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Biomedical subjects

E Castiglioni

Publications and source records attributed to E Castiglioni.

8 recordsLinked to original sources

Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety.

Two isomers of the hexahydro-tetraazaacenaphthylene templates (1 and 2) are presented as novel, potent, and selective corticotropin releasing factor-1 (CRF1) receptor antagonists. In this paper, we report the affinity and SAR of a series of compounds, as well as pharmacokinetic characterization of a chosen set. The anxiolitic activity of a selected example (2ba) in the rat pup vocalization model is also presented.

Acenaphthenes↗

Reliable assay of extreme enantiomeric purity values by a new circular dichroism based HPLC detection system.

A new sensitive, selective, and versatile circular dichroism (CD)-based HPLC detection system was used for the validation of the enantiomeric purity assay in the quality control of chiral drugs upon nonchiral stationary phases. The precision and the accuracy of the method were checked for selected samples showing values of the anisotropy factor on the order of 10(-1) to 10(-4). Very high accuracy has been obtained also in the case of extreme enantiomeric purity values (</=1% or >/=99% e.p.) and of a low anisotropy factor (g = 2 x 10(-4)) compound. The high selectivity of this detection system allows a selective monitoring of analytes in complex mixtures and makes the baseline stable.

Chromatography, High Pressure Liquid↗

An integrating sphere to measure CD from difficult samples

Integrating spheres are widely used with UV-Vis and occasionally with infrared spectrophotometers to measure different types of samples, either in transmission mode (scattered transmission accessories) or in total/diffuse reflectance mode. We built a prototype sphere of the demountable type, which fits easily the sample compartment of a commercial CD spectropolarimeter, requiring neither any alignment nor the use of a dedicated photomultiplier. Samples can be inserted either at the sphere entrance (for scattered transmission mode) or in the center of the sphere (for total reflectance experiments). Selected experimental data are presented to evaluate sphere efficiency, its wavelength range and results with a single sample in different forms. Copyright 2000 Wiley-Liss, Inc.

Journal Article↗

Blood flow in the internal carotid and middle cerebral arteries: effects of continuous oral conjugated equine estrogens administration with monthly progestogen supplementation on postmenopausal women.

OBJECTIVE: This study was designed in order to evaluate the effect of conjugated equine estrogens (CEE) on internal carotid and middle cerebral artery blood flow in postmenopausal women. DESIGN: Thirty-four healthy postmenopausal women with intact uteri were randomly divided into two groups of 17 subjects each. The first group was treated for 24 weeks with continuous CEE medication (0.625 mg daily) and cyclical supplementations of 5 mg/day of medrogestone acetate, given on the last 12 days of every 4-week period (Prempak, Wyeth, Italy). The second group received no treatment. The pulsatility indices (PI) of both the internal carotid artery and middle cerebral artery were measured. RESULTS: In the treated group, the PI of the interior carotid artery and MCA was reduced from respectively 0.736 (0.016) and 0.745 (0.009) at baseline, to 0.669 (0.021) and 0.670 (0.011) after 24 weeks (p = 0.01); in the control group, the PI values remained unchanged. The between-group difference for both arteries was significant (p < 0.01). CONCLUSIONS: The administration of CEE with cyclical medrogestone supplementation to postmenopausal women induces a statistically significant reduction in the PI of cerebral arteries.

Administration, Oral↗

Alteration in the pulsatility index values of the internal carotid and middle cerebral arteries after suspension of postmenopausal hormone replacement therapy: a randomized crossover study.

OBJECTIVE: The aim of the study was to investigate the effect of the suspension of hormone replacement therapy on blood flow in the internal carotid and the middle cerebral arteries. STUDY DESIGN: Doppler ultrasonography was used to measure the pulsatility index of the internal carotid and middle cerebral arteries of 23 women. The patients were all receiving continuous transdermal estradiol replacement therapy (50 micrograms/day) with a cyclic supplementation of medroxyprogesterone acetate every second month (10 mg/day for 12 days). The duration of the study was 12 months. The patients were randomly assigned to one of two groups. The first group (11 subjects) continued therapy for the first 6 months and then suspended it for the following 6 months; the second group (12 subjects) interrupted hormone replacement therapy for the first 6 months and then resumed it for the following 6 months. The internal carotid and middle cerebral artery pulsatility index was measured at the start of the 12-month period and then every 3 months. Serum estradiol levels were measured to check compliance. RESULTS: A statistically significant difference was found between the internal carotid and middle cerebral artery pulsatility index values of the two groups at each of the measurements after the first one. Over the first 6 months the pulsatility index values rapidly increased in the patients kept off hormone replacement therapy and remained stable in those receiving hormone replacement therapy. After the crossover at 8 months, the pulsatility index rapidly dropped to values similar to those at baseline in the patients who resumed hormone replacement therapy and increased in those who suspended therapy. CONCLUSIONS: Resistance to blood flow in cerebral vessels of postmenopausal women rapidly changes after hormone replacement therapy suspension. In postmenopausal women estrogen administration should be continued to maintain the favourable variations of vascular reactivity induced by hormone replacement therapy.

Body Mass Index↗

[A clinical case of demyelinating disease with basilar impression].

The authors report a clinical case of a 48-year-old female patient admitted to the Neurological Division following acute symptoms characterised by generalised asthenia, motory disorders (incoordination, equilibrium or gait deficit) accompanied by diplopia. Instrumental (medullary and encephalic NMR) and laboratory tests revealed a malformation of the atlo-occpital hinge with basilar impression and areas of corticosubcortical demyelinisation signifying multiple sclerosis. The liquor test was also positive for the presence of oligoclonal bands of IgG with a Link index of 0.97 (lower v.n. at 0.7). The association between these two pathologies is rare, whereas the need for a differential diagnosis between them often arises. Therefore, two pathologies which are mutually exclusive in many cases were present in an associated form in this case.

Demyelinating Diseases↗

Blood flow variations in internal carotid and middle cerebral arteries induced by postmenopausal hormone replacement therapy.

OBJECTIVE: Our purpose was to clarify the mechanisms by which postmenopausal estrogen replacement therapy exerts its protective effect on cardiovascular risk. STUDY DESIGN: By means of a bidirectional Doppler ultrasonographic system we measured pulsatility index variations the internal carotid artery and middle cerebral artery in 25 early postmenopausal women during a 6-month period of hormone replacement therapy. Transdermal estradiol (50 micrograms/day) was continuously administered. A 12-day course of medroxyprogesterone acetate (10 mg/day) was added every second month. RESULTS: The pulsatility index showed a significant (p = 0.0001) reduction in both arteries after 6 weeks. At 22 weeks a 25% reduction was measured. No variation of the estrogen-induced pulsatility index reduction was observed at the end of every cyclic progestogen supplementation. CONCLUSIONS: In early postmenopausal women hormone replacement therapy causes a rapid reduction of pulsatility index in brain arteries. Cyclical progestational supplementation does not modify this positive effect on reactivity of the blood vessels.

Administration, Cutaneous↗

Proinflammatory and regulatory cytokine levels in AIDS cachexia.

The serum concentrations of inflammatory (Interleukin-1 beta, Tumor necrosis alpha, Interleukin-6) and regulatory cytokines (Interleukin twelve) have been studied in ten AIDS cachectic patients and compared to a control group. A cytokine imbalance, and peculiarly a significant increase in proinflammatory cytokines (Interleukin-1, Interleukin-6, Tumor necrosis Factor alpha) and a decrease in regulatory cytokines such as Interleukin-12 were found. A significant correlation resulted between weight loss and Interleukin-1 beta and 6. A negative correlation between Interleukin-1 and 12 was noted, indicating that this last cytokine has an important regulatory role also in advanced state of the disease.

AIDS-Related Opportunistic Infections↗