The n-alkyl esters of gallic acid (CAS 13857-8) have a diverse range of uses as antioxidants in food, cosmetics and pharmaceutical industries. Pharmaceutical studies performed with these compounds have found that they have many therapeutic potentialities including anti-cancer, antiviral and antimicrobial properties. However, more interest has been devoted to their antioxidant activity due to the ability to scavenge and reduce reactive oxygen species (ROS) formation. In this study, gallic acid and 14 different alkyl gallates were tested. The cytotoxicity and anti-herpetic (HSV-1, KOS and 29-R strains) activity were studied by using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) colorimetric assay and the cell viability by using the Trypan blue dye exclusion method. The genotoxicity was studied by the Comet assay and the antioxidant activity by using the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging and microsomal lipid peroxidation-inhibiting activities. The results showed that all the tested compounds have anti-herpetic activity at non cytotoxic concentrations with selectivity indices (SI = CC50/EC50) varying from 0.89 to 18.34, depending on the used HSV-1 strain. It was observed that all tested alkyl gallates showed some degree of genotoxicity, at the tested concentrations, except cetyl gallate, at 256.60 micromol/L (p <0.05, t-Student test), probably induced by ROS released by infected cells and/or by the alkyl gallates that were not antioxidants, at the tested concentrations, in which they demonstrated anti-herpetic activity. The hydroxyl groups can induce DNA damage due interactions with some metal ions, which are naturally present in the culture medium supplemented with fetal bovine serum, probably explaining the genotoxicity detected. However, the obtained results showed considerable antioxidant activity at smaller concentrations, when compared to quercetin which is considered as a reference drug due to its already described antioxidant potential: DPPH radical scavenging activity with IC50 values varying from 17 to 31 micromol/L; and microsomal lipid peroxidation-inhibiting activity with IC50 values varying from 21 to 59 micromol/L. It was observed that the presence of hydroxyl groups in these molecules is important for their pharmacological profile, but the length of the lateral carbonic chain does not have considerable influence.
Flavonoids are dietary components and the most ubiquitous phenolic compounds found in nature, showing a range of pharmacological activities including antiviral action. This study describes the antiviral screening of 60 different flavones and flavonols against human rotavirus (Wa-1 strain) as well as their cytotoxicity in MA104 cells. Cytotoxicity was investigated by cell morphology assessment and antirotavirus activity by cytopathic effect inhibition. Results were expressed as CC(50) and IC(50), respectively, in order to calculate the selectivity index (SI = CC(50)/IC(50)) of each compound. Structure-activity relationships (SAR) were proposed based on antirotavirus activity.
This study evaluated the antiherpetic activity and genotoxicity of catechin and some of its derivatives using the MTT colorimetric and comet assays, respectively. The results showed that all compounds have antiviral activity with selective indices varying from 1.3 to 13, depending on the tested HSV-1 strain. It was observed that the same concentration of the compounds that protects the Vero cells against the viral infection induces genotoxicity. It was also observed that the molecules containing three hydroxyl groups on the B ring caused less DNA damage and showed better antiviral effect than those with two hydroxyls on the same ring, but if there is an additional galloyl group, these results can be altered. The bioavailability and stereochemistry could be related to the antiviral and genotoxic effects detected.
Some parameters for the quality control of P. glomerata and P. paniculata roots using their botanical and chemical characteristics are presented. It was also carried out an in vitro pharmacological screening to evaluate some biological properties of P. glomerata that could be related to its popular use as "tonic". Relating to biological assays, ethanolic extract from P. glomerata roots did not present antiviral, antiproliferative, antifungal or MAO inhibitory activities. The cytotoxicity evaluation of P. glomerata determined that IC 50 is >2,000 μg/mL. The main morphological and micrographic characteristics of P. glomerata and P. paniculata roots are described in this paper in order to aid in their unequivocal identification. UNITERMS:• Pfaffia glomerata
As demandas judiciais na Assistência Farmacêutica, as quais resultam no acesso a medicamentos e insumos por ordem judicial são crescentes, gerando desvio de recursos de outros setores, desorganização e fragilização do serviço,individualização de atendimentos em detrimento do coletivo, e mais ações judiciais, formando um ciclo. Os medicamentos fornecidos por ordem judicial não passam por avaliação de segurança, eficácia e custo/benefício (critérios básicos para padronização pelo SUS), ou mesmo se há real necessidade ou possibilidade de substituição. Parecem razoáveis ações pleiteando medicamentos padronizados quando a falta destes resulta da má gestão ou quando não existe política de tratamento (mesmo havendo terapia eficaz, segura e que o SUS possa financiá-la). Por outro lado, não há razão para ações quando há política pública de tratamento ou que pleiteiam produtos de eficácia e segurança duvidosas, sem indicação de uso e sem registro nos órgãos reguladores. É preciso analisar a origem da judicialização, as ações preventivas, o papel das instituições envolvidas e os desafios do administrador nessas demandas, como nos processos de aquisição dos produtos. É fundamental a inter-relação entre os profissionais do direito e de saúde a fim de equacionar alguns dilemas, como o confronto coletivo X individual. Há que se compreender a judicialização, mensurar sua amplitude e efeitos no SUS e na sociedade. Se por um lado as decisões judiciais visam o direito do cidadão, por outro, remetem ao gestor a responsabilidade de decisões que geralmente contradizem os princípios constitucionais da equidade e acesso à assistência à saúde de qualidade.
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