Biological activities of marine invertebrates extracts from the northeast brazilian coast / Atividades biológicas de extratos de invertebrados marinhos da costa nordeste do Brasil

Abstract This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing β-galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.

Resumo Este artigo reporta as atividades in vitro antiproliferativa, atiprotozoárica, anti-herpética e antimicrobiana de 32 extratos orgânicos provenientes de 14 esponjas marinhas e 14 corais coletados no litoral nordestino brasileiro. Os extratos etanólicos das esponjas Amphimedon compressa e Tedania ignis, e o extrato acetônico de Dysidea sp. demonstraram resultados promissores em relação aos efeitos antiproliferativos frente as linhagens celulares A549, HCT-8, PC-3 pelo método da sulforrodamina B, mas sem especificidade. Em relação à atividade antiprotozárica, os extratos etanólico de Amphimedon compressa e acetônico e etanólico de Dysidea sp. apresentaram atividade contra Leishmania amazonensis e Trypanosoma cruzi através do método de expressão de β-galactosidase em células THP-1. Na investigação preliminar de atividade antiviral frente ao vírus Herpes simplex tipo 1 (cepa KOS), os extratos etanólicos das esponjas Amphimedon compressa, Haliclona sp. e Chondrosia collectrix inibiram mais de 50% da replicação viral. O extrato etanólico da esponja Haliclona sp. demonstrou resultados promissores para atividade anti-herpética com altos índices de seletividade para as cepas KOS (IS >50) e 29R (IS>79) frente ao VHS-1 e cepa 333 (IS>108) frente ao VHS-2. O extrato etanólico da esponja Amphimedon compressa exibiu uma pequena atividade contra Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli pelo método de difusão em disco. De acordo com os resultados apresentados, os extratos das esponjas Amphimedon compressa, Tedania ignis e Dysidea sp. serão selecionados para futuros estudos de isolamento e identificação dos compostos bioativos para as atividades antiproliferativa e antiprozoárica. O extrato etanólico de Haliclona sp. será investigado por possuir atividade relevante anti-herpética.

Pneumonia por toxoplasmose em paciente imunocompetente / Toxoplasma pneumonia in an immunocompetent patient: case repor

Com grande distribuição mundial e incidência significativa, a toxoplamose é uma doença comum em mamíferos e pássaros, causada pelo protozoário Toxoplasma gondii. No homem, o parasitismo na fase proliferativa intracelular pode se apresentar sem sintomas, ou causar clínica transitória caracterizada por febre, fadiga e linfadenopatia. Por se tratar de patologia com sintomas inespecíficos e comuns a muitas outras, é fundamental a correta pesquisa de diagnósticos diferenciais, como citomegalovírus e Epstein-Barr. Relatamos o caso de um jovem e hígido, que desenvolveu pneumonia e, após confirmação sorológica para toxoplasmose e o tratamento adequado, apresentou melhora clínica.

With great worldwide distribution and significant incidence, toxoplamosis is a common disease in mammals and birds, caused by the protozoan Toxoplasma gondii. In humans, the parasitism in its intracellular proliferative phase may present no symptoms, or cause a transient condition characterized by fever, fatigue, and lymphadenopathy. Because it is a pathology with nonspecific symptoms that are common to many other conditions, it is fundamental to find the correct research of differential diagnoses, such as for Cytomegalovirus and Epstein Barr. We report a case of a young and healthy man who developed pneumonia and, after serological confirmation for toxoplasmosis and the appropriate treatment, presented clinical improvement

Anti-coccidial activity of the ethanol extract of Tribulus terrestris fruits on Eimeria tenella / 한국실험동물학회지

Anti-coccidial effects of the fruits of Tribulus terrestris (Tribuli fructus) ethanol extract (TTE) were studied with animal experiment following per oral administration with Eimeria (E.) tenella. This experiment was performed on the 3-day-old chicks (n=30). The animals were divided with 3 groups; TFE 15mg per animal+infected (n=10), TTE untreated+infected (n=10) and non-infected control (n=10). Animals were administrated with or without TTE during 1 week, and then inoculated with E. tenella. The anti-coccidial activity were evaluated with oocysts shedding numbers in stools, body weights changes and food intake changes. The TTE-inoclated animals revealed significantly decreased stool oocysts numbers (P < 0.05) when compared to the TTE untreated animals. Also, TTE-treated animals showed more increased body weight gains (P < 0.05) than the TTE untreated animals. These results demonstrate that TTE produce anticoccidial activities against E. tenella. TTE could be a promising treatment for the coccidiosis.

Aspectos patológicos da intoxicação por aceturato de diminazeno em camelídeos sul-americanos / Pathological aspects of diminazene aceturate toxicosis in american camelids

Aceturato de diminazeno é um fármaco quimioterápico sintético comumente usado na medicina veterinária para o tratamento de doenças causadas por parasitos hematozoários. Entretanto, seu uso pode levar a efeitos colaterais, como alterações neurológicas graves e morte. A criação de camelídeos é uma atividade recente no Brasil, fazendo-se necessário conhecer mais sobre as doenças que acometem essas espécies. De dez camelídeos (seis lhamas e quatro alpacas) da propriedade, seis tiveram sinais clínicos e, destes, apenas uma lhama com manifestações leves recuperou-se. Os sinais clínicos incluíam apatia, andar cambaleante, fraqueza, sialorreia, cabeça baixa e pendida lateralmente, dificuldade em levantar e dispneia, observados a partir de 18 horas após o uso do medicamento. À necropsia e ao exame histopatológico foram observadas alterações de encefalopatia hemorrágica bilateral e simétrica, mais graves em tronco encefálico e tálamo. Este trabalho descreve as principais lesões observadas em um surto de intoxicação por diminazeno em alpacas (Lama pacos) e lhamas (Lama glama) e alerta criadores e veterinários sobre o risco de intoxicação por aceturato de diminazeno em camelídeos sul americanos.(AU)

Diminazene aceturate is a synthetic chemotherapeutic drug commonly used in veterinary medicine for the treatment of diseases caused by hematozoan parasites. However, side effects as severe neurological disorders and death can occur. The raising of american camelids is a recent activity in Brazil, requiring knowledge about diseases that affect these species, in order to avoid misguided conducts. In a herd of ten camelids (six llamas and four alpacas) six showed clinical signs and five died; only a llama with mild signs recovered. The clinical signs included apathy, difficulty to stand up, staggering gait, weakness, down head and drooping the head laterally, dyspnea and drooling of saliva, observed from 18 hours after use of the drug. At necropsy and histopathological examination was found bilateral and symmetrical hemorrhagic encephalopathy, more severe in brainstem and thalamus. This paper describes the main lesions observed in an outbreak of diminazene aceturate poisoning in alpacas (Lama pacos) and llamas (Lama glama) and alert breeders and veterinarians about the risk of poisoning by this drug in american camelids.(AU)

A leishmaniose visceral ainda deve ser lembrada no diagnóstico diferencial de hepatoesplenomegalia febril? Revisão bibliográfica e relato de caso / Should visceral leishmaniasis still be remembered in the differential diagnosis of febrile hepatosplenomegaly? Literature review and case report

Apesar de não haver caso autóctone na Região Sudeste, a leishmaniose visceral é encontrada em pacientes que migram de regiões endêmicas. Como é uma doença que, se não reconhecida e conduzida adequadamente, apresenta alta mortalidade, realizamos uma revisão bibliográfica e destacamos, com o relato deste caso, a importância de a incluirmos no diagnóstico diferencial de hepatoesplenomegalia febril ainda na avaliação clínica inicial, pois o retardo no diagnóstico piora o prognóstico e a sobrevida do paciente, sendo sumária a introdução de terapêutica apropriada o mais breve possível.(AU)

Although there is no autochthonous case finding in the Southeast Region, visceral leishmaniasis is found in patients migrating from endemic areas. Because it is a disease that, if not properly recognized and treated, presents high mortality, we performed a bibliographic review and highlight, with the report of this case, the importance of including it in the differential diagnosis of febrile hepatosplenomegaly in the initial clinical evaluation. The late diagnosis worsens the patient's prognosis and survival, and the introduction of appropriate therapeutics should be made as soon as possible.(AU)

Biological activities of marine invertebrates extracts from the northeast brazilian coast

Abstract This paper reports the in vitro antiproliferative effects, antiprotozoal, anti-herpes and antimicrobial activities of 32 organic extracts of 14 marine sponges and 14 corals collected in northeast Brazilian coast. The ethanolic extracts of the sponges Amphimedon compressa and Tedania ignis, and the acetone extract of Dysidea sp. showed relevant results concerning the antiproliferative effects against A549, HCT-8, and PC-3 cell lines by sulforhodamine B assay, but also low specificity. Concerning the antiprotozoal screening, the ethanolic extract of Amphimedon compressa and the acetone and ethanolic extracts of Dysidea sp. were the most active against Leishmania amazonensis and Trypanosoma cruzi expressing -galactosidase in THP-1 cells. In the preliminary anti-HSV-1 (KOS strain) screening, the ethanolic extracts of the sponges Amphimedon compressa, Haliclona sp. and Chondrosia collectrix inhibited viral replication by more than 50%. The most promising anti-herpes results were observed for the ethanolic extract of Haliclona sp. showing high selective indices against HSV-1, KOS and 29R strains (SI> 50 and >79, respectively), and HSV-2, 333 strain (IS>108). The results of the antibacterial screening indicated that only the ethanolic extract of Amphimedon compressa exhibited a weak activity against Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli by the disk diffusion method. In view of these results, the extracts of Amphimedon compressa, Tedania ignis and Dysidea sp. were selected for further studies aiming the isolation and identification of the bioactive compounds with antiproliferative and/or antiprotozoal activities. The relevant anti-herpes activity of the ethanolic extract of Haliclona sp. also deserves special attention, and will be further investigated.

Resumo Este artigo reporta as atividades in vitro antiproliferativa, atiprotozoárica, anti-herpética e antimicrobiana de 32 extratos orgânicos provenientes de 14 esponjas marinhas e 14 corais coletados no litoral nordestino brasileiro. Os extratos etanólicos das esponjas Amphimedon compressa e Tedania ignis, e o extrato acetônico de Dysidea sp. demonstraram resultados promissores em relação aos efeitos antiproliferativos frente as linhagens celulares A549, HCT-8, PC-3 pelo método da sulforrodamina B, mas sem especificidade. Em relação à atividade antiprotozárica, os extratos etanólico de Amphimedon compressa e acetônico e etanólico de Dysidea sp. apresentaram atividade contra Leishmania amazonensis e Trypanosoma cruzi através do método de expressão de -galactosidase em células THP-1. Na investigação preliminar de atividade antiviral frente ao vírus Herpes simplex tipo 1 (cepa KOS), os extratos etanólicos das esponjas Amphimedon compressa, Haliclona sp. e Chondrosia collectrix inibiram mais de 50% da replicação viral. O extrato etanólico da esponja Haliclona sp. demonstrou resultados promissores para atividade anti-herpética com altos índices de seletividade para as cepas KOS (IS >50) e 29R (IS>79) frente ao VHS-1 e cepa 333 (IS>108) frente ao VHS-2. O extrato etanólico da esponja Amphimedon compressa exibiu uma pequena atividade contra Enterococcus faecalis, Pseudomonas aeruginosa and Escherichia coli pelo método de difusão em disco. De acordo com os resultados apresentados, os extratos das esponjas Amphimedon compressa, Tedania ignis e Dysidea sp. serão selecionados para futuros estudos de isolamento e identificação dos compostos bioativos para as atividades antiproliferativa e antiprozoárica. O extrato etanólico de Haliclona sp. será investigado por possuir atividade relevante anti-herpética.

Anti-infective, cytotoxic and antioxidant activity of Ziziphus oxyphylla and Cedrela serrata

Objective To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla (Z. oxyphylla) and Cedrela serrata (C. serrata) in Pakistan against infectious and liver diseases. Methods Factions of different polarity were tested in vitro for their antiprotozoal, antimalarial, antibacterial and antifungal activity against different pathogens. Cytotoxicity on MRC-5 cell lines (human lung fibroblasts) as well as, in vitro radical scavenging activity was evaluated using the 1, 1-diphenyl-2-picrylhydrazyl radical assay. Results The highest antiprotozoal activity was observed for the CHCl

Anti-infective, cytotoxic and antioxidant activity of Ziziphus oxyphylla and Cedrela serrata

Objective: To search for the most active antimicrobial and antioxidant sub-fractions related to traditional use of Ziziphus oxyphylla (Z. oxyphylla) and Cedrela serrata (C. serrata) in Pakistan against infectious and liver diseases. Methods: Factions of different polarity were tested in vitro for their antiprotozoal, antimalarial, antibacterial and antifungal activity against different pathogens. Cytotoxicity on MRC-5 cell lines (human lung fibroblasts) as well as, in vitro radical scavenging activity was evaluated using the 1, 1-diphenyl-2-picrylhydrazyl radical assay. Results: The highest antiprotozoal activity was observed for the CHCl3 fractions of Z. oxyphylla roots and leaves, and C. serrata bark. The CHCl3 and EtOAc fractions of Z. oxyphylla roots, the CHCl3 fraction of Z. oxyphylla leaves, the EtOAc and the residual MeOH: H2O fraction of C. serrata bark showed antibacterial activity against Staphylo-coccus aureus. The same residual MeOH: H2O fraction of C. serrata bark was active against Candida albicans. The highest antioxidant activity was observed for the more hydrophilic EtOAc fractions of Z. oxyphylla leaves, C. serrata bark and leaves, and the residual MeOH:H2O fraction of C. serrata bark. Conclusions: This study supports at least in part the traditional uses of these plants for antimicrobial purposes and against liver diseases.

Antiprotozoal assessment and phenolic acid profiling of five Fumaria (fumitory) species

Objective: To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases. Methods: Consequently, in the current study, antiprotozoal effect of the ethanol extracts obtained from five Fumaria species (Fumaria densiflora, Fumaria cilicica, Fumaria rostellata, Fumaria kralikii, and Fumaria parviflora) was investigated against the parasites; Plasmodium falciparum (malaria) and Trypanosoma bruceirhodesiense (human African trypanosomiasis) at 0.81 and 4.85 μg/mL concentrations. Results: Among them, Fumaria densiflora extract exerted the highest antiplasmodial (93.80%) and antitrypanasomal effect (55.40%), while the ethanol extracts of Fumaria kralikii (43.45%) and Fumaria rostellata (41.65%) showed moderate activity against Plasmodium falciparum. Besides, phenolic acid contents of the extracts were analyzed using high performance liquid chromatography (HPLC) and trans-cinnamic (4.32 mg/g) and caffeic (3.71 mg/g) acids were found to be the dominant phenolic acids in Fumaria densiflora. Conclusions: According to our results, Fumaria densiflora deserve further study for its promising antiprotozoal activity.

Antiprotozoal assessment and phenolic acid profiling of five Fumaria (fumitory) species

OBJECTIVE@#To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases.@*METHODS@#Consequently, in the current study, antiprotozoal effect of the ethanol extracts obtained from five Fumaria species (Fumaria densiflora, Fumaria cilicica, Fumaria rostellata, Fumaria kralikii, and Fumaria parviflora) was investigated against the parasites; Plasmodium falciparum (malaria) and Trypanosoma bruceirhodesiense (human African trypanosomiasis) at 0.81 and 4.85 μg/mL concentrations.@*RESULTS@#Among them, Fumaria densiflora extract exerted the highest antiplasmodial (93.80%) and antitrypanasomal effect (55.40%), while the ethanol extracts of Fumaria kralikii (43.45%) and Fumaria rostellata (41.65%) showed moderate activity against Plasmodium falciparum. Besides, phenolic acid contents of the extracts were analyzed using high performance liquid chromatography (HPLC) and trans-cinnamic (4.32 mg/g) and caffeic (3.71 mg/g) acids were found to be the dominant phenolic acids in Fumaria densiflora.@*CONCLUSIONS@#According to our results, Fumaria densiflora deserve further study for its promising antiprotozoal activity.

Antiprotozoal assessment and phenolic acid profiling of five Fumaria (fumitory) species

Objective: To explore some Fumaria species which were recorded to be traditionally used against malaria and other protozoal diseases. Methods: Consequently, in the current study, antiprotozoal effect of the ethanol extracts obtained from five Fumaria species (Fumaria densiflora, Fumaria cilicica, Fumaria rostellata, Fumaria kralikii, and Fumaria parviflora) was investigated against the parasites; Plasmodium falciparum (malaria) and Trypanosoma bruceirhodesiense (human African trypanosomiasis) at 0.81 and 4.85 μg/mL concentrations. Results: Among them, Fumaria densiflora extract exerted the highest antiplasmodial (93.80%) and antitrypanasomal effect (55.40%), while the ethanol extracts of Fumaria kralikii (43.45%) and Fumaria rostellata (41.65%) showed moderate activity against Plasmodium falciparum. Besides, phenolic acid contents of the extracts were analyzed using high performance liquid chromatography (HPLC) and trans-cinnamic (4.32 mg/g) and caffeic (3.71 mg/g) acids were found to be the dominant phenolic acids in Fumaria densiflora. Conclusions: According to our results, Fumaria densiflora deserve further study for its promising antiprotozoal activity.

Aspectos epidemiológicos, clínicos e anatomopatológicos da intoxicação por aceturato de diminazeno em cães / Epidemiological, clinical, and pathological aspects of diminazene aceturate toxicosis in dogs

Os aspectos epidemiológicos, clínicos e anatomopatológicos da intoxicação espontânea por aceturato de diminazeno foram estudados em 10 cães. Em todos os casos, os cães afetados demonstraram sinais de síndrome tálamo-cortical, principalmente alteração do nível de consciência, tetraparesia, rigidez extensora e crise convulsiva. Em alguns casos, os cães acometidos apresentaram sinais de síndrome cerebelar, como tremores musculares generalizados de alta frequência e baixa amplitude, e/ou de síndrome vestibular, como ataxia, inclinação de cabeça e quedas. Esses sinais ocorreram entre 24 e 48 horas após o uso do fármaco injetável por via intramuscular e se mantiveram até a morte ou eutanásia dos cães (entre 1 e 7 dias). Tais sinais clínicos refletiam encefalomalacia hemorrágica focal simétrica, que afetava a medula oblonga, a ponte, a medular do cerebelo, o tálamo, o mesencéfalo, os pedúnculos cerebelares e os núcleos da base. Esse artigo: 1) descreve e discute essa forma de intoxicação medicamentosa tão pouco citada na literatura internacional e desconhecida da maior parte dos clínicos e patologistas veterinários brasileiros, 2) estabelece critérios clínicos e anatomopatológicos para o seu diagnóstico e, principalmente, 3) atenta para os riscos da utilização desse princípio ativo na terapêutica canina.

The epidemiological, clinical, and pathological aspects of diminazene aceturate (DA) spontaneous toxicosis were evaluated in 10 dogs. All affected dogs developed signs of thalamic-cortical syndrome, characterized mainly by neurological changes in the conscience levels, tetraparesis, extensor stiffness, and seizures. In some cases there was also evidence of cerebellar syndrome, characterized by generalized muscle tremors (high-frequency and low-amplitude) and/or vestibular syndrome, characterized by or ataxia, head tilt, and falling. These clinical signs occurred between 24 and 48 hours following intramuscular administration of DA and persisted until spontaneous death or euthanasia occurred between 1 and 7 days after the onset of clinical signs. The mentioned clinical signs reflected lesions that consisted of focal symmetrical hemorrhagic encephalomalacia affecting medulla oblongata, pons, cerebellar medulla, thalamus, midbrain, cerebellar peduncles, and basal nuclei. This article (1) describes and discusses DA toxicosis in dogs, a poorly-described clinical entity that is unknown by most clinicians and pathologists in Brazil; (2) establishes the clinical and pathological criteria for the diagnosis of DA toxicosis in dogs; and (3) calls up the attention for the risks of using DA in dogs in clinical settings.

Inhibitory effect of Quassia amara Linn. crude bark extract on Entamoeba histolytica in vitro

BACKGROUND: Entamoeba histolytica is an important etiologic agent of diarrhea. Globally, it is estimated to infect 40 to 50 million people and cause 40,000 to 100,000 deaths per year. Metronidazole is effective but can cause adverse reactions in certain individuals. In search of alternatives, traditional medicinal plants are being studied. Several plants in Family Simaroubaceae have shown anti-amoebic activity. Quassia amara, a member of this family has not been tested.OBJECTIVE: To determine the effect of Q. amara crude extract on Entamoeba histolytica in vitro.METHODS: Initial testing of 104 µg/ml ethanolic bark extract was performed. Counts were made after 72 hours. Three trials in triplicates were performed.Nine (9) dilutions of extract were then tested (18.8 to 5,00 µg/ml). Test tubes were checked for viable amoeba after 24-hour and 72-hour incubation. Minimum inhibitory concentrations (MIC) were determined for the two incubation periods. At least two trials in triplicates for each dilution were performed. metronidazole served as positive control.RESULTS: At 104 µg/ml incubated for 72 hours, no viable amoeba was obtained and counted. The MIC after 24 hours was 5,000 µg/ml, while the MIC at 72 hours was 37.5 µg/ml.CONCLUSION: Q. amara crude extract has inhibitory effects on E. histolycain vitro.

In vitro antimicrobial assessment of Cuban propolis extracts

Propolis is a resinous mixture of different plant exudates collected by honeybees. Currently, propolis is widely used as a food supplement and in folk medicine. We have evaluated 20 Cuban propolis extracts of different chemical types, brown (BCP), red and yellow (YCP), with respect to their in vitro antibacterial, antifungal and antiprotozoal properties. The extracts inhibited the growth of Staphylococcus aureus and Trichophyton rubrum at low µg/mL concentrations, whereas they were not active against Escherichia coli and Candida albicans. The major activity of the extracts was found against the protozoa Leishmania, Trypanosoma and Plasmodium, although cytotoxicity against MRC-5 cells was also observed. The BCP-3, YCP-39 and YCP-60 extracts showed the highest activity against P. falciparum, with 50% of microbial growth (IC50) values of 0.2 µg/mL. A positive correlation between the biological activity and the chemical composition was observed for YCP extracts. The most promising antimicrobial activity corresponds to YCP subtype B, which contains acetyl triterpenes as the main constituents. The present in vitro study highlights the potential of propolis against protozoa, but further research is needed to increase selectivity towards the parasite. The observed chemical composition-activity relationship of propolis can contribute to the identification of the active principles and standardisation of this bee product.

Chemical constituents of the volatile oil from leaves of Annona coriacea and in vitro antiprotozoal activity

The essential oil of the leaves from Annona coriacea Mart., Annonaceae, was extracted by hydrodistillation in a Clevenger apparatus and analyzed by GC/MS and GC/FID. The oil yield was 0.05 percent m/m. Sixty compounds were identified, in a complex mixture of sesquiterpenes (76.7 percent), monoterpenes (20.0 percent) and other constituents (3.3 percent). Bicyclogermacrene was its major compound (39.8 percent) followed by other sesquiterpenes. Most of the monoterpenes were in low concentration (<1 percent). Only β-pinene and pseudolimonene presented the highest level of 1.6 percent. The volatile oil presented anti-leishmanial and trypanocidal activity against promastigotes of four species of Leishmania and trypomastigotes of Trypanosoma cruzi, showing to be more active against Leishmania (L.) chagasi (IC50 39.93 µ g/mL) (95 percent CI 28.00-56.95 µ g/mL).

In vitro antimalarial activity and cytotoxicity of some selected cuban medicinal plants / Actividad antimalárica in vitro y citotoxicidad de algunas plantas medicinales Cubanas seleccionadas

Terrestrial plants have been demonstrated to be sources of antimalarial compounds. In Cuba, little is known about antimalarial potentials of plant species used as medicinals. For that reason, we evaluated the antimalarial activity of 14 plant species used in Cuba as antimalarial, antipyretic and/or antiparasitic. Hydroalcoholic extracts were prepared and tested in vitro for the antimalarial activity against Plasmodium falciparum Ghana strain and over human cell line MRC-5 to determine cytotoxicity. Parasite multiplication was determined microscopically by the direct count of Giemsa stained parasites. A colorimetric assay was used to quantify cytotoxicity. Nine extracts showed IC50 values lower than 100 µg/mL against P. falciparum, four extracts were classified as marginally active (SI < 4), one as partially active (Parthenium hysterophorus) exhibiting SI equal to 6.2 and two extracts as active (Bambusa vulgaris and Punica granatum), showing SI > 10. B. vulgaris showed the most potent and specific antiplasmodial action (IC50 = 4.7 µg/mL, SI = 28.9). Phytochemical characterization of active extracts confirmed the presence of triterpenoids in B. vulgaris and polar compounds with phenol free groups and fluorescent metabolites in both extracts as major phytocompounds, by thin layer chromatography. In conclusion, antimalarial use of B. vulgaris and P. hysterophorus was validated. B. vulgaris and P. granatum extracts were selected for follow-up because of their strong antimalarial activity.

Las plantas terrestres han demostrado ser fuentes de compuestos antimaláricos. En Cuba, el conocimiento sobre el potencial antimalárico de las plantas medicinales es escaso. Por esta razón, evaluamos la actividad antimalárica de 14 especies de plantas usadas en Cuba como antimaláricas, antipiréticas y/o antiparasitarias. Se prepararon extractos hidroalcohólicos y se probaron in vitro frente a la cepa Ghana de Plasmodium falciparum para la actividad antimalárica y frente a la línea celular humana MRC-5 para determinar citotoxicidad. La multiplicación de los parásitos se determinó microscópicamente mediante el conteo directo de los parásitos teñidos con Giemsa. Un ensayo colorimétrico se utilizó para cuantificar la citotoxicidad. Nueve extractos mostraron valores de CI50 frente a Plasmodium falciparum por debajo de 100 µg/mL; cuatro extractos se clasificaron como marginalmente activos (IS < 4), uno parcialmente activo (Parthenium hysterophorus) exhibiendo IS de 6.2 y dos activos (Bambusa vulgaris y Punica granatum) mostrando IS>10. B. vulgaris, mostró la acción más potente y específica (CI50 = 4,7 µg/mL, IS = 28,9). La caracterización fitoquímica de los extractos más activos; confirmó la presencia de triterpenoides en B. vulgaris y de compuestos polares con grupos fenólicos libres y metabolitos fluorescentes en ambos extractos como fitocompuestos principales mediante cromatografía en capa delgada. En conclusión, se validó el uso antimalárico de B. vulgaris y P. hysterophorus. Los extractos de B. vulgaris y P. granatum se seleccionaron para seguimiento por su potente actividad antimalárica.

Parasitoses intestinais: uma revisão sobre seus aspectos sociais, epidemiológicos, clínicos e terapêuticos / Intestinal parasitic diseases: a review of social, epidemiologic, clinical and therapeutic aspects

No presente estudo, as enteroparasitoses mais prevalentes no Brasil foram avaliadas segundo determinantes sociais,aspectos epidemiológicos, clínicos e terapêuticos. Através de breve revisão de literatura e com base nos resultadosde estudos de prevalência, são sintetizados achados que corroboram a associação de sua alta prevalência à pobrezae ao subdesenvolvimento. Foi dedicada especial atenção adoenças tais como a esquistossomose, a giardíase, a ancilostomíase,a amebíase, a estrongiloidíase, a ascaridíase e ateníase. Também estão sumarizadas referências às principaisdrogas antiparasitárias, modo de ação, efeitos adversose avaliação da eficácia de cada tratamento. Destaca-se aimportante atualização dos profissionais da atenção primária nesse assunto e o reconhecimento de que esforços são necessários para maximizar os benefícios adquiridos com o tratamento medicamentoso e manter a qualidadeda saúde da população através da melhoria das condiçõesde saneamento e educação em saúde.

In the present study, the most prevalent enteroparasitosisin Brazil were assessed according to social, epidemiologic,clinical and therapeutic aspects. Through a brief review of the literature, and based on the results of several prevalence studies, high prevalence rates associated with povertyin under developed nations were found and stressed inthe article. Diseases such as schistosomiasis, giardiasis,ancylostomiasis, strongyloidiasis, ascaridiasis and taeniasiswere given more emphasis. There are also references to themain antiparasitc drugs and to their mechanism of action,adverse effects, and efficacy. Primary health care professional smust keep abreast of this subject, and be able toacknowledge that efforts are necessary in order to maximize the benefits of drug treatment and maintain the quality of health of the population, through the improvement of sanitary conditions and health education.

Leishmanicidal activity of Echinaster (Othilia) echinophorus crude extract / Atividade leishmanicida do extrato de Echinaster (Othilia) echinophorus

In this study, a methanolic extract from Echinaster (Othilia) echinophorus was evaluated for activity against Leishmania amazonensis. The extract showed activity against the promastigote and amastigote forms with IC50 values of 62.9 and 37.5 μg.mL-1 respectively. This extract showed a moderate toxicity on macrophages from BALB/c mice. A dose of 100 mg/kg/day was effective when administered during 15 days by intraperitoneal route to BALB/c mice infected experimentally.

Neste estudo descreve-se o efeito de um extrato metanólico de Echinaster echinophorus spp. no parasita Leishmania amazonensis. Em testes com as formas promastigotas e amastigotas, o IC50 do extrato foi 62,9 e 37,5 μg.mL-1, respectivamente. O extrato também tem toxicidade moderada em macrófagos de camundongos BALB/c. O tratamento de camundongos BALB/c infectados com L. amazonensis com doses diárias de 100 mg/kg/dia via intraperitoneal durante 15 dias mostrou-se relativamente efetivo no controle da infecção. Esta investigação confirma a importância de produtos naturais como fonte para a descoberta de fármacos com funções anti-Leishmania.

Trypanocidal activity of Piper arboreum and Piper tuberculatum (Piperaceae) / Atividade tripanocida de Piper arboreum e Piper tuberculatum (Piperaceae)

No escopo de nossas pesquisas sobre agentes bioativos da flora brasileira, vinte e quatro extratos e frações de Piper arboreum Aub. e Piper tuberculatum Jacq. (Piperaceae) tiveram sua atividade tripanocida avaliada através do ensaio colorimétrico com MTT. As atividades mais potentes foram manifestadas pelas frações hexânicas das folhas de P. arboreum (CI50 = 13,3 µg/mL) e P. tuberculatum (CI50 = 17,2 µg/mL). As frações hexânicas dos frutos de P. tuberculatum e P. arboreum também apresentaram efeito tóxico potente contra as formas epimastigotas de Trypanosoma cruzi, com valores de CI50 (µg/mL) de 32,2 e 31,3, respectivamente. Adicionalmente, o estudo fitoquímico da fração hexânica das folhas de P. arboreum forneceu duas amidas pirrolidínicas, piperilina (1) e 4,5-diidropiperilina (2), que podem ser responsáveis pela atividade antiprotozoária desta fração.

In the scope of our ongoing research on bioactive agents from Brazilian flora, twenty-four extracts and fractions obtained from Piper arboreum Aub. and Piper tuberculatum Jacq. (Piperaceae) were screened for trypanocidal activity by using MTT colorimetric assay. The strongest activity was found in hexane fractions from the leaves of P. arboreum (IC50= 13.3 µg/ mL) and P. tuberculatum (IC50 = 17.2 µg/mL). Hexane fractions of the fruits of P. tuberculatum and P. arboreum showed potent toxic effects on epimastigote forms of Trypanosoma cruzi, with values of IC50 (µg/mL) of 32.2 and 31.3, respectively. Additionally, the phytochemical study of the hexane fraction of P. arboreum leaves furnished two pyrrolidine amides, piperyline (1) and 4,5-dihydropiperyline (2), which could be responsible, at least in part for the observed antiprotozoal activity.

Búsqueda de nuevos agentes antiprotozoarios selectivos / In search of new selective antiprotozoal agents

Se da la información general sobre los fármacos antiprotozoarios que están usándose en clínica, se discuten nuevas dianas de los parásitos protozoarios útiles en la búsqueda de nuevos agentes antiprotozoarios, enfocando la atención al rol biológico de las proteasas de los parásitos protozoarios. Esta información importante será útil para los estudiantes e investigadores que se interesen a los problemas de química medicinal (un área naciente en Colombia) cuál aporta mucho al desarrollo de ciencias médicas. [Kouznetsov V, Meléndez C. Búsqueda de nueveos agentes antiprotozoarios selectivos. MedUNAB 2009; 12:33-45].

The information is given on the antiprotozoal drugs used in clinic, new useful targets of the parasites protozoa in the search of new antiprotozoal agents are discussed, focusing the attention to the biological role of proteasas of the parasites protozoa. This important information will be useful for students and researchers, which are interested in the problems of medicinal chemistry (an appearing area in Colombia) that gives much to the development of medicine sciences. [Kouznetsov V, Meléndez C. In search of new selective antiprotozoal agents. MedUNAB 2009; 12:33-45].