MR diagnosis of a rare adnexal mass: lithokelyphopedion.
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Adnexa Uteri↗
Biomedical subjects
S Grasso
Publications and source records attributed to S Grasso.
Synthesis and in vitro antitumor activity evaluation of 9-substituted 1,2,3,4-tetrahydrocarbazoles.
A series of 9-acetamido-1,2,3,4-tetrahydrocarbazoles (2) and 9-(aminoalkyloxyethyl)-1,2,3,4-tetrahydrocarbazoles (4) were prepared and tested for their in vitro antitumor activity. Compounds 4 are highly cytotoxic in almost all subpanel cell lines when tested at 10(-4) M, but showed a weak activity at the lowest concentrations employed.
Antineoplastic Agents↗
Anti-HIV agents. IV. Synthesis and in vitro anti-HIV activity of novel 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazoles.
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Antiviral Agents↗
Synthesis and antitumor activity evaluation of Delta2-1,2,4-oxadiazoline derivatives.
4-Adamantyl-5-aryl-3-phenyl-Delta2-1,2,4-oxadiazolines were synthesized and evaluated in vitro as antitumor agents against 60 human tumor cell lines. Some derivatives exhibit both cell selectivity and tumor growth inhibition activity. In particular, 2,6-dichlorophenyl derivative (2q), the most active of the series, possesses significant activity on 26 cell lines at 10(-5) M.
Antineoplastic Agents↗
GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice.
The behavioural and anticonvulsant effects of several 1-aryl-3,5-dihydro-4H-2,3-benzodiazepin-4-ones (2,3-BZs) and of 11b-aryl-7,11-dihydro-3-phenyl[1,2,4]oxadiazolo[5,4-a][2,3]benz odiazepin-6-ones (2,3-OBZs) were studied after intraperitoneal (i.p.) administration in DBA/2 mice, a strain genetically susceptible to sound-induced seizures. The seizures were evoked by means of auditory stimulation (109 dB, 12-16 kHz) in animals placed singly under a hemispheric Perspex dome. The 2,3-benzodiazepines studied after 30 min pretreatment were generally less potent than the related derivative 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride (GYKI 52466) except 3,5-dihydro-7,8-dimethoxy-1-phenyl-4H-2,3-benzodiazepin-4-one (2,3-BZ-2) and 2,3-BZ-2M (3-methyl derivative of 2,3-BZ-2) which showed comparable activity. Thirty minutes after i.p. administration of 2,3-benzodiazepines, the rank order of potency for anticonvulsant activity against clonus was 2,3-BZ-2 > GYKI 52466 > 2,3-BZ-2M > 2,3-BZ-1 > 2,3-BZ-3, > 2,3-OBZ-1, > 2,3-OBZ-2 2,3-OBZ-3. The intracerebroventricular (i.c.v.) injection of aniracetam on it own (12.5 - 100 nmol/mouse) had no convulsant activity, but it reversed the anticonvulsant effects of some 2,3-benzodiazepines. In particular, the pharmacological actions of GYKI 52466, 2,3-BZ-2 and 2,3-BZ-2M, which proved to be the most potent 2,3-benzodiazepine derivatives as anticonvulsants, were significantly reduced by an i.c.v. pretreatment with aniracetam (50 nmol/mouse). Concomitant treatment with aniracetam (50 nmol/mouse) shifted to the right the dose-response curves and significantly increased the ED50 values for GYKI 52466, 2,3-BZ-2 and 2,3-BZ-2M. After 30 min pretreatment 2,3-BZ-2 showed a similar potency to GYKI 52466 in antagonizing seizures induced by i.c.v. administration of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), thus suggesting a clear involvement of AMPA receptors in the anticonvulsant activity of these compounds. In addition, 2,3-BZ-2 and 2,3-BZ-2M showed anticonvulsant properties longer lasting than GYKI 52466.
Animals↗
Report of a case of congenital glioblastoma multiforme: an immunohistochemical study.
We report a rare case of congenital glioblastoma multiforme in a 13-day-old male neonate born at term who died from cardiocirculatory failure. The cerebral tumor was diagnosed in vivo by magnetic resonance imaging and confirmed histologically after autopsy. The histological and immunohistochemical features of this case were similar to those reported in the adult.
Brain↗
Distribution of extracellular matrix glycoproteins in the human mesonephros.
We analyzed the expression and distribution of collagen types IV and VI, laminin and fibronectin during the development and regression of the mesonephros in human embryos and fetuses ranging from 6 to 12 weeks of gestation by indirect immunoperoxidase methods. Type IV collagen, laminin and fibronectin were detected along the glomerular, tubular and capsular basement membranes of developing and mature nephrons. Only type IV collagen and fibronectin were found in the mesangium. Type VI collagen formed a delicate interstitial fibrillar network and a continuous basement membrane-like structure along the mesonephric nephrons. Basement membranes (GBM) of developing and mature glomeruli showed a distinct continuous staining for this collagen. The mesangial matrix was rich in type VI collagen. Mesonephric involution started during the 8th week of gestation and coincided with a moderate expansion of mesangial matrix and progressive collapse of the capillary walls, while the tubules became thinner and shorter. Staining for all extracellular matrix glycoproteins studied showed GBM wrinkling, gradual disintegration of some capillary loops and glomerulosclerosis. The sclerotic glomeruli were strongly positive for type IV collagen and less positive for type VI collagen and fibronectin. Laminin was absent. Our results indicate that collagen types IV, VI, laminin and fibronectin may be involved in the development and regression of the human mesonephros.
Collagen↗
Expression of cytokeratins, vimentin and basement membrane components in human fetal male müllerian duct and perimüllerian mesenchyme.
The expression and distribution of cytokeratins 8, 18, 19, pan-cytokeratin, vimentin, type IV collagen, laminin and fibronectin were investigated immunohistochemically in the Wolffian and Müllerian ducts and perimüllerian mesenchyme of human male fetuses ranging from 8 to 12 weeks of gestation. The epithelial cells of both genital ducts, the coelomic epithelium and the mesenchymal perimüllerian cells coexpressed cytokeratins 18, 19, pancytokeratin and vimentin. Type IV collagen, laminin, and fibronectin were detected in the basement membranes of both genital ducts, the coelomic epithelium and in the interstitium of the perimüllerian mesenchyme. The coelomic basement membrane adjacent to the müllerian duct showed interruptions and perimüllerian cells were in contact with the coelomic epithelium. The cytoskeletal immunophenotype of perimüllerian cells and their relationship with the coelomic epithelium suggested their coelomic origin. During the 12th week of gestation, müllerian duct began to regress with its basement membrane detaching from the surrounding mesenchyme. This coincided with the disappearance of vimentin from the ductal epithelial cells, as well as type IV collagen, laminin and fibronectin from perimüllerian mesenchyme. Thus müllerian ductal basement membrane dissolved. These findings indicate that the human müllerian duct regression is associated with changes in the interactions between Müllerian ductal and perimüllerian mesenchymal cells.
Basement Membrane↗
Placental thrombosis and fetal loss after passive transfer of mouse lupus monoclonal or human polyclonal anti-cardiolipin antibodies in pregnant naive BALB/c mice.
In the present study we evaluated the effect of passive transfer of a mouse monoclonal (CAM) or a human polyclonal anti-cardiolipin IgG on pregnancy outcome in BALB/c mice. The mice were immunized through the tail vein immediately after mating with 10 micrograms of monoclonal or polyclonal anti-cardiolipin antibodies. Two other groups of mice were given a mouse irrelevant monoclonal antibody or normal human polyclonal IgG respectively, at the same dose. In mice immunized with monoclonal or polyclonal anti-cardiolipin antibody we observed a significant increase in the number of fetal resorptions and a significant reduction of the mean weights of the embryos and the placentas. In mice immunized with CAM we also found a significant decrease in the number of healthy pups, while mice infused with human aCL antibody expressed a significant reduction in the fecundity rate. The histological examination showed widespread thrombosis and necrosis in the placentas derived from the mice immunized with the anti-cardiolipin antibodies. The model supports a possible direct pathogenetic effect of anti-phospholipid antibodies in recurrent fetal loss and points out that thrombotic events at placental level can be instrumental in the pathogenesis of the obstetric complications.
Animals↗
Relationship between structure and convulsant properties of some beta-lactam antibiotics following intracerebroventricular microinjection in rats.
The epileptogenic activities of several beta-lactam antibiotics were compared following their intracerebroventricular administration in rats. Different convulsant potencies were observed among the various beta-lactam antibiotics tested, but the epileptogenic patterns were similar. The patterns consisted of an initial phase characterized by wet-dog shakes followed by head tremor, nodding, and clonic convulsions. After the largest doses of beta-lactam antibiotics injected, clonus of all four limbs and/or the trunk, rearing, jumping, falling down, escape response, transient tonic-clonic seizures, and sometimes generalized seizures were observed, followed by a postictal period with a fatal outcome. At a dose of 0.033 mumol per rat, cefazolin was the most powerful epileptogenic compound among the drugs tested. It was approximately three times more potent than benzylpenicillin in generating a response and much more potent than other cephalosporins, such as ceftriaxone, cefoperazone, and cefamandole. No epileptogenic signs were observed with equimolar doses of cefotaxime, cefonicid, cefixime, and ceftizoxime in this model. The more convulsant compounds (i.e., cefazolin and ceftezole) are both characterized by the presence of a tetrazole nucleus at position 7 and show a marked chemical similarity to pentylenetetrazole. Imipenem and meropenem, the two carbapenems tested, also showed epileptogenic properties, but imipenem was more potent than meropenem, with a convulsant potency similar to those of ceftezole and benzylpenicillin. In addition, the monobactam aztreonam possessed convulsant properties more potent than those of cefoperazone and cefamandole. This suggest that the beta-lactam ring is a possible determinant of production of epileptogenic activity, with likely contributory factors in the substitutions at the 7-aminocephalosporanic or 6-aminopenicillanic acid that may increase or reduce the epileptogenic properties of the beta-lactam antibiotics. While the structure-activity relationship was also investigated, there seem to be no convincing correlations among the rank order of lipophilicities and the convulsant potencies of the compounds studied. The lack of marked convulsant properties of cefixime, cefonicid, cefuroxime, and cephradine suggests that these antibiotics may interact with a binding site which is different from that by which the beta-lactam antibiotics exert their convulsant effects or may demonstrate a reduced affinity for the relevant site(s).
Animals↗
Effects of sodium fusidate in animal models of insulin-dependent diabetes mellitus and septic shock.
We have evaluated the effects of the novel immunosuppressant sodium fusidate (fusidin) in the non-obese diabetic (NOD) mouse and in D-galactosamine (D-Gal)-presensitized BALB/c mice challenged with the bacterial superantigen, Staphylococcus aureus enterotoxin B (SEB) or with the endotoxin, Escherichia coli lipopolysaccharide (LPS). The NOD mouse model has clinical and histoimmunological features similar to those of human insulin-dependent diabetes mellitus (IDDM). The SEB- and LPS-treated BALB/c mouse models exhibit pathogenic similarities with human septic shock conditions. In the NOD mouse, fusidin suppressed the spontaneous development of insulitis (mean inhibition 73%) and hyperglycaemia (IDDM incidence 25% versus 0%) when administered at 40 mg/kg five times weekly for 8 consecutive weeks from the fourth week of age; concurrently treated animals exhibited reduced percentages of splenic T lymphocytes. This anti-diabetogenic effect was confirmed in the accelerated model of diabetes induced in the NOD mouse with cyclophosphamide (CY) (IDDM incidence 55% versus 21-6% using dosages of fusidin from 40 to 80 mg/kg five times weekly); protection from IDDM development was achieved even when the drug (80 mg/kg/day) was first administered 7 days after CY challenge. In contrast, fusidin did not reverse hyperglycaemia when administered to CY-treated animals within 3 days of IDDM development. In the two models of septic shock, prophylactic treatment with fusidin, 80 mg/kg given three times for 2 days prior to D-Gal/SEB or D-Gal/LPS challenge, drastically reduced the lethality compared with D-Gal/buffer-treated mice. This effect may depend on the inhibitory action of fusidin on the secretion of cytokines such as interferon-gamma and tumour necrosis factor-alpha, the serum levels of which were greatly diminished in the fusidin-treated mice (mean inhibition 50-90%). These results demonstrate that fusidin may have a role in the treatment of cell-mediated autoimmune diseases and cytokine-mediated infectious diseases in humans.
Animals↗
Novel pyrrolo- and thiazolo-imidazoles.
In this study, the synthesis and the stereochemical features of novel tricyclic derivatives containing an imidazole nucleus are described. The biological properties of the synthesized compounds as well as some aspects of the structure activity relationship are also discussed.
Animals↗
Synthesis and antihypertensive activity evaluation of indole derivatives N-acetamido substituted.
The synthesis of a series of 1-(alkyl- or aryl-aminocarbonylmethyl)-2-methyl- or 2-phenyl-indoles are described. All compounds were tested for antihypertensive activity on spontaneously hypertensive rats (SHR) and some of them showed a significant reduction of the arterial pressure.
Acetamides↗
Immunohistochemical distribution of S-100 protein and type IV collagen in human embryonic and fetal sympathetic neuroblasts.
The expression and distribution of S-100 protein and type IV collagen was studied immunohistochemically in sympathetic neuroblasts from the paravertebral region to the adrenal glands in human embryos and fetuses ranging from 7 to 12 weeks gestational age. From 7 weeks gestational age, S-100 protein was detected in round or oval cells mingling with sympathetic neuroblasts, and in spindle-shaped cells forming a continuous layer around them. The latter S-100 protein-positive cells were found in contact with the Schwann cells of nerve fibres entering the groups of sympathetic neuroblasts. Staining for type IV collagen showed that all groups of sympathetic neuroblasts were surrounded by a continuous basement membrane. By examining serial sections stained for type IV collagen and S-100 protein, a continuous basement membrane was found along the distribution pattern of the peripheral S-100 protein-positive spindle cells. The morphology of these cells, and their relationships with Schwann cells and with the basement membrane of the sympathetic neuroblasts, indicated that they were Schwann-like cells probably capable of synthesizing a continuous basement membrane separating the neuroblasts from the adjacent tissues. In contrast, the round or oval S-100 protein-positive cells, in contact with the sympathetic neuroblasts and not associated with nerve fibres, were considered as sustentacular or sustentacular precursor cells. At week 7 gestational age, the peri-adrenal sympathetic neuroblasts and their sustentacular and Schwann-like cells started to invade the adrenal glands and mingled with the adrenal cortical cells. These findings suggest the extra-adrenal origin of the sustentacular cells in embryonic and fetal adrenal glands.
Adrenal Glands↗
S-100 protein expression in a case of elastofibroma dorsi.
Elastofibroma is a rare tumorlike process that manifests as slowly growing, solid mass in the subscapular region of elderly persons. Histologically, it is characterized by the presence of fibrous connective tissue in which eosinophilic fibers and globular masses, stained by the elastic tissue stains, are interspersed. We report the immunohistochemical study of the cellular component in a case of subscapular elastofibroma in a 41-year-old man. An unexpected immunoreactivity for S-100 protein was detected in most fibroblast-like cells. S-100 protein expression may be related to a chondroid metaplasia of fibroblast-like cells in response to the continuous traumatic process occuring during the friction between the scapula and the underlying chest wall.
Adult↗
Protection from experimental autoimmune diabetes in the non-obese diabetic mouse with soluble interleukin-1 receptor.
We have evaluated the effects of a treatment with soluble interleukin-1 receptor (sIL-1R) in the accelerated model of autoimmune diabetes induced by cyclophosphamide (CY) in the non-obese diabetic (NOD) mouse. Prior to the CY challenge (350 mgkg body weight), female euglycemic NOD mice were randomly divided into three groups (A-C). Groups B and C were treated daily from 1 day before to 13 days after the CY challenge with sIL-1R at doses of 0.2 and 2 mg/kg body weight. Group A was treated with PBS. By 2 weeks after CY administration, an acute form of autoimmune diabetes with glycosuria, hyperglycemia and severe insulitis occurred in the majority (13/20, 65%) of the control mice (group A). In contrast, repeated injections with sIL-1R protected NOD mice from insulin-dependent diabetes mellitus (IDDM) development in a dose-dependent fashion; the incidence of IDDM was 53.3% (8/15) in the mice treated with 0.2 mg/kg and only 6.7% (1/15) in those treated with 2 mg/kg. However, none of the doses of the sIL-1R reduced the extent of insulitis in NOD mice. Importantly, the anti-diabetogenic property of sIL-1R may not involve major T cell function impairment; accordingly, in parallel experiments, splenic lymphoid cells from NOD mice not challenged with CY, but treated with 2 mg/kg sIL-1R for 5 consecutive days showed a normal distribution of mononuclear cell subsets and maintained their capacity to secrete interferon-gamma and IL-2 and to proliferate in response to polyclonal mitogenic stimulation with concanavalin A.
Animals↗
Anticonvulsant activity of pyrrolo[1',2':1,2]imidazo[4,5-b]pyridines, pyrrolo[2',1':2,3]imidazo[4,5-c] pyridines and pyrrolo[2,1-f]purines in DBA/2 mice.
1. The behavioural and anticonvulsant effects of eight pyrroloimidazopyridines (PI1a-d and PI2a-d) and four pyrrolopurines (PP) were studied after intraperitoneal administration in DBA/2 mice, a strain genetically susceptible to sound-induced seizures. 2. The anticonvulsant effects were evaluated in DBA/2 mice on seizures evoked by means of auditory stimulation (109 dB, 12-16 kHz) in animals placed singly under a perspex dome. 3. Hypothermic activity was observed after the highest doses of the pyrroloderivatives studied. 4. Our study demonstrated that the anticonvulsant effect of pyrroloimidazopyridines (PI1-7,8,8a,9-tetrahydro-6H-pyrrolo-[1',2':1,2]imidazo[4,5-b]pyrid in-6- ones) and pyrrolopurines (PP) was generally better than corresponding pyrrolobenzimidazoles (PB) and pyrroloimidazopyridines (PI2-5,5a,6,7-tetrahydro-8H-pyrrolo[2',1':2,3]imidazo[4,5-c]pyridin-8- ones) and, in some cases, comparable to that of phenytoin and desmethylclobazam. 5. The anticonvulsant potency of the derivatives studied cannot be directly related to their lipophilicity.
Animals↗
Synthesis and antitumor activity evaluation of 1-[(arylidene)amino]adamantanes.
Several 1-[(arylidene)amino]adamantanes were synthesized and evaluated in vitro as antitumor agents against 60 human tumor cell lines. Some of these derivatives showed specificity for human leukemia cell lines and 1-[(2-bromobenzylidene)amino]adamantane (2) (NSC 631076-L), the most active compound, was selected by the Biological Evaluation Committee (BEC), for in vivo testing.
Adamantane↗