Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 202
Filtrar
Mais filtros

Medicinas Complementares
Base de dados
Tipo de documento
Intervalo de ano de publicação
1.
ACS Nano ; 17(15): 15199-15215, 2023 08 08.
Artigo em Inglês | MEDLINE | ID: mdl-37486141

RESUMO

Since ferrous (Fe(II)) is the main form of plant absorption, traditional ferrous foliar fertilizers (TFFF) are widely used in modern agriculture. However, TFFF suffer from the shortcomings of weak antioxidant capacity (AC), low foliar adhesion efficiency (FAE), poor fertilizer utilization efficiency (FUE), and noncontrollable slow-release behavior. To overcome these limitations, an oxidation-resistant silicon nanosystem for intelligent controlled ferrous foliar delivery to crops was first developed by using environmentally friendly micro/nano structured hollow silicon as carrier, and combining with vitamin C (in situ antioxidant) to synthesize an oxidation-resistant ferrous foliar fertilizer (ORFFF) for ameliorating Fe-deficiency in crops and increasing crop yield. Compared with TFFF, the ORFFF has excellent ferrous AC (only 11.5% of Fe(II) was oxidized in ORFFF within 72 h), ultrahigh FAE (∼84% of adhesion percentage (%) after two-times simulated rain rinsing), nutrient slow-release ability (720 h gradually release 100.6 mg·g-1), pH-controlled release ability (pH 3-8), and verified high biological safety (100% survival rate for zebrafish and earthworm). The pot experiments showed that ORFFF can correct the Fe-deficiency symptoms of tomato seedlings promptly compared with TFFF, and the FUE of ORFFF is 4.2 times that of TFFF. The specific pH responsiveness of ORFFF can control the slow-release rate of Fe(II) to satisfy the needs of Fe in varying crops and different growing periods of crops. This work provides a feasible way to achieve green and safe Fe supplementation for crops, reduce Fe fertilizer waste, avoid soil pollution caused by Fe fertilizer abuse, and promote the sustainable development of modern nanoagriculture.


Assuntos
Antioxidantes , Silício , Animais , Fertilizantes/análise , Peixe-Zebra , Compostos Ferrosos/farmacologia , Solo
2.
Br J Nutr ; 129(3): 468-477, 2023 02 14.
Artigo em Inglês | MEDLINE | ID: mdl-35591764

RESUMO

Iron deficiency is the leading cause of anaemia. In Argentina, the prevalence of anaemia and iron deficiency is very high; for that reason, the Argentine Society of Pediatrics recommends daily ferrous sulphate supplementation as a preventive treatment strategy. Alternatively, weekly ferrous sulphate supplementation has also been shown to be effective for anaemia prevention. Excess iron could be related to oxidative stress, which may in turn cause cytomolecular damage. Both can be prevented with vitamin E supplementation. We evaluated the effect of both daily and weekly ferrous sulphate supplementation combined with two doses of vitamin E on cell viability, oxidative stress and cytomolecular damage in peripheral blood cultured in vitro. The experimental design included the following groups: untreated negative control, two vitamin E controls (8·3 and 16·6 µg/ml), weekly ferrous sulphate supplementation (0·55 mg/ml) with each vitamin E dose, daily ferrous sulphate supplementation (0·14 mg/ml) with each vitamin E dose and a positive control. Daily ferrous sulphate supplementation decreased cell viability and increased the levels of reactive oxygen species, lipid peroxidation and cytomolecular damage (P < 0·5) compared with the weekly supplementation, probably due to the excess iron observed in the former. Vitamin E seemed to reduce ferrous sulphate-induced oxidative stress and genomic damage.


Assuntos
Anemia Ferropriva , Anemia , Deficiências de Ferro , Sobrecarga de Ferro , Humanos , Criança , Vitamina E/farmacologia , Vitamina E/uso terapêutico , Suplementos Nutricionais , Compostos Ferrosos/farmacologia , Compostos Ferrosos/uso terapêutico , Ferro , Genômica , Modelos Teóricos
3.
Sci Rep ; 12(1): 2792, 2022 02 18.
Artigo em Inglês | MEDLINE | ID: mdl-35181698

RESUMO

Food fortification with iron nanoparticles (NPs) could help prevent iron deficiency anemia, but the absorption pathway and biodistribution of iron-NPs and their bioavailability in humans is unclear. Dietary non-heme iron is physiologically absorbed via the divalent metal transporter-1 (DMT1) pathway. Using radio- iron isotope labelling in mice with a partial knockdown of intestine-specific DMT1, we assessed oral absorption and tissue biodistribution of nanostructured ferric phosphate (FePO4-NP; specific surface area [SSA] 98 m2g-1) compared to to ferrous sulfate (FeSO4), the reference compound. We show that absorption of iron from FePO4-NP appears to be largely DMT1 dependent and that its biodistribution after absorption is similar to that from FeSO4, without abnormal deposition of iron in the reticuloendothelial system. Furthermore, we demonstrate high bioavailability from iron NPs in iron deficient anemic women in a randomized, cross-over study using stable-isotope labelling: absorption and subsequent erythrocyte iron utilization from two 57Fe-labeled FePO4-NP with SSAs of 98 m2g-1 and 188 m2g-1 was 2.8-fold and 5.4-fold higher than from bulk FePO4 with an SSA of 25 m2g-1 (P < 0.001) when added to a rice and vegetable meal consumed by iron deficient anemic women. The FePO4-NP 188 m2g-1 achieved 72% relative bioavailability compared to FeSO4. These data suggest FePO4-NPs may be useful for nutritional applications.


Assuntos
Anemia Ferropriva/dietoterapia , Proteínas de Transporte de Cátions/genética , Compostos Férricos/farmacologia , Ferro/metabolismo , Adsorção/efeitos dos fármacos , Adulto , Anemia Ferropriva/genética , Anemia Ferropriva/metabolismo , Anemia Ferropriva/patologia , Animais , Disponibilidade Biológica , Suplementos Nutricionais/efeitos adversos , Feminino , Compostos Férricos/química , Compostos Ferrosos/farmacologia , Alimentos Fortificados/efeitos adversos , Humanos , Ferro/farmacologia , Radioisótopos de Ferro/farmacologia , Nanopartículas Metálicas/química , Nanopartículas Metálicas/uso terapêutico , Camundongos , Nanoestruturas/uso terapêutico , Adulto Jovem
4.
ChemMedChem ; 17(2): e202100548, 2022 01 19.
Artigo em Inglês | MEDLINE | ID: mdl-34719875

RESUMO

A cancer-mitochondria dual-targeting nanoparticle based on lactose and ferrocenium derivatives conjugated polydopamine (PDA@Lac/Fc/Hyp) was constructed, which exhibited cancer-targeting and mitochondria-targeting ability deriving from lactose and ferrocenium derivatives due to the specific carbohydrate-protein interaction and cationic species properties, respectively. Moreover, PDA@Lac/Fc/Hyp showed great biocompatibility and phototherapeutic efficiency. This work displays a good example of constructing cancer-mitochondria dual-targeting nanoparticle for synergistic phototherapy.


Assuntos
Antineoplásicos/farmacologia , Compostos Ferrosos/farmacologia , Glicóis/farmacologia , Indóis/farmacologia , Neoplasias Hepáticas/tratamento farmacológico , Mitocôndrias/efeitos dos fármacos , Fotoquimioterapia , Polímeros/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Compostos Ferrosos/química , Glicóis/química , Células Hep G2 , Humanos , Indóis/química , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Mitocôndrias/metabolismo , Estrutura Molecular , Nanopartículas/química , Polímeros/química , Relação Estrutura-Atividade
5.
Biometals ; 35(1): 27-38, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34697758

RESUMO

Iron deficiency is one of the most common nutritional deficiencies worldwide and is often treated with oral iron supplements. However, commonly used supplements, including those based on ferrous iron salts, are associated with gastrointestinal side effects and unfavorable changes in the intestinal microbiome. Sucrosomial® iron is a novel iron formulation that is effective at treating iron deficiency, and with fewer gastrointestinal side effects, yet its effect on the gut microbiome has not been examined previously. Thus, we treated mice for two weeks with diets containing either Sucrosomial® iron or ferrous sulfate as the sole iron source and examined bacterial communities in the intestine using 16S Microbial Profiling of DNA extracted from feces collected both prior to and following dietary treatment. Mice treated with Sucrosomial® iron showed an increase in Shannon diversity over the course of the study. This was associated with a decrease in the abundance of the phylum Proteobacteria, which contains many pathogenic species, and an increase in short chain fatty acid producing bacteria such as Lachnospiraceae, Oscillibacter and Faecalibaculum. None of these changes were observed in mice treated with ferrous sulfate. These results suggest that Sucrosomial® iron may have a beneficial effect on the intestinal microbiome when compared to ferrous sulfate and that this form of iron is a promising alternative to ferrous iron salts for the treatment of iron deficiency.


Assuntos
Anemia Ferropriva , Microbioma Gastrointestinal , Deficiências de Ferro , Anemia Ferropriva/tratamento farmacológico , Animais , Suplementos Nutricionais , Compostos Ferrosos/farmacologia , Ferro , Camundongos , Sais/uso terapêutico
6.
Nutrients ; 13(7)2021 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-34209042

RESUMO

BACKGROUND AND AIMS: Altering dietary ferrous sulphate (FS) consumption exacerbates a murine model of colitis and alters the intestinal microbiome. We investigated the impact of oral ferric maltol (FM) and FS on mice with dextran sodium sulphate (DSS) induced colitis, and the microbiome of patients with iron deficiency. METHODS: Mice had acute colitis induced, with 2% DSS for 5 days, followed by water. During this period, groups of mice were fed standard chow (200 ppm iron, SC, n = 8), or SC with 200ppm FS supplementation (n = 16, FSS), or SC with 200 ppm FM supplementation (n = 16, FMS). Clinical, pathological and microbiome assessments were compared at days 1 and 10. Fecal bacterial gDNA was extracted and the microbiome assessed by sequencing. Statistical inferences were made using MacQIIME. Principal Coordinates Analysis were used to visualize beta-diversity cluster analysis. Ten patients with IDA were treated with FS, and six with inactive inflammatory bowel disease received FM, supplements for four weeks: pre- and mid-treatment fecal samples were collected: the microbiome was assessed (see above). RESULTS: In mice, after DSS treatment, there was a decrease in many genera in the SC and FSS groups: Lactobacillales increased in mice that received FMS. In humans, FS treatment led to an increase in five genera, but FM was not associated with any measurable change. The severity of DSS-induced colitis was greater with FSS than FMS. CONCLUSIONS: This study demonstrates differential and unique influences of ferric maltol and ferrous sulphate supplements on intestinal microbiota. These differences might contribute to the different side effects associated with these preparations.


Assuntos
Compostos Férricos/administração & dosagem , Compostos Férricos/farmacologia , Compostos Ferrosos/farmacologia , Pironas/administração & dosagem , Pironas/farmacologia , Administração Oral , Animais , Biodiversidade , Peso Corporal/efeitos dos fármacos , Colite/induzido quimicamente , Colite/microbiologia , Colite/patologia , Colo/efeitos dos fármacos , Colo/microbiologia , Colo/patologia , Sulfato de Dextrana , Fezes/microbiologia , Feminino , Microbioma Gastrointestinal/efeitos dos fármacos , Humanos , Ferro/metabolismo , Camundongos Endogâmicos C57BL , Filogenia
7.
Nutrients ; 13(5)2021 Apr 22.
Artigo em Inglês | MEDLINE | ID: mdl-33921980

RESUMO

Iron-fortified formulas and iron drops (both usually ferrous sulfate, FS) prevent early life iron deficiency, but may delay growth and adversely affect neurodevelopment by providing excess iron. We used a rat pup model to investigate iron status, growth, and development outcomes following daily iron supplementation (10 mg iron/kg body weight, representative of iron-fortified formula levels) with FS or an alternative, bioavailable form of iron, ferrous bis-glycinate chelate (FC). On postnatal day (PD) 2, sex-matched rat litters (n = 3 litters, 10 pups each) were randomly assigned to receive FS, FC, or vehicle control until PD 14. On PD 15, we evaluated systemic iron regulation and CNS mineral interactions and we interrogated iron loading outcomes in the hippocampus, in search of mechanisms by which iron may influence neurodevelopment. Body iron stores were elevated substantially in iron-supplemented pups. All pups gained weight normally, but brain size on PD 15 was dependent on iron source. This may have been associated with reduced hippocampal oxidative stress but was not associated with CNS mineral interactions, iron regulation, or myelination, as these were unchanged with iron supplementation. Additional studies are warranted to investigate iron form effects on neurodevelopment so that iron recommendations can be optimized for all infants.


Assuntos
Sistema Nervoso Central/crescimento & desenvolvimento , Suplementos Nutricionais , Compostos Ferrosos/farmacologia , Glicina/farmacologia , Quelantes de Ferro/farmacologia , Ferro/metabolismo , Ferro/farmacologia , Animais , Animais Recém-Nascidos , Sistema Nervoso Central/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Homeostase/efeitos dos fármacos , Ferro/sangue , Bainha de Mielina/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ratos Sprague-Dawley , Oligoelementos/análise , Aumento de Peso/efeitos dos fármacos
8.
Am J Clin Nutr ; 113(5): 1104-1114, 2021 05 08.
Artigo em Inglês | MEDLINE | ID: mdl-33675347

RESUMO

BACKGROUND: Fibroblast growth factor-23 (FGF23) regulates body phosphate homeostasis primarily by increasing phosphaturia. It also acts as a vitamin D-regulating hormone. Maternal iron deficiency is associated with perturbed expression and/or regulation of FGF23 and hence might be implicated in the pathogenesis of hypophosphatemia-driven rickets in their offspring. OBJECTIVES: We aimed to determine the effect of antenatal oral iron supplementation on FGF23 concentration and maternal and infant markers of bone-mineral regulation. METHODS: We performed a secondary analysis of a trial in which 470 rural Kenyan women with singleton pregnancies and hemoglobin concentrations ≥ 90 g/L were randomly allocated to daily, supervised supplementation with 60 mg elemental iron as ferrous fumarate or placebo from 13-23 weeks of gestation until 1 mo postpartum. As previously reported, iron supplementation improved iron status in mothers and neonates. For the present study, we reanalyzed all available plasma samples collected in mothers and neonates at birth, with primary outcomes being concentrations of FGF23, measured by 2 assays: 1 that detects intact hormone and C-terminal cleavage products (total-FGF23) and another that detects the intact hormone only (intact-FGF23). RESULTS: Analysis was performed on 433 women (n = 216, iron group; n = 217, placebo group) and 414 neonates (n = 207, iron group; n = 207, placebo group). Antenatal iron supplementation reduced geometric mean total-FGF23 concentrations in mothers and neonates by 62.6% (95% CI: 53.0%, 70.3%) and 15.2% (95% CI: -0.3%, 28.4%, P = 0.06), respectively. In addition, it increased geometric mean neonatal intact-FGF23 concentrations by 21.6% (95% CI: 1.2%, 46.1%), increased geometric mean maternal hepcidin concentrations by 136.4% (95% CI: 86.1%, 200.3%), and decreased mean maternal 25-hydroxyvitamin D concentrations by 6.1 nmol/L (95% CI: -11.0, -1.2 nmol/L). CONCLUSIONS: Analysis of this randomized trial confirms that iron supplementation can reverse elevated FGF23 production caused by iron deficiency in iron-deficient mothers and their neonates. Further investigations are warranted to assess to what extent iron supplementation can prevent FGF23-mediated hypophosphatemic rickets or osteomalacia.


Assuntos
Osso e Ossos/metabolismo , Suplementos Nutricionais , Compostos Ferrosos/administração & dosagem , Compostos Ferrosos/farmacologia , Fatores de Crescimento de Fibroblastos/metabolismo , Feminino , Fator de Crescimento de Fibroblastos 23 , Fatores de Crescimento de Fibroblastos/genética , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Lactente , Quênia , Período Pós-Parto
9.
Biochem Biophys Res Commun ; 545: 203-207, 2021 03 19.
Artigo em Inglês | MEDLINE | ID: mdl-33571909

RESUMO

The current COVID-19 pandemic requires urgent development of effective therapeutics. 5-amino levulinic acid (5-ALA) is a naturally synthesized amino acid and has been used for multiple purposes including as an anticancer therapy and as a dietary supplement due to its high bioavailability. In this study, we demonstrated that 5-ALA treatment potently inhibited infection of SARS-CoV-2, a causative agent of COVID-19, in cell culture. The antiviral effects could be detected in both human and non-human cells, without significant cytotoxicity. Therefore, 5-ALA is worth to be further investigated as an antiviral drug candidate for COVID-19.


Assuntos
Antivirais/farmacologia , Tratamento Farmacológico da COVID-19 , Ácidos Levulínicos/farmacologia , Animais , Antivirais/administração & dosagem , COVID-19/prevenção & controle , COVID-19/virologia , Células CACO-2 , Chlorocebus aethiops , Ácido Cítrico , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos/métodos , Compostos Ferrosos/farmacologia , Humanos , Ácidos Levulínicos/administração & dosagem , Células Vero , Ácido Aminolevulínico
10.
Sci Rep ; 11(1): 1347, 2021 01 14.
Artigo em Inglês | MEDLINE | ID: mdl-33446747

RESUMO

Iron deficiency anemia (IDA) is a common micronutrient deficiency among pregnant women with severe consequences including impaired immuno-inflammatory system, premature birth, fetal death etc. The present study aimed to investigate the effects of three iron supplements on IDA female rats and their offspring. The IDA female rat model was established with low iron diet and the rats were then mated. After pregnancy, rats were fed diets containing different iron supplements (iron polysaccharide complex, iron protein succinylate and ferrous sulfate) until their offspring were 42 days old. Pregnancy outcomes, haematological, iron metabolism, physical and neurological development indexes were determined. The results showed that all three iron supplements improved the levels of hematological parameters of both mother and offspring rats. After iron supplementation, serum iron, transferrin saturation and serum ferritin levels were increased compared with the IDA group. The level of ferritin light chain in the liver and spleen of both mother and offspring rats in iron supplemented groups was significantly higher than that of the IDA group. The average number of born alive per litter in the iron treatment groups was significantly higher than that in the IDA group. Iron supplements also improved the physical growth and neurobehavioral development of offspring rats. It was also found that iron supplementation improved the expression of ferritin light chain and the synaptic growth associated proteins in the brain and hippocampus. No significant difference was found in the efficacy of three iron supplements. These results suggest that pregnant and postpartum IDA affects pregnancy outcomes, offspring physical development and causes neural impairment. Sufficient iron supplementation can significantly improve IDA and its adverse effects on both mother and offspring.


Assuntos
Anemia Ferropriva , Compostos Ferrosos/farmacologia , Metaloproteínas/farmacologia , Complicações Hematológicas na Gravidez , Resultado da Gravidez , Succinatos/farmacologia , Anemia Ferropriva/sangue , Anemia Ferropriva/tratamento farmacológico , Animais , Feminino , Ferro/farmacologia , Gravidez , Complicações Hematológicas na Gravidez/sangue , Complicações Hematológicas na Gravidez/tratamento farmacológico , Ratos , Ratos Wistar
11.
Nutrients ; 12(12)2020 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-33327501

RESUMO

Ferrous iron supplementation has been reported to adversely alter the gut microbiota in infants. To date, the impact of iron on the adult microbiota is limited, particularly at low supplementary concentrations. The aim of this research was to explore the impact of low-level iron supplementation on the gut microbiota of healthy and Irritable Bowel Syndrome (IBS) volunteers. Anaerobic, pH-controlled in vitro batch cultures were inoculated with faeces from healthy or IBS donors along with iron (ferrous sulphate, nanoparticulate iron and pea ferritin (50 µmol-1 iron)). The microbiota were explored by fluorescence in situ hybridisation coupled with flow cytometry. Furthermore, metabolite production was assessed by gas chromatography. IBS volunteers had different starting microbial profiles to healthy controls. The sources of iron did not negatively impact the microbial population, with results of pea ferritin supplementation being similar to nanoparticulate iron, whilst ferrous sulphate led to enhanced Bacteroides spp. The metabolite data suggested no shift to potentially negative proteolysis. The results indicate that low doses of iron from the three sources were not detrimental to the gut microbiota. This is the first time that pea ferritin fermentation has been tested and indicates that low dose supplementation of iron is unlikely to be detrimental to the gut microbiota.


Assuntos
Suplementos Nutricionais , Fezes/microbiologia , Microbioma Gastrointestinal/efeitos dos fármacos , Ferro/farmacologia , Síndrome do Intestino Irritável/microbiologia , Técnicas de Cultura Celular por Lotes , Técnicas de Cultura de Células , Fermentação , Compostos Ferrosos/farmacologia , Humanos , Nanopartículas , Proteínas de Ervilha/farmacologia , Proteólise/efeitos dos fármacos
12.
J Helminthol ; 94: e190, 2020 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-32912343

RESUMO

The main goal of this work was to evaluate the in vitro biological activity of two ferrocenyl chalcones (FcC-1 and FcC-2) against Haemonchus contortus (third-stage larvae (L3)) and Nacobbus aberrans (second-stage juveniles (J2)). Both compounds were synthesized and characterized by usual spectroscopic methods and their molecular structures were confirmed by single-crystal X-ray diffractometry. Nematode strains were examined in terms of percentage mortality of H. contortus (L3) by the action of FcC-1, which showed an effectivity of 100% at a concentration of 342 µM in 24 h, with EC50 = 20.33 µM and EC90 = 162.76 µM, whereas FcC-2 had an effectivity of 72% at a concentration of 342 µM in 24 h, with EC50 = 167.39 µM and EC90 = 316.21 µM. The effect of FcC-1 against nematode phytoparasite N. aberrans showed a better percentage of 95% at a concentration of 342 µM, with EC50 = 7.18 µM and EC90 = 79.25 µM, whereas the effect of FcC-2 was 87% at 342 µM, with EC50 = 168 µM and EC90 = 319.56 µM at 36 h. After treatment, the scanning electron micrographs revealed deformities in the dorsal flank and posterior part close to the tail of H. contortus L3. They showed moderate in vitro nematicidal activity against H. contortus L3 and N. aberrans J2.


Assuntos
Antinematódeos/farmacologia , Chalconas/farmacologia , Compostos Ferrosos/farmacologia , Haemonchus/efeitos dos fármacos , Tylenchoidea/efeitos dos fármacos , Animais , Antinematódeos/química , Chalconas/química , Compostos Ferrosos/química , Hemoncose/parasitologia , Larva/efeitos dos fármacos , Extratos Vegetais/farmacologia
13.
Braz J Microbiol ; 51(4): 1475-1482, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32822003

RESUMO

Antibiotics and other antimicrobial compounds are the backbone of clinical medicine. Antimicrobial resistance can cause serious diseases to man. Nanotechnology can improve therapeutic potential of medicinal molecules and related agents. Widespread application of antibiotics and other antimicrobial compounds led to development of multidrug-resistant microbes, so there is need to develop novel therapeutic agents. Novel synthesized nanometric delafossite was assayed against two Gram-positive bacteria (Staphylococcus aureus and Micrococcus luteus), two Gram-negative bacteria (Escherichia coli and Klebsiella pneumoniae), four opportunistic fungi (Aspergillus flavus, A. fumigatus, A. niger, and Fusarium solani), and four Candida species (C. albicans, C. parapsilosis, C. krusei, and C. tropicalis) using diffusion assay method. The minimum inhibitory concentration (MIC) of the novel synthesized nanometric delafossite was determined using the dilution method. The assayed compounds showed different degrees of antifungal and antibacterial activities, depending on the annealing temperature of preparation of these compounds. Compounds prepared at room temperature showed greater antimicrobial activities than those prepared at higher temperatures. The antimicrobial activity depends also on the susceptibility of the test microbe.


Assuntos
Anti-Infecciosos/farmacologia , Cobre/farmacologia , Compostos Ferrosos/farmacologia , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Testes de Sensibilidade Microbiana
14.
Recent Pat Antiinfect Drug Discov ; 15(2): 157-172, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32753021

RESUMO

BACKGROUND: Malaria is a deadly disease. It is mostly treated using 4- aminoquinoline derivatives such as chloroquine etc. because it is well-tolerated, displays low toxicity, and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for the treatment of malaria. Furthermore, some patents reported hybrids 4-aminoquinolines containing ferrocene moiety with potent antimalarial activity. OBJECTIVE: The objective of the current study is to prepare 4-aminoquinoline-ferrocene hybrids via esterification and amidation reactions. The compounds were characterized via FTIR, LC-MS and NMR spectroscopy. In vitro screening against chloroquine-sensitive P. falciparum parasite (NF54) at concentrations (1 µM and 5 µM) and an inhibitory concentration (full dose-response) was studied. METHODS: The compounds were prepared via known reactions and monitored by Thin Layer Chromatography. The compounds were purified by column chromatography and characterized using FTIR, NMR and MS. In vitro antiplasmodial evaluation was performed against asexual parasite and chloroquine was used as a reference drug. RESULTS: The percentage inhibition effects of the hybrid compounds were in a range of 97.9-102% at 5 µM and 36-96% at 1 µM. Furthermore, the IC50 values of the compounds were in the range of 0.7-1.6 µM when compared to the parent drug, 4-ferrocenylketobutanoic acid. CONCLUSION: The hybrid compounds displayed significant antimalarial activity when compared to the parent drug. However, they were not as effective as chloroquine on the drug-sensitive parasite. The findings revealed that 4-aminoquinolines and ferrocene are potential scaffolds for developing potent antimalarials.


Assuntos
Aminoquinolinas/farmacologia , Antimaláricos/farmacologia , Compostos Ferrosos/farmacologia , Malária Falciparum/tratamento farmacológico , Metalocenos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Aminoquinolinas/química , Aminoquinolinas/uso terapêutico , Antimaláricos/química , Antimaláricos/uso terapêutico , Avaliação Pré-Clínica de Medicamentos , Compostos Ferrosos/química , Compostos Ferrosos/uso terapêutico , Humanos , Concentração Inibidora 50 , Malária Falciparum/parasitologia , Metalocenos/química , Metalocenos/uso terapêutico , Testes de Sensibilidade Parasitária , Patentes como Assunto
15.
J Anim Sci ; 98(7)2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32619217

RESUMO

A total of 140 weanling pigs (241 × 600, DNA, Columbus, NE; initially 5.5 ± 0.79 kg body weight) were used in a 32-d study evaluating the effects of increasing dietary Fe from either iron sulfate (FeSO4) or iron carbonate (FeCO3) on nursery pig growth performance and blood Fe status. The pigs used for this trial did not receive an Fe injection after birth in order to increase the sensitivity to added dietary Fe after weaning. Pigs were weaned at approximately 21 d and allotted to pens based on the initial weight in a completely randomized block design with five pigs in each pen and four pens per treatment. Experimental treatments were arranged as a 2 × 3 + 1 factorial with main effects of dietary Fe source (FeSO4 vs. FeCO3) and level (10, 30, or 50 mg/kg of added Fe) plus a negative control with no additional dietary Fe. The basal diet contained 40 mg/kg total dietary Fe based on ingredient contributions and was formulated with an Fe-free trace mineral premix. Experimental diets were formulated below the pigs recommended Fe requirement based on NRC (2012) estimates. Experimental diets were fed in pellet form in a single phase for the duration of the trial. From day 0 to 32, there was no evidence for source × level interactions for growth performance, hemoglobin (Hb), or hematocrit (Hct) values. There was no evidence for a difference (P > 0.10) in dietary Fe source. Providing increasing Fe levels in the diet from either FeSO4 or FeCO3 improved (P < 0.05) average daily gain, average daily feed intake, gain-to-feed ratio, and increased (P < 0.05) Hb and Hct values. A day effect (P = 0.001) was observed for both Hb and Hct with values increasing throughout the study. Increasing dietary Fe levels in the diet from either FeSO4 or FeCO3 increased (linear; P < 0.05) Hb and Hct values on days 14, 21, and 32. In summary, these data suggest that the micronized form of FeCO3 is a source of Fe that can be added to nursery diets to yield similar responses to those observed from FeSO4 supplementation. Similar to previous research, increasing dietary Fe improved the growth performance and increased Hb and Hct values when pigs have low Fe status at weaning.


Assuntos
Ração Animal/análise , Carbonatos/farmacologia , Compostos Férricos/farmacologia , Compostos Ferrosos/farmacologia , Ferro/administração & dosagem , Suínos/crescimento & desenvolvimento , Fenômenos Fisiológicos da Nutrição Animal , Animais , Peso Corporal/efeitos dos fármacos , Carbonatos/administração & dosagem , Dieta/veterinária , Feminino , Compostos Férricos/administração & dosagem , Compostos Ferrosos/administração & dosagem , Hematócrito/veterinária , Masculino , Oligoelementos
16.
Chem Res Toxicol ; 33(7): 1815-1821, 2020 07 20.
Artigo em Inglês | MEDLINE | ID: mdl-32299210

RESUMO

Oxidative stress is associated with the pathophysiology of many degenerative human diseases, including Alzheimer's disease, atherosclerosis, Parkinson's disease, and cancers. We discovered in our previous study that thioproline (SPro), a proline analogue, is generated in oxidant-exposed cells. With the prior observation that SPro served as an efficient nitrile trapping agent, we tested in this study the hypothesis that this oxidative stress generated cysteine-formaldehyde adduct, SPro, may serve as an antioxidant protecting cells from oxidative stress. Interestingly, results showed that HeLa cells cultured in SPro-supplemented culture media are more tolerant of oxidative stress, indicated by a dosage-dependent increase in cell viability. Investigation of the molecular mechanism of the observed increase in cell tolerance to oxidative stress revealed SPro acting as an effective antioxidant by sacrificial oxidation. Results also showed that SPro had been incorporated into cellular proteins and induced changes in protein expression profiles of treated cells. Despite being yet to determine the participation of individual factors to the observed increase of cell tolerance to oxidative stress, this study sheds light on the potential use of SPro as a dietary supplement for protecting humans from oxidative stress-associated degenerative human diseases.


Assuntos
Antioxidantes/farmacologia , Tiazolidinas/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Ácido Edético/farmacologia , Compostos Ferrosos/farmacologia , Glutationa/metabolismo , Células HeLa , Humanos , Peróxido de Hidrogênio/farmacologia , Oxidantes/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Proteômica , Hipoclorito de Sódio/farmacologia
17.
Life Sci ; 245: 117393, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-32017872

RESUMO

AIMS: Receptor for advanced glycation end products (RAGE) production is induced by diabetes. Microglial cells are activated by RAGE and produce inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and oxidative stress markers. Persistent production of TNF-α can provide a link between diabetes and Alzheimer's disease (AD). The purpose of this study was to investigate the effect of concomitant use of omega-3 polyunsaturated fatty acids (ω-3 PUFAs) with iron supplements on microglial cell activation and inflammatory conditions in the hippocampus of type 2 diabetic rats. MAIN METHODS: Diabetic and normal Wistar rats were divided into six groups. Oxidative stress markers (total oxidant status (TOS), total antioxidant capacity (TAC), and malondialdehyde (MDA)), mRNA expression and protein levels of RAGE and TNF-α were evaluated in the hippocampus of the controls and supplemented with ferrous sulfate and ω-3 PUFAs alone and together rats. Also, the entry of microglia cells into the hippocampus was evaluated by immunohistochemistry technique. KEY FINDINGS: Levels of the microglial activation (2.4 fold, p < 0.0001), MDA (84%, p < 0.0001) and oxidative stress index (OSI) (11%, p = 0.0094), mRNA expression and protein contents of RAGE (1.83 fold and 82% respectively) and TNF-α (2.25 fold and 86% respectively) were strongly influenced by negative effect of iron compared to the group receiving only ω-3 PUFAs which was dramatically improved by vitamin E. SIGNIFICANCE: These observations indicated that the co-supplementation of ferrous sulfate with ω-3 PUFAs decreases the anti-inflammatory ability of ω-3 PUFAs in the hippocampus of diabetic rats via RAGE/TNF-α-induced oxidative stress pathway up-regulation.


Assuntos
Diabetes Mellitus Experimental/metabolismo , Ácidos Graxos Ômega-3/farmacologia , Compostos Ferrosos/farmacologia , Hipocampo/efeitos dos fármacos , Animais , Hipocampo/química , Inflamação/tratamento farmacológico , Malondialdeído/metabolismo , Microglia/efeitos dos fármacos , Microglia/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Receptor para Produtos Finais de Glicação Avançada/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
18.
ACS Appl Mater Interfaces ; 12(7): 8915-8928, 2020 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-31971763

RESUMO

Microbial disinfection associated with medical device surfaces has been an increasing need, and surface modification strategies such as antibacterial coatings have gained great interest. Here, we report the development of polydopamine-ferrocene (PDA-Fc)-functionalized TiO2 nanorods (Ti-Nd-PDA-Fc) as a context-dependent antibacterial system on implant to combat bacterial infection and hinder biofilm formation. In this work, two synergistic antimicrobial mechanisms of the PDA-Fc coating are proposed. First, the PDA-Fc coating is redox-active and can be locally activated to release antibacterial reactive oxygen species (ROS), especially ·OH in response to the acidic microenvironment induced by bacteria colonization and host immune responses. The results demonstrate that redox-based antimicrobial activity of Ti-Nd-PDA-Fc offers antibacterial efficacy of over 95 and 92% against methicillin-resistant Staphylococcus aureus (MRSA) and Escherichia coli (E. coli), respectively. Second, the photothermal effect of PDA can enhance the antibacterial capability upon near-infrared (NIR) irradiation, with over 99% killing efficacy against MRSA and E. coli, and even suppress the formation of biofilm through both localized hyperthermia and enhanced ·OH generation. Additionally, Ti-Nd-PDA-Fc is biocompatible when tested with model pre-osteoblast MC-3T3 E1 cells and promotes cell adhesion and spreading presumably due to its nanotopographical features. The MRSA-infected wound model also indicates that Ti-Nd-PDA-Fc with NIR irradiation can effectively eliminate bacterial infection and suppress host inflammatory responses. We believe that this study demonstrates a simple means to create biocompatible redox-active coatings that confer context-dependent antibacterial activities to implant surfaces.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Materiais Revestidos Biocompatíveis/farmacologia , Compostos Ferrosos/farmacologia , Indóis/farmacologia , Metalocenos/farmacologia , Nanotubos/química , Polímeros/farmacologia , Próteses e Implantes , Células 3T3 , Animais , Escherichia coli/efeitos dos fármacos , Compostos Ferrosos/química , Indóis/química , Masculino , Metalocenos/química , Camundongos , Testes de Sensibilidade Microbiana , Microscopia de Força Atômica , Microscopia Eletrônica de Varredura , Microscopia Eletrônica de Transmissão , Nanotubos/ultraestrutura , Oxirredução , Fototerapia , Polímeros/química , Ratos , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Temperatura , Titânio/química , Titânio/farmacologia , Cicatrização/efeitos dos fármacos , Difração de Raios X
19.
Curr Pharm Biotechnol ; 21(7): 587-595, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31893988

RESUMO

OBJECTIVE: The current study reports a green, rapid and one-pot synthesis of FeSO4 nanoparticles using Hibiscus rosasinensis floral extract as a reducing and capping agent. 0.5M of FeSO4 was stirred with the floral extract of H. rosasinensis for around 20 minutes at 37ºC and pH 7. METHODS: The development of pink color was considered as the endpoint of reduction and the nanoparticles were characterized by UV-Vis spectrum, EDAX, DLS, FTIR, FESEM, and XRD. UV-Vis spectral analysis indicated a peak at 530 nm and EDAX measurement revealed the presence of Fe, S, O and C elements in the nanoparticle sample. The FTIR analysis showed amines, alcohol and alkene groups that act as capping agents for the produced nanoparticles. FESEM and XRD determination presented FeSO4 nanoparticles of 40-60 nm in size. The synthesized nanoparticles were found to have antibacterial activity against 6 pathogenic bacteria with MIC and MBC of 40 mg/mL. RESULTS: To determine the toxicity at the eukaryotic level, brine shrimp toxicity assay was conducted and 100% mortality was found at concentrations >0.06 mg/mL. Gel shift assay suggested the mechanism of toxicity of FeSO4 NPs by binding and degradation of DNA molecules. CONCLUSION: From the results, the authors demonstrate the ease of green synthesis of FeSO4 nanoparticles and its bioactivity that may have potential applications as drugs and drug delivery systems against various diseases.


Assuntos
Antibacterianos/química , Antineoplásicos/química , Dano ao DNA , Compostos Ferrosos/química , Química Verde/métodos , Nanopartículas/química , Animais , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Antineoplásicos/farmacologia , Antineoplásicos/toxicidade , Artemia/efeitos dos fármacos , Artemia/genética , Biofilmes/efeitos dos fármacos , Biofilmes/crescimento & desenvolvimento , Ensaio de Desvio de Mobilidade Eletroforética , Compostos Ferrosos/farmacologia , Compostos Ferrosos/toxicidade , Flores/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hibiscus , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Análise de Sobrevida
20.
Pediatr Neurol ; 104: 30-39, 2020 03.
Artigo em Inglês | MEDLINE | ID: mdl-31917100

RESUMO

BACKGROUND: Insomnia and low iron stores are common in children with autism spectrum disorders, and low iron stores have been associated with sleep disturbance. METHODS: We performed a randomized placebo-controlled trial of oral ferrous sulfate to treat insomnia in children with autism spectrum disorders and low normal ferritin levels. Twenty participants who met inclusion criteria and whose insomnia did not respond to sleep education were randomized to 3 mg/kg/day of ferrous sulfate (n = 9) or placebo (n = 11) for three months. RESULTS: Iron supplementation was well tolerated, and no serious adverse events were reported. Iron supplementation improved iron status (+18.4 ng/mL active versus -1.6 ng/mL placebo, P = 0.044) but did not significantly improve the primary outcome measures of sleep onset latency (-11.0 minutes versus placebo, 95% confidence interval -28.4 to 6.4 minutes, P = 0.22) and wake time after sleep onset (-7.7 minutes versus placebo, 95% confidence interval -22.1 to 6.6 min, P = 0.29) as measured by actigraphy. Iron supplementation was associated with improvement in the overall severity score from the Sleep Clinical Global Impression Scale (-1.5 points versus placebo, P = 0.047). Changes in measures of daytime behavior did not differ between groups. CONCLUSION: This trial demonstrated no improvement in primary outcome measures of insomnia in subjects treated with ferrous sulfate compared with placebo. Interpretation was limited by low enrollment.


Assuntos
Transtorno do Espectro Autista/complicações , Compostos Ferrosos/farmacologia , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Transtorno do Espectro Autista/sangue , Criança , Pré-Escolar , Método Duplo-Cego , Feminino , Ferritinas/sangue , Compostos Ferrosos/administração & dosagem , Humanos , Masculino , Avaliação de Resultados em Cuidados de Saúde , Distúrbios do Início e da Manutenção do Sono/sangue , Distúrbios do Início e da Manutenção do Sono/etiologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA