Estudo ficoquímico e avaliação da atividade microbiológica de algas marinhas do gênero sargassum.

S argassum is a genus of brown seaweed Sargassacea e family represented for 150 species . In the state of Paraíba , the marine flora began to be studied from th e first decades of this century . The pub l ication of the first list of species made by Luetzelburg between 1922 and 1923 can be considered the starting point o f the investigations fhycologi in Paraíba (Carvalho, 1983). Navies macroscopic algae despite arouse the attention of the scientific commu nity for their great potential as a pr oducer chemicals for industrial , economic and medical - pharmacological interest in Brazi l, especially in the Northeast , there are few studies conducted for this purpose , our group being a pioneer in research fhytocheis try . Given the availabili ty and diversity of our biomass , it is imperative that prospective studies be carried out to identify potential compounds derived from marine macroalgae with pharma cological activity . Next we observe some pharmacological activities of al gae described in the literature, among which we can mention: alginates, florotaninos, coumarins, chromones, quinones, and terpenoids feoftinas . Studies have shown that metabolites produced by algae of the genus Sargass umtiveram biological activities, such as anticoagulant, antioxidant, analgesic and antipyretic . It is important to demonstrate that knowledge about the chemical profile may contribute to the taxonomic studies of family Sargassaceae . This work, developed at the Laboratory of Pharmacology / Graduate Program in Natural and Synthetic Bioactive P roducts and Mycology Laboratory , Department of Pharmaceutical Scie nces ( Health Sciences Center ) , Federal University of Paraíba , intended to analyze the microbial activity antimicrobial constituents of the phases and seaweed of the genus Sargassum .Sargassum é um gênero de algas marinhas pardas da família Sargassaceae que é representada por cerca de 150 espécies . No estado da Paraíba, a flora marinha começou a ser estudada a partir das primeiras décadas deste século. A publicação da primeira lista de espécies efetuadas por Luetzelburg, entre 1922 e 1923, pode ser considerada o marco inicial das investigações ficológicas na Paraíba (Carvalho, 1983) . As algas macroscópicas marinhas apesar de despertar a atenção da comunidade científica pela grande potencialidade como prod utora de substâncias químicas e médico - farmacológico, no Brasil, em especial no Nordeste, são poucos os estudos efetuados com este prop ó sito . Tendo em vista a disponibilidade e a diversidade da nossa biomassa, torna - se imperativo que estudos prospectivos sejam realizados, objetiv ando a identificação de substâncias oriundos de macroalgas marinhas com atividade farmacológica. Foi possível ob servar algumas atividades farmacológicas de algas descritas na literatur a, entre as quais podemos citar atividade : anticoagulante , antioxidante, antipirético e analgésico . É importante demonstrar que o conhecimento sobre o perfil químico pode contribuir pa ra os estudos taxonómico da familia Sargassaceae. O presente trabalho, desenvolvido no Laboratório de Farmacoquímica/Programa de Pós Graduação em Produtos N aturais e Sintéticos Bioativos no Laboratório de Micologia do Departamento de Ciências Farmacêutica s (Centro de Ciências da Saúde), Universidad e Federal da Paraíba, tem como propósito ana lisar a atividade antimicrobiana das fases e constituintes isolados da alga do gênero Sargassum

Preparação de ésteres nitrocinâmicos e avaliação da sua atividade antimicrobiana

The present work aimed to prepare a series of esters derived from trans-2-nitrocinnamic acid, through Fischer esterification, nucleophilic substitution with halides and Mitsunobu reaction. All the derivatives were submitted to antimicrobial tests by the microdilution method in broth, and the antimicrobials chloramphenicol and nystatin as positive controls. This study resulted in the obtaining of 14 esters of trans-2-nitrocinnamic acid in yields ranging from 25 to 98%, nine of which were unpublished in the literature, and characterized by infrared spec-troscopic methods, 1H and 13C magnetic resonance, as well as High resolution mass spectrometry. The results of the antimicrobial evaluation showed that ten esters presented antifungal activity against Candida species. While two derivatives were bioactive in the an-tibacterial test. Of these, the EL4, EL6 and EL14 esters were the derivatives that obtained the most promising antifungal minimum inhibitory concentrations with MIC ranging from 128 to 256 μg / mL and considered to be strong activities. Regarding the bacterial activity, EL12 and EL13 derivatives showed activity on the Pseudomonas aeruginosa species with MIC 512 μg / mL. These results demonstrate that the increase of the alkyl chain in the substituent up to a certain size and the presence of hydroxyl, methoxy, or chlorine at the para position of the aromatic ring influence the antifungal activity of the 2-nitrocinnamic esters.Conselho Nacional de Pesquisa e Desenvolvimento Científico e Tecnológico - CNPqO presente trabalho teve como objetivo preparar uma série de ésteres derivados do ácido trans-2-nitrocinâmico, através da esterificação de Fischer, substituição nucleofílica com haletos e reação de Mitsunobu. Todos os derivados foram submetidos a testes antimicrobianos pelo método de microdiluição em caldo, tendo como controles positivos os antimicrobianos cloranfenicol e nistatina. O referido estudo resultou na obtenção de 14 ésteres do ácido trans-2-nitrocinâmico com rendimentos variando entre 25 e 98%, sendo nove derivados inéditos na literatura,caracterizados por métodosespectroscópicos de infravermelho, ressonância magnética de 1H e 13C, bem como porespectrometria de massas de alta resolução. O resultado da avaliação antimicrobiana demonstrou que dez ésteres apresentaram atividade antifúngica frente a espécies do gêneroCandida. Enquanto, dois derivados foram bioativos no teste antibacteriano. Destes, os ésteres EL4, EL6 e EL14 foram os derivados que obtiveram concentrações inibitórias mínimas antifúngicas mais promissoras com CIM que variaram entre 128 e 256 μg/mL, sendo consideradas atividades fortes. Com relação à atividade bacteriana, os derivados EL12 e EL13 demostraram atividade sobre a espécie de Pseudomonas aeruginosacom CIM 512μg/mL. Esses resultados demonstram que o aumento da cadeia alquílica no substituinte, até determinado tamanho, e a presença de hidroxila, metoxila ou cloro na posição para do anel aromático influenciam a atividade antifúngica dos ésteres 2-nitrocinâmicos

Gallic acid alkyl esters: Trypanocidal and Leishmanicidal activity, and target identification via modeling studies

Eight gallic acid alkyl esters (1-8) were synthesized via Fischer esterification and evaluated for their trypanocidal and leishmanicidal activity using bloodstream forms of Trypanosoma brucei and promastigotes of Leishmania major. The general cytotoxicity of the esters was evaluated with human HL-60 cells. The compounds displayed moderate to good trypanocidal but zero to low leish-manicidal activity. Gallic acid esters with alkyl chains of three or four carbon atoms in linear arrangement (propyl (4), butyl (5), and isopentyl (6)) were found to be the most trypanocidal compounds with 50% growth inhibition values of ~3 μM. On the other hand, HL-60 cells were less susceptible to the compounds, thus resulting in moderate selectivity indices (ratio of cytotoxic to trypanocidal activity) of >20 for the esters 4-6. Modeling studies combining molecular docking and molecular dynamics simulations suggest that the trypanocidal mechanism of action of gallic acid alkyl esters could be related to the inhibition of the T. brucei alternative oxidase. This suggestion is supported by the observation that trypanosomes became immobile within minutes when incubated with the esters in the presence of glycerol as the sole substrate. These results indicate that gallic acid alkyl esters are interesting compounds to be considered for further antitrypanosomal drug development

Analgesic Potential of Essential Oils

Pain is an unpleasant sensation associated with a wide range of injuries and diseases, and affects approximately 20% of adults in the world. The discovery of new and more effective drugs that can relieve pain is an important research goal in both the pharmaceutical industry and academia. This review describes studies involving antinociceptive activity of essential oils from 31 plant species. Botanical aspects of aromatic plants, mechanisms of action in pain models and chemical composition profiles of the essential oils are discussed. The data obtained in these studies demonstrate the analgesic potential of this group of natural products for therapeutic purposes

In Vivo Anti-Tumor Activity and Toxicological Evaluations of Perillaldehyde 8,9-Epoxide, a Derivative of Perillyl Alcohol

Recent studies have revealed the high cytotoxicity of p-menthane derivatives against human tumor cells. In this study, the substance perillaldehyde 8,9-epoxide, a p-menthane class derivative obtained from (S)-(−)-perillyl alcohol, was selected in order to assess antitumor activity against experimental sarcoma 180 tumors. Toxicological effects related to the liver, spleen, kidneys and hematology were evaluated in mice submitted to treatment. The tumor growth inhibition rate was 38.4%, 58.7%, 35.3%, 45.4% and 68.1% at doses of 100 and 200 mg/kg/day for perillaldehyde 8,9-epoxide, perillyl alcohol and 25 mg/kg/day for 5-FU intraperitoneal treatments, respectively. No toxicologically significant effect was found in liver and kidney parameters analyzed in Sarcoma 180-inoculated mice treated with perillaldehyde 8,9-epoxide. Histopathological analyses of the liver, spleen, and kidneys were free from any morphological changes in the organs of the animals treated with perillaldehyde 8,9-epoxide. In conclusion, the data suggest that perillaldehyde 8,9-epoxide possesses significant antitumor activity without systemic toxicity for the tested parameters. By comparison, there was no statistical difference for the antitumor activity between perillaldehyde 8,9-epoxide and perillyl alcohol

The Isopropyl Gallate Counteracts Cyclophosphamide-Induced Hemorrhagic Cystitis in Mice

Hemorrhagic cystitis is the main adverse effect associated with the clinical use of oxazaphosphorine, resulting in increased oxidative stress and proinflammatory cytokines, which culminate in injury of the bladder tissue. The aim of this study was to evaluate the protective effect of isopropyl gallate (IPG) against ifosfamide (IFOS)-induced hemorrhagic cystitis in mice. The induction of the hemorrhagic cystitis model was carried out using a single dose of IFOS (400 mg/kg, i.p.) four hours after oral pretreatment with IPG (6.25, 12.5, 25, and 50 mg/kg) or saline (vehicle). Mesna (positive control; 80 mg/kg, i.p.) was administered four hours before and eight hours after induction of cystitis. In the present study, IPG 25 mg/kg significantly decreased edema and hemorrhage, with a reduction of the bladder wet weight (36.86%), hemoglobin content (54.55%), and peritoneal vascular permeability (42.94%) in urinary bladders of mice. Interestingly, IPG increased SOD activity (89.27%) and reduced MDA levels (35.53%), as well as displayed anti-inflammatory activity by decreasing TNF-α (88.77%), IL-1β (62.87%), and C-reactive protein (56.41%) levels. Our findings demonstrate that IPG has a substantial protective role against IFOS-induced hemorrhagic cystitis in mice by enhancing antioxidant activity and proinflammatory mechanisms. Thus, IPG represents a promising co-adjuvant agent in oxazaphosphorine-based chemotherapy treatments

Safety of hospital discharge before return of bowel function after elective colorectal surgery

Background: Ileus is common after colorectal surgery and is associated with an increased risk of postoperative complications. Identifying features of normal bowel recovery and the appropriateness for hospital discharge is challenging. This study explored the safety of hospital discharge before the return of bowel function.Methods: A prospective, multicentre cohort study was undertaken across an international collaborative network. Adult patients undergoing elective colorectal resection between January and April 2018 were included. The main outcome of interest was readmission to hospital within 30 days of surgery. The impact of discharge timing according to the return of bowel function was explored using multivariable regression analysis. Other outcomes were postoperative complications within 30 days of surgery, measured using the Clavien-Dindo classification system.Results: A total of 3288 patients were included in the analysis, of whom 301 (9.2 per cent) were discharged before the return of bowel function. The median duration of hospital stay for patients discharged before and after return of bowel function was 5 (i.q.r. 4-7) and 7 (6-8) days respectively (P < 0.001). There were no significant differences in rates of readmission between these groups (6.6 versus 8.0 per cent; P = 0.499), and this remained the case after multivariable adjustment for baseline differences (odds ratio 0.90, 95 per cent c.i. 0.55 to 1.46; P = 0.659). Rates of postoperative complications were also similar in those discharged before versus after return of bowel function (minor: 34.7 versus 39.5 per cent; major 3.3 versus 3.4 per cent; P = 0.110).Conclusion: Discharge before return of bowel function after elective colorectal surgery appears to be safe in appropriately selected patients

Timing of nasogastric tube insertion and the risk of postoperative pneumonia: an international, prospective cohort study

Aim: Aspiration is a common cause of pneumonia in patients with postoperative ileus. Insertion of a nasogastric tube (NGT) is often performed, but this can be distressing. The aim of this study was to determine whether the timing of NGT insertion after surgery (before versus after vomiting) was associated with reduced rates of pneumonia in patients undergoing elective colorectal surgery. Method: This was a preplanned secondary analysis of a multicentre, prospective cohort study. Patients undergoing elective colorectal surgery between January 2018 and April 2018 were eligible. Those receiving a NGT were divided into three groups, based on the timing of the insertion: routine NGT (inserted at the time of surgery), prophylactic NGT (inserted after surgery but before vomiting) and reactive NGT (inserted after surgery and after vomiting). The primary outcome was the development of pneumonia within 30 days of surgery, which was compared between the prophylactic and reactive NGT groups using multivariable regression analysis. Results: A total of 4715 patients were included in the analysis and 1536 (32.6%) received a NGT. These were classified as routine in 926 (60.3%), reactive in 461 (30.0%) and prophylactic in 149 (9.7%). Two hundred patients (4.2%) developed pneumonia (no NGT 2.7%; routine NGT 5.2%; reactive NGT 10.6%; prophylactic NGT 11.4%). After adjustment for confounding factors, no significant difference in pneumonia rates was detected between the prophylactic and reactive NGT groups (odds ratio 1.03, 95% CI 0.56–1.87, P = 0.932). Conclusion: In patients who required the insertion of a NGT after surgery, prophylactic insertion was not associated with fewer cases of pneumonia within 30 days of surgery compared with reactive insertion