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1.
Infect Genet Evol ; 73: 390-400, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31173935

RESUMO

The Mayaro virus (MAYV) belongs to genus "Alphavirus" and family "Togaviridae". MAYV has distribution in the Amazonia, Central and Northeastern regions of Brazil. The abundance of mosquito vector Haemagogus janthinomys has major role in the outbreaks of arthralgia disease in Brazil. Vaccination or immunization is an alternative approach for the protection against this disease. To search the effective candidate for vaccine against Mayaro virus, various immunoinformatics tools were used to predict both the B and T cell epitopes from five structural polyproteins (capsid, E2, 6K, E3and E1). A multi subunit vaccine was designed and the final sequence was modeled for docking with TLR-3. Human b defensin based on previous studies was used as linker. The docked complexes of vaccine-TLR-3 were then subjected to dynamics stability and RMSD and RMSF results suggested that the complexes are stable. Further, to validate our final vaccine construct, in silico cloning was carried out using E. coli as host. The CAI value of 0.96 suggests that the vaccine construct properly expresses in the host. The current findings will be useful for the future experimental validations to ratify the immunogenicity and safety of the supposed structure of vaccine, and ultimately to treat the Mayaro virus, associated infections.


Assuntos
Infecções por Alphavirus/imunologia , Alphavirus/imunologia , Formação de Anticorpos/imunologia , Epitopos de Linfócito B/imunologia , Epitopos de Linfócito T/imunologia , Brasil , Biologia Computacional , Simulação por Computador , Escherichia coli/imunologia , Humanos , Modelos Moleculares , Poliproteínas/imunologia , Vacinas de Subunidades Antigênicas/imunologia , Vacinologia/métodos
2.
Braz. j. pharm. sci ; 52(1): 201-210, Jan.-Mar. 2016. tab, graf
Artigo em Inglês | LILACS | ID: lil-789085

RESUMO

ABSTRACT The aim of this study was to evaluate binding potential of Mulva neglecta mucilage (MNM) with subsequent comparison to PVP K30. Eight batches of Diclofenac sodium tablets were prepared by wet granulation technique keeping different concentrations (4, 6, 8 & 10% w/w) of Mulva neglecta mucilage (extracted from leaves of Mulva neglecta) and PVP K30 as standard binder. The granules of formulated batches showed bulk density (g/mL) 0.49 ± 0.00 to 0.57 ± 0.00, tapped density (g/mL) 0.59 ± 0.01 to 0.70 ± 0.01, Carr's index 09.27 ± 0.95 to 19.65 ± 0.59, Hausner's ratio 1.12 ± 0.00 to 1.24 ± 0.01 and angle of repose 30.37 ± 2.90 °C to 36.86 ± 0.94 °C. Tablets were compressed to hardness 7.50 to 7.95 kg/cm2. The tablets showed 0.39 ± 0.02 to 0.39 ± 0.01% friability and 7:20 to 14:00 min disintegration time. Granules and post-compression evaluation revealed that parameters assessed were all found to be within the pharmacopoeial limits. The results (hardness, disintegration and dissolution) proved that Mulva neglecta mucilage has better binding capacity for preparation of uncoated tablet dosage form as compared to PVP K30. Among all the formulations, MN-1 to MN-4 showed slow release as compared to PV-1 to PV-4 and thereby Mulva neglecta mucilage exhibited satisfactory drug release phenomenon tablets of diclofenac sodium.


RESUMO O objetivo deste estudo foi avaliar o potencial de ligação de mucilagem de Mulva neglecta (MNM), com posterior comparação ao PVP K30. Oito lotes de comprimidos de diclofenaco de sódio foram preparados pela técnica de granulação úmida, mantendo diferentes concentrações (4, 6, 8 e 10% w/w) de mucilagem de Mulva neglecta (extraída de folhas de Mulva neglecta) e PVP K30 como ligante padrão. Os grânulos de lotes formulados mostraram densidade aparente (g/mL) 0.49 ± 0.00-0.57 ± 0.00, densidade compactada (g/mL) 0.59 ± 0.01-0.70 ± 0.01, índice de Carr 09.27 ± 0.95-19.65 ± 0.59, a relação de Hausner 1.12 ± 0.00-1.24 ± 0.01 e ângulo de repouso 30.37 ± 2.90 °C a 36.86 ± 0.94 °C. Os comprimidos foram prensados à dureza de 7.50-7.95 kg/cm2. Os comprimidos apresentaram 0.39 ± 0.02-0.39 ± 0.01% friabilidade e 7:20-14:00 min de tempo de desintegração. A avaliação de grânulos e pós-compressão revelou que todos os parâmetros estavam dentro dos limites da farmacopeia. Os resultados (dureza, desintegração e dissolução) provaram que a mucilagem de Mulva neglecta tem maior capacidade de ligação na preparação da forma de dosagem de comprimido não revestido em relação à PVP K30. Entre todas as formulações, MN-1 e MN-4 mostraram liberação lenta em comparação com PV-1 e PV-4 e, assim, a mucilagem de Mulva neglecta exibiu liberação do fármaco satisfatória para os comprimidos de diclofenaco de sódio.


Assuntos
Malva , Mucilagem Vegetal/classificação , Comprimidos , Diclofenaco/análogos & derivados
3.
Biol Res ; 47: 65, 2014 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-25730474

RESUMO

BACKGROUND: The current era is facing challenges in the management of neoplasia and weeds control. The currently available anti-cancer and herbicidal drugs are associated with some serious side effects. Therefore numerous researchers are trying to discover and develop plant based alternative particularly for the rational management of cancer and weed control. Teucrium stocksianum possess antioxidant and analgesic activities. The current study was designed to evaluate crude saponins (CS), methanolic extract and sub-fractions of T. stocksianum for cytotoxic and phytotoxic potentials. CS, methanolic extract and sub-fractions were extracted from powdered plant material using different solvents. Cytotoxic potential of the extracts at a dose of 10, 100 and 1000 µg/ml were evaluated against Brine shrimp's nauplii. Phytotoxic assay also performed at the same concentration against Lemna minor. Etoposide and Paraquat were used as positive controls in cytotoxic and phytotoxic assays respectively. RESULTS: The percent yield of crude saponins was (5%). CS demonstrated tremendous brine shrimp lethality showing < 10 µg/ml LC50. The n-hexane (HF) and chloroform fractions (CF) demonstrated excellent cytotoxicity with 80 and 55 µg/ml LC50 respectively. Whereas the methanolic extract (TSME), ethyl acetate (EAF) and aqueous fractions (AF) revealed moderate cytotoxicity showing 620, 860 and 1000 µg/ml LC50 values respectively. In phytotoxic assay profound inhibition was displayed by HF (96.67%) and TSME (95.56%, 30 µg/ml LC50) against the growth of Lemna minor at 1000 µg/ml respectively. Both CF and EAF demonstrated profound phytoxicity (93.33%) respectively at highest concentration (1000 µg/ml), while AF and CS demonstrated weak phytotoxicity with 1350 and 710 µg/ml LC50 values respectively. CONCLUSION: Cytotoxicity and phytotoxicity assays indicated that the crude saponins, n-hexane and chloroform fractions of T. stocksianum could play a vital role in the treatment of neoplasia and as potential natural herbicides. Therefore these sub-fractions are recommended for further investigation with the aim to isolate novel anti-cancer and herbicidal compounds.


Assuntos
Citotoxinas/farmacologia , Extratos Vegetais/química , Saponinas/análise , Teucrium/química , Animais , Araceae/classificação , Araceae/efeitos dos fármacos , Artemia/efeitos dos fármacos , Citotoxinas/análise , Hexanos , Dose Letal Mediana , Medicina Tradicional/métodos , Metanol , Paquistão , Extratos Vegetais/toxicidade , Saponinas/toxicidade , Teucrium/classificação , Teucrium/toxicidade
4.
Biol. Res ; 47: 1-5, 2014. tab
Artigo em Inglês | LILACS | ID: biblio-950761

RESUMO

BACKGROUND: The current era is facing challenges in the management of neoplasia and weeds control. The currently available anti-cancer and herbicidal drugs are associated with some serious side effects. Therefore numerous researchers are trying to discover and develop plant based alternative particularly for the rational management of cancer and weed control. Teucrium stocksianum possess antioxidant and analgesic activities. The current study was designed to evaluate crude saponins (CS), methanolic extract and sub-fractions of T. stocksianum for cytotoxic and phytotoxic potentials. CS, methanolic extract and sub-fractions were extracted from powdered plant material using different solvents. Cytotoxic potential of the extracts at a dose of 10, 100 and 1000 µg/ml were evaluated against Brine shrimp's nauplii. Phytotoxic assay also performed at the same concentration against Lemna minor. Etoposide and Paraquat were used as positive controls in cytotoxic and phytotoxic assays respectively. RESULTS: The percent yield of crude saponins was (5%). CS demonstrated tremendous brine shrimp lethality showing < 10 µg/ml LC50. The n-hexane (HF) and chloroform fractions (CF) demonstrated excellent cytotoxicity with 80 and 55 µg/ml LC50 respectively. Whereas the methanolic extract (TSME), ethyl acetate (EAF) and aqueous fractions (AF) revealed moderate cytotoxicity showing 620, 860 and 1000 µg/ml LC50 values respectively. In phytotoxic assay profound inhibition was displayed by HF (96.67%) and TSME (95.56%, 30 µg/ml LC50) against the growth of Lemna minor at 1000 µg/ml respectively. Both CF and EAF demonstrated profound phytoxicity (93.33%) respectively at highest concentration (1000 µg/ml), while AF and CS demonstrated weak phytotoxicity with 1350 and 710 µg/ml LC50 values respectively. CONCLUSION: Cytotoxicity and phytotoxicity assays indicated that the crude saponins, n-hexane and chloroform fractions of T. stocksianum could play a vital role in the treatment of neoplasia and as potential natural herbicides. Therefore these sub-fractions are recommended for further investigation with the aim to isolate novel anti-cancer and herbicidal compounds.


Assuntos
Animais , Saponinas/análise , Extratos Vegetais/química , Citotoxinas/farmacologia , Teucrium/química , Paquistão , Artemia/efeitos dos fármacos , Saponinas/toxicidade , Extratos Vegetais/toxicidade , Araceae/classificação , Araceae/efeitos dos fármacos , Citotoxinas/análise , Teucrium/classificação , Teucrium/toxicidade , Metanol , Hexanos , Dose Letal Mediana , Medicina Tradicional/métodos
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