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Biomedical subjects

M Guarneri

Publications and source records attributed to M Guarneri.

142 records · Page 8Linked to original sources
PubMedDate not supplied

Binding of the soybean Bowman-Birk proteinase inhibitor and of its chymotrypsin and trypsin inhibiting fragments to bovine alpha-chymotrypsin and bovine beta-trypsin. A thermodynamic study.

The effect of pH and temperature on the apparent association equilibrium constant (Ka) for the binding of the soybean Bowman-Birk proteinase inhibitor (BBI) and of its chymotrypsin and trypsin inhibiting fragments (F-C(p), F-T(p) and F-T(t), respectively) to bovine alpha-chymotrypsin (alpha-chymotrypsin) and bovine beta-trypsin (beta-trypsin) has been investigated. On the basis of Ka values, the proteinase inhibitor affinity can be arranged as follows: alpha-chymotrypsin: BBI approximately beta-trypsin:BBI approximately beta-trypsin:F-T(t) approximately beta-trypsin:F-T(p) much greater than alpha-chymotrypsin:F-C(p). F-C(p), F-T(p) and F-T(t) do not inhibit beta-trypsin and alpha-chymotrypsin action, respectively. On lowering the pH from 9.5 to 4.5, values of Ka for BBI, F-C(p), F-T(p) and/or F-T(t) binding to alpha-chymotrypsin and beta-trypsin decrease, thus reflecting the acid-pK shift of the invariant His57 catalytic residue from 7.0, in the free enzymes, to 5.2, in the proteinase:inhibitor complexes. Considering the known molecular models, the observed binding behaviour of BBI, F-C(p), F-T(p) and F-T(t) was related to the inferred stereochemistry of the proteinase:inhibitor contact regions.

Animals↗
PubMedDate not supplied

Inhibition of 'in vitro' tumor cell growth by aromatic polyamidines exhibiting antiproteinase activity.

Aromatic polyamidines containing two, three or four benzamidine residues inhibit proteinase activity and proliferation of different human tumor cell lines, including leukemic (K562, HEL), melanoma (Colo 38) and B-lymphoid (WI-L2) cell lines. In addition, the benzamidine derivatives analysed in the present study inhibit cell growth of the Chinese hamster FHO6T1-1 cell line, obtained after transfection of primary lung cells with the activated human T24-Ha-ras-1 oncogene. After treatment of FHO6T1-1 cells with benzamidine derivatives, a sharp decrease of the content of Ha-ras-1 mRNA was found, but not of transferrin receptor mRNA. We found that inhibition of cell proliferation by tetra-benzamidine derivatives is not restricted to tumor cells, but concerns also non-tumorigenic cell lines as well as normal primary fibroblasts. Therefore, our analysis was extended to di- and tri-benzamidine derivatives, which could be proposed as useful substrates in the synthesis of drug-conjugated monoclonal antibodies or growth factors. The data obtained demonstrate that these latter compounds and their halo-derivatives also exhibit strong antiproliferative effects on in vitro cultured cells.

Amidines↗
PubMedDate not supplied

[The condition of families of patients with schizophrenia in Italy: burden, social network and professional support].

OBJECTIVE: This study aimed to describe: a) the interventions received by patients with schizophrenia attending Italian mental health services (MHS); b) the relatives' burden and social network and the professional support received by the families. DESIGN: The study has been carried out in 30 MHS, randomly selected and stratified by geographic areas and population density. 25 patients with a DSM-IV diagnosis of schizophrenia and 25 relatives were recruited in each MHS. Family burden was evaluated in relation to: a) geographic area; b) interventions received by the patients; c) social and professional support received by the families. MAIN OUTCOME MEASURES: a) patients: Brief Psychiatric Rating Scale (BPRS) and Disability Assessment Interview (AD); b) key-relatives: Family Problems Questionnaire (QPF) and Social Network Questionnaire (QRS); c) interventions received by the patients and their families: Scheda di Rilevazione degli Interventi--Pattern of Care Schedule (SRI). RESULTS: Data on 709 patients and their key-relatives were collected. In the two months preceding the data collection, 35% of patients attended rehabilitative programmes; 80% of the families were in regular contact with the MHS and 8% received family psychoeducational interventions. Family burden was higher in Southern than in Central and Northern Italy. This difference disappeared when rehabilitative interventions and family support were provided. CONCLUSIONS: This study highlights that the situation of the families of patients with schizophrenia is more burdensome in Southern Italy and is greatly influenced by the type of interventions provided by the MHS.

Adolescent↗
PubMedDate not supplied

[Causes and psychosocial consequences of schizophrenia: the opinions of patient's relatives].

OBJECTIVE: Description of the opinions on schizophrenia and its psychosocial consequences in a sample of relatives of patients with schizophrenia, recruited in 30 Italian Mental Health Centres (MHC), stratified by geographic areas and population density. DESIGN: Cross-sectional study on key-relatives of clinically stable patients with a DSM-IV diagnosis of schizophrenia. Evaluation of relatives' opinions on schizophrenia and its psychosocial consequences, in relation to: a) patient's clinical and family's socio-demographic variables; b) geographic areas and population density. SETTING: 30 Italian MHC randomised and stratified by geographic areas (Northern, Central, Southern Italy) and population density (> 100,000 inhabitants; between 100,000 and 25,000 inhabitants; < 25,000 inhabitants). Main outcome measures--Patient's clinical status and social functioning: Brief Psychiatric Rating Scale (BPRS) and Disability Assessment interview (AD). Interventions provided to patient and his/her family: Scheda di Rilevazione degli Interventi--Pattern of Care Schedule (SRI). Relatives' opinions on schizophrenia and its psychosocial consequences: Questionnaire on the Opinions of the Family (QOF). RESULTS: Data on 709 patients and their key-relatives were collected. Relatives' pessimistic opinions on social competence of patients with schizophrenia were found to be associated with: high levels of patient's disability, hostility and negative symptoms, relatives' knowledge of patient's diagnosis of schizophrenia, residence in a medium or low population density area, low levels of relative's education. Relatives' pessimistic opinions on social restrictions imposed by schizophrenia were found to be associated with high levels of disability and high number of hospital admissions in the patient and older age in the relative. CONCLUSIONS: The results of this study emphasise the need to: a) provide families with educational interventions covering not only clinical aspects of schizophrenia, but also those concerning disability and psychosocial consequences of the disorder; b) plan educational campaigns on mental illnesses which take into account the socio-cultural characteristics of the target populations.

Adolescent↗
PubMedDate not supplied

Pyrazolo[3,4-d][1,2,3]triazole-1-carboxamides and 5-alkylaminopyrazolo[3,4-d]oxazoles: synthesis and evaluation of the in vitro antifungal activity.

A series of N-alkyl-N'-(4-diazo-5-pyrazolyl)-ureas (4) was thermally and photochemically converted into pyrazolo [3,4-d][1,2,3]triazole derivatives (5,6) and 5-alkylaminopyrazolo[3,4-d]oxazoles (7) respectively. The products were tested for in vitro antifungal activity against Fusarium culmorum, Botrytis cinerea, Phoma betae, Pythium ultimum, Sclerotinia minor and Rhizoctonia solani. The MIC and ED50 values of compound (6) against some of the test fungi were comparable to those of the reference fungicides iprodione and mancozeb.

Aminoimidazole Carboxamide↗
PubMedDate not supplied

New synthetic retinoids: effects on proliferation and differentiation.

Nine retinoid analogues were synthesized and their effects on cell proliferation and differentiation of tumor cell lines were analysed and compared with those of natural retinoids (retinoic acid, retinol, retinal). Our results demonstrate differential inhibitory effects of the synthetic retinoids on cell growth. This inhibitory activity of the synthetic retinoids was, in some cases, higher than that of retinoic acid and retinol. Natural and synthetic retinoids were found to be able to induce to a different extent erythroid differentiation of murine erythroleukemia cells and adipogenic conversion of Chinese Hamster FHO6N1-1 cells. Our data suggest that studies on the relationship between structure and biological activity could be approached by using the analysed synthetic retinoids.

Animals↗
PubMedDate not supplied

Effects of benzamidine derivatives on Ha-ras-1 mRNA accumulation in a Chinese hamster cell line transformed with the activated human T24 Ha-ras-1 oncogene.

Tetra benzamidine derivatives were found to inhibit proteinase activity, cell proliferation and accumulation of the Ha-ras-1 mRNA in the FHO6T1-1 Chinese Hamster cell line, transformed with the activated human T24-Ha-ras-1 oncogene. Di- and Tri-benzamidine derivatives were also found to be potent inhibitors of proliferation of FHO6T1-1 cells. These latter compounds could be proposed as useful substrates in the synthesis of drug-conjugated monoclonal antibodies or growth factors.

Amidines↗
PubMedDate not supplied

[The neuroleptic malignant syndrome (NMS). A report of a clinical case with a protracted and recurrent course. A review of the literature].

Neuroleptic malignant syndrome (NMS), characterized by catatonic behavior, generalized muscular rigidity, hyperthermia and autonomic dysfunction, can suddenly arise in patients treated with neuroleptic agents and carries a high mortality rate even today. A case of NMS due to i.m. therapy with haloperidol decanoate is reported in this paper, characterized by sustained course and a severe relapse due to a different therapy with another neuroleptic agent. The patient however, after a prolonged remission from the relapse, was able to resume long term therapy with neuroleptic drugs. The importance of monitoring blood levels of CPK during the follow-up and the effectiveness of therapy with bromocriptine and dantrolene in confirmed. Although the patient presented a good clinical response, she developed permanent cerebral and muscular damage. A wide review of the literature on NMS is reported to throw light on this syndrome, whose recognition and prompt diagnosis are necessary to reduce mortality.

Adult↗