Synthesis of epoxypropyloxy chromones and allyl hydroxy chromones and in vitro-in vivo activity on protoscoleces of Echinococcus multilocularis (Cestoda).

Derivatives with epoxypropyloxy, allyloxy and allyl hydroxychromone structures were synthesized and tested against protoscoleces of Echinococcus multilocularis. Compounds IV-IX were tested in vitro and compound VII proved the most active of them with, at 0.1 mmol.L-1, 98% dead protoscoleces in open vesicles after 24 hours and 80% in closed vesicles within 96 hours. Compound VII was tested in vivo on Meriones unguiculatus infested by Echinococcus multilocularis, but was found to be rather inactive.

[Severe hyponatremia disclosing adenohypophyseal insufficiency with empty sella syndrome]. / Hyponatrémie sévère révélatrice d'une insuffisance anté-hypophysaire avec selle turcique vide.

We report a case of extremely severe hyponatraemia which led to the discovery of anterior hypophysis insufficiency associated with empty sella turcica in a dysimmune context. This type of hyponatraemia is consecutive to corticotropic and thyreo-tropic hormones deficiency and to inappropriate secretion of arginine vasopressin. These endocrine abnormalities are of suprapituitary origin. They can be explained by a hypothalamo-hypophyseal dysregulation of little known mechanism, or by a lesion of the hypothalamus.

Synthesis and in vitro activity of alkylaminoalkyloxy chromones on protoscoleces of Echinococcus multilocularis (Cestoda).

Twelve derivatives with alkylaminoalkyloxy chromone structures were synthesized and tested upon protoscoleces of Echinococcus multilocularis metacestode kept alive in vitro. Assays were performed with protoscoleces attached to the germinal layer in open and in closed vesicles. Compounds IVb and IIIe at the concentration of 0.1 mmol.L-1 killed 50% of the protoscoleces in open vesicles in 48 hours and compound IVb killed 100% of the protoscoleces in open vesicles within 96 hours at the same concentration. In closed vesicles after four days compound IVb killed all protoscoleces, compounds IIIe and IVd half of them, whereas in the controls all protoscoleces were alive. Trifluoperazine (TFP) was the reference compound; none of the new compounds showed better activity than TFP.

[Contribution of intra-operative measurement of intact parathormone in surgery for primary hyperparathyroidism]. / Apport du dosage per-opératoire de la parathormone intacte dans la chirurgie de l'hyperparathyroidie primaire.

Using a sensitive two-site immunoradiometric assay which detects intact parathormone (iPTH), we studied the decrease in peripheric and jugular plasmatic iPTH during surgical removal of abnormal parathyroid (s). In the next future, results of intact parathormone (iPTH) assay will be given in 45 minutes. In a prospective study of 33 patients operated on for hyperparathyroidism or for cold thyroid nodule, the serum levels of intact PTH was measured intraoperatively in peripheric and in jugular blood. The preoperative mean serum iPTH concentration was 119.23 +/- 172.48 pg/ml and fell to 34.5 +/- 32.21 pg/ml after surgery in 14 cases of primary hyperparathyroidism (p < 0.001). Thirteen out of 14 patients had serum iPTH values less than 65 pg/ml within 15 minutes after parathyroidectomy. The preoperative mean serum iPTH concentration in the 5 secondary hyperparathyroidism was 781.2 +/- 403.19 pg/ml. This value fell to 124 +/- 66.91 pg/ml after parathyroidectomy (p < 0.04). No significant decrease was observed in the mean serum concentration of the 14 patients operated on for cold thyroid nodule. Patients suffering from single parathyroid adenoma presented a significant gradient in jugular plasmatic PTH concentration between the adenoma side and the contralateral one. This gradient decreased during effective parathyroid adenomectomy (309.7 +/- 313.3 pg/ml to 3.7 +/- 35.1 pg/ml). Intraoperative serum iPTH concentration will provide a valuable tool to appreciate the effectiveness of surgical removal of parathyroid glands and to detect the location of parathyroid adenoma when the surgical research is negative.

Potential anti-echinococcal activity of alkylaminoethers.

Trans 2-phenoxy cyclohexanol ethers (IA, IIA, IIIA, IVA, VA, and VIA), the cyclohexanol analog (IB) and one coumarinic compound (IC) were obtained and their activity against Echinococcus multilocularis metacestodes was studied and compared with that of trifluoperazine (TFP). All of these compounds are analogous to IA and belong to three classes. Class A comprises trans 2-phenoxycyclohexanol aminoethers whose alkylaminoether group varies; compound VIA bears one more methylene in its aminoether group than does compound IA. Class B consists of one compound exhibiting no phenoxy function. Class C comprises one coumarinic analog. In vitro assays were performed using metacestodes whose protoscoleces were attached to the germinal layer in open and in closed vesicles. Compounds IA and IIA exhibited the highest activity, but it was lower than that displayed by TFP under the same conditions. Compound IA was tested in an in vivo assay in jirds (50 mg/kg/daily beginning at 80 days p.i.); it produced results that were analogous to those obtained using TFP without inducing the neuroleptic effect associated with the latter. After 40-90 days' treatment, the percentage of diminution in the entire parasitic mass in the jirds that survived minimal treatment (71%) was about 41% as compared with that in untreated jirds. Histologic examination of the parasites in treated jirds revealed numerous dead protoscoleces and some parasitic dedifferentiated cells. This parasitic response may indicate that in alveolar echinococcosis, these drugs exhibit only a parasitostatic effect.

[Efficacy of azidothymidine in thrombopenia associated with HIV infection]. / Efficacité de l'azidothymidine sur la thrombopénie associée à l'infection par le virus HIV.

We report an observation where a patient suffering HIV related thrombocytopenia was followed up for 23 months. Introduction or reintroduction of azidothymidine obtained a raise of platelet rate. When azidothymidine was stopped, platelet rate climbed down. This observation is in agreement with recent data suggesting efficiency of azidothymidine on HIV related thrombocytopenia.

Echinococcus multilocularis metacestodes: biochemical and ultrastructural investigations on the effect of isatin (2-3 indoline dione) in vivo.

A study on the biochemical and ultrastructural effects of isatin on Echinococcus multilocularis metacestodes in Meriones unguiculatus is reported. In the metacestode, after an 18 day treatment period, the alkaline phosphatase and lactate dehydrogenase activities decreased and the acid phosphatase activity increased. Glucose and glycogen stores declined significantly. Examinations of the ultrastructure revealed an increase of lysosomes and phagocytic reactions. The protoscolesces were damaged and an abnormal striated process appeared. The tegumental cytoplasmic syncytium remained unaltered. These observations suggest that isatin derivatives may have a role in the chemotherapy of infections caused by Echinococcus spp.

Physicochemical characteristics of Listeria specific antigen 2.

Listeria specific antigen 2 (Ag2) was purified to within 97% of homogeneity, with a high yield, using both gel filtration and polyacrylamide gel electrophoresis. Ag2 is a glycoprotein. Its isoelectric point is about 4.2. As determined by sodium dodecyl sulphate-polyacrylamid gel electrophoresis, its molecular weight in 16710 +/- 450. Ag2 may aggregate easily since it was previously found in gel filtration in a peak corresponding to a molecular weight of 160000. No enzyme activity has been found in Ag2.

[Study of the Sporothrix schenkii (yeast forms) extract. Electrophoretic and immunoelectrophoretic analyses: characterization of enzymatic activities]. / Etude d'un extrait de Sporothrix schenckii (forme levure). Analyse électrophorétique et immunoélectrophorétique; caracterisation des activités enzymatiques.

An extract from living yeast forms of S. schenckii was prepared. The yeasts originated from a shake culture in B.H.I. broth (Difco) incubated for 3 days at 35 degrees C in darkness; they were harvested, washed and disrupted with glass beads in a model MSK Braun mechanical cell homogenizer; a freezing-thawing was added to improve the extract. After electrophoretic separation in agarose gel, the extract's components were characterized by their enzymic activity; with this technique, 30 bands were revealed. These enzymic activities were also investigated on the antigenic fractions of the extract revealed by a rabbit hyperimmunserum: 16 among 22 immunoprecipitates are identified by their catalytic properties. Study of the earliest precipitating antibodies (appearing-order and enzymic caracterization) in rabbits just immunized completes this work. How to ameliorate the quality of the extract by culture and extraction conditions is also specified.

[Comparative enzymatic study of two strains of Aspergillus fumigatus and of A. fischeri of sapropytic origin or isolated from human or animal lesions: practical diagnostic applications]. / Etude enzymologique comparee de souches de Aspergillius fumigatus et de A. fischeri d'origine saprophytique ou isolees de lesions humaines ou animales. repercussions pratiques d'ordre diagnostique

14 enzymatic activities (3 dehydrogenases and 11 hydrolases) were systematically investigated in the extracts of 2 strains of Aspergillus fischeri and 14 strains of A. fumigatus (8 isolated from human or animal lesions named 'pathogenic' strains and 6 strains of saprophytic origin). The enzymic composition of A. fumigatus appeared to be very different from one strain to another but no relationships could be established between enzymic differences and origin of the strains. In addition, the immunoelectrophoretic analysis of these antigenic extracts using rabbits immunsera and sera of patients with pulmonary asperigllosis was performed. The type II chymotrypsic activity, corresponding to C arc, was shown more frequently and gave stronger reaction when antigenic extracts from pathogenic strains were allowed to react with sera of patients. Moreover, when sera of patients revealed a same enzymic activity in a saprophytic strain and a pathogenic strain, the number of precipitin lines was significantly larger with the latter one. Accordingly, antigenic extracts used for precipitin tests had to be preferably prepared from pathogenic strains and tested, for value, against sera of patients with pulmonary aspergillosis.