[Estrogens and cartilage: an ex vivo ultrastructural study]. / Estrogeni e cartilagine: studio ultrastrutturale ex vivo.

The ultrastructural change brought about by administration of oestrogens on articular cartilage were evaluated in the course of the present study. To this end 3 stabilized postmenopausal patients were selected who were to undergo bilateral hip prosthesis. After the first operation the patients were started on continuous estriol treatment by oral route for 6 months. For study purposes a cartilage fragment was obtained during the first (baseline time) operation and the second operation (final time, after 6 months of oestrogen therapy). The results of histologic examination of the semifine sections as well as the submicroscopic patterns of the various cell elements showed great similarity in all cases considered. Ultrastructure examination had evidenced signs of marked cell damage in the 3 initial samples. After treatment with oestrogens, chondrocyte metabolic activity was resumed, evidenced by the presence of extensive granular endoplasmic reticulum with hypertrophic cisternae, finely dispersed nuclear chromatin and more regular nuclear membrane. These findings would appear to support metabolic stimulation of articular cartilage by the oestrogens.

Faecal elimination of steroids in rats after oral administration of mepartricin.

Treatment of both male and female rats with 5 IU/day mepartricin for 7-10 days administered by gastric tubing resulted in an increased faecal excretion of some steroids. Mean rate of elimination of total oestrogens was enhanced by 45% in male rats and by 14% in female rats, and the average excretion of conjugated oestrogen was also increased in the female animals. Faecal elimination of cholesterol was 37% and 42% higher in male and female rats, respectively, after mepartricin treatment, and in male rats plasma concentrations of cholesterol were reduced following treatment. It is suggested mepartricin acts either by changing the intestinal flora or by acting directly on the steroid moieties, and it is speculated that a similar mechanism may occur in man.

Changes in the plasma pattern of sex steroids in patients with liver cirrhosis treated with mepartricin.

Mepartricin was given to cirrhotic patients in order to evaluate its effect on the imbalance of sex steroids which is typical of this disorder. Patients were divided into two group: one group received placebo (n = 19) and the other received 150,000 IU/day mepartricin for 30 days (n = 19). The patients were evaluated by separate medical staff who were unaware of the treatment. Mepartricin significantly decreased the plasma concentration of testosterone, oestradiol and prolactin as compared with the values at the start of the trial, while no significant changes were seen in the occurrence of gynaecomastia. No relevant changes were seen in patients receiving the control, except for a slight increase in the peripheral concentration of androstenedione, aldosterone and follicle stimulating hormone.

[Clinico-experimental correlation of the hypolipemic effects of mepartricin]. / Correlazione clinico-sperimentale degli effetti ipolipemizzanti della mepartricina.

Mepartricin (SPA-S-160) fat-lowering effect was evaluated in several groups of rats, normal or with experimental hyperlipidemia. The substance had a normalizing action on the lipid levels, and in particular on the cholesterol component. These findings, compared to those obtained in preliminary clinical studies, confirm a mechanism of action, common to some other polyenes, selecting as molecular target the interaction with the cholesterol component.

In vitro antimycoplasmal activity of mepartricin.

The in vitro antimycoplasmal activity of mepartricin was evaluated on several mycoplasma strains. The results demonstrate that this polyene antibiotic possesses a high efficacy against these microorganisms.

The effects of the polyene antibiotic mepartricin on polymorphonuclear leucocyte function: an in-vitro study.

Mepartricin, a polyene antibiotic with candidacidal and trichomonicidal activity, was found to be without toxic effects for human polymorphonuclear leucocytes; the drug seems to be unable to enter the human cells. Some synergism between the antifungal activities of mepartricin and of human leucocytes is seen if Candida cells are pre-incubated with sub-lethal concentrations of the drug.

Mepartricin, a polyene active on both Trichomonas and Candida. Lack of mutagenic activity.

Mepartricin, the methyl ester of partricin, is a new polyene antibiotic with antifungal and antiprotozoal activity. The antitrichomonas activity in vitro is comparable to that of metronidazole, the widely used drug recently demonstrated to possess mutagenic activity and thus to be used with caution in therapy. Clinical investigations have shown that mepartricin can be successfully used in the topic treatment of vaginal trichomoniasis and candidiasis. The mutagenic activity of mepartricin has been evaluated using the Ames' test and compared to that of metronidazole. No mutagenic activity was detected for mepartricin. The drug can thus be proposed as a safer and efficient alternative to metronidazole.

[Biliary elimination of N1,N1-diethyleniminobiguanido-methyl-tetracicline in humans]. / Eliminazione biliare della N1,N1-dietileniminobiguanido-metil-tetraciclina nell'uomo.

The investigations were carried out on 50 patients of both sexes, divided into 2 groups. The first group was formed by 30 patients, suffering from cholelithiasis, who underwent cholecystectomy. Half of these subjects were administered Xantociclina by oral route 5 hours before the operation, while the other half orally received an equivalent dose of tetracycline HC1. The antibiotic levels found in the bile taken during the operation, showed to be markedly higher after Xantociclina administration; the statistical analysis of the values obtained pointed out a most significant difference. The second group was formed by 20 patients suffering from acute cholecystitis; x-rays investigations had pointed out an obstruction of the gallbladder. In these subjects, divided into 2 groups of 10 each, and treated in the same way as those whose cystic ducts were free from obstruction, the antibiotic activity was determined not only in the bile but also in the homogenate of the gallbladder tissue. Markedly higher antibiotic concentrations were found after treatment with Xantociclina, both in the bile and in the gallbladder tissue homogenate. On the basis of the results obtained, the Authors maintain that the new antibiotic derivative can be usefully employed for the treatment of acute and chronic biliary disorders.