ABSTRACT
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.
Subject(s)
Animals , Porifera , Brazil , Plant Extracts , Enterococcus faecalis , Anti-Bacterial AgentsABSTRACT
The aim of this study is to explore the anti-HSV activity of P.vulgaris polysaccharides and gels in vitro and in vivo with the provision of scientific evidence for the further research of anti-HSV new drugs.Plaque reduction assay was adopted to determine the IC50 value of P.vulgaris polysaccharides on HSV-1 and HSV-2 in vitro.In addition,HSV-1 (skin) and HSV-2 (vulva) infected guinea-pig models were established for assessing the anti-HSV activity of polysaccharides and gels in vivo,and infected lesion degree,number of papulovesicle,typical lesion score and the DNA copy numbers of HSV-1 and HSV-2 viruses in the lesion tissue were taken as the indexes.It was found that the activities of HSV1 and HSV-2 viruses was inhibited by P.vulgaris polysaccharides in vitro,while HSV induced skin lesions in the guineapigs were ameliorated by P.vulgaris gel,exerting an anti-HSV action.In conclusion,it was demonstrated that P.vulgaris polysaccharides and gels performed an anti-HSV action both in vitro and in vivo with the hidden value of developing antiHSV agents.
ABSTRACT
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.
ABSTRACT
Spondias mombin L. (Anacardiaceae) é uma árvore de porte elevado, frutífera, frequente no Oeste da Índia, México, Peru, Brasil e conhecida popularmente como cajazeira. Todas as suas partes têm sido utilizadas pela medicina tradicional. A planta faz parte da REPLAME (Relação de Plantas Medicinais) do estado do Ceará e do projeto Farmácias Vivas com a indicação para o tratamento da herpes. O objetivo do presente estudo foi desenvolver um fitoproduto padronizado a partir das folhas de S. mombin, e avaliar seu potencial antiinflamatórioe antiviral (Herpes simplex 1). Para isso, inicialmente, foram estabelecidos o método de preparação (secagem em estufa com circulação/ renovação de ar) a 60 ± 5 ºC por 4horas e as especificações para o controle de qualidade da droga vegetal (DV). O método extrativo para obtenção do extrato padronizado de S. mombin foi a maceração dinâmica por2,5 h, a 30 °C e relação DV: solvente (etanol 30 % em água) de 0,3, caracterizado pelo teor defenóis totais (FT: 17,52 mg/mL), resíduo seco (RS: 7,12 %, p/v) e perfil cromatográfico por CLAE-DAD (Ácido clorogênico - AC: 0,83 mg/mL e Geraniina - GR: 7,37 mg/mL). Naavaliação do potencial anti-inflamatório, extrato de S. mombin (ESM) (1, 10, 50, 100 μg/mL)inibiu parcialmente a liberação de MPO (Mieloperoxidase) induzida por PMA (Folbol-12-miristato-13-acetato), sendo observado melhor efeito na maior concentração (% inibição:50,4), enquanto que o padrão GR (1, 10, 25, 50 e 100 μg/mL) promoveu um efeito dual, ampliando a desgranulação de neutrófilo induzida por PMA nas menores concentrações (1 25 μg/mL) e inibindo esta (40,3 e 83,5 %) nas maiores concentrações (50 e 100 μg/mL). Apenas a concentração de 200 μg/mL do ESM mostrou citotoxicidade em neutrófilos humanos no teste do MTT...
Spondias mombin L. (Anacardiaceae) is a large-sized tree, fruitful, frequent in western India,Mexico, Peru, Brazil and popularly known as cajazeira. All the parts have been used bytraditional medicine. The plant is part of REPLAME (List of Medicinal Plants) of the state ofCeará and Farmacias Vivas projects, indicated for the herpes treatment. The aim of this studywas to develop a standardized product from the leaves of S. mombin and evaluate its antiviral(Herpes Simplex 1) and anti-inflammatory potential. Therefore, was initially established onemethod of preparation (drying oven with air circulation / renovation) under 60 ± 5 ° C heating4 hours, and the specifications for quality control of plant drug (PD). The extractive methodfor obtaining a standardized extract of S. mombin was the dynamic maceration for 2.5 h at 30° C and a relation PD:solvent (30% ethanol in water) of 0.3, characterized as total phenolscontent (TF: 17.52 mg/mL), dry residue (7.12%, w/v) and chromatographic profile by HPLCPAD(Chlorogenic acid - CA: 0.83 mg/mL and Geraniin - GR: 7.3 mg/mL). The evaluation ofanti-inflammatory potential showed that extract of S. mombin (ESM) (1, 10, 50 and 100µg/mL) partially inhibited MPO (Myeloperoxidase) release induced by PMA (Phorbol-12-Myristate-13-Acetate), with best effect seen at the biggest concentration (% inhibition: 50,4),while the standard GR (1, 10, 25, 50 and 100 µg/mL) promoted a dual effect, expanding thedegranulation of neutrophils induced by PMA at low concentrations (1 - 25 µg/mL) andinhibiting (40.3 and 83.5%) at biggest concentrations (50 and 100 µg/mL). Only theconcentration 200 µg/mL of ESM showed citotoxicity on human neutrophils in MTT test...