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At least 19 recordsLinked to original sources
PubMed1992

Effects of cyclofenil diphenol, an agent which disrupts Golgi structure, on proteoglycan synthesis in chondrocytes.

1. Cyclofenil diphenol (F6060), a weak non-steroidal oestrogen, was shown previously to inhibit [35S]proteoglycan synthesis [Mason, Lineham, Phillipson & Black (1984) Biochem. J. 223, 401-412] and to induce fragmentation of the Golgi apparatus into small vesicles [Lancaster, Fryer, Griffiths & Mason (1989) J. Cell Sci. 92, 271-280] in cultures of Swarm chondrosarcoma chondrocytes. Two structurally related compounds, F6204 and F6091, show a similar concentration-related effect, with complete inhibition of [35S]proteoglycan synthesis at 90 micrograms/ml. The apparent [3H]protein synthesis is only approx. 40% inhibited with [3H]lysine as precursor. Stilboestrol, clomiphene and tamoxiphen are also potent inhibitors of [35S]proteoglycan synthesis. 2. Syntheses of chondroitin 4-[35S]sulphate and chondroitin 6-[35S]sulphate, which are Golgi-mediated events, are inhibited 40-68% and 3-48% respectively by concentrations of cyclofenil between 50 and 70 micrograms/ml. [3H]Hyaluronan synthesis, which occurs by a different mechanism at the plasma membrane, is inhibited by 47-66%. These results suggest that cyclofenil may act via more than one inhibitory mechanism. Cyclofenil diphenol inhibits polymerization of chondroitin sulphate on to p-nitrophenyl beta-xyloside even when the chondrocytes are loaded with the initiator prior to treatment. 3. Cyclofenil diphenol interferes with the cellular uptake of amino acids via the system A carrier, as shown by inhibition of uptake of methylaminoisobutyric acid, a specific substrate for this system. The drug had no effect on the uptake of 2-deoxyglucose by the cells. 4. Cyclofenil diphenol (90 micrograms/ml) caused a decrease in the pool size of UDP-N-acetylglucosamine, UDP-N-acetylgalactosamine and UDP-hexoses, but this was insufficient to account for the accompanying profound inhibition of [35S]proteoglycan synthesis. Entry of [3H]glucosamine into the cell and into the UDP-N-acetylhexosamine pool did not appear to be affected. 5. Cyclofenil diphenol inhibited the substitution of 3H-labelled proteoglycan core protein with chondroitin sulphate chains. Core protein was identified in treated cultures on the basis of immunoprecipitation with an antiserum against the hyaluronate-binding region and distinguished from precipitated proteoglycan on SDS/PAGE.

Animals↗
PubMed1988

Ultrasonic assessment of ovulation in cyclofenil induced ovulatory cycles.

Graafian follicle growth was studied by ultrasound scanning during the peri-ovulatory period in 64 ovulatory cycles in 32 infertile patients on cyclofenil treatment, and compared with a control group of 32 patients with confirmed ovulatory cycles assessed on the basis of serum progesterone levels in the middle of the second half of the cycle. The mean maximum diameters of the leading follicles before ovulation were 21.9 +/- 0.6 (S.E.) mm and 24.4 +/- 0.5 (S.E.) mm, respectively for the cyclofenil group and the normal control group (P greater than 0.05). In 79% of the cyclofenil stimulated group and 83% of the spontaneous ovulation group, ultrasonic evidence of ovulation was present between 12 and 36 h after the initial increase in urine LH levels. Ultrasound scanning was found to be simple, and a quick method of monitoring graafian follicle development and ovulation on cyclofenil therapy and the cycles were comparable to the spontaneous ovulatory cycles as assessed on the basis of graafian follicle diameter, and the time of ovulation. Cervical score was not found to be useful to assess ovulation time in the cyclofenil treated group since 31.3% achieved a score of 10 or more on day -4, 93.8% within 24 h of ovulation and 24% on day 3 following the ovulation.

Cresols↗
PubMed1992

Effect of cyclofenil on hormonal dynamics, follicular development and cervical mucus in normal and oligomenorrhoeic women.

Cyclofenil is a triphenylethylene derivative, similar in structure to clomiphene citrate, which is used to induce ovulation in anovulatory women. The effects of cyclofenil on a group of 10 normal cyclic and 10 oligomenorrhoeic subjects were examined in a double blind controlled cross-over study. Both groups of women were administered either cyclofenil or, following a washout cycle, a placebo in two treatment cycles. Urinary oestrone and pregnanediol excretion were measured daily and ultrasound scans performed to assess follicular development. Frequent sampling of blood was performed on day 6 to study luteinizing hormone (LH) and follicle stimulating hormone (FSH) pulsatile release. Cervical mucus changes and sperm-cervical mucus interaction were studied after identification of the LH peak. There were no significant differences between cyclofenil and placebo cycles in the following: ovulation rates, daily urinary oestrone and pregnanediol excretion, the number or size of developing follicles, LH pulsatility (parameters studied: number of peaks, pulse interval, pulse amplitude, pulse area and mean nadir LH), mean FSH level on day 6, cervical mucus and sperm-cervical mucus interaction. In view of our inability to demonstrate an effect on any parameter of endocrine function in normal and oligomenorrhoeic women, these results throw doubt on the therapeutic value of cyclofenil in its present dosage and formulation.

Adult↗
PubMed1989

Ultrastructural changes accompany inhibition of proteoglycan synthesis in chondrocytes by Cyclofenil diphenol.

Cyclofenil diphenol, a weak non-steroidal oestrogen, profoundly inhibits [35S]proteoglycan synthesis in cultures of Swarm chondrosarcoma chondrocytes under conditions in which protein synthesis is only marginally reduced. In the present experiments it was shown that after a 40-min treatment with Cyclofenil diphenol (90 micrograms ml-1) most of the normally abundant Golgi stacks in these cells disappeared and after 60 min they were absent. After 2-3 h treatment the cisternae of the endoplasmic reticulum (ER) were grossly distended and transformed into large ribosome-studded vesicles containing flocculent and filamentous material. These changes were dependent on the concentration of Cyclofenil and were fully reversible within 21 h of withdrawing the drug. The ultrastructural changes differed in some aspects if protein synthesis was blocked with cycloheximide for 15 min or 180 min before and during treatment with Cyclofenil. The Golgi disappeared but the ER cisternae, though distended, formed a continuous network and swollen ribosome-studded vesicles did not develop. However, non-membrane-bounded structures containing lipid droplets and material of low electron density developed in the cytoplasm under these conditions. The ultrastructural changes induced by Cyclofenil differ from those induced by monensin and diethylcarbamazine, suggesting that the drug acts at a different point in the secretory pathway for macromolecules.

Animals↗
PubMedDate not supplied

[Value of cyclofenil in the inhibition of lactation. Efficacy compared to bromocriptine].

The inhibitory effects of cyclofenil and bromocriptine on lactation as well as FSH, prolactin and estradiol levels have been compared in control and treated females. The clinical activity of cyclofenil was lower than that of bromocriptine but was virtually free of side-effects. Cyclofenil and bromocriptine only presented similar hormonal effects at the 20th day ; this suggests that the mechanism of action of cyclofenil is more linked to secondary increases in estrogen levels than to a primary effect. Cyclofenil is of particular value in cases of vascular hypersensitivity yo ergot derivatives and for toxemic patients treated with beta-blockers.

Adult↗
PubMed1986

The effects of Cyclofenil on the Cervical Mucus Score (Insler).

Daily simultaneous cervical mucus evaluation and ultrasonography of the Graafian follicular growth and ovulation were studied (in the mid-cycle) in 8 infertile British women during 30 Cyclofenil-stimulated cycles, and compared with 18 non-stimulated normal ovulatory cycles in 12 subjects (controls). In the 16 Cyclofenil-induced ovulatory cycles, there was an early (5 days prior to the day of ultrasonic ovulation) Full Cervical Mucus Score (Insler) in 69% of the cycles, and the Full Cervical Mucus Score lasted for 7 days or more in 63% of the cycles. In 38%, there was persistence of the Full Cervical Mucus Score on the third day after ultrasonic ovulation. In the 14 Cyclofenil-treated anovulatory cycles, a Full Cervical Mucus Score was recorded on one or more occasions in the mid-cycle in 29% of the cycles. The classical teaching of prediction of the probable timing of ovulation by Cervical Mucus Scoring is not applicable to Cyclofenil-stimulated cycles.

Adult↗
PubMed1992

A prospective, randomised, cross-over study comparing the effects of clomiphene citrate and cyclofenil on endometrial morphology in the luteal phase of normal, fertile women.

OBJECTIVE: To examine the effect of two anti-oestrogens, clomiphene citrate and cyclofenil, on endometrial morphology in the luteal phase. DESIGN: A prospective, randomised, cross-over study. SETTING: Jessop Hospital for Women, Sheffield, UK. SUBJECTS: 10 women who were previously fertile and regularly cycling. INTERVENTION: The administration of clomiphene citrate or cyclofenil in the treatment cycles. A LH timed endometrial biopsy was taken on day LH + 6. MAIN OUTCOME MEASURES: Histological dating and morphometric analysis of the endometrial sample. RESULTS: Only one out of 10 subjects had abnormal endometrium. There was no difference in the results between cycles treated with clomiphene citrate and cyclofenil. CONCLUSIONS: Clomiphene citrate or cyclofenil does not have a major adverse effect on endometrial morphology in the luteal phase of normal fertile subjects. The possible adverse effects of anti-oestrogens on endometrium may have been previously overestimated.

Adult↗
PubMed1977

[Comparative clinical studies on clomiphen, cyclofenil and epimestrol (author's transl)].

Report on the treatment of 310 anovulatory woment in 1173 treatment cycles with Clomiphen, Cyclofenil and Epimestrol. 63% of the patients had a biphasic basal body temperature record after treatment in 718 cycles. Patients with secondary amenorrhea of the first or the second degree had a satisfactory ovulation rate in 71% of the cases only by treatment with Clomiphen. In women with anovulatory cycles an overall ovulation rate of 75% was observed with all three medications. In 73 patients 78 pregnancies occurred. Of these, 38 pregnancies followed Cyclofenil, 25 pregnancies followed Clomiphen and 15 pregnancies followed Epimestrol corresponding to a 15%, 17% and 13% rate in the treated patients. 22 of these pregnancies ended in incomplete abortion. The side effects of Clomiphen especially visual and cystic ovarian and vasomotor side effects are more pronounced than the side effects of Cyclofenil and Epimestrol. The statistical analysis of the clinical results showed that Clomiphen and Cyclofenil had a higher rate of ovulation in secondary amenorrhea of the first or second degree than Epimestrol.

Amenorrhea↗
PubMedDate not supplied

The level of urinary and plasma steroids after oral administration of cyclofenil to hirsute women with menstrual disorders and obesity.

Cyclofenil 600 mg/day was given to 10 women with excessive skin hair and marked excretion of urinary androgens. The urinary values of androgenic metabolites as well as the plasmatic values of radioimmunoassayable testosterone remained unaltered. A significant increase was noticed in the radioimmunoassayable plasma estradiol. Urinary total estrogens could not be assayed in the women under cyclofenil because of a non-specific color reaction. It was concluded that the estrogenic effects of cyclofenil are mediated, at least partly, by release of gonadotropins from the hypophysis.

Cresols↗
PubMed1992

Long-term evaluation of penicillamine or cyclofenil in systemic sclerosis. Results from a two-year randomized study.

In a two-year prospective therapeutic trial 13 patients with systemic sclerosis (SSc) were treated with penicillamine, 9 with cyclofenil, and 7 with neither. At entry skin involvement and esophageal, lung, heart, and kidney function did not differ significantly between the groups. Reevaluation after one and two years did not show any significant changes in skin, esophageal, heart, and kidney manifestations, while lung function had slightly improved in both drug-treatment groups. This study thus shows little overall effect of penicillamine and cyclofenil, although both drugs may arrest worsening of pulmonary dysfunction.

Adult↗
PubMed1990

[Sterility from hormonal causes and unexplained sterility. Treatment with cyclofenil. Double-blind controlled study].

We treated 213 women during 3 cycles by cyclofenil versus placebo in a double-blind study. These women had infertility caused by ovulatory deficiencies, a cervical factor or idiopathic infertility. Twenty-six of the 114 women receiving cyclofenil became pregnant and 21 of the 99 receiving the placebo. The cumulative pregnancy rates were identical in the 2 groups: 22 per cent in 3 cycles. The authors insist on the importance of a good doctor-patient relationship and the role of the placebo effect in any treatment of infertility.

Adult↗
PubMed1977

The use of cyclofenil in menopausal women.

On the basis of some reports, a double-blind experimental trial comparing the activity of cyclofenil, estradiol valerate and placebo in post-menopausal disturbances was carried out. 60 women among those attending the menopausal clinic and affected by climateric disorders have been treated. The objective criterium for the admission had been established on the basis of the value of plasma FSH (greater or equal to 800 ng/ml). Besides the gynecological examination (including objective and subjective examination, hormone dosage, endometrial biopsy) patients underwent psychological examination (individual interview and psychometric tests) before and after 28 days of therapy The statistical evaluation of the results obtained with the 3 drugs showed a statistically significant difference between the placebo and the active compounds: no significant difference between cyclofenil and estradiol valerate was observed.

Cresols↗
PubMed1992

Acute hepatitis induced by cyclofenil: a case report.

The case of a 47-year old woman suffering from acute hepatitis caused by cyclofenil, a drug proposed for the treatment of anovulation and scleroderma, is presented. Hepatitis developed seven weeks after the beginning of administration of the drug and its course was reversible after withdrawal. The case is documented on the basis of liver histology and the exclusion of other causes of acute hepatitis.

Acute Disease↗
PubMed1977

[Ovulation induction by cyclofenil (author's transl)].

The ovulation-inducing action of cyclofenil was investigated in 135 sexually mature women aged 20--35 years. The patients were only included in the trial if no ovulation in 2 consecutive cycles with the following criteria: basal temperature, cervix score, ascorbic acid retention, basophil count, serum hormone levels, e. g. LH and progesterone and the estrogens in the 24-hour urine could be determined. Ovulation was only considered to have occurred when all the parameters named indicated it. The lack of ovulation was accompanied by amenorrhea in 21 of the 135 patients. The ovulation rate in the 241 cycles observed was 101, corresponding to 42%. In the 114 patients with anovulatory cycles, the ovulation rate in the 184 cycles observed was 95, corresponding to 50%. In the 21 amenorrheic patients, ovulation occurred 6 times in the 57 cycles observed. Nausea or vomiting occurred as side effects in only 2 cases.

Adult↗