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Biomedical subjects

C Brunet

Publications and source records attributed to C Brunet.

At least 163 records · Page 9Linked to original sources
PubMed1985

Pharmacological study of nine antimicrotubular drugs with acrylophenone structure on Triton WR 1339-induced hyperlipidemia in rats.

Nine (amino-methyl)-2 acrylophenone derivatives having in vitro antimicrotubular activities very similar to those of colchicine are tested on Triton WR 1339-induced hyperlipidemia in rats. By producing a disorganization of the microtubular system, these drugs reduce the lipoprotein secretory process from hepatocytes, and more particularly the triglyceride-rich VLDL secretory process, such that the serum triglyceride, cholesterol and phospholipid levels are decreased. On the other hand, HDL-cholesterol and HDL-phospholipids are increased in a significant manner. Other studies show that serum apoprotein B levels are decreased while serum apoprotein A1 levels are increased. These results are interesting since atherogenous risk is now known to be dyslipemia-related, and is not the same according to the fact that lipids are bound to one or another lipoprotein. Among the four most effective compounds (5,7,8 and 9) three of them possess a methoxy group on the aromatic ring, which seems to distinguish that series from the other two.

Animals↗
PubMed1984

Anatomical bases of the transhiatus approach to the greater splanchnic nerve.

The level of origin and mode of constitution of the greater splanchnic nerve and its relations in the posterior mediastinum were studied. The aim of this work was to identify the anatomical basis of the transhiatus approach to the right and left greater splanchnic nerves. The azygos venous system was seen to be the main anatomical relation of these nerves. The results of this study should allow the surgeon to perform total bilateral neurotomy.

Humans↗
PubMed1984

2-(4-methyl-1-piperazinylmethyl) acrylophenone dihydrochloride: a new antimicrotubular drug.

With the relation between chemical structure and pharmacological activity as a guide, we have been for some time synthetizing a wide range of beta-amino-ketone derivatives. One of them, 2-(4-methyl-1-piperazinylmethyl) acrylophenone, MPMAP, possesses antimicrotubular activities. This product inhibits 50% of the microtubule polymerization at a 3.10(-5) M concentration. It does not prevent tubulin paracrystal formation induced by vinblastine, and binding experiments reveal that this product is a weak inhibitor of colchicine binding. The structure of this compound is different from the other antimicrotubular agents and has the advantage of being far less complex, highly soluble and easy to synthesize. Thus, this product and related compounds should be a new tool for the study of antimicrotubular activities and tubulin assembly.

Animals↗
PubMed1984

Preliminary note: effect of microtubule inhibitors with acrylophenone structure on Triton WR 1339 induced hyperlipidemia in rats.

Acrylophenone derivatives having in vitro antimicrotubular activity very similar to that of Colchicine were tested on Triton WR 1339 induced hyperlipidemia in rats. By inducing a disorganization of the microtubular system these compounds decreased the movement of very low density lipoproteins (VLDL) to the extracellular space and consequently decreased hypertriglyceridemia. On the other hand, contrary to Colchicine, these derivatives decreased cholesterolemia more significantly and this could be explained by a second action mechanism.

Acrylates↗
PubMed1984

[Alkyl-6-benzoxazolinones. A chemical and pharmacodynamic study].

A series of 6-alkylbenzoxazolinones was synthesized by reduction of corresponding acyl derivatives. Two reduction processes were used, Clemmensen reduction and triethylsilane-trifluoroacetic acid reduction, but only the latter represents a general procedure for synthesis of alkyl derivatives. Pharmacological study shows that reduction of the carbonyl group is accompanied by a decrease of analgesic activity with appearance of a psycholeptic profile.

Analgesics↗
PubMed1984

Antimicrotubular effects of ethacrynic acid.

Ethacrynic acid is a well known diuretic drug. We present here evidence that this compound is also an antimicrotubular agent which inhibits the brain tubulin polymerization and can displace 3H colchicine from its binding site. Since 2-mercaptoethanol reversibly inhibits the anti-microtubular properties, we conclude that ethacrynic acid binds covalently to brain tubulin through a cysteine near the colchicine site.

Animals↗
PubMed1984

Binding of colchicine to beef brain tubulin: influence of methodology on binding constants.

We have evaluated the effects that methodology (incubation time, concentration of beef brain tubulin) have on the measurement of the interaction of tubulin with colchicine. The results show that, with DEAE filter paper assay, binding is maximal for 3 hr of incubation at 37 degrees C, and for low concentrations of tubulin (0.05 mg/ml). In these conditions binding constants determined with SCATCHARD plot are: constant of dissociation (KD) of complex tubulin-colchicine equal to 9.8 X 10(-7) M and stechiometry equal to 0.57 mole of colchicine bound for 1 mole of tubulin dimer. Competition of drugs with colchicine binding site may be evaluated with this methodology. IC50 and affinity constants (Ki) of podophyllotoxin, a competitive inhibitor of colchicine-binding determined with these experimental conditions were 1.3 X 10(-6) M and 1.1 X 10(-6) M, respectively.

Animals↗
PubMed1984

[Systematization of the musculo-tendinous architecture of the human biceps (musculus biceps brachii)].

The structure of the brachial biceps is studied based upon the bilateral dissections of six subjects. The object of this work consists of determining the distribution of the group and muscular fibers in relation to the two proximal insertions and the two distal insertions. It is possible to describe the subgroups within each structure. The objective of each of these subgroups is considered within the framework of the coordination between the two muscular formation and the double insertions on the structure of the forearm. It is probable that this muscular formation corresponds to two different movements of the forearm during the locomotory progression. This work can be utilised in the sphere of the comparative biomechanical observation. Also electromyographic and the histochemical characteristics of the muscular group.

Arm↗
PubMed1983

Lymphocytes T and pharmacokinetics after a single oral dose of levamisole in healthy and cancer subjects.

Levamisole, an anthelmintic drug with immunopotentiating activity, is shown to have variable effects on cell-mediated immunity. We have studied the effect of a single oral dose (2.5 mg/kg or 5 mg/kg) on early and spontaneous E rosettes percentages in healthy and cancer patients. Pharmacokinetic study of this compound was conducted in parallel. The results indicated that single administration of levamisole (2.5 mg/kg) in healthy men can promote an increase of early E rosettes with mean peak plasma level of 0.8 micrograms. ml-1. On the other hand, there was no change in the proportion of early E rosettes in cancer patients and in the proportion of spontaneous E rosettes in healthy and cancer subjects.

Humans↗
PubMed1983

[Topographic distribution of arsenous anhydride in pregnant mice using macroscopic autoradiography].

Radioactive arsenic trioxide is given to pregnant mice in order to complete a recent pharmacokinetics study in the same species and to investigate an eventual transplacental passage, whole body autoradiographic study is performed in the mouse after a single administration of that compound considering its fast elimination process. Both in mice and foetus a fixation has particularly kept our attention: the radioactivity is well fixed in the bone marrow and it might be related to some malformations which occur in the newborns.

Animals↗
PubMed1982

Chemical and pharmacological studies of anorectic drugs with phenylpiperazinyl structure.

Chemical and pharmacological properties of potent anorectic compounds with phenylpiperazinyl structure were studied. Among them, the three derivatives having the most interesting anorectic activity are product VI obtained by pharmacomodulation from amfepramone and the compounds IV and V, analogs of GABA. The derivative VI possesses an anorectic activity very similar to that of fenfluramine, namely: modification of feeding behaviour in treated rats, wasting away and decrease of adipose tissue. The two other compounds and more particularly compound V seem to be effective even when treatment is over. Perhaps this is in relation with metabolic effects modifying the regulation of feeding behaviour in the central nervous system. In fact, these compounds have substituents able to interfere with GABA systems.

Amphetamine↗
PubMed1982

[Fractures of the frontal sinus. Therapeutic indications].

Attitudes towards therapy of frontal sinus fractures, in the Plastic and Maxillofacial Surgical Department of the Foch Medical-Surgical Unit, are discussed. Only those fractures with displacement, a possible cause of complications, are envisaged, the conduct adopted being described in detail as a function of the wall affected. Treatment should be directed along the following lines: --A harmonious frontal outline can be obtained by osteosynthesis of the bone fragments if certain conditions are fulfilled, or by a bone graft. --The sinus cavity should be excluded and filled by spongy grafts when an anterior wall graft is inserted. --Neurosurgical explorations are necessary if a posterior wall defect provides a threat to the meninges, followed by cranialization and obturation of the nasofrontal canal. --Physiological drainage must be ensured for the sinus cavity, particularly in inferior wall fractures.

Fracture Fixation, Internal↗
PubMed1982

[Pharmacokinetics of arsenic trioxide in the mouse].

Considering the diversity of previous observations given by literature about the metabolic fate or arsenic, the authors using a radioactive tracer, study the pharmacokinetics of that arsenical derivative after giving the mouse a non toxic dose. By the oral route, this compound is quickly absorbed and resorbed. The elimination process mainly occurs by renal route then by the faecal route. The blood results or the concentrations in the tissues do not reveal any retention process though the latter always rise above blood levels. During the first two hours the concentrations in the thymus seem to be particularly interesting.

Animals↗
PubMed1981

[Application of various types of osteosynthesis in facial injuries (author's transl)].

The authors describe their results obtained in facial injuries treated by various osteosynthesis methods. They recall the different techniques available (steel wires, screws, plates, and pins), and give, for each localization, their opinion as to the best method for obtaining the most satisfactory functional result with the best possible reduction and immobilization, using the simplest and least disturbing procedure for the injured patient.

Facial Injuries↗