Inter-phyla studies on neuropeptides: the potential for broad-spectrum anthelmintic and/or endectocide discovery

Flatworm, nematode and arthropod parasites have proven their ability to develop resistance to currently available chemotherapeutics. The heavy reliance on chemotherapy and the ability of target species to develop resistance has prompted the search for novel drug targets. In view of its importance to parasite/pest survival, the neuromusculature of parasitic helminths and pest arthropod species remains an attractive target for the discovery Of novel endectocide targets. Exploitation of the neuropeptidergic system in helminths and arthropods has been hampered by a limited Understanding of the functional roles of individual peptides and the structure of endogenous targets, such as receptors. Basic research into these systems has the potential to facilitate target characterization and its offshoots (screen development and drug identification). Of particular interest to parasitologists is the fact that selected neuropeptide families are common to metazoan pest species (nematodes, platyhelminths and arthropods) and fulfil specific roles in the modulation of muscle function in each of the three phyla. This article reviews the inter-phyla activity of two peptide families, the FMRFamide-like peptides and allatostatins, on motor function in helminths and arthropods and discusses the potential of neuropeptide signalling as a target system that could uncover novel endectocidal agents.

Rapid analysis of ecstasy and related phenethylamines in seized tablets by Raman spectroscopy

Raman spectroscopy with far-red excitation has been used to study seized, tableted samples of MDMA (N-methyl-3,4-methylenedioxyamphetamine) and related compounds (MDA, MDEA, MBDB, 2C-B and amphetamine sulfate), as well as pure standards of these drugs. We have found that by using far-red (785 nm) excitation the level of fluorescence background even in untreated seized samples is sufficiently low that there is little difficulty in obtaining good quality data with moderate 2 min data accumulation times. The spectra can be used to distinguish between even chemically-similar substances, such as the geometrical isomers MDEA and MBDB, and between different polymorphic/hydrated forms of the same drug. Moreover, these differences can be found even in directly recorded spectra of seized samples which have been bulked with other materials, giving a rapid and non-destructive method for drug identification. The spectra can be processed to give unambiguous identification of both drug and excipients (even when more than one compound has been used as the bulking agent) and the relative intensities of drug and excipient bands can be used for quantitative or at least semi-quantitative analysis. Finally, the simple nature of the measurements lends itself to automatic sample handling so that sample throughputs of 20 samples per hour can be achieved with no real difficulty.

Desenvolvimento de um sistema multidimensional para classificação e gestão de informação em saúde: aplicabilidade à informação clínica

Introdução: A profusão de informação na área médica cria problemas de gestão, sendo necessários métodos sistematizados para armazenamento e recuperação. Quando a informação se insere no contexto do processo clínico, os métodos devem integrar terminologias biomédicas controladas e igualmente devem integrar as características desejáveis dirigidas à estrutura, conteúdo e resultados clínicos. O objectivo deste artigo é testar a aplicabilidade e capacidade de recuperação, de um sistema multidimensional desenvolvido para classificação e gestão de informação em saúde. Métodos: A partir das questões recebidas em seis anos (Serviço de Informação de Medicamentos, Serviços Farmacêuticos, Hospitais da Universidade de Coimbra), seleccionaram-se 300 questões sobre informação clínica, por método aleatório informatizado. Caracterizou-se e avaliou-se a aplicabilidade pela quantidade classificada e pela necessidade de alterações ao sistema que é constituído por várias dimensões independentes e que englobam conceitos por vezes hierarquizados. A recuperação das questões foi testada pesquisando informação numa dimensão ou cruzamento de dimensões. Resultados: Todas as questões foram classificadas: 53% são casos clínicos com incidência nas doenças geniturinárias; doenças metabólicas, nutricionais e endócrinas; neoplasias; infecções e doenças do sistema nervoso. Em 81%, o objecto é o medicamento, sobretudo anti-infecciosos e anti-neoplásicos. As áreas de terapêutica e segurança foram as mais solicitadas, incidindo principalmente sobre os assuntos: utilização, reacções adversas, identificação de medicamentos e tecnologia farmacêutica. Na aplicabilidade, foi necessário adicionar alguns conceitos e modificar alguns grupos hierárquicos que não modificaram a estrutura base, nem colidiram com as características desejáveis. As limitações prenderam-se com os sistemas de classificação externos integrados. A pesquisa na dimensão assunto, do conceito administração de medicamentos, recuperou 19 questões. O cruzamento de duas dimensões: anti-infecciosos (externa) e teratogenicidade (assunto), recuperou três questões. Nos dois exemplos recupera-se informação a partir de qualquer um dos níveis da hierarquia, do mais geral ao mais específico e mesmo a partir de dimensões externas. Conclusões: A utilização do sistema nesta amostra demonstrou aplicabilidade na classificação e arquivo de informação clínica, capacidade de recuperação e flexibilidade, sofrendo alterações sem interferir com as características desejáveis. Esta ferramenta permite a recuperação da evidência que interessa orientada para o doente. Introduction: The large amount of information in the medical area creates management problems, being necessary systematic methods for filing and retrieval. With information on the context of clinical records, methods must integrate controlled biomedical terminologies and desirable characteristics oriented to the structure, content and clinical results. The objective is to test the applicability and capacity for retrieval of a multidimensional system developed for classification and management of health information. Methods: Three hundred questions were randomly selected, by computerized method, from the questions received in six years (Medicine Information Service, Pharmaceutical Department, Coimbra University Hospitals). They were characterized and applicability evaluated by classified amount and need to alter the system, which is composed of various independent dimensions, incorporating concepts sometimes hierarchical. Questions retrieval was tested searching information in a dimension or between dimensions. Results: All questions were classified: 53% are clinical cases with illnesses incidence in the genitourinary system; metabolic, nutritional and endocrine disease; cancer; infections and nervous system. In 81%, the object is a drug, mostly anti-infectious and anti-neoplastic agents. The therapeutic and safety areas had been the most requested, regarding the subjects: use, adverse reactions, drug identification and pharmaceutical technology. As to applicability, it was necessary to add some concepts and modify same hierarchical groups, that didn’t modify the basic structure, nor had collided with the desirable characteristics. The limitations were related with the incorporated external classification systems. The search in the subject dimension of the concept drug administration retrieved 19 questions. The search between two dimensions: antiinfectious (external) and teratogenicity (subject) retrieved three questions. In the two examples, it was possible to retrieve information from any one of the levels of the hierarchy, from the most general to the most specific and even from external dimensions. Conclusions: The use of the system in this sample showed its applicability in clinical information classification and filing, retrieval capacity and flexibility, supporting modifications without interfering with desirable characteristics. This tool allows retrieval of patient-oriented evidence that matters.

Segurança do paciente no sistema de medicação: análise de enfermeiros de um hospital de ensino

This study aimed to identify and describe the factors related to Patient Safety in a medication system according to the nurses analysis in a teaching hospital from the photographic analysis method. This was a cross-sectional, descriptive study with mixed approach in a teaching hospital in Rio Grande do Norte. The population consisted of 42 nurses from inpatient units, of which 34 composed the study sample. As eligibility criteria, we defined nurses from public service and nurses who agreed to participate. Ethical determinations were observed, the study was submitted to the Ethics and Research of the University Hospital Onofre Lopes, obtaining the assent with ethical assessment certificate (CAAE 0098.0.051.294-11). For data collection, we used the photographic method (Photographic Analysis Technique) by Patricia Marck (Canada). It was developed in two phases: at first, we randomly captured photos from the medication system, resulting in 282 images; then we selected/processed the photographs, which were reduced to 10 images in Microsoft Excel 2010; in the second phase, the nurses answered the questionnaire divided into socio-professional profile and Digital Photography Scoring Tool (questions a and b ). For analysis of the question a , we used the content analysis technique, and for b , we used the Statistical Package for the Social Sciences 20.0 (temporary license). The socio-professional profile revealed the predominance of females; age group 34-43 years; professionals with specialization; 10-18 years of length of service; and nurses working exclusively in the hospital and who know the Patient Safety. The photographic analysis in relation to Patient Safety resulted in specific categories for each stage of the medication system. Regarding disposal, we identified Proper verification ; Improper verification ; Correct identification ; Disposal in single doses ; and Improper Environment , with predominance of that last category. As for storage: Proper storage ; Improper storage ; Risk of exchange/disappearance ; and Poor hygiene , with special reference to improper storage. In preparation: Risk of exchanging medication/patient ; Inappropriate physical space ; and Inadequate 9 preparation of controlled drugs , highlighting the first category. In drug administration: Lack of Personal Protective Equipment ; Use of Personal Protective Equipment ; Improper administration technique ; Proper administration technique ; Correct drug identification ; Incorrect drug identification ; and Peripheral venous access without identification . From the safety assessment of 10 photographs, by adapting the scores (1-10) to the Likert Scale, we identified three Totally Unsafe (Level 1), three Unsafe (Level 2), three Partially Safe (Level 3), one Safe (Level 4), and no photograph considered Totally Safe. This study identified the prevalence of unsafety in the medication system in the nurses opinion. We were also able to understand that, although nurses identify safety aspects, the most prevalent categories characterize an unsafe assessment. Nursing needs to reflect on its practice, identifying gaps in the medication system in order to achieve a proper and safe care

Rapid spot test analysis for the detection of urotropine in pharmaceutical preparations

The widespread falsification and/or adulteration of commercially available pharmaceutical preparations call for reliable methods of drug identification, preferably through selective and rapid sorting color tests that could be undertaken with minimum equipment remote from laboratory facilities. The present work deals with a convenient adaptation and refinement of a spot test devised by Feigl (1966) for urotropine, based on the hydrolytic cleavage of that substance in the presence of sulfuric acid, splitting out formaldehyde which is identified by its color reaction with chromotropic acid. A simple emergency kit was developed for the quick, efficient, inexpensive and easy performance of urotropine tests by semiskilled personnel even in the drugstore laboratory (or office) as well as in a mobile screening operation. It is shown that when the reagents are added according to the recommended sequence a self-heating system is generated, increasing substantially the reactions' rates and the test sensitivity as well. The identification limit found was 25 mug of urotropine, for both solid and liquid samples. The possible interference of 84 substances/materials was investigated. Interference was noted only for methylene blue, acriflavine, Ponceau Red, Bordeaux Red (these dyes are often included in urotropine dosage forms), pyramidone, dipyrone, quinine and tetracycline. A simple procedure for removing most of the interferences is described. Data for 8 commercial dosage forms and results obtained from their analysis are presented.

GLICOALCALOIDES DOS FRUTOS DO SOLANUM FLACCIDUM VELL

From the fruits of Solanum flaccidum Vell, two glycoalkaloids (solamargine and solasonine) and one aglycone (solasodine) were isolated and identified.

Coumarins and terpenoids from Dorstenia asaroides Gardn. in Hook

Phytochemical investigation of rhizomes and leaves of Dorstenia asaroides Gardn. in Hook. (Moraceae) afforded the furocoumarins psoralen and bergapten, the triterpenes α-amyrin, α-amyrin acetate, β-amyrin acetate, lupeyl acetate and simiarenol and saccharose.

Constituintes de Sorocea bomplandii Baillon

The chemical investigation of the leaves of Sorocea bomplandii Baillon (Moraceae) led to the identification of pentacyclic triterpenes, fatty acid ester and isoprenoids. Chromatographyc comparison between the infusion S. bomplandii with that of Maytenus aquifolium - a Celastraceae with proved antiulcer activity - has shown that they have different compositions: the first one is based on sugars and the last one is based on flavonoid glycosides.

A review of antifertility folkloric plants tested in laboratory animals

The use of natural active principals is widespread among a great proportion of the rural population, or by people who do not have easy access to medical assistance. These active principles are used as food or medicines, and even for purposes of contraception. It becomes necessary to establish a relationship between the folklore habits and current information on the nature of anti-fertility substances, and knowledge of their mechanisms. Anti-fertility agents may exert their actions in a number of areas, (hypothalamus, anterior pituitary, oviduct, uterus, and vagina), inhibiting synthesis and/or liberation of hormones (follicle-stimulating, luteinizing, and steroid hormones), ovulation, ovum transportation, and implantation process. Therefore, a review of literature was carried out, including of several plants used by women as abortifacient and anti-fertility agents to compare their effects with those obtained among laboratory animals.

Advances in prodrug design

The background of prodrug design is presented herein as the basis for introducing new and advanced latent systems, taking into account mainly the versatility of polymers and other macromolecules as carriers. PDEPT (Polymer-Directed Enzyme Prodrug Therapy); PELT (Polymer-Enzyme Liposome Therapy); CDS (Chemical Delivery System); ADEPT(Antibody-Directed Enzyme Prodrug Therapy); GDEPT/VDEPT (Gene-Directed Enzyme Prodrug Therapy/Virus-Directed Enzyme Prodrug Therapy); ODDS (Osteotropic Drug Delivery System) and LEAPT (Lectin-directed enzyme-activated prodrug therapy) are briefly described and some examples are given. © 2005 Bentham Science Publishers Ltd.

Compostos fenólicos e atividade antioxidante de Leiothrix flavescens (Bong.) Ruhland (Eriocaulaceae)

This paper describes a chemical investigation (by high-speed counter-current chromatography) of an extract in methanol of the capitula (flower-heads) of the endemic Brazilian herb Leiothrix flavescens (Bong.) Ruhland (Eriocaulaceae). Fractionation of this extract by preparative chromatography and identification of the isolated compounds by spectrometric methods (IR, UV, ESI-MS, NMR) led to the identification of flavones (apigenin, luteolin and 6-methoxyluteolin) and 1,3-di-O-feruloyl glycerol. The antioxidant activity of the extract was determined by DPPH reduction and the total phenolic content by the Folin-Ciocalteau assay. It was found that the methanolic extract of L. flavescens possesses strong antioxidant activity. Additionally, the chemical profile provided useful data for a discussion of the taxonomy of the Eriocaulaceae.

Identificação de diterpenos clerodânicos em diferentes órgãos de Casearia sylvestris Swartz

Casearia sylvestris Swartz (Salicaceae) is a tree or shrub distributed widely in Brazil, where it is used in popular medicine. Several bioactive clerodane diterpenes typical of Casearia have been isolated from this species (e.g. casearins and casearvestrins). The main objective of this study was to identify clerodane diterpenes in various organs of C. sylvestris, using chromatographic and spectroscopic analytical techniques. The extracts of the different plant parts were analyzed by thin layer chromatography, high performance liquid chromatography with diode array detector and 1H nuclear magnetic resonance. In the chromatographic analysis, clerodane diterpenes isolated from C. sylvestris were used as standards, including rel-19Sacetóxi-18R- butanoilóxi-18,19- epóxi -6S -hidróxi -2R-(2-metilbutanoilóxi) -5S, 8R, 9R, 10S -cleroda-3,13(16),14-triene, isolated for the first time from the stems. Phytochemical profiles of the organs were produced, which indicated the presence of clerodane diterpenes in all parts of the plant, notably in the leaves. The results also suggest that the main clerodane diterpenes in the stems, flowers and roots had conjugated double-bond patterns that differed from those found in the leaves.

Pharmacognostical evaluation of fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae)

This study describes the chemical and physical-chemical profile of plant drug and ethanolic extract obtained from fruits of Solanum lycocarpum A. St.-Hill. (Solanaceae). The physical and chemical analysis involved the granulometry determination, non-compacted apparent density, loss on drying in oven and in infrared scale, pH, ash values and extractive values. The results determined the physical-chemical characteristics of the drug plant. It was also carried out the microbiological control of the plant drug. The preliminary phytochemical screening featured the presence of tannins, flavonoids and saponins in the plant drug and alkaloids and steroids in the ethanolic exctract. The solamargine and solasonine glycoalkaloids were identified through TLC and GC/ MS. The levels of total phenols and tannins were quantified in the extract (8.90% and 6,85% respectively). Such studies contribute to the chemical identification and quality control of S. lycocarpum fruits. © 2010 Phcog.net.