[p-arsanilic acid derivatives: N-substitution effects on parasiticide activity (author's transl)].
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Biomedical subjects
Publications and source records attributed to P Timon-David.
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The effect of Paragerm spray from either a hand pressurized can or from a general room mist device (MCR device) on mattress mite populations was compared with the effect of a control spray. After 1 month a reduction in mite population due to the cleaning procedures was evident in the control treated mattresses; Paragerm treated mattresses had significantly fewer mites, notably those treated with the aerosol can spray, nine out of fifteen of which were mite free. Dissection of the mattresses showed that some mites survive and they could form the nucleus from which reinfestation could occur.
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Attempts to reduce the growth of house dust pyroglyphid mites by vacuum cleaning, and modifications of temperature and humidity are useful but not sufficient. Their absence in dust from hospital beds which are disinfected led the authors to test PARAGERM AK, a non toxic bactericidal and fungicidal spray. This proved highly effective as an acaricide, killing off cultures of Dermatophagoides spp. and other mites with acceptable and easily produced concentrations, thus providing a new way of combating the house dust allergy mite.
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Harmane, harmine, and harmaline were investigated for their in vitro antileishmanial activity toward parasites of the species Leishmania infantum. Harmane and Harmine displayed a moderate antiproliferative activity toward human monocytes and exerted a weak antileishmanial activity toward both the promastigote and the amastigote forms of the parasite. Their mechanism of action on the promastigote form of the parasite involved interactions with DNA metabolism leading to an accumulation of parasites in the S-G(2)M phases of the cell-cycle. Harmaline, at the contrary, was deprived from toxicity toward human cells and Leishmania promastigotes, however it exerted a strong antileishmanial activity toward the intracellular amastigote form of the parasite. This property was shown to partly result from the capacity of the molecule to prevent parasite internalization within macrophages by inhibiting Leishmania PKC activity.
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The resistance of plasmodiums to the current antimalarial agents has spurred the search for new active molecules of vegetal origin or chemical synthesis. The screening of antimalarial molecules "in vitro" was done by simple but tedious techniques such as quantification of parasitemia through optical microscopy or by using radioactive markers. We have developed a new method to evaluate parasitemia by using the ODAM ATC 3000 flow cytometer and biological cell sorter. We selected the ethidium bromide for labelling the nucleic acids of Plasmodium falciparum, and we optimised the method by using a mathematical model: the design of Hadamar. This simple technique presents the advantage of being an objective and rapid count of large number of red cells (10(6) x 10(7)). This method is rapid, reliable, reproducible, devoid of subjectivity and provides more precise results than those of optical microscopy. The good correlation between paraitemia measured by optical microscopy and fluorescence obtained by flow cytometry allows us to recommend this technic for the screening of new antimalarial molecules.
Various hydrazones of thiophene carboxaldehyde were tested in vitro on two Plasmodium falciparum strains and in vivo on mice experimentally infected with Plasmodium berghei. These hydrazones were obtained by condensation of appropriate hydrazines with thiophene-2-carboxaldehyde (series 1), thiophene-3- carboxaldehyde (series 2) and 5-Nitrothiophene-2-carboxaldehyde (series 3). Compounds of series 3, 5-Nitrothiophene-2-carboxaldehyde presented significant effects in vitro. In vivo tests confirmed the antimalarial activity observed in vitro with two compounds of this series.
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The authors sum up the principal morphological, biological and ecological characteristics of the human lice. Moreover they recall the therapeutic and prophylactic measures which could be used against them, and they bring to mind their "in vitro and in vivo" research technics on comparative effectiveness of certain insecticides against head lice.
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Acetyl-cysteine, its origin, nature, the constitution of its molecule and its main properties are reviewed. This study involved essentially the best means of using the mucolytic properties of this amino acid. Acetyl-cysteine has an excellent detergent effect on the mucosa, with good evacuation, and favourises the adhesion of barium, all the better when the particles of the latter are finer. It is thus possible to obtain good thin layer and double contrast pictures. Prior preparation remains of the utmost importance.
We report our first 100 cases of Alzheimer's (AD) patients treated with tacrine (Cognex) for a period of one year. At the beginning of treatment the mean Mini-Mental-Status (MMS) score was 15.1. To date 71 patients are still under treatment (12 for more than 12 months). Forty-three instances of side-effects were observed, of which 31 involved hepatic side-effects with an increase in ALAT > IN (normal value) (6 cases > 3N), the mean date of appearance was 10.4 +/- 6.8 weeks, there were 16 cholinergic side-effects (nausea, vomiting, diarrhoea), plus 4 neurologic and 2 cutaneous side-effects. These side-effects led to the arrest of the treatment in 19 cases (16 for hepatic toxicity). Treatment was reattempted after interruption in 13 cases; successfully in 3 instances only. The measure of tacrine efficacy was based on 52 MMS score re-evaluations in week 18: there was an increase of the MMS score in 22 cases (3.3 points +/- 2.5), a stabilisation in 11 cases and a decrease in 19 cases (3.3 points +/- 2.2.). In week 30, the MMS scores (35 patients) increased in 9 cases (3.6 points +/- 2.4), stabilized in 5 cases and decreased in 21 cases (3.9 points +/- 3.3). At week 52, only 28 per cent of the patients were considered as either improved or stabilized. We conclude that there is a necessity for close follow-up of tacrine-treated patients, and that globally at 8 months there is an improvement or a stabilization in 40 per cent of patients and long term (at one year) a stabilizing effect on AD patients.