end of the first year the infection rate varied between 0 and 5%. A tsetse population disappeared from a heavily infested habitat after six treatments. The average tick infestation was 3-10 times lower than in a control site inspite of the repeated use of another acaricide. Between 3282 and 8624 animals were treated five times in the second year at intervals of about two months. 130 monoconical insecticide impregnated traps were deployed in habitats which were inaccessible for the cattle. The highest infection rate of the sentinel herd was 1.4%. Among another 150 eartagged cattle scattered over a district of about 1000 m2 the prevalence of AAT dropped to 4.8% at the end of the second year. Emphasis is put on an active and financial participation of the rural communities to ensure a viable campaign and good prospects of a taking over by local organizations once the external interventions have stopped.

Administration, Topical↗
PubMed1990

Evaluation of an arsenical compound (RM 110, mel Cy, Cymelarsan) against susceptible and drug-resistant Trypanosoma brucei brucei and T.b. evansi.

The trypanocidal activity of an arsenical compound (RM 110; mel Cy; Cymelarsan) was tested in susceptible and drug-resistant stocks of T.b. brucei and T.b. evansi in vitro and in vivo. The trypanosome stocks showed different levels of susceptibility in an in vitro test, their IC50 values ranging from 3-26.9 nM. Mel Cy was 2.2-2.7 times more active against T.b. brucei stocks when compared to another arsenical (mel W; Trimelarsan). The logarithmically transformed IC50 values for both drugs obtained with T.b. brucei stocks correlated significantly. Significant correlations were also found between the log IC50 values of each of the two drugs and diminazene aceturate. In mice, the least susceptible stock was cured with a single i.p. dose of mel Cy which was about 16 times higher than that needed to cure a susceptible stock.

Animals↗
PubMed1985

The treatment of kala-azar: a review with comments drawn from experience in Kenya.

Pentavalent antimony (Sbv) compounds have been used in the treatment of kala azar for over 60 years. Their introduction was preceded by the use, for a few years, of SbIII compounds, especially tartar emetic. Although the exact usage of Sbv varies from country to country, with correct use, cure rates of over 90% can, in most countries, be expected. There is little problem with toxicity, though occasional unexplained deaths that do not appear to be directly due to Sbv do occur during treatment. The main second line drugs, pentamidine and amphotericin, are less effective and relatively toxic. Other second line treatments that have been used in resistant kala azar in Kenya include allopurinol, diminazene aceturate, and Sbv liposomes. Splenectomy has been used as a last resort.

Allopurinol↗
PubMed1982

Immunosuppression in bovine trypanosomiasis: response of cattle infected with Trypanosoma congolense to foot-and-mouth disease vaccination and subsequent live virus challenge.

The primary and secondary antibody responses to foot-and-mouth disease virus vaccine were examined in cattle infected with Trypanosoma congolense and the response of some of these animals to live foot-and-mouth disease virus challenge was assessed. Infected groups of cattle had rather lower antibody responses than uninfected control cattle after primary vaccination but the antibody titres were not significantly depressed until after secondary vaccination. These levels remained depressed for the duration of the experiment, ie, 183 days. Trypanocidal therapy with diminazene aceturate of infected cattle at the time of vaccination did not significantly improve the antibody response to primary vaccination. Their subsequent response to live virus challenge was somewhat equivocal in that the number of animals protected was not significantly different in comparison to the untreated infected and uninfected controls. It was concluded that trypanosome-infected cattle do not produce optimal responses to foot-and-mouth disease vaccination. Nevertheless, the antibody titres are generally above those considered adequate to confer 95 per cent protection against needle challenge.

Animals↗
PubMed1983

Babesiosis in the Greyhound.

Babesiosis was diagnosed in five 11- to 18-day old Greyhound pups. In 3 pups, Babesia canis organisms were identified by examination of a Wright's-Giemsa-stained smear of blood. In 2 pups, the diagnosis was established by examination of a splenic impression smear obtained at necropsy. Findings in the 3 clinical cases included depression, weakness, anorexia, pallor, anemia, and thrombocytopenia. Subcutaneous administration of diminazene aceturate resulted in rapid clinical recovery in these cases. In the 2 pups that were necropsied, variable numbers of erythrocytes containing Babesia organisms were observed in the microvasculature of tissues. Subinoculation of blood into an intact dog and a splenectomized dog resulted in parasitemia and B canis serum titers, as determined by indirect fluorescent antibody testing. A site visit to the kennel from which the pups had originated led to identification of numerous Rhipicephalus sanguineus in small buildings and pens. Of 107 dogs from this kennel that were tested, 63 had an indirect fluorescent antibody titer for B canis. A limited serologic survey of Greyhound kennels in West Virginia, Oklahoma, Texas, Mississippi, and Florida identified a large number of dogs with indirect fluorescent antibody titers for B canis.

Animals↗
PubMed1994

Cerebellar ataxia as a possible complication of babesiosis in two dogs.

A 6-month-old Miniature Doberman Pinscher was presented with inappetance and cerebellar signs. Babesia canis organisms were found on a capillary bloodsmear. The cerebellar signs resolved rapidly following treatment with diminazene aceturate. A 7-month-old Siberian Husky developed cerebellar signs, blindness and quadriparesis 9 d after presentation with clinical signs typical of uncomplicated canine babesiosis. The dog responded favourably to treatment with prednisolone. Both acute and delayed cerebellar ataxia have been associated with malaria in humans. The clinical signs shown by these dogs were similar to those reported for malaria in humans. Cerebellar ataxia should be considered a possible complication of canine babesiosis.

Animals↗
PubMed1994

Evaluation of a short-term in vitro growth-inhibition test to determine susceptibility of Trypanosoma vivax stocks to various trypanocides.

Two Trypanosoma vivax stocks were initiated in culture with tsetse or culture-derived metacyclics. They were propagated axenically as bloodstream trypomastigotes at 35 degrees C in 4% CO2 in air. Populations of trypanosomes were incubated with various concentrations of antitrypanosomal compounds, namely diminazene aceturate, quinapyramine sulphate, DL-alpha-difluoromethylornithine, isometamidium chloride, suramin and melCy. Growth was monitored after 24 h of incubation and the growth inhibition was calculated. All six drugs tested showed little effect upon the growth of the parasite populations. These results indicate that a 24-h growth-inhibition test was not suitable for determining the drug susceptibility of T. vivax stocks in vitro. Neither did the results correlate with those obtained with susceptible or resistant stocks of T.b. brucei, T.b. evansi or T. simiae described in the literature, or with the results of these two T. vivax stocks tested in cattle.

Animals↗
PubMed1996

Production of autoantibodies against DNA and collagen after inoculation of rabbits with Trypanosoma equiperdum.

The aim of the study was to investigate the induction of autoantibodies in rabbits after the inoculation with Trypanosoma equiperdum. Eight female rabbits were inoculated s.c. with 5 x 10(6) parasites of Trypanosoma equiperdum. Four of these animals were treated with Diminazen (Berenil) at a dosage of 28 mg per rabbit by intramuscular injection 35 days p. i. Two additional non-infected rabbits served as negative controls. 9 days p.i. all infected animals possessed serum antibodies against Typanosoma equiperdum. Titers peaked to 1:2048, measured between 14 and 30 days p.i. and were persistent until the end of examinations. In parallel, there was an increase of anti-dsDNA and anti-collagen autoantibodies, but not of autoantibodies against recombinant U1RNP and La antigens. In comparison to patients with systemic lupus erythematosus, the anti-DNA binding of rabbit's sera was reduced more strongly in presence of increasing salt concentrations. In addition, the sera of inoculated rabbits recognized several unknown bands of a cell extract in immunoblotting. The parallel increase of antibodies against Trypanosoma, control foreign antigens, DNA and collagen suggests a polyclonal stimulation of the immune system. It was concluded that this rabbit model seems to be sufficient to investigate the mechanisms which are able to induce autoimmune phenomena.

Animals↗
PubMedDate not supplied

The influence of the exocyclic amino group characteristic of GC base pairs on molecular recognition of specific nucleotide sequences in DNA by berenil and DAPI.

The expedient of preparing homologous DNA samples substituted with inosine for guanosine residues, 2,6-diaminopurine (DAP) for adenine residues, or both, has been used to investigate the role of the purine 2-amino group in determining the preferred binding sites for the drugs berenil [1,3-bis(4-phenylamidinium) triazene] and DAPI (4',6-diamidino-2-phenyl indole) on DNA. The selectivity of these two minor groove binders for AT-rich sequences is seen to be radically altered in the substituted DNA molecules. Neither berenil nor DAPI bind to DAP-substituted DNA where all purine residues bear a 2-amino group. By contrast, they bind to AT-rich, IC-rich and even mixed sequences of the inosine DNA where all purine residues lack the 2-amino group. With the inosine and DAP double substituted DNA, both berenil and DAPI bind preferentially to IC-rich clusters instead of their canonical tracts endowed with an extra 2-amino group through substitution with DAP. These results establish that the location of the purine 2-amino group represents a critical determinant for recognition of DNA nucleotide sequences by the two drugs.

2-Aminopurine↗
PubMed2006

Quantitative analysis of DNA-porphyrin interactions.

The binding of manganese(III)-tetra(4-N-methylpyridyl)porphyrin (MnTMpyP) with synthetic poly(dA-dT)2, poly(dI-dC)2, and poly(dG-dC)2 DNAs as well as calf thymus (CT) DNA has been quantitatively studied in detail using induced CD (circular dichroism) spectroscopy in the Soret absorption band. The CD spectra, which changed greatly depending on the porphyrin to DNA base-pair molar ratio (r), were normalized with respect to DNA concentration and deconvoluted. Three independent component binding modes (named mode 1, 2, and 3 in the order of increasing r values) were identified, which successfully simulated the observed CD spectra with negligibly small residuals for a wide range of r values. In the case of poly(dA-dT)2, poly (dI-dC)2, and CT DNA, all the three modes appeared, whereas in the case of poly(dG-dC)2 DNA, only modes 1 and 3 appeared in the r range studied. The r dependence of each binding mode, i.e., its relative affinity toward DNA, has been revealed by this analysis. Mode 1, which appeared as a single binding mode at very low r values (r < or = ca. 0.05), was inhibited by the addition of methyl green, a drug that preferentially binds to the major groove of poly (dA-dT)2 DNA. Berenil, a known minor groove binder to poly(dA-dT)2 or poly(dI-dC)2 DNA, inhibited modes 2 and 3. From these inhibition experiments as well as comparison of the component spectra for DNAs of different sequence, a binding site on DNA was proposed for each component binding mode. The number of DNA base pairs covered by a single molecule of porphyrin was estimated.

Biopolymers↗
PubMed1990

Crystal structure of a berenil-dodecanucleotide complex: the role of water in sequence-specific ligand binding.

The three-dimensional structure of a complex between the dodecanucleotide d(CGCGAATTCGCG) and the anti-trypanocidal drug berenil, has been determined to a resolution of 2.5 A. The structure has been solved by molecular replacement and refined to an R factor of 0.177. A total of 49 water molecules have been located. The drug is bound at the 5'-AAT-3' region of the oligonucleotide. At one end of the drug the amidinium group is in hydrogen-bonded contact with N3 of the adenine base complementary to the thymine of the AAT. The other amidinium group does not make direct interactions with the DNA. Instead, a water molecule mediates between them. This is in hydrogen-bonded contact with an amidinium nitrogen atom, N3 of the 5' end adenine base and the ring oxygen atom of an adjacent deoxyribose. Molecular mechanics calculations have been performed on this complex, with the drug at various positions along the sequence. These show that the observed position is only 0.8 kcal/mol higher in energy than the best position. It is suggested that there is a broad energy well in the AATT region for this drug, and that water molecules as well as the neighbouring sequence, will determine precise positioning. More general aspects of minor groove binding are discussed.

Amidines↗
PubMed1993

Voltammetric behavior of berenil.

Berenil is reduced on mercury drops electrode in buffered aqueous media. The reduction of -N=N- group is controlled by diffusion. Polarographic waves are of analytical usefulness. The hydrogen discharge is favored by the basic centers of the molecule in Co(II)/ammonia-buffered media.

Diminazene↗
PubMed1993

Gametocytogenesis induction by Berenil in cultured Plasmodium falciparum.

Berenil, which is known to inhibit synthesis of nucleic acid, DNA and RNA, and polyamine, induced gametocytogenesis in cultured Plasmodium falciparum, although the mechanism by which Berenil induces gametocytogenesis is unknown. Asexual parasites of a strain of P. falciparum that seldom produce gametocytes in in vitro culture began gametocytogenesis after 2-24 hr treatment with RPMI 1640 medium containing Berenil (final concentration, 0.1-10.0 micrograms/ml) with horse serum. Gametocytogenesis was consistently observed from 3 days after the addition of Berenil to culture. After parasites were cultivated in RPMI 1640 medium containing Berenil (final concentration, 3.0-10.0 micrograms/ml) and concanavalin A with horse serum for 2 hr, Berenil and concanavalin A were removed from culture medium by centrifugation. Nevertheless, induction of gametocytogenesis was observed. The addition of concanavalin A (final concentration, 10 micrograms/ml) to RPMI 1640 medium containing Berenil enhanced the induction of gametocytogenesis by Berenil. However, when RPMI 1640 medium with concanavalin A was used without the addition of Berenil, no gametocytogenesis was observed as in RPMI 1640 medium alone.

Animals↗