Genotoxicity and Anticancer Effects of the Aminothiophene Derivatives SB-44, SB- 83, and SB-200 in Cancer Cells.

Introduction: Thiophene derivatives have been widely studied as promising options for the treatment of solid tumors. Previous studies have shown that thiophene derivatives have antileishmanial activity and cytotoxic activity against breast, colon, and ovarian cancer cells.

Methods: In our study, we evaluated the anticancer activities of three aminothiophene derivatives: SB-44, SB-83, and SB-200, in prostate and cervical adenocarcinoma cells.

Adult Native Joint Septic Arthritis: A Nine-Year Retrospective Analysis in a Portuguese University Hospital.

Introduction: Septic arthritis of a native joint represents a medical emergency. Drainage and effective antibiotic treatment are critical to avoid joint destruction and long-term impairment. The aim of this study was to evaluate epidemiological and clinical characteristics of patients with the diagnosis of septic arthritis to help establish local guidelines for empirical antibiotic treatment.

Deep neck space infection and Lemierre's syndrome caused by : A case report.

Introduction: Deep neck space infections most commonly arise from a septic focus of the mandibular teeth, tonsils, parotid gland, middle ear or sinuses, usually with a rapid onset and frequently with progression to life-threatening complications. Lemierre's syndrome is classically defined by an oropharyngeal infection with internal jugular vein thrombosis followed by metastatic infections in other organs.

Case Presentation: A 32-year-old female patient, with no significant past medical history, was diagnosed with a dental abscess on her left inferior 3 molar.

Mart. Fractions Promote Cell Cycle Arrest and Inhibit Autophagic Flux in Human Cervical Cancer Cell Lines.

Plant-based compounds are an option to explore and perhaps overcome the limitations of current antitumor treatments. Mart. is a plant with a broad spectrum of biological activities, but its antitumor activity is still unclear.

Improvement of antimalarial activity of a 3-alkylpiridine alkaloid analog by replacing the pyridine ring to a thiazole-containing heterocycle: Mode of action, mutagenicity profile, and Caco-2 cell-based permeability.

The development of new antimalarial drugs is urgent to overcome the spread of resistance to the current treatment. Herein we synthesized the compound 3, a hit-to‑lead optimization of a thiazole based on the most promising 3-alkylpyridine marine alkaloid analog. Compound 3 was tested against Plasmodium falciparum and has shown to be more potent than its precursor (IC values of 1.

[Late Neuroborreliosis in an Erasmus Programme Student].

Lyme disease is an endemic zoonosis, the most prevalent tick-transmitted infection in temperate areas of Europe, North America and Asia. It is a multisystemic disease with cutaneous, musculoskeletal, neurologic and cardiac manifestations, according to the stage of the disease. We describe a case of late neuroborreliosis in an Erasmus programme student living in Porto.

Target-Guided Synthesis and Antiplasmodial Evaluation of a New Fluorinated 3-Alkylpyridine Marine Alkaloid Analog.

The need to develop new alternatives for antimalarial treatment is urgent. Herein, we report the synthesis and antimalarial evaluation of a small library of synthetic 3-alkylpyridine marine alkaloid (3-APA) analogs. First, the compounds were evaluated in vitro against .

Digoxin reduces the mutagenic effects of Mitomycin C in human and rodent cell lines.

Digoxin is a drug widely used to treat heart failure and studies have demonstrated its potential as anticancer agent. In addition, digoxin presents the potential to interact with a series of other compounds used in medicine. The aim of the present study was to evaluate in vitro the cytotoxicity, genotoxicity and mutagenicity of digoxin and its potential to interact with the mutagen Mitomycin C (MMC).

Tapirira guianensis Aubl. Extracts Inhibit Proliferation and Migration of Oral Cancer Cells Lines.

Cancer of the head and neck is a group of upper aerodigestive tract neoplasms in which aggressive treatments may cause harmful side effects to the patient. In the last decade, investigations on natural compounds have been particularly successful in the field of anticancer drug research. Our aim is to evaluate the antitumor effect of Aubl.

γ-Benzylidene digoxin derivatives synthesis and molecular modeling: Evaluation of anticancer and the Na,K-ATPase activity effect.

Cardiotonic steroids (CS), natural compounds with traditional use in cardiology, have been recently suggested to exert potent anticancer effects. However, the repertoire of molecules with Na,K-ATPase activity and anticancer properties is limited. This paper describes the synthesis of 6 new digoxin derivatives substituted (on the C17-butenolide) with γ-benzylidene group and their cytotoxic effect on human fibroblast (WI-26 VA4) and cancer (HeLa and RKO) cell lines as well as their effect on Na,K-ATPase activity and expression.

Leishmanicidal, antiproteolytic, and mutagenic evaluation of alkyltriazoles and alkylphosphocholines.

A series of 16 simple long-chain alkyltriazoles and two novel alkylphosphocholine derivatives containing an azide moiety were evaluated in vitro for their leishmanicidal activity against. Among the 18 compounds tested, the eight most active compounds against promastigote forms were selected for further evaluation against amastigote forms. These compounds were also evaluated for their cytotoxicity against murine macrophages and tested as inhibitors of cysteine protease rCPB2.

Effect of eosinophil cationic protein on human oral squamous carcinoma cell viability.

The exact function of eosinophils in cancer, particularly in oral squamous cell carcinoma (OSCC), has not yet been elucidated and the possible antitumor effect of these leukocytes is associated with the release of cytotoxic proteins, particularly eosinophil cationic protein (ECP). The aim of this study was to evaluate the effect of ECP on human OSCC lines and to provide novel insights into the role of eosinophils in these tumors. The viability of the SCC-4 and SCC-25 OSCC cell lines was assessed by colorimetric assay using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT).

21-Benzylidene digoxin: a proapoptotic cardenolide of cancer cells that up-regulates Na,K-ATPase and epithelial tight junctions.

Cardiotonic steroids are used to treat heart failure and arrhythmia and have promising anticancer effects. The prototypic cardiotonic steroid ouabain may also be a hormone that modulates epithelial cell adhesion. Cardiotonic steroids consist of a steroid nucleus and a lactone ring, and their biological effects depend on the binding to their receptor, Na,K-ATPase, through which, they inhibit Na+ and K+ ion transport and activate of several intracellular signaling pathways.

Effects of digoxin and Na, K-ATPase immunoexpression on human oral squamous carcinomas.

Aim: The present study evaluated the expression of α1 and β1 Na,K-ATPase, as well as the effects of digoxin (DGX) on oral squamous cell carcinomas (OSCCs).

Patients And Methods: Immunohistochemical expression of α1 and β1 Na,K-ATPase were evaluated in 60 patients who underwent treatment at the São João de Deus Hospital. SCC-25 viability was assessed by the colorimetric assay.

Synthesis and biological evaluation of novel 3-alkylpyridine marine alkaloid analogs with promising anticancer activity.

Cancer continues to be one of the most important health problems worldwide, and the identification of novel drugs and treatments to address this disease is urgent. During recent years, marine organisms have proven to be a promising source of new compounds with action against tumoral cell lines. Here, we describe the synthesis and anticancer activity of eight new 3-alkylpyridine alkaloid (3-APA) analogs in four steps and with good yields.

Evaluation of healing wound and genotoxicity potentials from extracts hydroalcoholic of Plantago major and Siparuna guianensis.

Despite the large use of the Plantago major and Siparuna guianensis in traditional medicine, there are no studies demonstrating the effectiveness from extracts of these plants in the healing process by the present methodology. This study reported the effects and toxicity of the P. major and S.

In vitro photodynamic therapy against Foncecaea pedrosoi and Cladophialophora carrionii.

Photodynamic therapy (PDT) has been originally developed for cancer treatment, but recently, it has been successfully employed against microorganisms, including fungi. Chromoblastomycosis is a subcutaneous fungal infection that is recalcitrant to conventional antifungal drug therapy. The most frequent species involved are Foncecaea pedrosoi and Cladophialophora carrionii.

Genotoxicity of polar and apolar extracts obtained from Qualea multiflora and Qualea grandiflora.

Ethnopharmacological Relevance: The species Qualea grandiflora and Qualea multiflora, which belong to the Vochysiaceae family, are common in the Brazilian savannah (Cerrado biome), and the local inhabitants use these species to treat external ulcers and gastric diseases and as an anti-inflammatory agent. Studies have demonstrated that these plants contain compounds that exhibit pharmacological activities; however, the risks associated with their consumption are not known.

Material And Methods: In the present study, the mutagenicity of polar and apolar extracts from Qualea grandiflora and Qualea multiflora were assessed by employing the Ames assay with and without metabolic activation.

Photodynamic therapy for pathogenic fungi.

Photodynamic therapy (PDT) is a minimally invasive approach, in which a photosensitiser compound is activated by exposure to visible light. The activation of the sensitiser drug results in several chemical reactions, such as the production of oxygen reactive species and other reactive molecules, whose presence in the biological site leads to the damage of target cells. Although PDT has been primarily developed to combat cancerous lesions, this therapy can be employed for the treatment of several conditions, including infectious diseases.

Assessment of the genetic risks of a metallic alloy used in medical implants.

The use of artificial implants provides a palliative or permanent solution for individuals who have lost some bodily function through disease, an accident or natural wear. This functional loss can be compensated for by the use of medical devices produced from special biomaterials. Titanium alloy (Ti-6Al-4V) is a well-established primary metallic biomaterial for orthopedic implants, but the toxicity of the chemical components of this alloy has become an issue of concern.

Phenolic compounds in leaves of Alchornea triplinervia: anatomical localization, mutagenicity, and antibacterial activity.

Phenolic compounds are produced by secretory idioblasts and hypodermis, and by specialized cells of the epidermis and chlorenchyma of leaves of Alchornea triplinervia. Phytochemical investigation of these leaves led to the isolation of the known substances quercetin, quercetin-7-O-beta-D-glucopyranoside, quercetin-3-O-beta-D-glucopyranoside, quercetin-3-O-beta-D-galactopyranoside, quercetin-3-O-alpha-L-arabinopyranoside, amentoflavone, brevifolin carboxylic acid, gallic acid, and methyl gallate from the methanolic extract, and stigmasterol, campesterol, sitosterol, lupeol, friedelan-3-ol, and friedelan-3-one from the chloroform extract. In studies of antibacterial activity and mutagenicity, the methanolic extract showed promising activity against Staphylococcus aureus (MIC = 62.

Inhibition of virulence factors of Candida spp. by different surfactants.

Candida yeasts are opportunistic pathogens responsible for infections in immunocompromised individuals. Among the virulence factors present in these yeasts we can mention the ability to adhere to host cells, exoenzyme production and germ tube formation. Several compounds, such as antifungal agents, plants extracts, protein inhibitors and surfactants, have been tested regarding their capacity in inhibit Candida spp.

Low-level laser therapy (LLLT) attenuates RhoA mRNA expression in the rat bronchi smooth muscle exposed to tumor necrosis factor-alpha.

Low-level laser therapy (LLLT) has been found to produce anti-inflammatory effects in a variety of disorders. Bronchial smooth muscle (BSM) hyperreactivity is associated with increased Ca+2 sensitivity and increased RhoA mRNA expression. In the current study, we investigated if LLLT could reduce BSM contraction force and RhoA mRNA expression in tumor necrosis factor-alpha (TNF-alpha)-induced BSM hyperreactivity.