Showing papers in "Annales pharmaceutiques françaises in 1990"

[Rosmarinic acid, total hydroxycinnamic derivatives and antioxidant activity of Apiaceae, Borraginaceae and Lamiceae medicinals].

Abstract: A number of medicinal species of the Apiaceae, Borraginaceae and Lamiaceae families present high rosmarinic acid and total hydroxycinnamic derivative contents. Species of genera Sanicula (Apiaceae), Lycopus, Melissa, Mentha, Origanum and Salvia (Lamiaceae) contain rosmarinic acid in large amount, more than 3%, based on dry weight. The antioxidant activity of hydroalcoholic extracts, on DPPH, is partly in relation with the hydroxycinnamic derivative content.

Teneurs en acide rosmarinique, en dérivés hydroxycinnamiques totaux et activité antioxydante chez les apiacées, les borraginacées et les laminacées médicinales

Abstract: Un certain nombre d'especes medicinales appartenant aux familles des Apiacees, des Borraginacees et des Lamiacees presentent des teneurs importantes en acide rosmarinique et en derives hydroxycinnamiques totaux. Les especes etudiees des genres Sanicula (Apiacees), Lycopus, Melissa, Mentha, Origanum et Salvia (Lamiacees) renferment, en poids sec, plus de 3% d'acide rosmarinique. L'activite antioxydante des extraits hydroalcooliques sur le DPPH est en partie liee aux teneurs en derives hydroxycinnamiques

Research of antifungal substances secreted by higher fungi in culture

Abstract: A screening in vitro of antifungic activity of 24 strains of Basidiomycetes was realized with their culture filtrate. Lycoperdon perlatum Pers. = Pers., Oudemansiella platyphylla (Pers. ex Fr.) Mos., Agrocybe dura (Bolt) Singer have shown an activity against Candida albicans, Candida tropicalis and Aspergillus fumigatus; Pholiota spumosa (Fr.) Singer towards Botrytis cinerea and Lycoperdon perlatum Pers. = Pers. towards Alternaria solani, Botrytis cinerea and Verticillium dahliae. More extensive studies of the kinetics of antifungic substances production from Lycoperdon perlatum Pers. = Pers. were effectued with 2 different media and 2 different seeding technics on the strains which were sensible to the inhibitory character of this Gasteromycete.

Teneur en tanins et activite inhibitrice de l'elastase chez les rosaceae

Abstract: From 42 Rosaceae species, only the Rosoideae species exhibit high tannin content and elastase inhibiting activity such as Filipendula ulmaria, Geum montanum, G. rivale, Alchemilla xanthochlora and Sanguisorba minor. Other studied species from Spiraeoideae, Maloideae and Prunoideae subfamilies are less rich in tannin and also less active.

Alkaloids and flavonoid from aerial parts of Hammada articulata ssp. scoparia

Abstract: Two alkaloids (N-methylisosalsoline and carnegine) had been previously described from the aerial parts of Hammada articulata ssp. scoparia. A thorough study of this plant material has now led to the isolation of eight minor alkaloids and one flavonoid. The alkaloids include four isoquinolines (isosalsoline, salsolidine, dehydrosalsolidine and isosalsolidine), one isoquinolone (N-methylcorydaldine), tryptamine, N-omega-methyltryptamine and one beta-carboline (tetrahydroharman). The flavonoid has been identified as isorhamnetin-3-O-beta-D-robinobioside. The structures have been elucidated on the basis of spectral data, mainly mass spectrometry (D-IC) and 1H NMR.

[Antibacterial activity of extracts from plants used in preparation as antidiarrheals at Kinshasa, Zaire].

Abstract: A preliminary and anterior bacteriological study about 38 plant antidiarrheic traditional preparations, has demonstrated that 35 of them have bactericidal activity Thirty inhibit the growth of all select germs and 5 exert this bactericidal effect on some germs Some extracts proceeding of these possess a bactericidal activity, specially if they contain polyphenols (flavonoids, catechics tanins), saponins and alkaloids

[Antispasmodic activity of extracts from plants used as anti-diarrhea preparations in Kinshasa, Zaïre].

Abstract: A preliminary and anterior pharmacological study about 68 plant antidiarrheic traditional preparations, has proved the antispasmodic activity for 42 of them. Some extracts proceeding of these possess an antispasmodic activity, specially if they contain polyphenols (flavonoids, catechics tanins), saponins and alkaloids.

In vitro evaluation of antimicrobial activity of fusafungine

Abstract: Fusafungine is an antibiotic extracted from the fungus Fusarium laterium WR strain 437. The antimicrobial activity of fusafungine was determined on strains from laboratory collections and clinical isolates; since fusafungine is not soluble in the classical media, the usual techniques had to be modified. MICs for all the Gram-positive cocci and bacteria tested, aerobic, or anaerobic, were below 30 mcg/ml. The antimicrobial activity included Mycoplasma pneumoniae (MIC less than 18 mcg/ml) and Streptococcus mutans (MIC less than 30 mcg/ml). An antifungal activity was shown for most of the Candida albicans tested (MIC less than 32 mcg/ml) and for different Nocardia sp. (MIC less than 13 mcg/ml). Moreover, fusafungine induced neither acquired resistance nor cross-resistance towards the antibiotics classically used in therapy.

Hétérosides des feuilles de Mussaenda arcuata Lam. ex Poiret.

Abstract: Fractionation of the methanolic extract of Mussaenda arcuata leaves resulted in the isolation of four flavonoid glycosides and of two phenylpropanoid derivatives. The flavonoids were identified as astragalin 2, isoquercitrin 3, kaempferol-3-O-beta-D-rutinoside 5 and rutin 6 and the two phenylpropanoid derivatives as melilotoside 4 and dihydromelilotoside 1. This latter compound is a novel natural product. The structures of compounds 1-6 have been elucidated on the basis of their spectral data and of those of their acetyl derivatives.

[Effect of some GABA, glycine, or glutamic acid derivatives on the forced swimming test in mice].

Abstract: Three GABA derivatives, the GABA-steatamide (GS), the GABA-linoleamide (GL) and the progabide, two glycine derivatives, the glycine-steatamide (SG) and the glycine-linoleamide (LG) and, lastly, a glutamic acid derivative, the glutamic acid palmitamide (PGt), were studied in the forced swimming test (Porsolt's test) on mice. The anti-immobility effect, referring to the existence of antidepressive properties, was significant for the SG, LG, GL and PGt. It seems that the relative intensity of the anti-immobility effect on the one hand and the sedative properties on the other, could operate on the experimental profile of these derivatives in the Porsolt's test.

[Synthesis of new fluorogenic substrates derivated of 7-amino-4-trifluoromethylcoumarin. Detection of gram-negative bacteria, Streptococci group A and Enterococci].

Abstract: The synthesis of substrates having 7-amino 4-trifluoromethyl coumarin as fluorogenic reagent is described. The first group is performed from L-alanine derivative in order to investigate L-alanine aminopeptidase activity for the detection of Gram-negative bacteria. The second group is synthesized from the L-pyrrolidon carboxylic acid. It allows us to detect the PYRase activity of group A Streptococci and Enterococci. These substrates are evaluated with the N-protected form and the amino free one.

Chemical and pharmacological study of Phragmites communis Trin

Abstract: A chemical study of the aerial parts of Phragmites communis Trin. concerning free amino-acids, fatty acids, sterols, tocopherols and polyphenols has been carried out. The amino-acids content was studied at two different periods (winter, summer) in order to elucidate differences. The isolated polyphenols were investigated for antibacteriophage properties.

[Fungal spores in the atmosphere at Besançon, France: seasonal and annual variations during 1988 and 1989].

Abstract: Airborne spora in the atmosphere of Besancon were weekly determined, searching links between appearance of species and seasonal allergies. By comparison of the results of the two years, it is easy to see many variations. At first, the number of colonies collected is very different, 2,990 colonies in 1988, 9,841 in 1989. During 1989, some genera are present in greatest quantities. It is the case of Cladosporium and Epicoccum in summer and Aspergillus in autumn. For the allergologists, Alternaria, very abundant during 1989, is perhaps the outstanding incident, this genus being considerated as very allergenic.

Isolation of human thrombin by affinity chromatography with silicate to be used in the preparation of biological glue

Abstract: At present the preparations of fibrin glue used a thrombin from equine or bovine origin. In order to remove the problems of antigenicity we developed a method of purification from acidified plasma. We used one affinity chromatography on benzamidine-Spherodex and compared three methods of elution: non specific (sodium chloride gradient) and biospecific competitors (arginin methylester or benzamidin). The yield is evaluated between 64 and 84% and the purification factor close to 160. The obtained thrombin is better than animal thrombin in the preparations of fibrin glue.

Effets de l'aescine et de l'aesculine sur l'excrétion rénale d'eau et d'électrolytes chez le rat.

Abstract: Effects of aescine and aesculine, active principles of the horsechestnut, on urinary excretion of water and electrolytes, were investigated in saline loaded rats. Results indicate that aesculin shows a moderated diuretic activity, increasing significantly the renal loss of sodium, chloride and potassium. Nevertheless, only the highest dose of aescine caused the same degree of minease in saluresis with aesculin, where a doses-response relationship was observed.

Quality control and optimization of therapeutic activity with the use of thermoanalytic methods

Abstract: Thermogravimetry, differential scanning calorimetry, thermomicroscopy, transparency measure permit drug quality control: knowledge of solvated or unsolvated mole, thermal stability, identification of crystalline form (polymorphism) quick determination of total impurity with graphs. These methods can be used for therapeutic activity optimization of very weakly soluble drugs: research of the polymorph showing the best kinetic dissolution, establishment of phase diagram drug/inert substance by example for determination invariant composition particularly eutectic for which the drug solubility is increased.

Preparation of derivatives of the aldehydic functions of gossypol

Abstract: Several new derivatives of the aldehydic functions of (+/-) gossypol are described: an hydrosoluble hydrazide resulting from the reaction with the Girard's reagent T and Schiff bases with polyamines. The condensation between the two aldehyde groups and cadaverine, putrescine or spermidine gives macrocyclic bridged products. A disubstituted non cyclic derivative is obtained with an excess of cadaverine. These products are of biological interest.

Comparison of refractometric and ultraviolet detection methods in lactulose assay by high performance liquid chromatography

Abstract: Dosage of lactulose and determination of related sugars (lactose, fructose, galactose, epilactose) were undertaken by high performance liquid chromatography (HPLC). The present note described two modes of detection used simultaneously and compared: refractive index detector (RI) and multiwavelength ultraviolet detector (UV). HPLC is performed with an aminopropylsylil phase as stationary phase and an isocratic mobile phase containing acetonitrile and aqueous sodium phosphate. The results are outlined and discussed.

Effect of buprenorphine on external pancreatic secretion in rats

Abstract: 2-deoxyglucose stimulates pancreatic secretion through a mainly vagal neural pathway. Buprenorphine antagonized this stimulation in a dose-related fashion between 0.017 and 0.45 mg/kg. i.v. The effect of buprenorphine was suppressed by naloxone, but not by alpha and beta-adrenoceptor blocking agents. The effect of methadone was similar, at doses about ten times larger.

[Synthesis and biological activity of 2-dialkylaminoalkoxybenzylidene-benzo-(b)-cyclanones].

Abstract: The synthesis and the study of the cardiovascular and antiallergic properties of 2-(4-dialkylaminoalkoxybenzylidene)-benzo-[b]-1-cyclanones analogues to benzarone and amiodarone were performed. They showed the influence of the length of the basic dialkylaminoalkoxy group and that of a methoxy substitutant of the tetralone on the studied activities.

[Working hypothesis for the effect of GABAergic, glycinergic or glutamatergic drugs in the treatment of Parkinson disease].

Abstract: The data obtained during the past decade in experimental and clinical pharmacology show that the GABAergic drugs, with central activity, do not ameliorate the symptoms of the Parkinson's disease (PD), but would worsen the akineto-rigid syndrome, the dyskinesias and the deteriorating mental status in the later stages of the PD. On the other hand, recent data of experimental pharmacology suggest the possibility that glycinergic or glutamatergic derivatives, with central activity, would have a beneficial effect on the syndromes of the later stages of PD (declining efficacy of L-DOPA, dyskinesias, deteriorating mental status), which constitute, with the fluctuation of the response to L-DOPA, ("on-off" effects), the major problems of the PD's treatment. Some theoretical and experimental data also suggest the possibility of a beneficial effect of the glutamatergic drugs in the treatment of the "on-off" effects.

[Are there glutamatergic, anti-GABAergic or antiglycinergic components in the action mechanism of adamantamines? Study of convulsions induced by amantadine or 1-adamantylcyclopentanamine in mice].

Abstract: Convulsions induced on mice by a dose of 200 mg/kg i.p. of amantadine (Ama) or 1-adamantylcyclopentanamine (Ad1) were studied with tricyclic antidepressants (imipramine, desipramine, chlorimipramine), possessing antiglutamatergic properties, or with GABA-linoleamide, a centrally acting GABAergic drug, or with glycine-linoleamide, a centrally acting glycinergic drug, or with glutamic acid palmitamide, a centrally acting glutamatergic drug. The results of these studies could suggest the existence of important glutamatergic and anti-GABAergic components and, probably, of a slight antiglycinergic activity in the pharmacological action profile of the Ad1. Moderate glutamatergic and anti-GABAergic components could operate in the Ama's mechanism of action.

[Comparison of two Elapidae venoms: Naja naja and Naja nigricollis].

Abstract: In our study on the identification of snake venoms by electrofocusing technics, the protein profiles of Naja naja naja, Naja nigricollis pallida and Naja nigricollis West Africa were compared. The typical profile of venoms of Elapidae was easily identified in this comparison. The two species could easily be differentiated, whereas the differences between the two sub-species were more difficult to evidence, since they are geographic variants of the same type.

[New route of 2-N-(carboxypropylamino)-2-deoxy-D-glucopyranose synthesis].

Abstract: A new route to 2-N-(carboxypropylamino)-2-deoxy-D-glucopyranose synthesis is reported, involving the Schiff-base derivative of beta-D-glucosamine with benzyl 4-oxobutyrate. Improvement in the synthesis of benzyl-4-oxobutyrate is also described. Biological compounds action was investigated by evaluating sedative and dopaminergic activities on male mice.

Degradation of diazepam in aqueous solution. Simulation essay by action of diluted hydrogen peroxide

Abstract: The mild oxidation of diazepam by hydrogen peroxide in neutral medium at room temperature in daylight is reported. The oxidation product has been isolated and purified and its purity determined by thin layer chromatography. It has been identified by spectroscopy, chiefly by infrared and mass spectroscopy. Finally it has been compared, by high pressure liquid chromatography, to the product from an aqueous diazepam solution placed 6 months at room temperature in daylight.

[Comparative study of the toxicity of cyanic derivatives and/or aromatic amides].

Abstract: The toxical potentiality of the cyanic radicle and the detoxicating characteristic of the amide group are studied following the evolution of the benzonitrile and benzamide toxicity when a cyanic or amide radicle is added to the original molecule. This comparative study shows that the presence of amide group has not always given a higher toxicity to the organic molecules that own it. It is the respective localization of the cyanic or amide radicles which appears to play the most important role.

[Contribution of parachor to the study of structure-activity relationship. Aromatase inhibitor activity of androstenediones].

Abstract: Parachor has been used extensively in physical organic chemistry for structure determination, but rarely in quantitative correlation of structure and biological activity. The purpose of this study is the contribution of the parachor in the QSAR of androstenediones derivatives and their inhibition of aromatase enzyme. Good correlations were obtained for two classes of steroids inhibitors of oestrogens biosynthesis.

Problems posed by the development of exogenous surfactants for the treatment of hyaline membrane disease

Abstract: The hyaline membrane disease (HMD) is a respiratory distress occurring at birth of some premature infants, attributed to an endogenous pulmonary surfactant deficiency. The present treatments are iatrogenic and inefficient for the most diseased infants. The exogenous surfactant supplementation intends to give to the baby formulations playing in vivo the role of the natural surfactant. The research developed for the formulation and the diffusion of these exogenous surfactants have to solve physicochemical problems but also of industrial production and of safety use. In spite of their adequate physicochemical and pharmacological properties, surfactants of natural sources, for industrial grounds, are not still distributed at a large scale. The efficiency of artificial surfactants is variable, and the use of non-biodegradable molecules in several preparations let to safety problems. The development of new types of artificial surfactants, more efficient and safe, implies a better knowledge of the physico-chemical mechanisms intervening in the pulmonary surfactant dynamics.