Protease-inhibiting, molecular modeling and antimicrobial activities of extracts and constituents from Helichrysum foetidum and Helichrysum mechowianum (compositae)

Background Helichrysum species are used extensively for stress-related ailments and as dressings for wounds normally encountered in circumcision rites, bruises, cuts and sores. It has been reported that Helichysum species are used to relief abdominal pain, heart burn, cough, cold, wounds, female sterility, menstrual pain. Results From the extracts of Helichrysum foetidum (L.) Moench, six known compounds were isolated and identified. They were 7, 4′-dihydroxy-5-methoxy-flavanone (1), 6′-methoxy-2′,4, 4′-trihydroxychalcone (2), 6′-methoxy-2′,4-dihydroxychalcone -4′-O-β-D-glucoside (3), apigenin (4), apigenin-7-O-β-D-glucoside (5), kaur-16-en-18-oic acid (6) while two known compounds 3,5,7-trihydroxy-8-methoxyflavone (12), 4,5-dicaffeoyl quinic acid (13) together with a mixture of phytosterol were isolated from the methanol extract of Helichrysum mechowianum Klatt. All the compounds were characterized by spectroscopic and mass spectrometric methods, and by comparison with literature data. Both extracts and all the isolates were screened for the protease inhibition, antibacterial and antifungal activities. In addition, the phytochemical profiles of both species were investigated by ESI-MS experiments. Conclusions These results showed that the protease inhibition assay of H. foetidum could be mainly attributed to the constituents of flavonoids glycosides (3, 5) while the compound (13) from H. mechowianum contributes to the stomach protecting effects. In addition, among the antibacterial and antifungal activities of all the isolates, compound (6) was found to possess a potent inhibitor effect against the tested microorganisms. The heterogeneity of the genus is also reflected in its phytochemical diversity. The differential bioactivities and determined constituents support the traditional use of the species. Molecular modelling was carried out by computing selected descriptors related to drug absorption, distribution, metabolism, excretion and toxicity (ADMET).

In vivo assessment of genotoxic, antigenotoxic and anticarcinogenic activities of Solanum lycocarpum fruits glycoalkaloidic extract

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Piperine, a natural bioenhancer, nullifies the antidiabetic and antioxidant activities of curcumin in streptozotocin-diabetic rats

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Mutagenicity and chemopreventive activities of Astronium species assessed by Ames test

In the neotropical savannah, Astronium species are used in popular medicine to treat allergies, inflammation, diarrhea and ulcers. Given that natural products are promising starting points for the discovery of novel potentially therapeutic agents, the aim of the present study was to investigate the mutagenic and antimutagenic activities of hydroalcoholic extracts of Astronium spp. The mutagenicity was determined by the Ames test on Salmonella typhimurium strains TA98, TA97a, TA100 and TA102. The antimutagenicity was tested against the direct-acting and indirect-acting mutagens. The results showed that none of the extracts induce any increase in the number of revertants, demonstrating the absence of mutagenic activity. On the other hand, the results on the antimutagenic potential showed a moderate inhibitory effect against NPD and a strong protective effect against B[a]P and AFB1. This study highlights the importance of screening species of Astronium for new medicinal compounds. The promising results obtained open up new avenues for further study and provide a better understanding the mechanisms by which these species act in protecting DNA from damage. However, further pharmacological and toxicological investigations of crude extracts of Astronium spp., as well as of its secondary metabolites, are necessary to determine the mechanism(s) of action to guarantee their safer and more effective application to human health.

Antimicrobial and antileishmanial activities of diterpenoids isolated from the roots of salvia deserta

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Acute and subchronic antihyperglycemic activities of bowdichia virgilioides roots in non diabetic and diabetic rats

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Greening of the essential activities of an Engineering School: a case study in the Area/Department of Production Engineering

This article analyzes the inclusion of the issue of “environmental management” in the department of Production Engineering of the “Alfa” School of Engineering. For this, a case study was conducted at the School of "Alpha" Engineering, with a focus on the area of Production Engineering. Professors were interviewed; documents were reviewed as well as information collected from direct observations by of one of the authors of this article. It was observed that the department of Production Engineering at the Alpha School of Engineering has been developing activities covering all those aspects proposed by Jabbour [8]. "Environmental management" has been included in the curriculums of: (a) Teaching: in the creation of undergraduate courses (obligatory) and graduate Master's degree (optional), (b) Research: formalization of research groups in environmental management for the creation of master’s post graduation research, formalization of environmental management as one of the subjects that should be chosen by candidates for a Professorship in the area of production engineering; (c) Extension: Course in Environmental Management, Symposium (which in recent years has been focusing on environmental issues), creation of sustainability indicators for universities, (d) University Management: initiatives to raise awareness, distribution of reusable mugs and installation of special bins for selective collection in the Campus.

The chemical composition and pharmacological activities of geopropolis produced by Melipona fasciculata Smith in northeast Brazil

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Antioxidant, anti-acetylcholinesterase and cytotoxic activities of ethanol extracts of peel, pulp and seeds of exotic Brazilian fruits Antioxidant, anti-acetylcholinesterase and cytotoxic activities in fruits

Ethanol extracts of powdered genipap (Genipa americana L), umbu (Spondia tuberosa A.) and siriguela (Spondia purpurea L) prepared from separate pulp, seeds and peel were investigated for their (i) antioxidant capacity, which was evaluated by various known methods; (ii) acetylcholinesterase (AChE) inhibitory activity; and (iii) cytotoxic effect on corneal epithelial cells of sheep. The highest values of total phenolic content were obtained with peel and seed extracts. Siriguela and umbu (seeds and peel) extracts displayed the highest antioxidant activities. Lipid peroxidation assays using mimetic biomembranes and mouse liver homogenates indicated that genipap pulp is a promising antioxidant. The investigation of phenols and organic acid contents revealed the presence of quercetin, citric and quinic acids, chlorogenic acid derivatives, among others, in several extracts, with the highest amount found in siriguela seeds. Genipap pulp and siriguela seed ethanol extracts presented an AChE inhibition zone similar to that of the positive control, carbachol. AChE inhibition assay with chlorogenic acid, one of the main constituents of siriguela seeds, revealed that this acid showed activity similar to that of the control physostigmine. These data suggest that these extracts are potentially important antioxidant supplements for the everyday human diet, pharmaceutical and cosmetic industries. (C) 2012 Elsevier Ltd. All rights reserved.

Instrumental activities of daily living performance in healthy and cognitively intact seniors from a Brazilian sample and its relation to age and other socio-demographic variables

Background: Studies on functional capacity in community-dwelling older people have shown associations between declines in instrumental activities of daily living (IADL) and several factors. Among these, age has been the most consistently related to functional capacity independent of other variables. We aimed at evaluating the performance of a sample of healthy and cognitively intact Brazilian older people on activities of daily living and to analyze its relation to social-demographic variables. Methods: We conducted a secondary analysis of data collected for previous epidemiological studies with community-dwelling subjects aged 60 years or more. We selected subjects who did not have dementia or depression, and with no history of neurological diseases, heart attack, HIV, hepatitis or arthritis (n = 1,111). Functional capacity was assessed using the Brazilian version of the Older American Resources and Services Questionnaire (BOMFAQ). ADL performance was analyzed according to age, gender, education, and marital status (Pearson's chi(2), logistic regression). Results: IADL difficulties were present in our sample, especially in subjects aged 80 years or more, with lower levels of education, or widowed. The logistic regression analysis results indicated that "higher age" and "lower education" (p <= 0.001) remained significantly associated with IADL difficulty. Conclusions: Functional decline was present in older subjects even in the absence of medical conditions and cognitive impairment. Clinicians and researchers could benefit from knowing what to expect from older people regarding IADL performance in the absence of medical conditions.

Leishmanicidal and cholinesterase inhibiting activities of phenolic compounds of Dimorphandra gardneriana and Platymiscium floribundum, native plants from Caatinga biome

Nos últimos anos, o Ministério da Saúde do Brasil e a Organização Mundial da Saúde tem apoiado a investigação de novas tecnologias que possam contribuir para a vigilância, novos tratamentos e controle da leishmaniose visceral no país. Assim, o objetivo deste trabalho foi isolar compostos de plantas do bioma Caatinga, e investigar a toxicidade destes compostos contra as formas promastigotas e amastigotas de Leishmania infantum chagasi, principal parasita responsável pela leishmaniose visceral na América do Sul, e avaliar a sua capacidade para inibir a enzima acetil-colinesterase (AChE). Após a exposição aos compostos em estudo, foram realizados testes utilizando a forma promastigota que expressa luciferase e ELISA in situ para medir a viabilidade das formas promastigotas e amastigota, respectivamente. O ensaio colorimétrico MTT foi realizado para determinar a toxicidade destas substâncias utilizando células monocíticas murina RAW 264.7. Todos os compostos foram testados in vitro para as sua propriedade anti-colinesterásica. Um cumarina, escoparona, foi isolada a partir de hastes de Platymiscium floribundum, e os flavonóides, rutina e quercetina, foram isolados a partir de grãos de Dimorphandra gardneriana. Estes compostos foram purificados, utilizando cromatografia em coluna gel eluída com solventes orgânicos em misturas de polaridade crescente, e identificados por análise espectral. Nos ensaios leishmanicidas, os compostos fenólicos mostraram eficácia contra as formas extracelulares promastigotas, com EC50 para escoporona de 21.4µg/mL e para quercetina e rutina 26 e 30.3µg/mL, respectivamente. Os flavonóides apresentaram resultados comparáveis à droga controle, a anfotericina B, contra as formas amastigotas com EC50 para quercetina e rutina de 10.6 e 43.3µg/mL, respectivamente. Os compostos inibiram a enzima AChE com halos de inibição variando de 0,8 a 0,6cm, indicando um possível mecanismo de ação para a atividade leishmanicida.

Limitations in activities of people affected by leprosy after completing multidrug therapy: application of the SALSA scale

Objectives: To identify people affected by leprosy with impairments after completing multidrug therapy for leprosy, and to assess their limitations in conducting daily activities by applying the Screening of Activity Limitation and Safety Awareness (SALSA) scale. Methods: A cross-sectional study was performed of all residents of a medium-sized city who were treated for leprosy from 1998 to 2006. A specific questionnaire was applied to obtain general and clinical data and the SALSA scale was used to assess limitations in activities. Impairments were assessed using the 'World Health Organization leprosy disability grading system' (WHO-DG). Findings: Of the 335 people affected by leprosy treated in the period, 223 (62.1%) were located and interviewed. A total of 51.6% were female with a mean age of 54 years (SD +/- 15.72) and 67.9% had up to 6 years formal education. The borderline form predominated among interviewees (39.9%) and 54.3% suffer from associated diseases with hypertension (29.1%) and diabetes (10.3%) being the most common. Pain was reported by 54.7% of interviewees. By multiple logistic regression analysis, associations were found between limitations in activities and being female (P < 0.025), family income <= 3 minimum wages (P-value < 0.003), reports of major lesions (P-value < 0.004), pain (P-value < 0.001), associated diseases (P-value < 0.023) and the WHO-DG (P-value < 0.001). Disabilities, as identified using the WHO-DG, were less common (32%) than limitations in activities as evaluated by the SALSA scale (57.8%). Conclusion: Limitations in activities proved to be common in people affected by leprosy and were. associated with low income, being female, reported major lesions, disability, disease and pain.

Gender differences in incidence and determinants of disability in activities of daily living among elderly individuals: SABE study

Determining the groups that are most susceptible to developing disability is essential to establishing effective prevention and rehabilitation strategies. The aim of the present study was to determine gender differences in the incidence of disability regarding activities of daily living (ADL) and determinants among elderly residents of Sao Paulo, Brazil. In 2000, 1634 elderly with no difficulties regarding ADL (modified Katz Index) were selected. These activities were reassessed in 2006 and disability was the outcome for the analysis of determinants. The following characteristics were analyzed at baseline: sociodemographic, behavioral, health status, medications, falls, hospitalizations, depressive symptoms, cognition, handgrip, mobility and balance. The incidence density was 42.4/1000 women/year and 17.5/1000 men/year. After adjusting for socioeconomic status and health conditions, women with chronic diseases and social vulnerability continued to have a greater incidence of disability. The following were determinants of the incidence of disability: age and depressive symptoms in both genders; stroke and slowness on the sit-and-stand test among men; and osteoarthritis and sedentary lifestyle among women. Better cognitive performance and handgrip strength were protective factors among men and women, respectively. Adverse clinical and social conditions determine differences between genders regarding the incidence of disability. Decreased mobility and balance and health conditions that affect the central nervous system or lead to impaired cognition disable men more, whereas a sedentary lifestyle, reduction in muscle strength and conditions that affect the osteoarticular system disable women more. (C) 2012 Elsevier Ireland Ltd. All rights reserved.

The correlation between the phenolic composition and biological activities of two varieties of Brazilian propolis (G6 and G12)

Biological assays that have been performed on different types of Brazilian propolis have shown that type 6 propolis (G6) has a strong antimicrobial activity and a low flavonoid content. This study aimed to evaluate the correlation between the phenolic composition and the biological activities displayed by propol is G6 from the state of Bahia and green propol is, also known as type 12 (G12). The values of the flavonoids and the total phenolics in propol is G6 were different than those in propolis G12. Although the G12 variety presented greater antioxidant activity, propolis G6 proved to have greater antimicrobial and cytotoxic activities. The results showed that the phenolic compounds may not be the only compounds responsible for the biological activity. More detailed studies of the chemical composition and an assessment or the biological activity are required to establish the quality of propolis.

Effect of Nintendo Wii (TM)-based motor and cognitive training on activities of daily living in patients with Parkinson's disease: A randomised clinical trial

Objectives To investigate the effect of Nintendo Wii (TM)-based motor cognitive training versus balance exercise therapy on activities of daily living in patients with Parkinson's disease. Design Parallel, prospective, single-blind, randomised clinical trial. Setting Brazilian Parkinson Association. Participants Thirty-two patients with Parkinson's disease (Hoehn and Yahr stages 1 and 2). Interventions Fourteen training sessions consisting of 30 minutes of stretching, strengthening and axial mobility exercises, plus 30 minutes of balance training. The control group performed balance exercises without feedback or cognitive stimulation, and the experimental group performed 10 Wii Fit (TM) games. Main outcome measure Section II of the Unified Parkinson's Disease Rating Scale (UPDRS-II). Randomisation Participants were randomised into a control group (n = 16) and an experimental group (n = 16) through blinded drawing of names. Statistical analysis Repeated-measures analysis of variance (RM-ANOVA). Results Both groups showed improvement in the UPDRS-II with assessment effect (RM-ANOVA P < 0.001, observed power = 0.999). There was no difference between the control group and the experimental group before training {8.9 [standard deviation (SD) 2.9] vs 10.1 (SD 3.8)}, after training [7.6 (SD 2.9) vs 8.1 (SD 3.5)] or 60 days after training [8.1 (SD 3.2) vs 8.3 (SD 3.6)]. The mean difference of the whole group between before training and after training was -0.9 (SD 2.3, 95% confidence interval -1.7 to -0.6). Conclusion Patients with Parkinson's disease showed improved performance in activities of daily living after 14 sessions of balance training, with no additional advantages associated with the Wii-based motor and cognitive training. Registered on http://www.clinicaltrials.gov (identifier: NCT01580787). (C) 2012 Chartered Society of Physiotherapy. Published by Elsevier Ltd. All rights reserved.