Ethnopharmacological Characteristics of Pycnanthus angolensis (Welw.) Warb. (Myristicaceae), a Plant Used in the Traditional Treatment of Viral and Parasitic Diseases

Background: Pycnanthus angolensis (Welw.) Warb. (Myristicaceae) is a medicinal plant used in traditional Ivorian medicine. A recent ethnobotanical survey has discovered Pycnanthus angolensis in the traditional treatment of viral and parasitic diseases. Aim: The present study aims to highlight the distinctive ethnopharmacological characteristics of Pycnanthus angolensis. Methods: The aim was to identify some groups of chemical compounds by thin layer chromatography, to assay some minerals and finally to characterise the specific anatomical and micrographic features of the plant. Results: Terpenes and sterols, saponosides, flavonoids and tannins are the main phytocompounds revealed. Magnesium with 621.3 mg/100 g dry matter is the most abundant mineral. Anatomical sections and plant powder revealed starch grains, calcium oxalate crystals, secretory pockets and tector hairs that are responsible for the formation of various biological substances in the plant. Conclusion: These results add to the data on Pycnanthus angolensis, a taxon much used in traditional Ivorian medicine for the treatment of antiparasitic and antiviral diseases.

Amoebicidal and trichomonicidal capacity of polymeric nanoparticles loaded with extracts of the plants Curcuma longa (Zingiberaceae) and Berberis vulgaris (Berberidaceae) / Capacidad amebicida y tricomonicida de nanopartículas poliméricas cargadas con extractos de las plantas Curcuma longa (Zingiberaceae) y Berberis vulgaris (Berberidaceae)

Abstract Introduction: Pathogenic protozoans, like Entamoeba histolytica and Trichomonas vaginalis, represent a major health problem in tropical countries; and polymeric nanoparticles could be used to apply plant extracts against those parasites. Objective: To test Curcuma longa ethanolic extract and Berberis vulgaris methanolic extracts, and their main constituents, against two species of protozoans. Methods: We tested the extracts, as well as their main constituents, curcumin (Cur) and berberine (Ber), both non-encapsulated and encapsulated in polymeric nanoparticles (NPs), in vitro. We also determined nanoparticle characteristics by photon correlation spectroscopy and scanning electron microscopy, and hemolytic capacity by hemolysis in healthy erythrocytes. Results: C. longa consisted mainly of tannins, phenols, and flavonoids; and B. vulgaris in alkaloids. Encapsulated particles were more effective (P < 0.001); however, curcumin and berberine nanoparticles were the most effective treatments. CurNPs had IC50 values (µg/mL) of 9.48 and 4.25, against E. histolytica and T. vaginalis, respectively, and BerNPs 0.24 and 0.71. The particle size and encapsulation percentage for CurNPs and BerNPs were 66.5 and 73.4 nm, and 83.59 and 76.48 %, respectively. The NPs were spherical and significantly reduced hemolysis when compared to non-encapsulated extracts. Conclusions: NPs represent a useful and novel bioactive compound delivery system for therapy in diseases caused by protozoans.

Resumen Introducción: Los protozoos patógenos, como Entamoeba histolytica y Trichomonas vaginalis, representan un importante problema de salud en los países tropicales; y se podrían usar nanopartículas poliméricas para aplicar extractos de plantas contra esos parásitos. Objetivo: Probar los extractos etanólicos de Curcuma longa y Berberis vulgaris, y sus principales constituyentes, contra dos especies de protozoos. Métodos: Probamos los extractos, así como sus principales constituyentes, curcumina (Cur) y berberina (Ber), tanto no encapsulados como encapsulados en nanopartículas poliméricas (NPs), in vitro. También determinamos las características de las nanopartículas por espectroscopía de correlación de fotones y microscopía electrónica de barrido, y la capacidad hemolítica por hemólisis en eritrocitos sanos. Resultados: C. longa tenía principalmente: taninos, fenoles y flavonoides; y B. vulgaris, alcaloides. Las partículas encapsuladas fueron más efectivas (P < 0.001); sin embargo, las nanopartículas de curcumina y berberina fueron los tratamientos más efectivos. CurNPs tenía valores IC50 (µg/mL) de 9.48 y 4.25, contra E. histolytica y T. vaginalis, respectivamente, y BerNPs 0.24 y 0.71. El tamaño de partícula y el porcentaje de encapsulación para CurNPs y BerNPs fueron: 66.5 y 73.4 nm, y 83.59 y 76.48 %, respectivamente. Los NP son esféricos y redujeron significativamente la hemólisis en comparación con los extractos no encapsulados. Conclusiones: Las NP representan un sistema de administración de compuestos bioactivos útil y novedoso para la terapia enfermedades causadas por protozoos.

Practices employed by veterinary practitioners for controlling canine gastrointestinal helminths and ectoparasites / Práticas realizadas por veterinários para controle de helmintos gastrintestinais e ectoparasitos de cães

Abstract The present study attempted to evaluate the practical experience and methods employed by Brazilian veterinary practitioners for control of parasites. Twenty-one questions were asked of 403 veterinary practitioners based in different climatic zones with reference to parasite epidemiology from the country. Administration of a combination of drugs at three-month intervals was the most common regime recommended for prophylaxis against gastrointestinal helminths, with a single treatment repeated after 15 days. Routine prophylaxis against dog ectoparasites was recommended by 82.4% veterinary practitioners, and 46.6% changed the drug compound used. Monthly prophylaxic treatments for ectoparasites, using systemic, topical and/or collar-impregnated drugs, was recommended by 21.5% veterinary practitioners. Side-effects of ectoparasiticide-impregnated collars were suspected by 58% of the veterinary practitioners. Isoxazolines were the most frequently used chemical group to treat ectoparasites in dogs. Poor efficacy of fipronil in controlling ticks was suspected by 79.5% of the veterinary practitioners. The isoxazolines and combination of anthelmintic compounds are the most common drugs to prevent or treat ectoparasites and gastrointestinal nematodes, respectively. The suspect of the inefficacy of antiparasitic drugs is shared among the veterinary practitioners from part of Brazil. Guidelines are needed, specifically for the control of gastrointestinal helminths and ectoparasites in Brazilian dogs.

Resumo O presente estudo avaliou os métodos de controle empregados por médicos veterinários clínicos para o controle de parasitos de cães no Brasil. Vinte e uma perguntas foram feitas a 403 veterinários de diferentes regiões do país. O uso de associações de compostos ativos em intervalos de três meses foi o mais recomendado para profilaxia de helmintos gastrointestinais, repetido após 15 dias. A profilaxia de rotina contra ectoparasitos foi recomendada por 82,4% dos veterinários, e 46,6% mudam rotineiramente o composto indicado. Tratamentos profiláticos mensais para ectoparasitos, com produtos sistêmicos, tópicos e / ou impregnados com colar, foram recomendados por 21,5% dos veterinários. Os efeitos colaterais das coleiras impregnadas com ectoparasiticidas foram relatados por 58% dos médicos veterinários. As isoxazolinas foram o grupo químico mais utilizado para tratar ectoparasitos em cães. A baixa eficácia do fipronil no controle de carrapatos foi suspeitada por 79,5% dos médicos veterinários. As isoxazolinas e a associação de compostos anti-helmínticos são os medicamentos mais comuns para prevenir ou tratar ectoparasitos e nematoides gastrointestinais, respectivamente. A suspeita da ineficácia dos antiparasitários é compartilhada entre os médicos veterinários de algumas regiões do Brasil. Orientações são necessárias, especificamente para o controle de helmintos e ectoparasitos gastrointestinais em cães no Brasil.

Anthelmintic effect of four extracts obtained from Caesalpinia coriaria foliage against the eggs and larvae of Haemonchus contortus / Efeito anti-helmíntico de quatro extratos obtidos da folha de Caesalpinia coriaria contra ovos e larvas de Haemonchus contortus

Abstract To investigate the in vitro anthelmintic efficacy of dividivi (Caesalpinia coriaria), a traditional medicinal plant used in Central America and the northern part of South America, extracts from the foliage of this plant were subjected to the egg hatching test (EHT) and larval exsheathment inhibition test (LEIT), against Haemonchus contortus. Four different extracts were evaluated: acetone-water (AW), methanol-water (MW), acetone-water-dichloromethane (AWD) and methanol-water-dichloromethane (MWD). The concentrations used for the EHT and LEIT tests ranged from 500 to 4000 µg mL-1 and six repetitions per concentration. The effective concentrations (EC50) were calculated using Probit analysis. The EC50 for EHT were 2947.0, 3347.0, 3959.6 and 4538.7 µg mL-1 for MWD, MW, AW and AWD, respectively. The EC50 for LEIT were 2883.4, 5927.4, 9876.3 and 9955.4 µg mL-1 for AWD, AW, MWD and MW, respectively. The methanol extracts were the most effective in inhibiting the hatching of eggs, while the acetone extracts showed efficacy in inhibiting larval exsheathment. This study explains the importance that C. coriaria has as a medicinal plant in Central and South American countries.

Resumo Para investigar a eficácia anti-helmíntica de Divi-divi (Caesalpinia coriaria), uma planta medicinal tradicional usada na América Central e no norte da América do Sul. Extratos das folhas dessa planta foram utilizados em testes in vitro de inibição da eclosão de ovos (EHT) e desembainhamento larvar (LEIT) de Haemonchus contortus. Quatro diferentes extratos foram avaliados: acetona-água (AW), metanol-água (MW), acetona-água-diclorometano (AWD) e metanol-água-diclorometano (MWD). Para os testes EHT e LEIT, as concentrações utilizadas variaram de 500 a 4000 µg mL-1, em seis repetições por concentração. As concentrações efetivas (EC50) foram calculadas, usando-se a análise Probit. A EC50 para EHT foram 2947,0; 3347,0; 3959,6 e 4538,7 µg mL-1 para MWD, MW, AW e AWD, respectivamente. As EC50 para LEIT foram 2883,4; 5927,4; 9876,3 e 9955,4 µg mL-1 para AWD, AW, MWD e MW, respectivamente. Os extratos de metanol foram os mais eficazes em inibir a eclosão de ovos, enquanto os extratos de acetona mostraram-se eficazes em inibir a desembainhamento larvar. Este estudo ajuda a explicar a importância da C. coriaria como planta medicinal nos países da América Central e América do Sul.

Nitazoxanida para o tratamento de COVID-19 / Nitazoxanide for or COVID-19 treatment

CONTEXTO: A COVID-19 é uma pandemia de risco muito alto a nível global pela OMS. Até o momento não existem terapias específicas, embora diferentes tratamentos estejam em investigação. Mais recentemente, tem havido crescente interesse no uso da nitazoxanida no tratamento de COVID-19, dada sua atividade antiviral de amplo espectro. OBJETIVOS: Identificar, avaliar sistematicamente e sumarizar as melhores evidências científicas disponíveis sobre a eficácia e a segurança da nitazoxanida para COVID-19. MÉTODOS: Revisão sistemática rápida (rapid review methodology). RESULTADOS: Após o processo de seleção, foram avaliados cinco estudos clínicos em andamento. CONCLUSÃO: Cinco estudos com o objetivo de avaliar a eficácia e segurança da nitazoxanida no tratamento de COVID-19 estão em andamento. Devido à ausência de evidência sobre o uso deste medicamento para o tratamento de infecções por coronavírus que causem infecções respiratórias, não é possível recomendar seu uso como terapia para COVID-19.(AU)

Berberina, curcumina y quercetina como potenciales agentes con capacidad antiparasitaria / Berberine, curcumin and quercetin as potential antiparasitic agents

Introducción: El uso indiscriminado de agentes antiparasitarios ha resultado en el establecimiento de resistencia a ellos. Por lo cual es necesario el desarrollo de nuevas alternativas de tratamiento. Los productos naturales poseen diversas cualidades como posibles coadyuvantes en terapias contra distintos agentes etiológicos, entre los que destaca sus efectos antiparasitarios. Objetivo: Evaluar la actividad antiparasitaria, antioxidante, citotóxica y citoprotectora de Berberina (Ber), Curcumina (Cur) y Quercetina (Qr). Metodología: Se prepararon soluciones de Ber, Cur y Qr grado analítico y se realizaron alícuotas a diferentes concentraciones para su evaluación en contra de: Entamoeba histolytica, Trichomonas vaginalis y Strongyloides venezuelensis, paraello, se determinó la concentración inhibitoria media (IC50), además se determinó la capacidad antioxidante (CE50) mediante la prueba de DPPH, ambos por la prueba de Probit. Mediante la técnica de hemólisis se determinó la actividad citotóxica y citoprotectora, se aplicó Anova y la prueba de Tukey para determinar la diferencia de las medias en los tratamientos evaluados. Resultados: Ber, Cur y Qr, presentaron actividad en contra de E. histolytica, T. vaginalis y S. venezuelensis in-vitro. Ber presentó IC50 de 1.7, 1.2 y 1.9 μM respectivamente siendo más efectivo en comparación de Cur con IC50 de 55.3, 40.6 y 13.7 μM o Qr con IC50 de 147.2, 93.2 y 110.9 μM, sin embargo, la mejor actividad antioxidante (EC50 = 1.1 μg/ml), citoprotectora y menos hemolítica, fue presentada por Qr (P < 0.001) en comparación con el control evaluado. Conclusiones: Los metabolitos de origen natural berberina, curcumina y quercetina, poseen actividad en contra de trofozoítos de E. histolytica, T. vaginalisy larvas de S. venezuelensis en dosis bajas comparables con los fármacos de referencia para el caso de Ber. Además, estos productos de origen natural, no sintético podrían ser objeto de futuras investigaciones para coadyuvar al tratamiento de parasitosis, ya que, en dosis bajas, mostraron actividad antioxidante sin mostrar hemólisis considerable en eritrocitos humanos.

Introduction: The indiscriminate use of antiparasitic agents has resulted in the establishment of resistance to them. Therefore, the development of new treatment alternatives is necessary. Natural products have various qualities as possible adjuvants in therapies against different etiological agents, among which its antiparasitic effects stand out. Objective: To evaluate the antiparasitic, antioxidant, cytotoxic, and cytoprotective activity of Berberine (Ber), Curcumin (Cur), and Quercetin (Qr). Methods: Analytical grade Ber, Cur, and Qr solutions were prepared, and aliquots were made at different concentrations for their evaluation against Entamoeba histolytica, Trichomonas vaginalis, and Strongyloides venezuelensis. To do this, the mean inhibitory concentration (IC50) was determined, and the antioxidant capacity (EC50) was also determined by the DPPH assay, both using the Probit statistical test. The cytotoxic and cytoprotective activity was determined by the hemolysis technique, Anova and Tukey's test were applied to determine the difference in the means in the treatments evaluated. Results: Ber, Cur, and Qr, showed activity against E. histolytica, T. vaginalis, and S. venezuelensisin-vitro. Ber presented IC50 of 1.7, 1.2, and 1.9 μM respectively, being more effective compared to Cur with IC50 of 55.3, 40.6, and 13.7 μM, or Qr with IC50 of 147.2, 93.2, and 110.9 μM, however, the best antioxidant activity (EC50 = 1.1 μg/ml), cytoprotective and less hemolytic, was presented by Qr (P < 0.001) compared to the evaluated control. Conclusions: The metabolites of natural origin berberine, curcumin, and quercetin, have activity against trophozoites of E. histolytica, T. vaginalis and larvae of S. venezuelensis in low doses comparable to the reference drugs in the case of Ber. Furthermore, these non-synthetic products of natural origin could be the subject of future research to help treat parasitosis, since in low doses, they showed antioxidant activity without showing considerable cytotoxicity in human erythrocytes.

Anti-microsporidial effect of thymoquinone on Encephalitozoon intestinalis infection in vitro

To evaluate the anti-microsporidial effects of the active component of Nigella sativa seeds, thymoquinone, against Encephalitozoon intestinalis using an in vitro model. Methods: Anti-microsporidial effect of thymoquinone against Encephalitozoon intestinalis was evaluated by using various concentrations of thymoquinone (0, 1, 5, 10, 15, 20, 30, 35, and 40 uM) and sterile dimethyl sulfoxide. Real time PCR was used to evaluate the inhibitory effects of thymoquinone on the life cycle of Encephalitozoon intestinalis. Results: The cytotoxic effect of thymoquinone on HEK293 cell line was observed with 30, 35, and 40 uM concentrations of thymoquinone after 24, 48, and 72 hours of incubation. It was observed that 10, 15, 20, and 30 uM concentrations of thymoquinone decreased the spore density compared with the control; however, it was significant only at 30 uM. Conclusions: Thymoquinone shows potent anti-microsporidial effects against Encephalitozoon intestinalis in the in vitro model; however, the toxic concentrations of thymoquinone are also toxic to the host cells.

Anti-microsporidial effect of thymoquinone on Encephalitozoon intestinalis infection in vitro

Objective: To evaluate the anti-microsporidial effects of the active component of Nigella sativa seeds, thymoquinone, against Encephalitozoon intestinalis using an in vitro model. Methods: Anti-microsporidial effect of thymoquinone against Encephalitozoon intestinalis was evaluated by using various concentrations of thymoquinone (0, 1, 5, 10, 15, 20, 30, 35, and 40 μM) and sterile dimethyl sulfoxide. Real time PCR was used to evaluate the inhibitory effects of thymoquinone on the life cycle of Encephalitozoon intestinalis. Results: The cytotoxic effect of thymoquinone on HEK293 cell line was observed with 30, 35, and 40 μM concentrations of thymoquinone after 24, 48, and 72 hours of incubation. It was observed that 10, 15, 20, and 30 μM concentrations of thymoquinone decreased the spore density compared with the control; however, it was significant only at 30 μM. Conclusions: Thymoquinone shows potent anti-microsporidial effects against Encephalitozoon intestinalis in the in vitro model;however, the toxic concentrations of thymoquinone are also toxic to the host cells.

Presence of benznidazole conjugated metabolites in urine identified by β-glucuronidase treatment

Chagas disease is a serious public health problem in Latin America and, due to migration, in other non-endemic regions. Benznidazole (BNZ) is first choice drug in pediatric therapeutics. However, little is known regarding its metabolism in humans. The aim of the study was to isolate and identify products of human BZN metabolism in urine samples obtained from a pediatric Chagas patient and a healthy adult volunteer both treated with BZN. Urine samples were collected after dose of BNZ. Urine was treated with β-glucuronidase followed by an extraction procedure under two different pH conditions and a HPLC/UV and MS/MS identification of BZN and its metabolites. BZN (m/z 260.09847) was identified in all urine extracts. Peaks from each extracted chromatograms were selected for MS and MS/MS identification. Three compounds structurally related to BZN were identified: BZN-Na+ (m/z 283.08009), N-amine-BZN (m/z 230.12307) and N-hydroxi-amine-BZN (m/z 246.11702). BNZ-Na+ was identified in all extracts, but N-amine-BZN and N-hydroxi-amine-BZN were only observed in those extracts treated with β-glucuronidase. This is the first experimental report showing elimination of BZN N-reduced metabolites in urine. As they were released after treatment with β-glucuronidase it can be suggested that glucuronization plays a role in BNZ metabolism and renal elimination.

Estudo comparativo da ação sanitizantes de uso caseiros em hortaliças contaminadas com Ancilostomídeos / Comparative sanitizers study of domestic aplication in vegetables contaminated with hookworms / Estudio comparativo de la acción higiénica de los cuidadores en vegetales contaminados con anquilostomas

Objetivo: O presente trabalho tem como objetivo verificar a efetividade de sanitizantes de uso caseiros quanto a capacidade de paralisar e desinfetar larvas de Ancilostomídeos. Método Para obtenção das larvas de Ancilostomídeos foi utilizado o método de Hoffman, Pons e Janer (HPJ). Em seguida, foram preparadas lâminas com o sedimento e adicionou-se concentrações diferentes de saneantes empregados na rotina doméstica. Simultaneamente, foi avaliado, através de microscopia óptica, o tempo cronometrado que cada saneante em diferentes concentrações, necessitaria para paralisação completa do helminto. Resultados: O ácido acético e o hipoclorito não apresentaram efetividade em nenhuma das concentrações testadas. Já o vinagre de álcool puro na diluição de 40% paralisou 90% das larvas em um período de 14 minutos e 31 segundos. O vinagre composto de álcool, na concentração de 40% foi capaz de paralisar mais de 90% das larvas em um tempo médio de 9 minutos e 50 segundos. Conclusão: A utilização de 40% de sanitizantes de vinagre se mostraram eficazes na desinfecção de larvas de Ancilostomídeos. No entanto, este estudo alerta que a eliminação de larvas não é segura quando se leva em conta a concentração usada na rotina doméstica atual.

Objective: The present work aims to verify the effectiveness of homemade sanitizers for the ability to paralyze and disinfect hookworm larvae. Method: To obtain hookworm larvae, the method of Hoffman, Pons, and Janer (HPJ) was applied. The next slides were prepared with the sediment, and different sanitizing concentrations, routinely used in the domestic, were added. Simultaneously, we evaluated, by optical microscopy, the chronometer time that each sanitizer in different concentrations, would require for complete helminth paralysis. Results: Acetic acid and hypochlorite were not effective in any of the tested concentrations. Pure alcohol vinegar in the 40% dilution paralyzed 90% of the larvae in 14 minutes and 31 seconds. The vinegar composed of alcohol, in the 40% concentration, was able to paralyze more than 90% of the larvae in an 9,50 minutes average. Conclusion: The use of 40% of vinegar sanitizers proved to be useful in disinfecting hookworms larvae. However, this study cautions that larvae elimination is not safe when taking into account the concentration handled in the current domestic routine.

Objetivo: el presente trabajo tiene como objetivo verificar la efectividad de los desinfectantes caseros para la capacidad de paralizar y desinfectar larvas de anquilostomas. Método: para obtener larvas de anquilostomas, se utilizó el método de Hoffman, Pons y Janer (HPJ). Luego se prepararon los portaobjetos con el sedimento y se agregaron diferentes concentraciones de agentes desinfectantes utilizados en la rutina doméstica. Simultáneamente, se evaluó, usando microscopía óptica, el tiempo cronometrado que cada desinfectante en diferentes concentraciones necesitaría para completar la parálisis del helminto. Resultados: el ácido acético y el hipoclorito no fueron efectivos en ninguna de las concentraciones probadas. El vinagre puro de alcohol en la dilución al 40% paralizó el 90% de las larvas en un período de 14 minutos y 31 segundos. El vinagre compuesto de alcohol, en la concentración del 40%, fue capaz de paralizar más del 90% de las larvas en un tiempo promedio de 9 minutos y 50 segundos. Conclusión: el uso del 40% de desinfectantes de vinagre demostró ser eficaz para desinfectar larvas de anquilostomas. Sin embargo, este estudio advierte que la eliminación de las larvas no es segura cuando se tiene en cuenta la concentración utilizada en la rutina doméstica actual.

Activity of Piperaceae extracts and fractions in the control of Phytomonas serpens / Atividade de extratos e frações de Piperaceae no controle de Phytomonas serpens

ABSTRACT: Protozoa of the genus Phytomonas are harmful parasites to several agricultural crops of economic importance. Due to their recognized biological activity, crude extracts of Piper aduncum, P. crassinervium, P. hispidum, and P. amalago leaves, were tested using the microdilution plate technique to assess the antiparasitic potential against Phytomonas serpens. Results showed that the ethanolic crude extract of P. crassinervium and P. amalago presented the best inhibitory concentration for 50% of the cells (IC50), 16.5 µg mL-1 in chloroform phase, and 18 µg mL-1 in aqueous phase, respectively, after 48 h treatment. Cytotoxicity analyses were performed using the colorimetric method of sulforhodamine-B in LLCMK2 mammalian cells. The chloroform phase of P. crassinervium was subjected to the fractionation process, in which the ethyl acetate and dichloromethane fractions obtained better IC50 values. Scanning electron microscopy (SEM) images showed alterations in the cell membrane of the treated parasites. The data obtained indicate a potential antiparasitic effect of the Piper species analyzed against P. serpens, being considered promising candidates for formulations of bioproducts to control the parasite.

RESUMO: Protozoários do gênero Phytomonas são parasitas prejudiciais a várias culturas agrícolas de importância econômica. Devido a sua atividade biológica reconhecida, extratos brutos de folhas de Piper aduncum, P. crassinervium, P. hispidum e P. amalago, foram testadas pela técnica de microdiluição em placa para avaliar o seu potencial antiparasitário contra Phytomonas serpens. Os resultados mostraram que o extrato bruto etanólico de P. crassinervium e P. amalago apresentaram as melhores concentrações inibitórias para 50% das células (IC50), 16,5 µg mL-1 na fase clorofórmio e 18 µg mL-1 na fase aquosa, respectivamente, após 48 h de tratamento. Análises de citotoxicidade foram realizadas através do método colorimétrico da sulforodamina-B, em células de mamíferos LLCMK2. A fase clorofórmio de P. crassinervium foi submetida ao processo de fracionamento, no qual as frações acetato de etila e diclorometano obtiveram melhores valores de IC50. Imagens de microscopia eletrônica de varredura (MEV) mostraram alterações na membrana celular dos parasitas tratados com fase aquosa de P. amalago. Os dados obtidos indicam potencial efeito antiparasitário das espécies de Piper analisadas contra P. serpens, sendo consideradas candidatas promissoras para formulações de bioprodutos para controle do parasito.

Chemical profiling, antibacterial and antiparasitic studies of Imperata cylindrica

Imperata cylindrica is a common grass with little known medicinal properties. The underground part (comprising rhizome with roots) is used by the Mizo people for the treatment of microbial and intestinal worm infections. To understand the chemical and pharmacological properties of the plant part, a methanol extract was prepared in a Soxhlet apparatus, and the extract was concentrated using a vacuum rotary evaporator. Chemical analysis was done using gas chromatography-mass spectrometry. Antibacterial activity was tested by Kirby–Bauer test and antiparasitic activity by survival test in vitro. Fourteen volatile compounds were detected; out of which the most abundant were n-hexadecanoic acid and (Z)-18-octadec-9-enolide. Some compounds detected including 2-methoxy-4-vinylphenol, 6-methylenebicyclo [3.2.0] hept-3-en-2-one and phenol,2,4-bis (1,1-dimethylethyl) are already known biologically active compounds. The plant extract was effective against all bacteria tested that included Gram-negative bacteria such as Pseudomonas aeruginosa and Klebsiella pneumoniae, and a Gram-positive bacterium Bacillus subtilis. It was also effective against two avian intestinal worms such as the tapeworm Raillietina echinobothrida and the roundworm Ascaridia galli. These findings reveal the importance of this plant as a source of therapeutic compounds.

Complete Resolution of Electrocardiographic Changes Induced by Acute Chagas Myocarditis

We present a case of a female adolescent with severe acute Chagas myocarditis, acquired by oral transmission in an endemic area in the Brazilian western Amazon, who had electrocardiographic changes normalized after empirical treatment with the antiparasitic drug benznidazole combined with conventional treatment for severe heart failure

Antiparasitic phytotherapy perspectives, scope and current development / Perspectivas, enfoque y actual desarrollo de la fitoterapia antiparasitaria

Tropical protozoan diseases are currently a major public health problem throughout the world and are strongly linked with poverty, this combined with a lack of commercial markets for potential drugs has created a large burden on the health and economic development of low-income and middle-income countries in Africa, Asia, and the Americas. Due to the low research interest and the high increase of resistance against the existing treatments, as well as increasing ineficiency, toxicity, prolonged treatment schedules and costs, there is an urgent need for cost-effective, safe and easy-to-administer, new effective compounds with novel mechanisms of action. Several studies of crude plant extracts have already identifed potential compounds to treat Chagas' disease, Leishmaniasis, Toxoplasmosis, Giardiasis, and Malaria among other protozoan parasites. Natural compounds of medicinal plants have shown lower toxicity together with higher specificity, creating an optimistic view of new treatments for diseases. Out of 1010 new active substances approved as drugs for medical conditions by regulatory agencies during the past 25 years, 490(48.5%) were from a natural origin.

Las enfermedades tropicales por protozoarios son un problema importante de salud pública en todo el mundo y están ligadas fuertemente con la pobreza. Esto lleva a que falte investigación por las empresas farmacéuticas con ánimo de lucro, que sólo se motivan por posibilidades de mercado. Adicionalmente el aumento en resistencia a los tratamientos disponibles, la toxicidad y la necesidad de largos periodos de tratamiento y los costos de muchos de ellos, hacen que exista una urgente necesidad de nuevos medicamentos costo efectivos, seguros y fáciles de administrar y que tengan mecanismos de acción novedosos. Varios extractos crudos de plantas han mostrado propiedades que permiten ser eficaces para tratar la enfermedad de Chagas, la leishmaniasis, la toxoplasmosis, la giardiasis y la malaria. Los compuestos derivados de plantas han mostrado menor toxicidad con mayor especificidad, mostrando un panorama optimista para encontrar nuevos medicamentos. Esto es evidente al analizar las cifras que muestran entre 1.010 nuevas sustancias activas aprobadas para condiciones médicas por las agencias regulatorias en los últimos 25 años, 490 (48,5%) son de origen natural.

A Review of Quercus infectoria (Olivier) Galls as a Resource for Anti-parasitic Agents: In Vitro and In Vivo Studies

@#Parasitic diseases represent one of the causes for significant global economic, environmental and public health impacts. The efficacy of currently available anti-parasitic drugs has been threatened by the emergence of single drug- or multidrug-resistant parasite populations, vector threats and high cost of drug development. Therefore, the discovery of more potent anti-parasitic drugs coming from medicinal plants such as Quercus infectoria is seen as a major approach to tackle the problem. A systematic review was conducted to assess the efficacy of Q. infectoria in treating parasitic diseases both in vitro and in vivo due to the lack of such reviews on the anti-parasitic activities of this plant. This review consisted of intensive searches from three databases including PubMed, Science Direct and Scopus. Articles were selected throughout the years, limited to English language and fully documented. A total of 454 potential articles were identified, but only four articles were accepted to be evaluated based on inclusion and exclusion criteria. Although there were insufficient pieces of evidence to account for the efficacy of Q. infectoria against the parasites, this plant appears to have anti-leishmanial, anti-blastocystis and anti-amoebic activities. More studies in vitro and in vivo are warranted to further validate the anti-parasitic efficacy of Q. infectoria.

Inclusion complexes and self-assembled cyclodextrin aggregates for increasing the solubility of benzimidazoles

Albendazole and fenbendazole are imidazole derivatives that exhibit broad spectrum activity against parasites, but the low solubility of these drugs considerably reduces their effectiveness. Complexation of albendazole and fenbendazole with cyclodextrins (ß-cyclodextrin and hydroxypropyl-ß-cyclodextrin) in both water and an aqueous solution of polyvinylpyrrolidone (PVP-k30) was studied to determine if it could increase the solubility and dissolution rate of the drugs. In an aqueous solution, ß-cyclodextrin increased the solubility of albendazole from 0.4188 to ~93.47 µg mL-1 (223×), and of fenbendazole from 0.1054 to 45.56 µg mL-1 (432×); hydroxypropyl-ß-cyclodextrin, on the other hand, increased solubility to ~443.06 µg mL-1 (1058×) for albendazole and ~159.36 µg mL-1 (1512×) for fenbendazole. The combination of hydroxypropyl-ß-cyclodextrin and polyvinylpyrrolidone enabled a solubility increase of 1412× (~591.22 µg mL-1) for albendazole and 1373× (~144.66 µg mL-1) for fenbendazole. The dissolution rate of the drugs was significantly increased in binary and ternary systems, with hydroxypropyl-ß-cyclodextrin proving to be more effective. The presence of the water-soluble PVP-k30 increased the dissolution rate and amorphization of the complexes. Analysis of the changes in displacement and the profile of the cyclodextrin bands in the 1H NMR spectra revealed a molecular interaction and pointed to an effective complexation in the drug/cyclodextrin systems. Monomeric forms and nanoclusters of cyclodextrins were observed in the drug/cyclodextrin systems, suggesting that the increase in solubility of the drugs in the presence of cyclodextrins should not be attributed only to the formation of inclusion complexes, but also to the formation of cyclodextrin aggregates

Resultados académicos en Farmacología de estudiantes de Enfermería Universidad Kmpa Vita. Uíge, Angola / Academic results in Pharmacology obtained by Nursing students. Kimpa Vita University. Uíge, Angola

Introducción: Los conocimientos en Farmacología tienen un lugar destacado en el ejercicio de la Enfermería. Es imprescindible que el estudiante de Enfermería en lo académico pueda asimilar todos los aspectos de la Farmacología durante la formación universitaria. Objetivo: Describir los resultados académicos en Farmacología de los estudiantes de Enfermería de la Universidad Kimpa Vita de Uíge en Angola. Materiales y Métodos: Estudio retrospectivo de los estudiantes de tercero, cuarto y quinto años de Licenciatura en Enfermería. La Farmacología se impartió por el programa de estudio de 2008 de Cuba, y se utilizó el sistema de evaluación establecido en Angola. Se revisaron las actas de examen y se aplicó una pregunta de respuesta simple para evaluar el nivel de conocimientos en el tema fármacos antimicrobianos y antiparasitarios. Resultados: Los resultados en Farmacología I fueron fundamentalmente:suficiente (74,83 por ciento), y en Farmacologia II: suficiente (61,57 por ciento) y bien (34,01 por ciento). Los resultados del tema evaluado fueron principalmente en los estudiantes de tercer año: suspensos (41,75 por ciento), cuarto año: suficiente (45,10 por ciento), y en quinto año: suficiente (32,58 por ciento) y bien (37,08 por ciento). Conclusiones: Los resultados en Farmacología se obtienen por el progreso en los métodos de estudio, la atencion individualizada al estudiante y la integración de sus contenidos en las disciplinas propias de la profesión(AU)

Introduction: The knowledge of Pharmacology has a significant importance in the practice of Nursing. It is indispensable that the Nursing student achieves the assimilation of knowledge of all the aspects of Pharmacology from the academic point of view during the university formation. Objectives: To describe the academic results in Pharmacology obtained by Nursing students of the Kimpa Vita University of Uíge in Angola. Materials and Methods: A retrospective study was carried out with third, fourth and fifth year Nursing students. Pharmacology was taught according to the Cuban curriculum of 2008, and the evaluation system established in Angola was used. Official documents were reviewed, and a question with a simple answer was applied to evaluate the level of knowledge of antimicrobial and anti-parasitic drugs. Results: The results in Pharmacology I were mainly satisfactory (74.83 percent); and in Pharmacology II they were satisfactory (61.57 percent) and good (34.01 percent). The results of the evaluation related to the topics were: third-year students: failed (41.75 percent); fourth-year students: satisfactory (45.10 percent), and fifth-year ones: satisfactory (32.58 percent and good (37, 08 percent). Conclusions: The results in Pharmacology are achieved by the progress in the study methods, the individualized attention to the student, and the integration of their contents to the disciplines related to the profession(AU)

Evaluation of antiparasitic, anticancer, antimicrobial and hypoglycemic properties of organic extracts from Panamanian mangrove plants

Objective: To investigate 33 organic extracts of mangrove plants for: antiparasitic, anticancer, and antibacterial activities, as well as their ability to inhibit the activity of the -glucosidase enzyme. Methods: Leaves from all different plant mangrove species located in five mangrove zones of the Pacific coast of Panama were collected according to standard procedures. Qualitative phytochemical analysis of the organic extracts was performed by thin layer chromatography. The antiparasitic activity against Plasmodium falciparum, Trypanosoma cruzi and Leishmania donovani, toxicity against Artemia salina, anticancer activity in MCF-7 cell line, and antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa of all organic extract were investigated according protocols stablished in our institution. Finally, the ability to inhibit the enzymatic activity of -glucosidase was evaluated by monitoring the hydrolysis of p-nitrophenyl -Dglucopyranoside. Results: Thirty-three different samples belonging to nine different species of vascular plants with seeds of true mangroves were collected. Triterpenoids, phenolics, and tannins were the main groups of compounds found in the sampled mangroves. Saponins, quinones, and coumarins were found in less than 50% of the samples. Laguncularia racemosa showed moderate activity against Plasmodium falciparum. None of the extracts presented anticancer activity. Rhizophora mangle exhibited potent activity against Staphylococcus aureus and Bacillus subtilis [(90.41±7.33)% and (96.02±6.14)% of inhibition]; Avicennia germinans and Conocarpus erectus had activity against Escherichia coli [(71.17±6.15)% and (60.60±5.13)% of inhibition, respectively]. About 60% of the mangroves showed -glucosidase inhibitory activity. In particular, extracts from Laguncularia racemosa, Pelliciera rhizophorae, Conocarpus erectus, Mora oleifera, and Tabebuia palustris species showed -glucosidase inhibitory potential, with IC50 values of (29.45±0.29), (20.60±0.70), (730.06±3.74), (25.59±0.37), and (853.39±5.30) µg/mL, respectively. Conclusions: Panamanian mangroves are mainly a promising potential source of hypoglycemic compounds, specifically -glucosidase inhibitors. These results highlight the therapeutic virtues of extracts from American mangrove plants.

Changes of brain CT imaging of cerebral cysticercosis patients during the period of anti-cysticercus chemotherapy / 中国血吸虫病防治杂志

Objective To investigate the changes of brain CT imaging in patients with cerebral cysticercosis during the period of anti-cysticercus chemotherapy. Methods A total of 380 inpatients that were conformed to the practical diagnostic criteria of cerebral cysticercosis were enrolled in this study in the Third Affiliated Hospital of Shandong Academy of Medical Sciences from May 2010 to May 2015. All the patients were given anti-cysticercus chemotherapy (albendazole and praziquantel). All the patients received brain CT scan, and of which 210 received enhanced scan. The data of CT imaging were systematically reviewed. Results Before the treatment, the CT images of the patients showed single or multiple small cystic (s) with low density and small nodule-like cephalomere with high density. The re-examinations of CT showed that there were 81.58% (310/380) of the patients whose low density foci were completely absorbed, there were 16.32% (62/380) of the patients whose foci were mostly absorbed, and there were 2.11% (8/380) of the patients whose foci were calcified. Along with the prolongation of treatment time, the side effects were gradually reduced, and in the third course of treatment, the foci were absorbed or calcified in most of the patients. Conclusion CT examination can diagnose the lesion site, range and classification of cerebral cysticercosis, and can evaluate the effect of the therapy according to the changes of CT imaging during the period of anti-cysticercus chemotherapy.

Changes of brain CT imaging of cerebral cysticercosis patients during the period of anti-cysticercus chemotherapy / 中国血吸虫病防治杂志

Objective To investigate the changes of brain CT imaging in patients with cerebral cysticercosis during the period of anti-cysticercus chemotherapy. Methods A total of 380 inpatients that were conformed to the practical diagnostic criteria of cerebral cysticercosis were enrolled in this study in the Third Affiliated Hospital of Shandong Academy of Medical Sciences from May 2010 to May 2015. All the patients were given anti-cysticercus chemotherapy (albendazole and praziquantel). All the patients received brain CT scan, and of which 210 received enhanced scan. The data of CT imaging were systematically reviewed. Results Before the treatment, the CT images of the patients showed single or multiple small cystic (s) with low density and small nodule-like cephalomere with high density. The re-examinations of CT showed that there were 81.58% (310/380) of the patients whose low density foci were completely absorbed, there were 16.32% (62/380) of the patients whose foci were mostly absorbed, and there were 2.11% (8/380) of the patients whose foci were calcified. Along with the prolongation of treatment time, the side effects were gradually reduced, and in the third course of treatment, the foci were absorbed or calcified in most of the patients. Conclusion CT examination can diagnose the lesion site, range and classification of cerebral cysticercosis, and can evaluate the effect of the therapy according to the changes of CT imaging during the period of anti-cysticercus chemotherapy.