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1.
J Cell Physiol ; : e31422, 2024 Sep 26.
Article in English | MEDLINE | ID: mdl-39324358

ABSTRACT

The cystic fibrosis transmembrane conductance regulator (CFTR) is a cyclic adenosine monophosphate (cAMP)-regulated chloride and bicarbonate ion channel found in many human cells. Its unique biochemical characteristics and role as a member of the adenosine triphosphate (ATP)-binding cassette transporters superfamily are pivotal for the transport of several substrates across cellular membranes. CFTR is known to interact, physically and functionally, with several other cellular proteins. Hence, its properties are essential for moving various substances across cell membranes and ensuring correct cell functioning. Genetic mutations or environmental factors may disrupt CFTR's function resulting in different possible phenotypes due to gene variations that affect not only CFTR's function, localization, and processing within cells, but also those of its interactors. This has been reported as an underlying cause of various diseases, including cystic fibrosis. The severe clinical implications of cystic fibrosis have driven intense research into the role of CFTR in lung function but its significance to fertility, particularly in men, has been comparatively understudied. However, ongoing and more recent research into CFTR and its interacting proteins in the testis or specific testicular cells is beginning to shed light on this field. Herein, we provide a comprehensive and up-to-date overview of the CFTR, its interactome, and its crucial role in male reproduction, highlighting recent discoveries and advancements in understanding the molecular mechanisms involved. The comprehension of these complex interactions may pave the way for potential therapeutic approaches to improve fertility of men suffering from alterations in the function of CFTR.

2.
Drug Dev Res ; 85(3): e22194, 2024 May.
Article in English | MEDLINE | ID: mdl-38704828

ABSTRACT

The aim the present study was to investigate the impact of novel pentavalent organobismuth and organoantimony complexes on membrane integrity and their interaction with DNA, activity against Sb(III)-sensitive and -resistant Leishmania strains and toxicity in mammalian peritoneal macrophages. Ph3M(L)2 type complexes were synthesized, where M = Sb(V) or Bi(V) and L = deprotonated 3-(dimethylamino)benzoic acid or 2-acetylbenzoic acid. Both organobismuth(V) and organoantimony(V) complexes exhibited efficacy at micromolar concentrations against Leishmania amazonensis and L. infantum but only the later ones demonstrated biocompatibility. Ph3Sb(L1)2 and Ph3Bi(L1)2 demonstrated distinct susceptibility profiles compared to inorganic Sb(III)-resistant strains of MRPA-overexpressing L. amazonensis and AQP1-mutated L. guyanensis. These complexes were able to permeate the cell membrane and interact with the Leishmania DNA, suggesting that this effect may contribute to the parasite growth inhibition via apoptosis. Taken altogether, our data substantiate the notion of a distinct mechanism of uptake pathway and action in Leishmania for these organometallic complexes, distinguishing them from the conventional inorganic antimonial drugs.


Subject(s)
Antimony , Antiprotozoal Agents , Cell Membrane , Drug Resistance , Organometallic Compounds , Antimony/pharmacology , Antimony/chemistry , Animals , Organometallic Compounds/pharmacology , Mice , Cell Membrane/drug effects , Antiprotozoal Agents/pharmacology , Macrophages, Peritoneal/drug effects , Macrophages, Peritoneal/parasitology , Leishmania/drug effects , DNA, Protozoan , Leishmania infantum/drug effects , Leishmania infantum/genetics , Mice, Inbred BALB C
3.
Vox Sang ; 118(9): 798-806, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37463772

ABSTRACT

At the symposium organized by the International Plasma and Fractionation Association and European Blood Alliance, experts presented their views and experiences showing that the public sector and its blood establishments may strengthen the collection and increase the supply of plasma using the right strategies in plasma donor recruitment, retention and protection, scaling-up collection by increasing the number of donors within improved/new infrastructure, supportive funding, policies and legislation as well as harmonization of clinical guidelines and the collaboration of all stakeholders. Such approaches should contribute to increased plasma collection in Europe to meet patients' needs for plasma-derived medicinal products, notably immunoglobulins and avoid shortages. Overall, presentations and discussions confirmed that European non-profit transfusion institutions are committed to increasing the collection of plasma for fractionation from unpaid donors through dedicated programmes as well as novel strategies and research.


Subject(s)
Blood Transfusion , Plasma , Humans , Europe , Plasma/chemistry , Immunoglobulins/analysis
4.
Neurochem Res ; 45(10): 2456-2473, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32779097

ABSTRACT

Neuroinflammation is a predisposing factor for the development of cognitive impairment and dementia. Among the new molecules that are currently being studied, ellagic acid (EA) has stood out for its neuroprotective properties. The present study investigated the effects of ellagic acid in the object recognition test, oxidative stress, cholinergic neurotransmission, glial cell expression, and phosphorylated Tau protein expression. For this, 32 male Wistar rats received an intraperitoneal (IP) application of lipopolysaccharides (LPS) at a dose of 250 µg/kg or 0.9% saline solution (SAL) for 8 days. Two hours after the IP injections, the animals received 100 mg/kg of EA or SAL via intragastric gavage. Behavioral parameters (open field test and object recognition) were performed on days 5, 6, and 7 of the experimental periods. The results showed that the treatment with EA in the LPS group was able to inhibit cognitive impairment, modulate the immune system response by significantly reducing glial cell expression, attenuating phosphorylated Tau and oxidative damage with consequent improvement in the antioxidant system, as well as preventing the increase of acetylcholinesterase activity. Thus, the neuroprotective effects of EA and its therapeutic potential in cognitive disorders secondary to neuroinflammation were demonstrated.


Subject(s)
Cognitive Dysfunction/drug therapy , Ellagic Acid/therapeutic use , Inflammation/drug therapy , Neuroprotective Agents/therapeutic use , Acetylcholinesterase/metabolism , Animals , Body Weight/drug effects , Cerebral Cortex/drug effects , Cognitive Dysfunction/chemically induced , Hippocampus/drug effects , Inflammation/chemically induced , Lipopolysaccharides , Male , Open Field Test/drug effects , Oxidative Stress/drug effects , Phosphorylation/drug effects , Rats, Wistar , tau Proteins/chemistry , tau Proteins/metabolism
5.
Molecules ; 24(11)2019 Jun 07.
Article in English | MEDLINE | ID: mdl-31181667

ABSTRACT

Two new complexes of Ru(II) with mixed ligands were prepared: [Ru(bpy)2smp](PF6) (1) and [Ru(phen)2smp](PF6) (2), in which smp = sulfamethoxypyridazine; bpy = 2,2'-bipyridine; phen = 1,10-phenanthroline. The complexes have been characterized by elemental and conductivity analyses; infrared, NMR, and electrospray ionization mass spectroscopies; and X-ray diffraction of single crystal. Structural analyses reveal a distorted octahedral geometry around Ru(II) that is bound to two bpy (in 1) or two phen (in 2) via their two heterocyclic nitrogens and to two nitrogen atoms from sulfamethoxypyridazine-one of the methoxypyridazine ring and the sulfonamidic nitrogen, which is deprotonated. Both complexes inhibit the growth of chronic myelogenous leukemia cells. The interaction of the complexes with bovine serum albumin and DNA is described. DNA footprinting using an oligonucleotide as substrate showed the complexes' preference for thymine base rich sites. It is worth notifying that the complexes interact with the Src homology SH3 domain of the Abl tyrosine kinase protein. Abl protein is involved in signal transduction and implicated in the development of chronic myelogenous leukemia. Nuclear magnetic resonance (NMR) studies of the interaction of complex 2 with the Abl-SH3 domain showed that the most affected residues were T79, G97, W99, and Y115.


Subject(s)
Antineoplastic Agents/chemical synthesis , Leukemia, Myelogenous, Chronic, BCR-ABL Positive/metabolism , Organometallic Compounds/chemical synthesis , Ruthenium/chemistry , Sulfamethoxypyridazine/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Circular Dichroism , Humans , K562 Cells , Leukemia, Myelogenous, Chronic, BCR-ABL Positive/drug therapy , Molecular Structure , Organometallic Compounds/chemistry , Organometallic Compounds/pharmacology , Proto-Oncogene Proteins c-abl/chemistry , Proto-Oncogene Proteins c-abl/metabolism , Spectrometry, Mass, Electrospray Ionization , X-Ray Diffraction , src Homology Domains
6.
Bioorg Med Chem ; 22(5): 1608-19, 2014 Mar 01.
Article in English | MEDLINE | ID: mdl-24530030

ABSTRACT

1,2,3-Triazole-, arylamino- and thio-substituted naphthoquinones (24, 8, and 2 representatives, respectively) were synthesized in moderate yields and evaluated against several human cancer cell lines (blood, ovarian, breast, central nervous system, colon, and prostate cancers and melanoma), showing, for some of them, IC50 values below 2 µM. The cytotoxic potential of the tested naphthoquinones was also assayed on non-tumor cells such as human peripheral blood mononucluear cells (PBMC) and two murine fibroblast lines (L929 and V79 cells). α-Lapachone- and nor-α-lapachone-based 1,2,3-triazoles and arylamino-substituted naphthoquinones showed potent cytotoxicity against different cancer cell lines. The compounds may represent promising new lead derivatives for anticancer drug development. The electrochemical properties of selected compounds were evaluated in an attempt to correlate them with antitumor activity.


Subject(s)
Naphthoquinones/chemistry , Triazoles/chemistry , Cell Proliferation , Click Chemistry , Humans , Models, Molecular , Molecular Structure , Structure-Activity Relationship
7.
J Stroke Cerebrovasc Dis ; 23(5): 850-4, 2014.
Article in English | MEDLINE | ID: mdl-23954607

ABSTRACT

BACKGROUND: Hyponatremia is a risk factor for stroke and cardiovascular disease. Even mild hyponatremia is associated with increased 30-day mortality after myocardial infarction, and it has recently shown to increase the 3-year mortality after a stroke. In this work, we investigated both acute and chronic clinical outcomes after a stroke in hyponatremic patients. METHODS: We reviewed all patients admitted between 2004 and 2011 with the diagnosis of acute ischemic stroke. Hyponatremia was defined as serum sodium level less than 135 mmol/L and recorded on admission. All hemorrhagic strokes were excluded. Data were analyzed using multivariate logistic regression. RESULTS: A total of 3585 patients with stroke were identified. Hyponatremia was observed in 565 (16%) patients. Baseline characteristics were similar between groups except heart failure (P = .015), cancer (P = .038), diabetes (P < .001), and dementia (P = .015). Hyponatremic patients had higher National Institutes of Health Stroke Scale (NIHSS) score on admission (P = .032) and at discharge (P = .02). Despite similar modified Barthel Index (mBI) preadmission, patients with hyponatremia had worse mBI on admission (P = .049). Hyponatremia was associated with higher mortality in hospital (P = .039) and at 3-month (P = .001) and 12-month follow-ups (P = .001). A poorer discharge disposition was seen in the hyponatremia group (P = .004). Complications during admission were similar between groups except for urinary infection (P = .008). Patients with hyponatremia had worse NIHSS and mBI values on admission, and their deficits worsened during their hospitalization. CONCLUSIONS: This is the first study to demonstrate that hyponatremia is associated with acute mortality and poorer discharge dispositions and to confirm that higher mortality occurs in these patients, even after 12 months after a stroke.


Subject(s)
Brain Ischemia/complications , Hyponatremia/complications , Stroke/complications , Aged , Aged, 80 and over , Biomarkers/blood , Brain Ischemia/diagnosis , Brain Ischemia/mortality , Brain Ischemia/therapy , Comorbidity , Disability Evaluation , Female , Humans , Hyponatremia/blood , Hyponatremia/diagnosis , Hyponatremia/mortality , Hyponatremia/therapy , Logistic Models , Male , Middle Aged , Multivariate Analysis , Patient Admission , Patient Discharge , Prognosis , Risk Factors , Sodium/blood , Stroke/diagnosis , Stroke/mortality , Stroke/therapy , Time Factors
8.
Molecules ; 19(5): 6009-30, 2014 May 12.
Article in English | MEDLINE | ID: mdl-24824136

ABSTRACT

Two novel organoantimony(V) and two organobismuth(V) complexes of the type ML2 were synthesized, with L = acetylsalicylic acid (HL1) or 3-acetoxybenzoic acid (HL2) and M = triphenylantimony(V) (M1) or triphenylbismuth(V) (M2). Complexes, [M1(L1)2] (1), [M1(L2)2]∙CHCl3 (2), [M2(L1)2], (3) and [M2(L2)2] (4), were characterized by elemental analysis, IR and NMR. Crystal structures of triphenylantimony(V) dicarboxylate complexes 1 and 2 were determined by single crystal X-ray diffraction. Structural analyses revealed that 1 and 2 adopt five-coordinated extremely distorted trigonal bipyramidal geometries, binding with three phenyl groups in the equatorial position and two deprotonated organic ligands (L) in the axial sites. The metal complexes, their metal salts and ligands were evaluated in vitro for their activities against Leishmania infantum and amazonensis promastigotes and Staphylococcus aureus and Pseudomonas aeruginosa bacteria. Both the metal complexes showed antileishmanial and antibacterial activities but the bismuth complexes were the most active. Intriguingly, complexation of organobismuth(V) salt reduced its activity against Leishmania, but increased it against bacteria. In vitro cytotoxic test of these complexes against murine macrophages showed that antimony(V) complexes were the least toxic. Considering the selectivity indexes, organoantimony(V) complexes emerge as the most promising antileishmanial agents and organobismuth(V) complex 3 as the best antibacterial agent.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antimony/pharmacology , Benzoic Acid/pharmacology , Organometallic Compounds/pharmacology , Terphenyl Compounds/pharmacology , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Antimony/chemistry , Benzoic Acid/chemical synthesis , Benzoic Acid/chemistry , Leishmania infantum/drug effects , Ligands , Macrophages/drug effects , Mice , Organometallic Compounds/chemical synthesis , Organometallic Compounds/chemistry , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects , Terphenyl Compounds/chemical synthesis , Terphenyl Compounds/chemistry
9.
Acta Crystallogr C Struct Chem ; 80(Pt 9): 478-486, 2024 Sep 01.
Article in English | MEDLINE | ID: mdl-39115535

ABSTRACT

It is well known that Hirshfeld surfaces provide an easy and straightforward way of analysing intermolecular interactions in the crystal environment. The use of atomic Hirshfeld surfaces has also demonstrated that such surfaces carry information related to chemical bonds which allow a deeper evaluation of the structures. Here we briefly summarize the approach of atomic Hirshfeld surfaces while further evaluating the kind of information that can be retrieved from them. We show that the analysis of the metal-centre Hirshfeld surfaces from structures refined via Hirshfeld Atom Refinement (HAR) allow accurate evaluation of contacts of type M...H, and that such contacts can be related to the overall shape of the surfaces. The compounds analysed were tetraaquabis(3-carboxypropionato)metal(II), [M(C4H3O4)2(H2O)4], for metal(II)/M = manganese/Mn, cobalt/Co, nickel/Ni and zinc/Zn. We also evaluate the sensitivity of the surfaces by an investigation of seemingly flat surfaces through analysis of the curvature functions in the direction of C-C bonds. The obtained values not only demonstrate variations in curvature but also show a correlation with the hybridization of the C atoms involved in the bond.

10.
Acta Crystallogr C Struct Chem ; 80(Pt 9): 505-513, 2024 Sep 01.
Article in English | MEDLINE | ID: mdl-39177772

ABSTRACT

The crystal structures of two coordination compounds, (acetato-κO)(2,2'-bipyridine-κ2N,N')(1,10-phenanthroline-κ2N,N')copper(II) acetate hexahydrate, [Cu(C2H3O2)(C10H8N2)(C12H8N2)](C2H3O2)·6H2O or [Cu(bipy)(phen)Ac]Ac·6H2O, and (acetato-κO)bis(2,2'-bipyridine-κ2N,N')copper(II) acetate-acetic acid-water (1/1/3), [Cu(C2H3O2)(C10H8N2)2](C2H3O2)·C2H4O2·3H2O or [Cu(bipy)2Ac]Ac·HAc·3H2O, are reported and compared with the previously published structure of [Cu(phen)2Ac]Ac·7H2O (phen is 1,10-phenanthroline, bipy for 2,2'-bipyridine, ac is acetate and Hac is acetic acid). The geometry around the metal centre is pentacoordinated, but highly distorted in all three cases. The coordination number and the geometric distortion are both discussed in detail, and all complexes belong to the space group P-1. The analysis of the geometric parameters and the Hirshfeld surface properties dnorm and curvedness provide information about the metal-ligand interactions in these complexes and allow comparison with similar systems.

11.
Behav Anal Pract ; 17(2): 456-470, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38966257

ABSTRACT

Given the advancement of behavioral research in culture and social behavior, it seems natural for the community of behavior analysts to progress towards increased political engagement and a dedication to social justice. To reach this goal, it is necessary to act inside one's own communities and organizations. The purpose of this article is to report on the efforts of the Brazilian Association for Behavioral Psychology and Medicine (ABPMC) to increase equity and social justice during the 2017-2018 term. First, we present an overview of the ABPMC. Next, we describe the process of identifying, planning, and implementing equity and social justice actions in the association. The problems targeted were the discontinuation of policies from one term to another, elitism and centralization, the lack of topics with social and political relevance in the annual conference's scientific program, and the lack of support for the participation of women (especially mothers) in clinical and academic practice. Supplementary Information: The online version contains supplementary material available at 10.1007/s40617-020-00510-2.

12.
Rev Bras Med Trab ; 22(2): e20231213, 2024.
Article in English | MEDLINE | ID: mdl-39371286

ABSTRACT

Introduction: The increasing prevalence ofsedentary behavior at work, which has been exacerbated by technological advancement and remote work models, can compromise worker health, leading to both physical and mental problems. Increasing research on sedentary behavior has resulted in interventions such as active breaks. Objectives: This study addresses the impact of sedentary behavior at work and the effects of active breaks. Methods: This descriptive-exploratory study with a mixed-methods approach included 70 professionals of both sexes, 86% women (35.2 [SD, 10.2] years) and 14% men (33.5 [SD, 11] years), who worked remotely in administrative roles. The intervention was a 25-week active break protocol involving lectures, a questionnaire, and an app. Results: At the end of the intervention, 64% of participants were taking active breaks. Spending > 10 hours a day in sedentary behavior reduced significantly (from 31% to 14%), as did the proportion of workers who did not exercise (from 43% to 26%; p = 0.002). There were also reductions in post-lunch sleepiness, perceived stress (p < 0.01), and pain/discomfort (p < 0.01). Conclusions: Management programs for sedentary behavior should consider the use of active breaks, since they can reduce sedentary behavior and perceived sleepiness, stress, and pain. This will result in a healthier work environment, increasing employee quality of life as well as company productivity.


Introdução: Com a predominância do sedentarismo ocupacional, agravado pelo avanço tecnológico e pelo trabalho remoto, a saúde dos trabalhadores pode ser comprometida, incluindo problemas físicos e mentais, o que faz com que estudos sobre o comportamento sedentário e intervenções como pausas ativas ganhem destaque. Objetivos: O estudo aborda o impacto do sedentarismo no ambiente de trabalho e a relevância das pausas ativas para mitigar seus efeitos. Métodos: Tratou-se de estudo descritivo-exploratório com abordagem qualiquantitativa, realizado com 70 profissionais de ambos os sexos, 86% mulheres (35,2±10,2 anos) e 14% homens (33,5±11 anos). Todos trabalhavam remotamente em funções administrativas. Os participantes foram orientados a seguir uma rotina de pausas ativas durante 25 semanas. O estudo usou palestras, um questionário e um aplicativo para a prática. Resultados: Dos participantes, 64% adotaram as pausas ativas após a intervenção. Foi observada uma redução significativa no tempo sedentário (superior a 10 horas), de 31 para 14%, e no número de trabalhadores que não se exercitavam, de 43 para 26% (p = 0,002). Notou-se também uma redução na sonolência após o almoço, na percepção do estresse (p < 0,01) e nas dores e/ou desconforto no corpo (p < 0,01). Conclusões: A rotina de pausas ativas parece ser uma estratégia para diminuir o comportamento sedentário e melhorar a percepção quanto a sonolência, estresse e dores. Portanto, a implementação de programas de gestão ativa do comportamento sedentário, por meio de pausas ativas, pode proporcionar um ambiente de trabalho mais produtivo e saudável, beneficiando a qualidade de vida dos funcionários e a produtividade da empresa.

13.
Cancer Treat Res Commun ; 40: 100832, 2024.
Article in English | MEDLINE | ID: mdl-39033692

ABSTRACT

BACKGROUND: Amivantamab, an EGFR-MET bispecific antibody, is the first approved targeted therapy for patients with EGFR Ex20ins NSCLC after prior platinum-based chemotherapy-a population with historically poor outcomes before amivantamab approval. As antitumor activity in single-arm studies typically focuses on responders, the evaluation of outcomes in patients with stable disease (SD) as best response is of clinical interest. PATIENTS AND METHODS: Among 114 patients with post-platinum EGFR Ex20ins NSCLC in CHRYSALIS (NCT02609776; data cutoff: March 30, 2021), response was assessed by blinded independent central review via RECIST v1.1. Patients alive and receiving therapy at 12 weeks were grouped by response at this landmark: partial or complete response (PR+), SD, or progressive disease (PD). Progression-free survival (PFS) and overall survival (OS) by response cohort were determined using the Kaplan-Meier method; hazard ratios (HRs) and 95% confidence intervals (CIs) between response cohorts were calculated using Cox proportional hazards regression. RESULTS: Among patients alive and receiving therapy at 12 weeks (n=107), 42 (39%) had PR+, 52 (49%) had SD, and 13 (12%) had PD. Among patients with PR+ and SD, median PFS was 12.2 and 7.0 months, respectively. A corresponding improvement in OS was observed in patients achieving PR+ (median: not reached; HR vs PD=0.21 [95% CI: 0.08-0.54]) and SD (median: 23.0 months; HR vs PD=0.33 [95% CI: 0.14-0.77]), relative to those with PD (median: 14.0 months). CONCLUSION: SD was observed in 49% of patients receiving amivantamab, with corresponding increases in OS that dramatically improved the prognoses of this patient population.


Subject(s)
Carcinoma, Non-Small-Cell Lung , ErbB Receptors , Lung Neoplasms , Adult , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Antibodies, Bispecific/administration & dosage , Antibodies, Bispecific/adverse effects , Carcinoma, Non-Small-Cell Lung/drug therapy , Carcinoma, Non-Small-Cell Lung/genetics , Carcinoma, Non-Small-Cell Lung/pathology , Carcinoma, Non-Small-Cell Lung/mortality , ErbB Receptors/genetics , ErbB Receptors/antagonists & inhibitors , Exons , Lung Neoplasms/drug therapy , Lung Neoplasms/genetics , Lung Neoplasms/pathology , Lung Neoplasms/mortality , Mutation , Progression-Free Survival
14.
Bioorg Med Chem ; 21(21): 6337-48, 2013 Nov 01.
Article in English | MEDLINE | ID: mdl-24074878

ABSTRACT

In our continued search for novel trypanocidal compounds, twenty-six derivatives of para- and ortho-naphthoquinones coupled to 1,2,3-triazoles were synthesized. These compounds were evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease. Compounds 17-24, 28-30 and 36-38 are described herein for the first time. Three of these novel compounds (28-30) were found to be more potent than the standard drug benznidazole, with IC50/24h values between 6.8 and 80.8µM. Analysis of the toxicity to heart muscle cells led to LC50/24h of <125, 63.1 and 281.6µM for 28, 29 and 30, respectively. Displaying a selectivity index of 34.3, compound 30 will be further evaluated in vivo. The electrochemical properties of selected compounds were evaluated in an attempt to find correlations with trypanocidal activity, and it was observed that more electrophilic quinones were generally more potent.


Subject(s)
Naphthoquinones/chemistry , Triazoles/chemistry , Trypanocidal Agents/chemical synthesis , Animals , Cell Survival/drug effects , Cells, Cultured , Crystallography, X-Ray , Electrochemical Techniques , Electrodes , Mice , Molecular Conformation , Myocytes, Cardiac/cytology , Structure-Activity Relationship , Triazoles/chemical synthesis , Triazoles/toxicity , Trypanocidal Agents/chemistry , Trypanocidal Agents/toxicity , Trypanosoma cruzi/drug effects
15.
Biometals ; 26(5): 677-91, 2013 Oct.
Article in English | MEDLINE | ID: mdl-23749148

ABSTRACT

Complexes [Au(2Ac4oT)Cl][AuCl2] (1), [Au(Hpy2Ac4mT)Cl2]Cl·H2O (2), [Au(Hpy2Ac4pT)Cl2]Cl (3), [Pt(H2Ac4oT)Cl]Cl (4), [Pt(2Ac4mT)Cl]·H2O (5), [Pt(2Ac4pT)Cl] (6) and [Pt(L)Cl2OH], L = 2Ac4mT (7), 2Ac4oT (8), 2Ac4pT (9) were prepared with N(4)-ortho- (H2Ac4oT), N(4)-meta- (H2Ac4mT) and N(4)-para- (H2Ac4pT) tolyl-2-acetylpyridine thiosemicarbazone. The cytotoxic activities of all compounds were assayed against U-87 and T-98 human malignant glioma cell lines. Upon coordination cytotoxicity improved in 2, 5 and 8. In general, the gold(III) complexes were more cytotoxic than those with platinum(II,IV). Several of these compounds proved to be more active than cisplatin and auranofin used as controls. The gold(III) complexes probably act by inhibiting the activity of thioredoxin reductase enzyme whereas the mode of action of the platinum(II,IV) complexes involves binding to DNA. Cells treated with the studied compounds presented morphological changes such as cell shrinkage and blebs formation, which indicate cell death by apoptosis induction.


Subject(s)
Antineoplastic Agents/pharmacology , Glioma/drug therapy , Organogold Compounds/chemistry , Organogold Compounds/pharmacology , Organoplatinum Compounds/chemistry , Organoplatinum Compounds/pharmacology , Thiosemicarbazones/chemistry , Thiosemicarbazones/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Death/drug effects , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Glioma/pathology , Humans , Models, Molecular , Molecular Structure , Structure-Activity Relationship , Tumor Cells, Cultured
16.
Acta Crystallogr C ; 69(Pt 9): 1010-2, 2013 Sep.
Article in English | MEDLINE | ID: mdl-24005510

ABSTRACT

The crystal structure of the title complex, [Cu(C5H7O2)I(C10H8N2)], in the space group P1 with Z = 4, is stabilized by π-π interactions and weak C-H···I interactions. The presence of two molecules in the asymmetric unit is associated with different intermolecular π-π interactions between two symmetry-related molecules of each type.

17.
Res Sports Med ; 21(4): 355-66, 2013.
Article in English | MEDLINE | ID: mdl-24067121

ABSTRACT

The purposes of this study were to compare the repetition performance and rating of perceived exertion (RPE) in different exercises order of three resistance training (RT) exercises: bench press (BP), shoulder press (SP), and triceps extension (TE). Twelve trained men participated in this study (26.75 ± 2.49 years; 177 ± 4.66 cm; 77.7 ± 6.20 kg; 12.61 ± 2.01% body fat; RT experience 3.58 ± 1.24 years). Data were collected in two phases: (1) 10 RM test for BP, SP, and TE and (2) performance of six RT sequences. The sequences were: SEQA (BP, SP, TE), SEQB (BP, TE, SP), SEQC (SP, BP, TE), SEQD (SP, TE, BP), SEQE (TE, BP, SP), and SEQF (TE, SP, BP). The repetition performance on SEQD was significantly smaller than SEQE and SEQF. No significant differences were found for repetition performance and RPE among other sequences. These data indicate that priority might be given to exercises performed in the beginning of the RT session.


Subject(s)
Athletic Performance/physiology , Resistance Training/methods , Adult , Cross-Over Studies , Humans , Male , Muscle Fatigue/physiology , Physical Exertion/physiology
18.
Rev Esp Sanid Penit ; 25(2): 70-79, 2023.
Article in English | MEDLINE | ID: mdl-37552276

ABSTRACT

OBTECTIVES: Good communication is essential for resolving social conflicts, especially in closed communities such as prisons. When communication is interrupted by factors such as hearing loss or difficulties in coordination, voice, language, fluency, or disruption of any of the biological systems required to communicate, Human Communication Disorders can appear. This review aimed to identify the most prevalent communication disorders amongst prison inmates. MATERIAL AND METHOD: Systematic review through databases of studies that analyze individual inmates with communication disorders over the last 38 years. After reading the titles and abstracts and applying the eligibility criteria, 25 articles were selected and included in the final review. RESULTS: A sample of 2,188 individuals was evaluated, two studies were conducted with a female population only, while twelve studied exclusively males, and 11 articles had a mixed population. All the studies included evaluated language and communication disorders in general, with language impairment being more prevalent There are no English language studies evaluating language and communication disorders in incarcerated individuals from African countries, Latin America or Asia. DISCUSSION: Inmates have a high prevalence of language and communication disorders, and thus end up being more vulnerable within the prison system. Speech therapists are important members of the legal workforce and improve the health, well-being and participation of people in contact with or at risk of contact with the judicial system through the prevention, early detection, assessment and treatment of communication disorders.


Subject(s)
Language Disorders , Prisoners , Male , Humans , Female , Asia , Africa , Prisons
19.
Acta Crystallogr B Struct Sci Cryst Eng Mater ; 79(Pt 4): 281-295, 2023 Aug 01.
Article in English | MEDLINE | ID: mdl-37402161

ABSTRACT

Experimental charge density analysis is conducted on the coordination compound tetraaquabis(hydrogenmaleato)nickel(II), which exhibits a short intramolecular hydrogen bond. Through topological analysis, the nature of Ni-O bonds is concluded to be intermediate between ionic and covalent, but mainly presenting an ionic character, while the short hydrogen bond is classified as covalent in nature. The compound was also analysed after Hirshfeld atom refinement performed using NoSpherA2. A topological analysis was conducted on the molecular wavefunction and the results are compared with those obtained from experiment. In general, there is good agreement between the refinements, and the chemical bonds involving H atoms are in better agreement with what is expected from neutron data after HAR than they are after multipole refinement.

20.
Cranio ; : 1-8, 2023 Nov 13.
Article in English | MEDLINE | ID: mdl-37955100

ABSTRACT

This systematic review aimed to assess the prevalence of temporomandibular disorders (TMD) in the Brazilian population, with studies that used the RDC/TMD or DC/TMD as diagnostic tools. A total of 6365 people from 11 studies were included. Sample mean age ranged from 12 to 69.5 years. The pooled prevalence of TMD was 33.6% (95% CI 31.5-35.8; I2 = 37.2). Prevalence of TMD was higher in females (37.0%) than in males (29.3%). Our results indicate that TMD is a prevalent condition across Brazil's territories. The results from this meta-analysis can help calculate more accurate sample sizes for future studies.

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