Pharmacobotanical characterization of Monteverdia ilicifolia (Mart. ex Reiss.) Biral leaves and its adulterants sold as medicinal tea in Brazil: a contribution to quality control / Caracterización farmacobotánica de hojas de Monteverda ilicifolia (Mart. ex Reiss.) Biral y sus adulterantes vendidos como té medicinal en Brasil: una contribución al contol de calidad

Leaves of Monteverdia ilicifolia ("espinheira-santa") are considered a medicinal tea by the Brazilian Sanitary Surveillance Agency (Anvisa), by their anti-dyspeptic, anti-acid and protective of the gastric mucosa properties. Their spiny margins are similar to those of other botanical species, which may lead to misidentifications. The aim of this work was to evaluate the authenticity of 32 samples of herbal drugs commercialized as "espinheira-santa" in the formal trade in Brazil, by macro and microscopic morphological studies of the leaves. The evaluation of the botanical authenticity was based on leaf venation patterns, shape and anatomy of the petiole and midrib region in cross section, vascular system arrangement and epidermal characters. Analysis of these characters compared to literature data suggests that 34% of the samples are M. ilicifolia and the remaining 66% are Sorocea bonplandii, a species with no clinical studies assuring its effective and safe use, representing thus a potential risk to public health.

Las hojas de Monteverdia ilicifolia ("espinheira-santa") son consideradas tés medicinales por la Agencia Nacional de Vigilancia Sanitaria (Anvisa), Brasil, por las indicaciones terapéuticas como antidispépticos, antiácidos y protectores de la mucosa gástrica. Sus márgenes foliares espinescentes se parecen a los de otras especies, conduciendo a identificaciones erróneas. El objetivo de este trabajo fue evaluar la autenticidad de 32 muestras de drogas vegetales vendidas como "espinheira-santa" en el comercio legal de Brasil, realizando un estudio morfológico de las hojas. Esta evaluación se ha basado en observar de la hoja, sus patrones de nerviación, su forma y anatomía (pecíolo y nervadura central en corte transversal), disposición del sistema vascular y caracteres epidérmicos. El análisis de la morfología, comparado con los datos de literatura, sugiere que el 34% de las muestras son M. ilicifoliay el 66% son Sorocea bonplandii, una especie que no cuenta con los estudios clínicos que garantizan su uso efectivo y seguro, representando un riesgo para la salud pública.

Anatomical, Histochemical and Biological Studies of Clusia grandiflora Splitg. (Clusiaceae)

Abstract Clusia grandiflora belongs to an important botanical family which is known for its medicinal value, however there are few reports in literature about the species, highlighting the relevance of this study. Anatomical studies with leaves and stems were performed using traditional techniques. In this investigation it was identified particularities of the species such as the presence of vascular system arranged in an opened arc-shaped with the flexed ends towards the inside of the arch with accessory bundles in the petiole. In histochemical studies, performed with different reagents, alkaloids, phenols substances, carbohydrates and lipids were located. The cytotoxic activity of the extracts was performed by tetrazole salt and showed promising results for ethanolic extracts of stems (IC50 human colon cells of 24.30 μg/ mL) and leaves (IC50 ascites gastric cells of 44.15 μg/ mL), without cell membrane disruption of erythrocytes. The antibacterial activity was evaluated by tryptic soy agar and minimal inhibitory concentration assays and showed positive results for Pseudomonas aeruginosa and Escherichia coli, with better result for adventitious roots (32 μg/ mL and 16 μg/ mL, respectively), stems (64 μg/ mL and 32 μg/ mL, respectively) and leaves (64 μg/ mL and 32 μg/ mL, respectively) ethanolic extracts. Thus, these studies were able to characterize the species and show its potential as promising source of active substances.

Clusia criuva Cambess. (Clusiaceae): anatomical characterization, chemical prospecting and antioxidant activity

ABSTRACT This study aims the anatomical description and chemical characterization of aerial parts of Clusia criuva Cambess., Clusiaceae in addition to the evaluation of the antioxidant activity of crude extracts, correlated to the flavonoid content. The morphological characterization was performed using traditional techniques of plant anatomy. For phytochemical studies, crude extracts were obtained by static maceration and analyzed by thin layer chromatography. The antioxidant activity and the flavonoids content were determined by colorimetric methods involving, respectively, 2,2-diphenyl-1-picrylhydrazyl free radical and aluminum chloride. C. criuva has uniseriate epidermis, paracytic stomata, hypostomatic leaves, cuticular flanges and cordiform vascular cylinder with accessory bundles. Chemical prospecting confirmed the abundant presence of terpenes and phenols in the extracts of leaves and of fruits. The methanolic extract of seeds showed the lowest EC50 value, but the methanolic extract of pericarps exhibited the highest maximum antioxidant activity. The results suggested a high percentage of flavonoids in the hexanic extract of pericarps, however, this could represent, in fact, the presence of benzophenones. Secretory ducts and the shape of the midrib are diagnostic for C. criuva. The antioxidant activity is not directly related to the flavonoids. The results indicate the importance of future studies with C. criuva chemical constituents.

Laboratory evaluation of Clusia fluminensis extracts and their isolated compounds against Dysdercus peruvianus and Oncopeltus fasciatus

ABSTRACT The effects of the hexanic extracts of the fruits and flowers of Clusia fluminensis Planch. & Triana, Clusiaceae, as well as their main constituents, the triterpene lanosterol and the benzophenone clusianone, were evaluated on hemipterans Dysdercus peruvianus and Oncopeltus fasciatus. The topical treatments of insects with the hexanic extracts significantly affected the survival of O. fasciatus, but not that of D. peruvianus. Concomitantly, extracts delayed the development of both hemipterans. Moreover, isolated lanosterol significantly reduced both the survival and development of O. fasciatus and D. peruvianus, while clusianone only reduce the survival of D. peruvianus and marginally inhibited the development of both insects. The results show the specific activity of lanosterol and clusianone against the two evaluated insect species and indicate the potential of compounds derived from C. fluminensis for the development of specific biopesticides for the control of agricultural pests. Subsequent work will examine the mode of action of lanosterol and clusianone isolates from C. fluminensis.

Biocontrol evaluation of extracts and a major component, clusianone, from Clusia fluminensisPlanch. & Triana againstAedes aegypti

Studies evaluated the effects of hexanic extracts from the fruits and flowers ofClusia fluminensis and the main component of the flower extract, a purified benzophenone (clusianone), against Aedes aegypti. The treatment of larvae with the crude fruit or flower extracts from C. fluminensis did not affect the survival ofAe. aegypti (50 mg/L), however, the flower extracts significantly delayed development of Ae. aegypti. In contrast, the clusianone (50 mg/L) isolate from the flower extract, representing 54.85% of this sample composition, showed a highly significant inhibition of survival, killing 93.3% of the larvae and completely blocking development of Ae. aegypti. The results showed, for the first time, high activity of clusianone against Ae. aegypti that both killed and inhibited mosquito development. Therefore, clusianone has potential for development as a biopesticide for controlling insect vectors of tropical diseases. Future work will elucidate the mode of action of clusianone isolated from C. fluminensis.

Cytotoxic and Antiviral Activity of Extracts and Compounds Isolated from Clusia Fluminensis Planch. & Triana (Clusiaceae) / Atividade Citotóxica e Antiviral de Extratos e Compostos Isolados de Clusia Fluminensis Planch. & Triana (Clusiaceae)

The worldwide distribution of herpes simplex virus type 1 (HSV-1) allied to the emergence of resistant strains makes necessary and urgent the search and development of new substances capable of preventing and treating HSV-1 infections. Studies demonstrate synergy between genital herpes and human immunodeficiency virus type 1 (HIV-1), which represents a major concern for global public health. Objective: The objective of this study was to evaluate the activity of crude extracts and isolated substances from C. fluminensis in the in vitro replication of the HSV-1 virus and HIV-1-RT activity. Methods: This study evaluated the activity of extracts and isolated compounds from Clusia fluminensis Planch. & Triana against HSV-1 using Vero cells in culture and against HIV-1 using a recombinant reverse transcriptase enzyme (HIV -1 RT). The percentage of inhibition against HSV-1 was determined from viral lysis plaque reduction assay, and the anti-HIV-1-RT test was performed by a fluorimetric assay. It was also evaluated the cytotoxic activity of the samples using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]. Results: The crude extracts showed high percentage of inhibition against HSV-1, reaching 81.4 to 100.0% inhibition in non-cytotoxic concentration (50 µg/mL). The isolated compounds, lanosterol and clusianone, demonstrated 100% inhibition in non-cytotoxic concentration (50 µg/mL). We also examined the effects of the extracts and isolates on the activity of the HIV-1-RT. Among the crude extracts, only the methanolic extract of leaves and methanolic extract of stems showed inhibitory activity against HIV-1-RT. Regarding the isolated compounds, lanosterol showed a moderate activity. Conclusion: Our data demonstrate that extracts and isolates compounds Clusia fluminensis Planch. & Triana have promising antiviral activity inhibiting HSV-1 replication and HIV-1 by inhibiting the anti-RT activity.

A distribuição mundial do vírus herpes simplex tipo 1 (HSV-1) aliada ao surgimento de cepas resistentes torna necessária e urgente a busca e o desenvolvimento de novas substâncias capazes de prevenir e tratar infecções HSV-1. Estudos demonstram sinergia entre herpes genital e vírus da imunodeficiência humana tipo 1 (HIV-1), o que representa uma grande preocupação para a saúde pública global. Objetivo: O objetivo deste estudo foi avaliar a atividade de extratos brutos e substâncias isoladas de Clusia fluminensis Planch. & Triana na replicação in vitro do vírus HSV-1 e na atividade anti HIV-1-RT. Métodos: Este estudo avaliou a atividade de extratos e substâncias isoladas de Clusia fluminensis Planch. & Triana contra o HSV-1 utilizando células Vero em cultura e contra o HIV-1 utilizando a enzima transcriptase reversa recombinante (HIV-1 RT). A porcentagem de inibição contra o HSV-1 foi determinada a partir do ensaio de redução de placas de lise viral, e o ensaio anti-HIV-1 RT foi realizado por um ensaio fluorimétrico. Também foi avaliada a atividade citotóxica das amostras utilizando MTT [brometo de 3- (4,5-dimetiltiazol-2-il) -2,5-difeniltetrazólio]. Resultados: Os extratos demonstraram elevada percentagem de inibição contra o HSV-1, atingindo 81,4 a 100,0% de inibição em concentração não citotóxica (50 µg/mL). Os compostos isolados, lanosterol e clusianona, demonstraram 100% de inibição em concentração não citotóxica (50 µg/mL). Examinamos também os efeitos dos extratos e isolados sobre a atividade anti-HIV-1 RT. Entre os extratos brutos, apenas o extrato metanólico das folhas e caules apresentaram atividade anti-HIV-1 RT. Em relação aos compostos isolados, lanosterol mostrou uma atividade moderada. Conclusão: Nossos dados demonstram que os extratos e compostos isolados de Clusia fluminensis Planch. & Triana possuem atividade antiviral promissora inibindo a replicação do HSV-1 e HIV-1 através da inibição da atividade anti-RT.

A influência das comorbidades, do uso de medicamentos e da institucionalização na capacidade funcional dos idosos / The influence of comorbidities, use of drugs and institutionalization in the functional capacity of the elderly

Introdução: Nos países em desenvolvimento, como o Brasil, a transição demográfica caracteriza-se pelo aumento progressivo do número de idosos. Predominam as doenças crônico-degenerativas de letalidade baixa e de incapacidade alta. Capacidade funcional é definida como a habilidade física e mental para manter uma vida independente e autônoma. Um dos instrumentos mais usados para avaliar a capacidade funcional é o índice de independência nas atividades de vida diária (Índice de Katz). O envelhecimento assim como os fatores demográficos, socioeconômicos e de condições de saúde influenciam nesta capacidade. Objetivo: O objetivo do estudo foi avaliar a capacidade funcional de idosos da cidade de Barbacena-MG e correlaciona-la com a presença de comorbidades, uso de medicamentos, características sociodemográficas e institucionalização. Materiais e métodos: Estudo de corte transversal com 81 idosos institucionalizados e 254 não institucionalizados, avaliados através do Índice de Katz e de um questionário, no qual foram quantificadas variáveis sociodemográficas, comorbidades apresentadas e uso de medicamentos contínuos nos 12 meses precedentes à entrevista. Resultados: Os fatores independentes associados à incapacidade funcional, que possuíram valor estatisticamente significativo, foram: possuir 80 anos ou mais, ser do gênero feminino, morar acompanhado ou em Instituição de Longa Permanência, usar continuamente uma média de 4,7 ± 2,8 medicamentos e fazer uso regular de fármacos psicotrópicos. Conclusão: Dentre os idosos com menor capacidade funcional houve maior prevalência de institucionalização, idade mais avançada, predomínio do gênero feminino e maior uso de medicamentos. Diferente do esperado, os gerontes dependentes funcionais não apresentaram maior número de comorbidades, quando comparados com os independentes.

Introduction: In developing countries, like Brazil, the demographic transition is characterized by a progressive increase in the number of elderly. Prevalent diseases are chronic degenerative diseases of low mortality and high disability. Functional capacity is defined as the physical and mental ability to maintain an independent and autonomous life. One of the most commonly used instruments to evaluate the functional capacity is the index of independence in activities of daily living (Katz Index). Aging as well as the demographic, socioeconomic and health factors influence this ability. Objective: The study objective is to evaluate the functional capacity of the elderly in Barbacena-MG and to correlate this fact to the presence of comorbidities, medication use, sociodemographic characteristics and institutionalization. Methods: Cross-sectional study of 81 institutionalized elderly and 254 non-institutionalized, evaluating them through the Katz Index and a questionnaire in which sociodemographic variables, comorbidities and use of continuous medicines in the 12 months preceding the interview were quantified. Results: Independent factors associated to functional capacity having statistically significant value were: to be 80 or older, to be female, living together or in long-stay institution, continually use of an average of 4.7 ± 2.8 medications and regular use of psychotropic drugs. Conclusion: Among elderly patients with lower functional capacity, there was prevalence of institutionalization, older age, higher proportion of women and increased use of medications. Different than expected, the functional dependent elderly didn't have more comorbidities, when compared with the independents.

Chemical composition fluctuations in roots of Plumbago scandens L. in relation to floral development

Plumbago scandens L. is a Brazilian tropical/subtropical species that occurs along the coast. Chemically it is mainly represented by naphthoquinones, flavonoids, terpenoids and steroids. The aim of the present work is to study quantitative changes in the root metabolic production of Plumbago scandens during different physiologic developmental stages relative to floration. The results indicated the presence of four substances in the extracts: plumbagin, epi-isoshinanolone, palmitic acid and sitosterol, independent on developmental stage. The naphthoquinone plumbagin has always showed to be the major component of all extracts. Naphthoquinones exhibited their highest content during floration, while the content of the two others components decreased during this stage, revealing an inverse profile. The chemical composition changed depending on the plant requirements.

Plumbago scandens L. é uma espécie brasileira tropical/subtropical que ocorre ao longo da costa. Quimicamente, é principalmente representada por naftoquinonas, flavonóides, terpenóides e esteróides. objetivo do presente trabalho é estudar mudanças quantitativas da produção metabólica nas raízes de Plumbago scandens durante diferentes estágios de desenvolvimento fisiológico, relativos à floração. Os resultados indicaram a presença de quatro substâncias nos extratos: plumbagina, epi-isoshinanolona, ácido palmítico e sitosterol, independente do estágio de desenvolvimento. A naftoquinona plumbagina tem sempre mostrado ser o componente majoritário de todos os extratos. Naftoquinonas exibiram seus maiores conteúdos durante a floração, enquanto o conteúdo dos dois outros componentes decresceu durante este estágio, revelando um perfil inverso. A composição química modificou dependendo das necessidades da planta.

Antimicrobial activity in vitro of plumbagin isolated from Plumbago species

Plumbagin is a naturally occurring naphthoquinone isolated from roots of Plumbago scandens. The plant was collected at the Campus of Fundação Oswaldo Cruz, Rio de Janeiro, Brazil. P. scandens is used as a traditional medicine for the treatment of several diseases. The antimicrobial activity of plumbagin was evaluated using the macrodilution method. The compound exhibited relatively specific activity against bacteria and yeast. The minimum inhibitory concentration test showed the growth inhibiton of Staphylococcus aureus at a concentration of 1.56 æg/ml and of Candida albicans at a concentration of 0.78 æg/ml. These results suggest the naphthoquinone plumbagin as a promising antimicrobial agent.