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Biomedical subjects

J Paris

Publications and source records attributed to J Paris.

At least 163 records · Page 9Linked to original sources

Effects of ethyl N-N-benzyl-methyl-oxamate in Meriones unguiculatus infected with Echinococcus multilocularis metacestodes. Biochemical and ultrastructural observations.

Ethyl N-N-benzyl-methyl-oxamate is a N-substituted derivative of the oxamic acid, well-known as inhibitor of the lactate dehydrogenase activity. The biochemical and ultrastructural effects of this drug in Echinococcus multilocularis metacestodes and the repercussions in the livers of receptive host, Meriones unguiculatus, were investigated. This compound decreased the specific activity of the lactate dehydrogenase in the metacestodes and the host liver by 81 and 86.8%, respectively. This N-methyl compound has shown an important repercussion on the lactate dehydrogenase activity due to its greater lipophilicity and thus allows a better penetration of the molecule. In the host liver, a fall of the alkaline and acid phosphatases activity was observed. The glucose and glycogen concentrations were also decreased. The ultrastructural study provided an alteration of the tegument of the metacestodes and damages of the muscular system. The parenchyma was disorganized. In conclusion, these biochemical and ultrastructural data obtained with ethyl-N-N-benzyl-methyl oxamate in E. multilocularis metacestodes show clearly the importance of the lactate dehydrogenase activity in the metacestodes.

Acid Phosphatase↗

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.

Acid Phosphatase↗

Perceptions of parental bonding in borderline patients.

Eighteen borderline and 29 nonborderline female patients were scored on perceptions of care and of protection by each of their parents. The two groups differed significantly in that borderline patients perceived less care than did nonborderline patients, particularly from their mothers.

Borderline Personality Disorder↗

Predictors of suicide in borderline personality disorder.

One hundred patients with borderline personality disorder who were followed for a mean of 15 years were compared with 14 borderline patients who committed suicide. The most significant predictors of completed suicide were previous attempts and higher education.

Borderline Personality Disorder↗

Regulation of rat uterine steroid receptors by nomegestrol acetate, a new 19-nor-progesterone derivative.

The regulatory effects of nomegestrol acetate (NOM-Ac: 17 alpha-acetoxy-6 alpha-methyl-19-nor-pregna-4,6-diene-3,20-dione), a new 19-nor-progesterone derivative, active p.o. progestin, were studied on rat uterine estrogen (ER) and progestogen receptor (PgR) levels. The actions of estradiol (E2), progesterone (P) and various progestins were investigated. The effects of E2 were reproduced with 5 micrograms/animal: a 2-fold increase in activated ER level in the nucleus at 30 min, 2-fold stimulation of cytosolic ER replenishment at 48 hr and a 4-fold induction of PgR synthesis at 48 hr. The negative regulatory effects of P were also reproduced at doses ranging from 0.25 to 2 mg/animal: inhibition of basal and E2-stimulated cytosolic ER replenishment and inhibition of E2-induced PgR synthesis. NOM-Ac reproduced these negative regulatory effects. The 50% effective doses in reducing estrogen receptor levels and the corresponding potencies relative to P showed NOM-Ac to be 2.4-fold more active than P and to present, when compared to the other progestins, the highest antiestrogenic capacity. Furthermore, in contrast with norethisterone acetate, a 19-nor-testosterone derivative, it was completely devoid of estrogenic potency.

Animals↗

Changes in the polyadenylation of specific stable RNA during the early development of Xenopus laevis.

The distribution of four specific RNA species between the poly(A)+ and poly(A)- fractions has been studied during the first hours of Xenopus laevis development, before the mid-blastula transition (MBT). Two of these specific RNA species correspond to clones selected by differential hybridization from a Xenopus egg cDNA library. Another corresponds to Xenopus c-raf mRNA and the last one to RNA revealed by a mouse ornithine decarboxylase probe. We show that two of these RNAs are adenylated after fertilization and remain in the poly(A)+ population. During the same period, the other two RNAs are deadenylated and these new poly(A)- RNAs remain stable at least until the MBT. These results show (i) that polyadenylation of specific RNA species occurs after fertilization in Xenopus and (ii) that, in the absence of transcription, adenylation and deadenylation can occur simultaneously in the fertilized egg.

Animals↗

Identification of a flunixin metabolite in the horse by gas chromatography-mass spectrometry.

The main metabolite of flunixin, a hydroxylated product, has been identified by gas chromatography-mass spectrometry and 1H NMR spectroscopy in equine urine and plasma. The method also permits the qualitative monitoring of the urinary elimination of the drug and its metabolite. The two products are detected up to 175 and 54 h, respectively, after a single intravenous administration at the dose of 1 mg/kg. Simultaneous detection of the two compounds increases the reliability of anti-doping control analysis.

Animals↗

Effect of nomegestrol acetate, a new 19-nor-progesterone derivative, on pituitary-ovarian function in women.

After two control cycles, 13 normally menstruating women were treated from day 5 to 25 of the third consecutive cycle with nomegestrol acetate (NOM Ac) 1.25, 2.5 or 5 mg once a day. Plasma oestradiol, FSH and LH concentrations were assayed daily from day 5 to day 25 and plasma progesterone concentrations from day 12 to day 25. Ovulation was inhibited in every woman; LH and progesterone levels were uniformly depressed. With 5 and 2.5 mg/day, plasma oestradiol remained low with high FSH values. With 1.25 mg/day, oestradiol concentrations reached levels similar to those achieved during the control follicular phase, with a concomitant decrease in FSH secretion. These results show an hypothalamic-pituitary effect and suggest an ovarian action, both responsible for a potentially useful contraceptive property.

Adult↗

Effects of progestogens on lipemia and lipolysis in rat: effects of progesterone, megestrol acetate, norethindrone acetate, and nomegestrol acetate.

Effects of 4 progestogens at equal dosages (5 mg/kg/day) on lipid metabolism and plasma glucose levels of adult female rats were compared. The 4 progestogens studied were progesterone (P) by SC injection, and megestrol acetate (MEG), norethindrone acetate (NOR), and nomegestrol acetate (NOM) PO. MEG, a 17 alpha-hydroxyprogesterone derivative, induced significant increases in glucose, total and high-density lipid (HDL) cholesterol, triglyceride, and phospholipid plasma levels. Treatment with NOR, a 19-nortestosterone derivative, resulted in a reduced gain in body wt and in a marked decrease in all plasma lipid parameters. The 19-norprogesterone derivative NOM, like P, did not alter lipid or glucose metabolism, despite a significant increase in body wt gain. In particular, no reduction in the HDL cholesterol level occurred. Plasma and tissue lipolytic activities remained unchanged. The results of this study confirm interest in the therapeutic class of 19-norprogesterone-derived progestogens, exemplified by NOM, with respect to their lack of metabolic side effects.

Animals↗

Psychological factors in the choice of psychiatry as a career.

A survey of psychiatrists and non-psychiatrists in a medical faculty examined questions bearing on two hypotheses, that psychiatrists choose their career either to heal themselves or to heal their families. The results provided some support for the psychiatrist as a "wounded healer". The findings did not appear to be an artifact of more psychiatrists having been in therapy. The results were the same whether or not psychiatrists specialized in psychotherapy.

Adaptation, Psychological↗

The cellular mechanism of the antiandrogenic action of nomegestrol acetate, a new 19-nor progestagen, on the rat prostate.

Nomegestrol acetate, like other synthetic progestins such as medroxyprogesterone acetate (MPA), chlormadinone acetate, megestrol acetate and cyproterone acetate, is able to modify the physiological actions of androgens. In the present study, the effects of nomegestrol acetate and other antiandrogens on the binding of androgen to the androgen receptor (AR) and on the 'activation' of this receptor were investigated, using rat ventral prostate as target model. Relative binding affinities (RBA) for AR were first estimated in vitro with respect to [3H]testosterone for a series of structurally-related compounds. The values obtained ranged as follows: dihydrotestosterone (DHT) much greater than megestrol acetate greater than or equal to testosterone (T) greater than nomegestrol acetate greater than 19-nor progesterone (19NP) greater than progesterone (P). An assay was established, using two different incubation times (3 h and 24 h) to further investigate relationships between binding affinity and androgenic, or antiandrogenic, activity. The following order (as %) was obtained for progestins as against [3H]mibolerone (DMNT): 1) DMNT (100) much greater than nomegestrol acetate (42) greater than megestrol acetate (29) greater than chlormadinone acetate (9) greater than MPA (8) greater than cyproterone acetate (6) after 3 h and 2) DMNT (100) much greater than MPA (53) much greater than nomegestrol acetate (19) greater than megestrol acetate (12) greater than chlormadinone acetate (14) and cyproterone acetate (8) after 24 h. Since the RBA of nomegestrol acetate declined with time, these results indicate that this substance may act like an antiandrogen rather than an androgen, while the contrary prevails concerning MPA.(ABSTRACT TRUNCATED AT 250 WORDS)

Androgen Antagonists↗

Extinction of mineralocorticoid effects in 19-norprogesterone derivatives: structure-activity relationships.

19-Norprogesterone (19-NOR-P) is a potent progestagen in mammals by s.c. injection, but is almost inactive when given p.o. In the rat, 19-NOR-P also shows marked salt-retaining and hypertensive effects, consistent with its high affinity for mineralocorticoid receptors (MR). We synthetized recently some p.o. active 19-NOR-P derivatives, and have examined the extent to which the structural changes made on the parent compound can modify the affinity for MR and the salt-retaining potency. Compared with aldosterone, 19-NOR-P has a 47% affinity for rat renal cytosolic MR, decreasing to 13% with alpha-hydroxylation on C-17 (17 alpha-OH-19-NOR-P). The addition of a methyl group combined with the formation of a double bond at C-6 led to nomegestrol, the relative affinity of which was 1.2%. Binding was almost abolished completely (0.23%) by acetylation of the 17 alpha-OH group (nomegestrol-acetate). A single s.c. injection of 19-NOR-P, 20 micrograms/animal, induced a marked decline of [Na+]/[K+] ratio in urine of adrenalectomized male rats. The antinatriuretic effect was still observed after a 11-day period of daily administrations of the same dosage. 17 alpha-OH-19-NOR-P decreased the [Na+]/[K+] ratio only at a high p.o. dose (2500 micrograms/animal). NOM-Ac did not affect the [Na+]/[K+] ratio after a single s.c. or p.o. administration, but increased it at the end of a 11-day p.o. treatment. Thus, the chemical modifications that lead to potent p.o. active progestins derived from 19-NOR-P induce stepwise reductions in the affinity for MR and of the mineralocorticoid effects of the parent compound.

Adrenalectomy↗

[In vivo inhibition by ethyloxanilates of alkaline phosphatases of the cestode Echinococcus multilocularis].

Alkaline phosphatases (E.C.3.1.3.1), membranous enzymes of the cestode Echinococcus multilocularis have been studied in the parasite and in the experimental host liver. Synthetic inhibitors interaction with metacestode alkaline phosphatases is reported. In regard to the alkaline phosphatases inhibition, the ethyloxanilate 2 is more efficient in the cestode itself than in the host liver.

Alkaline Phosphatase↗