Lucindo Quintans

Redox properties and cytoprotective actions of atranorin, a lichen secondary metabolite.

Atranorin (ATR) is a lichenic secondary metabolite with potential uses in pharmacology. Antinociceptive and antiinflammatory actions have been reported, and the use of atranorin-enriched lichen extracts in folk medicine is widespread. Nonetheless, very few data on ATR biological actions are available. Here, we evaluated free radical scavenging activities and antioxidant potential of ATR using various in vitro assays for scavenging activity against hydroxyl radicals, hydrogen peroxide, superoxide radicals, and nitric oxide. The total reactive antioxidant potential (TRAP) and total antioxidant reactivity (TAR) indexes and in vitro lipoperoxidation were also evaluated. Besides, we determined the cytoprotective effect of ATR on H(2)O(2)-challenged SH-SY5Y cells by the MTT assay. ATR exerts differential effects towards reactive species production, enhancing hydrogen peroxide and nitric oxide production and acting as a superoxide scavenger; no activity toward hydroxyl radical production/scavenging was observed. Besides, TRAP/TAR analysis indicated that atranorin acts as a general antioxidant, although it demonstrated to enhance peroxyl radical-induced lipoperoxidation in vitro. ATR was not cytotoxic, and also protected SH-SY5Y cells against H(2)O(2)-induced cell viability impairment. Our results suggest that ATR has a relevant redox-active action, acting as a pro-oxidant or antioxidant agent depending on the radical. Also, it will exert cytoprotective effects on cells under oxidative stress induced by H(2)O(2).

Signs and symptoms of temporomandibular dysfunction in fibromyalgic patients.

ObjectiveThe objective of this study was to determine the frequency of signs and symptoms of temporomandibular disorder (TMD) in fibromyalgic patients. MethodsSixty subjects of both sexes (mean age, 49.2 ± 13.8 years) with fibromyalgia (FM) diagnosis were included in this study. All patients were examined by a calibrated investigator to identify the presence of TMD using the Research Diagnostic Criteria for TMD. ResultsThe most common signs (A) and symptoms (B) reported by FM patients were (A) pain in the masticatory muscles (masseter, 80%; posterior digastric, 76.7%), pain in the temporomandibular joint (83.3%), and 33.3% and 28.3%, respectively, presented joint sounds when opening and closing the mouth; (B) headache (97%) and facial pain (81.7%). In regard to the classic triad for the diagnosis of the TMD, it was found that 35% of the FM patients presented, at the same time, pain, joint sounds, and alteration of the mandibular movements. It was verified that myofascial pain without limitation of mouth opening was the most prevalent diagnosis (47%) for the RDC subgroup I. For the subgroup II, the disk displacement with reduction was the most prevalent diagnosis (21.6%). For the subgroup III, 36.7% of the subjects presented osteoarthritis. ConclusionsThus, there is a high prevalence of signs and symptoms of TMD in FM patients, indicating the need for an integrated diagnosis and treatment of these patients, which suggest that the FM could be a medium- or long-term risk factor for the development of TMD.

Nanostructured transdermal hormone replacement therapy for relieving menopausal symptoms: a confocal Raman spectroscopy study

OBJECTIVE: To determine the safety and efficacy of a transdermal nanostructured formulation of progesterone (10%) combined with estriol (0.1%) + estradiol (0.25%) for relieving postmenopausal symptoms. METHODS: A total of 66 postmenopausal Brazilian women with climacteric symptoms of natural menopause received transdermal nanostructured formulations of progesterone and estrogens in the forearm daily for 60 months to mimic the normal ovarian secretory pattern. Confocal Raman spectroscopy of hormones in skin layers was performed. Clinical parameters, serum concentrations of estradiol and follicle-stimulating hormone, blood pressure, BI-RADS classification from bilateral mammography, and symptomatic relief were compared between baseline and 60 months post-treatment. Clinicaltrials.gov: NCT02033512. RESULTS: An improvement in climacteric symptoms was reported in 92.5% of women evaluated before and after 60 months of treatment. The serum concentrations of estradiol and follicle-stimulating hormone changed significantly (p<0.05) after treatment; the values of serum follicle-stimulating hormone decreased after 60 months from 82.04±4.9 to 57.12±4.1 IU/mL. A bilateral mammography assessment of the breasts revealed normal results in all women. No adverse health-related events were attributed to this hormone replacement therapy protocol. CONCLUSION: The nanostructured formulation is safe and effective in re-establishing optimal serum levels of estradiol and follicle-stimulating hormone and relieving the symptoms of menopause. This transdermal hormone replacement therapy may alleviate climacteric symptoms in postmenopausal women.

EFFECTS OF A NEW TESTOSTERONE TRANSDERMAL DELIVERY SYSTEM, BIOLIPID B2®-TESTOSTERONE IN HEALTHY MIDDLE AGED MEN: A CONFOCAL RAMAN SPECTROSCOPY STUDY

The Transdermal Delivery System (BIOLIPID B2®) is a nanoemulsion that can be a pplied directly to the skin by a metered pump to deliver hormones into the systemic circulation. The ai ms of this study were to assess the efficacy of BIOLIPID B2 ® to deliver testosterone systemically and evaluate the short - term effects on Thyroid - Stimulating Hormone (TSH), C - reactive protein (CRP) serum levels and blood pressure in middle aged men with tes tosterone deficiency . An open label randomized prospective study enrolled 14 Brazilian middle aged men with testosterone deficiency . The volunteers received in the forearm 50mg of transdermal BIOLIPID B2® - testosterone nanostructured formulation daily for 3 months. Confocal Raman Spectroscopy (CRS) was used to determine depth and concentration of testosterone on skin layers. Clinical parameters and serum concentrations were compared between the base line and 3 months after treatment. Serum concentrations of t estosterone, CPR and TSH changed significantly (p 0.05) and no changes were observed in the blood pressure . N o adverse events were attribu ted to this transdermal hormone replacement therapy protocol. The BIOLIPID B2 ® nanoemulsion formulation is safe and effective in reestabli shing testosterone and Thyroid - Stimulating Hormone (T SH) serum levels. This transdermal protocol may serve as a strate gy for hormone replacement therapy in middle aged men.

Gastroprotective effect and mechanism of action of Croton rhamnifolioides essential oil in mice

BACKGROUND Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C. rhamnifolioides Pax (OECC) in mice. METHODS The essential oil of Croton rhamnifolioides was obtained by hydrodistillation and analyzed by gas-phase chromatography coupled to mass spectrometry (GC/MS). The median lethal dose was determined employing an acute toxicity test. The gastroprotective activity of the OECC was investigated using animal models of gastric ulcer induced by the administration of absolute ethanol, acidified ethanol or indomethacin. Mechanisms of action were investigated using the physical barrier test and by in vivo evaluation of the involvement of the following molecular pathways: nitric oxide, ATP - dependent potassium channels, α2 - noradrenergic receptors, capsaicin - sensitive afferent neurons and opioid receptor. RESULTS We identified the presence of 21 compounds in OECC, including spathulenol and 1,8 - cineole as major constituents. In orally administered mice, OECC caused no significant toxicity. OECC significantly prevented gastric lesions in all mice models. The barrier test demonstrated that the gastroprotective activity of OECC occurs in a systemic dimension. Our results demonstrated that the gastroprotective effect of OECC involves mechanisms that are related to modulation of opioid receptors and nitric oxide. CONCLUSION In conclusion, OECC demonstrated significant gastroprotective activity associated with low toxicity, providing scientific evidences that C. rhamnifolioides have the potential for the development of new antiulcer drugs.

Quality analysis of research on the use of benzodiazepines by elderly patients in the emergency room:a systematic review

PurposeTo analyze the quality of research on the use of benzodiazepines (BZDs) in the emergency room by the elderly population through the Strengthening the Reporting of Observational Studies in Epidemiology (STROBE) initiative.MethodsA systematic review was carried out according to the following steps: (1) identification of studies, in which studies were selected from different combinations of the descriptors “elderly–aged,” “benzodiazepines,” and “emergency room” in the EMBASE–MEDLINE, SciELO, Scopus, and Web of Science databases; (2) evaluation of studies, in which the title, abstract, and full text of the studies were assessed; (3) evaluation of the methodological quality of the studies. The criteria used were those included in the STROBE recommendations.ResultsAt the end of the selection process, only six articles were identified which met the specific criteria. The sample sizes in these studies varied from 118 to 1,611 patients. More than half (4) of the studies did not describe the type of design used, whereas all collected demographic data and analyzed details on the use of BZDs, such as type administered and/or its relationship to the symptoms, were shown. No article fully complied with the STROBE criteria.ConclusionsThis review shows a lack of methodological quality in the studies performed to date that have evaluated the use of BZDs in elderly patients in emergency rooms. These findings should guide future research in this subject area, providing a more complete approach on aspects related to the use of medications by this specific population.

Pharmacological Effects Of Carvacrol In Vitro Studies: A Review

Carvacrol has a high therapeutic potential, with in vitro studies showing promising results in different cellular models using a variety of methodological designs. Therefore, the objective of this study was to conduct a systematic review to analyze the pharmacological effects of carvacrol in in vitro studies. A comprehensive search of the literature was made using four databases: Science Direct, Scopus, MEDLINE-PubMed, and Web of Science using different combinations of the following keywords: carvacrol, drug therapy, therapeutic uses, in vitro study. The search of the databases was for studies conducted in the period up to and including September 2016. A total of 3,269 studies were initially identified, with only 31 meeting the inclusion criteria. The included studies contained a variety of in vitro models able to determine the properties of Carvacrol. The following properties of Carvacrol were identified: antimicrobial (7 studies), bactericidal (4), bactericidal and antifungal (1), antiinflammatory (4), anticancer (4), mutagenic (4), antioxidant (3), antifungal (3), antidepressant (1), as a modulator of nerve impulses (1) and an immunological modulator (1). The In vitro studies with Carvacrol included in this review showed a diversity of models and confirmed the therapeutic potential of this product in relation to several diseases.