Topical monomethylsilanetriol can deliver silicon to the viable skin.

OBJECTIVE: Organic silicon has been linked to positive effects on the skin rejuvenation, mainly by the oral route. Thus, the main objective of the present study was to assess whether monomethylsilanetriol (MMST, a source of organic silicon) can deliver silicon to the epidermis and dermis, when applied topically in a cream. Once the hypothesis was confirmed, the present study also evaluated whether the product was toxic to keratinocytes; additionally, its possible antioxidant activity was assessed. METHODS: The ex vivo skin permeation profile was determined using human skin in Franz-cells equipment; cytotoxicity was assessed using HaCaT keratinocytes. Antioxidant capacity was determined as scavenging activity, measured according to the 1,1-diphenyl-2-picrylhydrazil free radical method. RESULTS: The permeation percentage was almost 60% of the applied MMST, with a large quantity of drug found in the viable epidermis and dermis. The cell viability assay showed no significant difference in the percentage of viable keratinocytes among the treated groups at the doses used. In terms of antioxidant activity, the IC50 value obtained was 2400 µg mL-1 . Low antioxidant activity, negligible toxicity for keratinocytes and a significant percentage of permeation were observed. CONCLUSION: We provide evidence that MMST applied topically can deliver silicon to the skin in biorelevant levels for cosmetic purposes.

OBJECTIF: Le silicium organique a été associé à des effets positifs sur le rajeunissement de la peau, principalement par voie orale. Ainsi, l'objectif principal de la présente étude était d'évaluer si le monométhylsilanetriol (MMST, une source de silicium organique) pouvait livrer du silicium à l'épiderme et au derme, lorsqu'il était appliqué localement dans une crème. Une fois l'hypothèse confirmée, la présente étude a également évalué si le produit était toxique pour les kératinocytes; de plus, son éventuelle activité antioxydante a été évaluée. MÉTHODES: Le profil de permeation cutanée ex vivo a été déterminé en utilisant de la peau humaine dans un équipement à cellules Franz; la cytotoxicité a été évaluée à l'aide de kératinocytes HaCaT. La capacité d'antioxydant a été déterminée en tant qu'activité de piégeage, mesurée selon la méthode des radicaux libres au 1,1-diphényl-2-picrylhydrazil. RÉSULTATS: Le pourcentage de perméation était proche de 60% du MMST appliqué, une grande quantité de médicament se trouvant dans l'épiderme et le derme viables. Le test de viabilité cellulaire n'a montré aucune différence significative dans le pourcentage de kératinocytes viables parmi les groupes traités aux doses utilisées. En termes d'activité antioxydante, la valeur de la CI50 obtenue était de 2400 µg mL−1 . Une faible activité antioxydante, une toxicité négligeable pour les kératinocytes et un pourcentage important de perméation ont été observés. CONCLUSION: Nous apportons la preuve que le MMST appliqué localement peut délivrer du silicium sur la peau à des niveaux biologiquement pertinents à des fins esthétiques.

Screening antimycobacterial activity of Baccharis dracunculifolia, Centella asiatica, Lantana camara and Pterodon emarginatus / Atividade anti-micobacteriana de Baccharis dracunculifolia, Centella asiatica, Lantana camara e Pterodon emarginatus

ABSTRACT The permanent investigation of new antimycobacterial drugs is necessary for the eradication programs of tuberculosis and other mycobacterium-related diseases. The aim of the present study is to search for new sources of antimycobacterial drugs using plant materials. In this study, 11 plant materials (extracts, essential oils and some fractions) obtained from 4 species of medicinal plants traditionally used as general therapeutics for different illnesses and specifically as treatment of tuberculosis, were evaluated using the microplate resazurin assay against 2 species of the Mycobacterium tuberculosis Complex and 3 nontuberculous mycobacteria. The results showed the hexane extract and the essential oil from fruits of Pterodonemarginatus (Vogel) as potential sources of antimycobacterial drugs against 4 species of tested mycobacteria. The hexane fraction of methanol extract from leaves of Centella asiatica also presented significant mycobacterial growth inhibition, but against M. chelonae only. In conclusion, it was possible to contribute to the antimycobacterial investigations by presenting three new samples of plants with significant antimicrobial activity against four Mycobacteriumspp and suggest future studies about the antimycobacterial properties of fruits from P. emarginatus.

RESUMO A investigação permanente de novas drogas antimicobacterianas é necessária no programa de erradicação da tuberculose e de outras doenças relacionadas com micobactérias. O objetivo deste estudo foi buscar novas fontes de drogas antimicobacterianas usando material vegetal. Neste estudo, 11 materiais de base vegetal (extratos, óleos essenciais e algumas frações) foram avaliados contra 5 espécies de micobactérias. Estes materiais foram obtidos a partir de 4 espécies de plantas medicinais tradicionalmente utilizadas como terapêutica geral para diferentes doenças e, especificamente, no tratamento de tuberculose (Baccharis dracunculifolia, Centella asiatica, Lantana camara, Pterodon emarginatus). Os ensaios foram realizados em microplacas com resazurina contra duas espécies do Complexo Mycobacteriumtuberculosis e 3 espécies de micobactérias não tuberculosas. Os resultados mostraram o extrato hexânico e o óleo essencial de frutos de P.emarginatus como potenciais fontes para drogas antimicobacterianas contra quatro espécies de micobactérias testadas. A fração hexânica do extrato metanólico das folhas de C. asiatica também apresentou significativa inibição do crescimento de micobactérias apenas contra M.chelonae. Em conclusão, foi possível contribuir para as investigações de antimicobacterianos por apresentar três novas amostras de plantas com atividade antimicrobiana significativa contra quatro Mycobacterium spp e sugerir a realização de estudos futuros sobre as propriedades antimicobacterianas de frutos de P. emarginatus.

Cytotoxicity and expression of genes involved in the cellular stress response and apoptosis in mammalian fibroblast exposed to cotton cellulose nanofibers.

Cellulose nanofibers (CNF) have mechanical properties that make them very attractive for applications in the construction of polymeric matrices, drug delivery and tissue engineering. However, little is known about their impact on mammalian cells. The objective of this study was to evaluate the cytotoxicity of CNF and their effect on gene expression of fibroblasts cultured in vitro. The morphology of CNF was analyzed by transmission electron microscopy and the surface charge by Zeta potential. Cell viability was analyzed by flow cytometry assay and gene expression of biomarkers focused on cell stress response such as Heat shock protein 70.1 (HSP70.1) and Peroxiredoxin 1 (PRDX1) and apoptosis as B-cell leukemia (BCL-2) and BCL-2 associated X protein (BAX) by RT-PCR assay. Low concentrations of CNF (0.02-100 µg ml(-1)) did not cause cell death; however, at concentrations above 200 µg ml(-1), the nanofibers significantly decreased cell viability (86.41 ± 5.37%). The exposure to high concentrations of CNF (2000 and 5000 µg ml(-1)) resulted in increased HSP70.1, PRDX1 and BAX gene expression. The current study concludes that, under the conditions tested, high concentrations (2000 and 5000 µg ml(-1)) of CNF cause decreased cell viability and affect the expression of stress- and apoptosis-associated molecular markers.

Altered neurotrophin, neuropeptide, cytokines and nitric oxide levels in autism.

INTRODUCTION: Modifications in neurotrophins, neuropeptides, cytokines and nitric oxide (NO) levels in autism may represent different biological aspects of the disease. In the present study we investigate simultaneously all these variables as an attempt to clarify their interrelationships in autism. METHODS: Plasma levels of vasoactive intestinal peptide (VIP), neurotrophin-3 (NT-3), cytokines and nitric oxide (NO) were determined in children with DSM-IV autistic disorder (n = 24) and in age- and gender-matched healthy controls (n = 24). VIP, NT-3, IFN-γ and IL-1ß levels were measured by ELISA, TNF-α, IL-10, IL-6, IL-4, IL-2 were evaluated by fl ow cytometry, and NO by Griess reaction. RESULTS: Plasma levels of VIP, IFN-γ and NO were significantly higher and NT-3 plasma levels were significantly lower in children with autism, compared to the healthy subjects. In children with autism there was a positive correlation between plasma levels of NO and IFN-γ. DISCUSSION: Our results indicate the presence of altered levels of neurotrophin and neuropeptide in infantile autism and provide additional evidence that higher levels of IFN-γ may be associated with increased oxidative stress in autism.

Eficácia e toxicidade do pó comercial de Hoodia gordonii (Masson) swet ex decne utilizado no tratamento da obesidade / Efficacy and toxicity of Hoodia gordonii commercial powder used to combat obesity

A obesidade é atualmente o principal problema de saúde em países desenvolvidos e em desenvolvimento. Diversos recursos terapêuticos têm sido empregados para o tratamento da obesidade destacando-se os fitoterápicos, consagrados pelo conhecimento popular. Nesse contexto, a planta Hoodia gordonii tem despertado atualmente grande interesse mundial, principalmente pelas recentes descobertas e comprovações científicas da inibição do apetite e da sede pelo glicosídeo ativo P57 isolado de espécies da planta. Apesar disso, tais efeitos ainda não foram avaliados e comprovados em amostras comerciais do pó de H. gordonii (PHG), não existindo evidências científicas que garantam a sua eficácia e segurança. Portanto, o objetivo deste trabalho foi realizar ensaios biológicos com ratos para avaliar a atividade farmacológica e a toxicidade de amostras comerciais do pó de H. gordonii. As amostras foram administradas por gavagem em doses equivalentes a 20 vezes as recomendadas para humanos em ratas Wistar durante 4 semanas sendo avaliados os parâmetros indicadores do efeito terapêutico. Após as 4 semanas, os animais foram sacrificados, e amostras de sangue e órgãos foram coletados e submetidos à avaliação dos indicadores metabólicos, endócrinos, hematológicos e histopatológicos. Os resultados demonstraram que para todos os parâmetros avaliados não houve diferenças significativas entre o grupo controle que recebeu somente solução salina estéril e os grupos tratados com PHG indicando que os mesmos, apesar de não apresentarem quaisquer indícios de toxicidade, são incapazes de produzir os supostos efeitos de inibição de apetite e consequente tratamento da obesidade.

Obesity is currently the main health problem in developed and developing countries. Several therapeutic methods have been employed for the treatment of obesity, especially herbal medicines, highlighted by popular knowledge. In this context, the plant Hoodia gordonii has currently aroused great interest worldwide, especially for recent discoveries and scientific proof of inhibition of appetite and thirst by the active glycoside P57 isolated from plant species. Nevertheless, such effects have not been evaluated and proven for commercial samples of H. gordonii powder (PHG), with no scientific evidence to ensure its effectiveness and safety. Therefore, the aim of this study was to conduct biological tests with rats to evaluate the pharmacological activity and toxicity of commercial samples of H. gordonii powder. The samples were administered through gavage, at doses equivalent to 20 times those recommended for humans, in female Wistar rats during 4 weeks for evaluation of the parameters indicative of therapeutic efficacy. After 4 weeks, the animals were sacrificed and blood and organ samples were collected and subjected to the evaluation of metabolic, endocrine, hematological and histopathological indicators. Results showed that for all evaluated parameters, there were no significant differences between the control group that only received sterile saline solution and the groups treated with PHG, indicating that the latter, although presenting no evidence of toxicity, are unable to produce the alleged effects of appetite inhibition and subsequent obesity treatment.

Body mass index increase, serum leptin, adiponectin, neuropeptide Y and lipid levels during treatment with olanzapine and haloperidol.

INTRODUCTION: Body mass index (BMI) increase is an undesired effect associated with antipsychotics, and crucial for patients' global health and treatment compliance. We aimed to investigate the relation between BMI during olanzapine or haloperidol treatments and leptin, neuropeptide Y (NPY), adiponectin and lipid serum levels. METHODS: In this 9-month, randomized and naturalist study, 34 male patients, 18 on olanzapine and 16 on haloperidol group were enrolled, all were under monotherapy. Patient outcome was evaluated with positive and negative syndrome scale (PANSS) at every 3-month period. In each visit, BMI, leptin, NPY, lipid, olanzapine or haloperidol levels were also monitored. RESULTS AND DISCUSSION: Leptin levels positively correlated with BMI in olanzapine (r=0.64, p<0.001) and haloperidol (r=0.73, p<0.001) groups; only in olanzapine patients, the former also correlated with PANSS score (r=0.54, p<0.05). NPY levels negatively correlated with olanzapine levels (r=− 0.65, p<0.01). Adiponectin levels had not significantly varied. CONCLUSION: Antipsychotics probably interfere on leptin and NPY signalling ways and disturb these hormones in eating behaviour control.