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1.
Viruses ; 13(2)2021 02 02.
Artigo em Inglês | MEDLINE | ID: mdl-33540713

RESUMO

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has spread globally. Although measures to control SARS-CoV-2, namely, vaccination, medication, and chemical disinfectants are being investigated, there is an increase in the demand for auxiliary antiviral approaches using natural compounds. Here we have focused on hydroxytyrosol (HT)-rich aqueous olive pulp extract (HIDROX®) and evaluated its SARS-CoV-2-inactivating activity in vitro. We showed that the HIDROX solution exhibits time- and concentration-dependent SARS-CoV-2-inactivating activities, and that HIDROX has more potent virucidal activity than pure HT. The evaluation of the mechanism of action suggested that both HIDROX and HT induced structural changes in SARS-CoV-2, which changed the molecular weight of the spike proteins. Even though the spike protein is highly glycosylated, this change was induced regardless of the glycosylation status. In addition, HIDROX or HT treatment disrupted the viral genome. Moreover, the HIDROX-containing cream applied on film showed time- and concentration-dependent SARS-CoV-2-inactivating activities. Thus, the HIDROX-containing cream can be applied topically as an antiviral hand cream. Our findings suggest that HIDROX contributes to improving SARS-CoV-2 control measures.


Assuntos
Antivirais/farmacologia , Olea , Álcool Feniletílico/análogos & derivados , Extratos Vegetais/farmacologia , /efeitos dos fármacos , Administração Tópica , Animais , Antivirais/química , Carboidratos/química , Chlorocebus aethiops , Genoma Viral/efeitos dos fármacos , Glicosilação , Testes de Sensibilidade Microbiana , Álcool Feniletílico/administração & dosagem , Álcool Feniletílico/farmacologia , Fosfoproteínas/química , Extratos Vegetais/química , /fisiologia , Creme para a Pele , Glicoproteína da Espícula de Coronavírus/química , Células Vero , Inativação de Vírus/efeitos dos fármacos
2.
Molecules ; 26(2)2021 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-33430068

RESUMO

Cutaneous melanoma is the deadliest type of skin cancer, characterized by a high molecular and metabolic heterogeneity which contributes to therapy resistance. Despite advances in treatment, more efficient therapies are needed. Olive oil compounds have been described as having anti-cancer properties. Here, we clarified the cytotoxic potential of oleic acid, homovanillyl alcohol, and hydroxytyrosol on melanoma cells. Metabolic viability was determined 48 h post treatment of A375 and MNT1 cells. Metabolic gene expression was assessed by qRT-PCR and Mitogen-Activated Protein Kinase (MAPK) activation by Western blot. Hydroxytyrosol treatment (100 and 200 µM) significantly reduced A375 cell viability (p = 0.0249; p < 0.0001) which, based on the expression analysis performed, is more compatible with a predominant glycolytic profile and c-Jun N-terminal kinase (JNK) activation. By contrast, hydroxytyrosol had no effect on MNT1 cell viability, which demonstrates an enhanced oxidative metabolism and extracellular signal-regulated kinase (ERK) activation. This compound triggered cell detoxification and the use of alternative energy sources in A375 cells, inhibiting JNK and ERK pathways. Despite oleic acid and homovanillyl alcohol demonstrating no effect on melanoma cell viability, they influenced the MNT1 glycolytic rate and A375 detoxification mechanisms, respectively. Both compounds suppressed ERK activation in MNT1 cells. The distinct cell responses to olive oil compounds depend on the metabolic and molecular mechanisms preferentially activated. Hydroxytyrosol may have a cytotoxic potential in melanoma cells with predominant glycolytic metabolism and JNK activation.


Assuntos
Antineoplásicos Fitogênicos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Melanoma , Azeite de Oliva/química , Álcool Feniletílico/análogos & derivados , Neoplasias Cutâneas , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Técnicas de Reprogramação Celular , Humanos , Melanoma/tratamento farmacológico , Melanoma/metabolismo , Melanoma/patologia , Proteínas de Neoplasias/metabolismo , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Neoplasias Cutâneas/tratamento farmacológico , Neoplasias Cutâneas/metabolismo , Neoplasias Cutâneas/patologia
3.
Int J Mol Sci ; 22(3)2021 Jan 27.
Artigo em Inglês | MEDLINE | ID: mdl-33513799

RESUMO

The Mediterranean diet (MD) is a combination of foods mainly rich in antioxidants and anti-inflammatory nutrients that have been shown to have many health-enhancing effects. Extra-virgin olive oil (EVOO) is an important component of the MD. The importance of EVOO can be attributed to phenolic compounds, represented by phenolic alcohols, hydroxytyrosol, and tyrosol, and to secoiridoids, which include oleocanthal, oleacein, oleuropein, and ligstroside (along with the aglycone and glycosidic derivatives of the latter two). Each secoiridoid has been studied and characterized, and their effects on human health have been documented by several studies. Secoiridoids have antioxidant, anti-inflammatory, and anti-proliferative properties and, therefore, exhibit anti-cancer activity. This review summarizes the most recent findings regarding the pharmacological properties, molecular targets, and action mechanisms of secoiridoids, focusing attention on their preventive and anti-cancer activities. It provides a critical analysis of preclinical, in vitro and in vivo, studies of these natural bioactive compounds used as agents against various human cancers. The prospects for their possible use in human cancer prevention and treatment is also discussed.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Iridoides/farmacologia , Neoplasias/prevenção & controle , Azeite de Oliva/análise , Aldeídos/química , Aldeídos/farmacologia , Aldeídos/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Antineoplásicos/uso terapêutico , Antioxidantes/uso terapêutico , Monoterpenos Ciclopentânicos/química , Monoterpenos Ciclopentânicos/farmacologia , Monoterpenos Ciclopentânicos/uso terapêutico , Dieta Mediterrânea , Glucosídeos/química , Glucosídeos/farmacologia , Glucosídeos/uso terapêutico , Humanos , Iridoides/química , Iridoides/isolamento & purificação , Iridoides/uso terapêutico , Neoplasias/dietoterapia , Azeite de Oliva/farmacologia , Fenóis/química , Fenóis/farmacologia , Fenóis/uso terapêutico , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Álcool Feniletílico/uso terapêutico , Piranos/química , Piranos/farmacologia , Piranos/uso terapêutico
4.
Food Chem ; 335: 127576, 2021 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-32739805

RESUMO

The main causes of food spoilage come from the process of oxidation and the contamination by microorganisms. For the purpose of increasing food shelf-life the industries employ different techniques, being the addition of preservatives, one of the most used. The aim of this contribution was to investigate the potential antioxidant properties of tyrosol (4-hydroxyphenethyl alcohol, 4-OH) and tyrosol derived isomers (2-hydroxyphenethyl alcohol, 2-OH and 3-hydroxyphenethyl alcohol, 3-OH) against reactive oxygen species (ROS) and the antimicrobial effect on Staphylococcus aureus and Escherichia coli. Furthermore, the type of antioxidant effect of substrates and commercial antioxidants mixtures was studied. Upon visible-light, the substrates interacted with the vitamin B2 and different ROS were generated. All the compounds deactivated O2(1Δg) and O2●-, whereas only 2-OH and 3-OH inhibited H2O2 and HO●. The substrates exhibited a synergistic antioxidant effect when combined with commercial antioxidants. 2-OH showed antimicrobial activity against strains tested.


Assuntos
Aditivos Alimentares/farmacologia , Álcool Feniletílico/análogos & derivados , Riboflavina/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Sinergismo Farmacológico , Peróxido de Hidrogênio/química , Radical Hidroxila/química , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia
5.
Ecotoxicol Environ Saf ; 207: 111578, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33254423

RESUMO

Cadmium (Cd), an environmental pollutant, is evidenced to cause hepatotoxicity. In this study, the potential protective effect of caffeic acid phenethyl ester (CAPE) on cadmium-induced liver damage was investigated. Forty male mice were treated daily with either CdCl2 (1.5 mg/kg body weight (b.w.), gavage) or CAPE (10 µmol/kg b.w., gavage) or both for 4 weeks. CAPE administration significantly reduced Cd level and liver and body weight, and increased AST, ALT and ALP level. Moreover, CAPE prevented CdCl2-induced oxidative stress via PI3K/Akt/mTOR pathway and inhibited apoptosis by regulating apoptosis markers. CAPE also suppressed the CdCl2-induced inflammation by reducing the inflammatory mediators, including TNF-α, IL-6 and IL-1ß. Furthermore, CAPE alleviated CdCl2-induced reduction of TLR4. It should be noted that this effect was achieved by targeting miR-182-5p, and CAPE improved miR-182-5p level. The improvement of the liver tissue histopathology by CAPE confirmed the biochemical data. These results show for the first time that miR-182-5p/TLR4 axis involved in CAPE's protection against CdCl2-induced hepatotoxicity, and may provide novel insights into the treatment of cadmium-related diseases.


Assuntos
Cádmio/toxicidade , Ácidos Cafeicos/farmacologia , Poluentes Ambientais/toxicidade , Álcool Feniletílico/análogos & derivados , Substâncias Protetoras/farmacologia , Animais , Apoptose/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas , Inflamação , Mediadores da Inflamação/metabolismo , Masculino , Camundongos , MicroRNAs/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Fosfatidilinositol 3-Quinases/metabolismo , Papel (figurativo) , Receptor 4 Toll-Like/metabolismo
6.
Food Chem ; 345: 128468, 2021 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-33341300

RESUMO

Antioxidant interactions of γ-terpinene with α-tocopherol mimic 2,2,5,7,8-pentamethyl-6-chromanol (PMHC) and caffeic acid phenethyl ester (CAPE), used as models, respectively, of mono- and poly-phenols were demonstrated by differential oximetry during the inhibited autoxidation of model substrates: stripped sunflower oil, squalene, and styrene. With all substrates, γ-terpinene acts synergistically regenerating the chain-breaking antioxidants PMHC and CAPE from their radicals, via the formation of hydroperoxyl radicals. The inhibition duration for mixtures PMHC/γ-terpinene and CAPE/γ-terpinene increased with γ-terpinene concentration, while rate constants for radical-trapping were unchanged by γ-terpinene, being 3.1 × 106 and 4.8 × 105 M-1s-1 for PMHC and CAPE in chlorobenzene (30 °C). Using 3,5-di-tert-butylcatechol and 3,5-di-tert-butyl-1,2-bezoquinone we demonstrate that γ-terpinene can reduce quinones to catechols enabling their antioxidant activity. The different synergy mechanism of γ-terpinene with mono- and poly-phenolic antioxidants is discussed and its relevance is proven in homogenous lipids using natural α-tocopherol and hydroxytyrosol as antioxidants, calling for further studies in heterogenous food products.


Assuntos
Monoterpenos Cicloexânicos/química , Monoterpenos Cicloexânicos/farmacologia , Peróxidos/química , Fenóis/química , Fenóis/farmacologia , Polifenóis/química , Polifenóis/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Ácidos Cafeicos/química , Ácidos Cafeicos/farmacologia , Cromanos/química , Cromanos/farmacologia , Sinergismo Farmacológico , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia
7.
Artigo em Inglês | MEDLINE | ID: mdl-32575426

RESUMO

Recent advances in phytomedicine have explored some potential candidates for nerve regeneration, including hydroxytyrosol (HT). This study was undertaken to explore the potential effects of HT on human Schwann cells' proliferation. Methods: The primary human Schwann cell (hSC) was characterized, and the proliferation rate of hSC supplemented with various concentrations of HT was determined via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell cycle analysis and protein expression of glial fibrillary acidic protein (GFAP) and p75 nerve growth factor receptor (p75 NGFR) were evaluated via the immunofluorescence technique. Results: In vitro culture of hSCs revealed spindle-like, bipolar morphology with the expression of specific markers of hSC. Hydroxytyrosol at 10 and 20 ng/mL significantly increased the proliferation of hSCs by 30.12 ± 5.9% and 47.8 ± 6.7% compared to control (p < 0.05). Cell cycle analysis showed that HT-treated hSCs have a higher proliferation index (16.2 ± 0.2%) than the control (12.4 ± 0.4%) (p < 0.01). In addition, HT significantly increased the protein expression of GFAP and p75NGFR (p < 0.05). Conclusion: HT stimulates the proliferation of hSCs in vitro, indicated by a significant increase in the hSC proliferation index and protein expression of hSCs' proliferation markers, namely p75 NGFR and GFAP.


Assuntos
Antioxidantes , Proliferação de Células , Regeneração Nervosa , Álcool Feniletílico/análogos & derivados , Células de Schwann , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Humanos , Regeneração Nervosa/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Células de Schwann/efeitos dos fármacos
8.
Adv Exp Med Biol ; 1195: 77-91, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32468462

RESUMO

Neurodegenerative diseases lead to the death of nerve cells in the brain or the spinal cord. A wide range of diseases are included within the group of neurodegenerative disorders, with the most common ones being dementia, Alzheimer's, and Parkinson's diseases. Millions of older people are suffering from such pathologies. The global increase of life expectancy unavoidably leads to a consequent increase in the number of people who will be at some degree affected by neurodegenerative-related diseases. At this moment, there is no effective therapy or treatment that can reverse the loss of neurons. A growing number of studies highlight the value of the consumption of medical foods, and in particular olive oil, as one of the most important components of the Mediterranean diet. A diet based on extra virgin olive oil seems to contribute toward the lowering of risk of age-related pathologies due to high phenol concentration. The link of a polyphenol found in extra virgin olive oil, namely, tyrosol, with the protein tyrosinase, associated to Parkinson's disease is underlined as a paradigm of affiliation between polyphenols and neurodegenerative disorders.


Assuntos
Doenças Neurodegenerativas/prevenção & controle , Azeite de Oliva/química , Azeite de Oliva/farmacologia , Polifenóis/química , Polifenóis/farmacologia , Dieta Mediterrânea , Humanos , Doenças Neurodegenerativas/dietoterapia , Azeite de Oliva/uso terapêutico , Álcool Feniletílico/análogos & derivados , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Álcool Feniletílico/uso terapêutico , Polifenóis/uso terapêutico
9.
Ecotoxicol Environ Saf ; 197: 110610, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32298858

RESUMO

Cadmium pollution and poisoning are serious environmental and pharmacological concerns, and effective drugs can alleviate or offset cadmium-induced toxicity are badly needed. In this study, Caffeic acid phenethyl ester (CAPE), a major active component of propolis, showed protective effect against CdCl2-induced toxicology by suppressing autophagy in HepG2 cells. CircRNAs are increasingly perceived as vital regulators in the process of autophagy. However, it remain unclear whether circRNAs are involved in CAPE's protection against CdCl2-induced autophagy. Under this context, the roles of CircRNA (hsa_circ_0040768) in CAPE's protection against CdCl2-induced damage were investigated by PCR and Western blot. Results showed that CAPE significantly (P < 0.05) increased cell viability via inhibiting CdCl2-induced autophagy, and this process was regulated by hsa_circ_0040768/MAP1LC3B axis. Overexpressing hsa_circ_0040768 led to reduced cell viability and increased autophagy in CAPE-treated HepG2 cells exposed to CdCl2. In contrast, silencing hsa_circ_0040768 showed similar protective effect to CAPE. These results show for the first time the involvement of the hsa_circ_0040768/MAP1LC3B axis in the CAPE's protection against CdCl2-induced autophagy, and provide novel insights into the pathogenesis and potential prevention/treatment of cadmium-associated diseases.


Assuntos
Autofagia/efeitos dos fármacos , Cádmio/toxicidade , Ácidos Cafeicos/farmacologia , Poluentes Ambientais/toxicidade , Álcool Feniletílico/análogos & derivados , RNA Circular/metabolismo , Autofagia/genética , Células Hep G2 , Humanos , Álcool Feniletílico/farmacologia
10.
Sci Rep ; 10(1): 6512, 2020 04 16.
Artigo em Inglês | MEDLINE | ID: mdl-32300184

RESUMO

Sustainable, low impact control methods, including mating disruption and microbial insecticides against L. botrana have been available for decades. Yet, successful implementation has been restricted to only a few grapevine districts in the world. A limiting factor is the lack of a female attractant to either monitor or control the damaging sex. Volatile attractants for both female and male insects can be used to assess when L. botrana populations exceed economic thresholds, and to decrease the use of synthetic pesticides within both conventional and pheromone programs. Rather than using host-plant volatiles, which are readily masked by background volatiles released by the main crop, we tested the attractiveness of volatiles that signify microbial breakdown and more likely stand out against the background odour. A two-component blend of 2-phenylethanol (2-PET) and acetic acid (AA) caught significant numbers of both sexes. Catches increased with AA and, to a minimal extent, 2-PET loads. However, a higher load of 2-PET also increased bycatches, especially of Lepidoptera and Neuroptera. Major (ethanol, ethyl acetate, 3-methyl-1-butanol) or minor (esters, aldehydes, alcohols and a ketone) fermentation volatiles, did surprisingly not improve the attraction of L. botrana compared to the binary blend of 2-PET and AA alone, but strongly increased bycatches. The most attractive lure may thus not be the best choice in terms of specificity. We suggest that future research papers always disclose all bycatches to permit evaluation of lures in terms of sustainability.


Assuntos
Lepidópteros/efeitos dos fármacos , Odorantes , Comportamento Sexual Animal/efeitos dos fármacos , Compostos Orgânicos Voláteis/farmacologia , Ácido Acético/química , Ácido Acético/farmacologia , Animais , Feminino , Humanos , Lepidópteros/patogenicidade , Lepidópteros/fisiologia , Masculino , Controle de Pragas , Praguicidas/química , Praguicidas/farmacologia , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Feromônios/antagonistas & inibidores , Feromônios/metabolismo , Atrativos Sexuais/química , Atrativos Sexuais/farmacologia , Especificidade da Espécie , Vitis/parasitologia , Compostos Orgânicos Voláteis/química
11.
Int J Mol Sci ; 21(7)2020 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-32276415

RESUMO

Numerous studies highlighted the beneficial effects of the Mediterranean diet (MD) in maintaining health, especially during ageing. Even neurodegeneration, which is part of the natural ageing process, as well as the foundation of ageing-related neurodegenerative disorders like Alzheimer's and Parkinson's disease (PD), was successfully targeted by MD. In this regard, olive oil and its polyphenolic constituents have received increasing attention in the last years. Thus, this study focuses on two main olive oil polyphenols, hydroxytyrosol (HT) and oleuropein aglycone (OLE), and their effects on ageing symptoms with special attention to PD. In order to avoid long-lasting, expensive, and ethically controversial experiments, the established invertebrate model organism Caenorhabditis elegans was used to test HT and OLE treatments. Interestingly, both polyphenols were able to increase the survival after heat stress, but only HT could prolong the lifespan in unstressed conditions. Furthermore, in aged worms, HT and OLE caused improvements of locomotive behavior and the attenuation of autofluorescence as a marker for ageing. In addition, by using three different C. elegans PD models, HT and OLE were shown i) to enhance locomotion in worms suffering from α-synuclein-expression in muscles or rotenone exposure, ii) to reduce α-synuclein accumulation in muscles cells, and iii) to prevent neurodegeneration in α-synuclein-containing dopaminergic neurons. Hormesis, antioxidative capacities and an activity-boost of the proteasome & phase II detoxifying enzymes are discussed as potential underlying causes for these beneficial effects. Further biological and medical trials are indicated to assess the full potential of HT and OLE and to uncover their mode of action.


Assuntos
Acetatos/uso terapêutico , Monoterpenos Ciclopentânicos/uso terapêutico , Neurônios Dopaminérgicos/metabolismo , Doença de Parkinson/prevenção & controle , Álcool Feniletílico/análogos & derivados , Piranos/uso terapêutico , alfa-Sinucleína , Acetatos/farmacologia , Animais , Animais Geneticamente Modificados , Caenorhabditis elegans/efeitos dos fármacos , Monoterpenos Ciclopentânicos/farmacologia , Modelos Animais de Doenças , Neurônios Dopaminérgicos/fisiologia , Álcool Feniletílico/farmacologia , Álcool Feniletílico/uso terapêutico , Polifenóis/farmacologia , Piranos/farmacologia , Resultado do Tratamento
12.
Sci Rep ; 10(1): 6361, 2020 04 14.
Artigo em Inglês | MEDLINE | ID: mdl-32286485

RESUMO

Olive oil intake has been linked with a lower incidence of breast cancer. Hypoxic microenvironment in solid tumors, such as breast cancer, is known to play a crucial role in cancer progression and in the failure of anticancer treatments. HIF-1 is the foremost effector in hypoxic response, and given that hydroxytyrosol (HT) is one of the main bioactive compounds in olive oil, in this study we deepen into its modulatory role on HIF-1. Our results in MCF-7 breast cancer cells demonstrate that HT decreases HIF-1α protein, probably by downregulating oxidative stress and by inhibiting the PI3K/Akt/mTOR pathway. Strikingly, the expression of HIF-1 target genes does not show a parallel decrease. Particularly, adrenomedullin and vascular endothelial growth factor are up-regulated by high concentrations of HT even in HIF-1α silenced cells, pointing to HIF-1-independent mechanisms of regulation. In fact, we show, by in silico modelling and transcriptional analysis, that high doses of HT may act as an agonist of the aryl hydrocarbon receptor favoring the induction of these angiogenic genes. In conclusion, we suggest that the effect of HT in a hypoxic environment is largely affected by its concentration and involves both HIF-1 dependent and independent mechanisms.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Subunidade alfa do Fator 1 Induzível por Hipóxia/genética , Azeite de Oliva/farmacologia , Fenol/farmacologia , Álcool Feniletílico/análogos & derivados , Neoplasias da Mama/genética , Feminino , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Células MCF-7 , Azeite de Oliva/química , Fenol/química , Álcool Feniletílico/metabolismo , Álcool Feniletílico/farmacologia , Fosfatidilinositol 3-Quinases/genética , Proteínas Proto-Oncogênicas c-akt/genética , Transdução de Sinais/efeitos dos fármacos , Serina-Treonina Quinases TOR/genética
13.
J Appl Microbiol ; 129(2): 278-286, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32097516

RESUMO

AIMS: The aim of the study was to investigate the antifungal effects of a quorum sensing-molecule, 2-phenylethanol, against the food spoilage moulds Penicillium expansum and Penicillium nordicum. METHODS AND RESULTS: Conidial germination of the tested Penicillium spp. (three strains in total) were inhibited by treatments with 2-phenylethanol in a concentration-dependent manner. Germinated conidia was significantly reduced from 4·4-16·7% at 7·5 mmol l-1 and completely inhibited at 15 mmol l-1 2-phenylethanol. Integrity of conidial cell membranes was unaffected by 2-phenylethanol resulting in reversible inhibition pattern of germination. In contrast, membrane permeability of actively growing hyphae was severely compromised, showing 63·5 - 75·7% membrane damage upon treatment with 15 mmol l-1 2-phenylethanol. The overall inhibitory effect of 2-phenylethanol on colony development and growth of P. expansum and P. nordicum was additionally confirmed. CONCLUSIONS: 2-phenylethanol inhibits conidial germination and growth of P. expansum and P. nordicum in a nonlethal, reversible and concentration-dependent manner. SIGNIFICANCE AND IMPACT OF THE STUDY: The study indicates that 2-phenylethanol can find potential application as an antifungal agent for biological control of moulds in the food industry.


Assuntos
Antifúngicos/farmacologia , Penicillium/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Hifas/efeitos dos fármacos , Penicillium/crescimento & desenvolvimento , Percepção de Quorum , Esporos Fúngicos/efeitos dos fármacos , Esporos Fúngicos/crescimento & desenvolvimento
14.
Molecules ; 25(3)2020 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-32033066

RESUMO

The incidence of gastrointestinal cancers is increasing every year. Irinotecan (CPT-11), a drug used in the treatment of colorectal cancer and gastric cancer, is metabolized by carboxylesterases to an active metabolite, SN-38, which is more cytotoxic. CAPE (caffeic acid phenethyl ester) is an active component of propolis, which has a high antibacterial, antiviral, and antineoplastic potential. This study analyses the impact of CAPE on the cytotoxic (MTT assay), genotoxic (comet assay) and proapoptotic (caspase-3/7 activity) potential of irinotecan and its metabolite SN-38 in cultures of gastrointestinal neoplastic cells (HCT116, HT29, AGS). Cytotoxicity and genotoxicity activities of these compounds were carried out in comparison with human peripheral blood lymphocytes (PBLs) in vitro. The antioxidant potential of CAPE was investigated in relation H2O2-induced oxidative stress in the both neoplastic cells and PBLs. CAPE expressed cytotoxic, genotoxic, and pro-apoptotic activity against AGS, HCT116, and HT29 tumor cells. CAPE, in the presence of different concentrations of irinotecan or SN38, decreased the cytotoxicity, genotoxicity, and pro-apoptotic activity in these cell lines, but it has no such action on normal human peripheral blood lymphocytes.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Ácidos Cafeicos/farmacologia , Neoplasias do Colo/tratamento farmacológico , Irinotecano/farmacologia , Álcool Feniletílico/análogos & derivados , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citotoxinas/farmacologia , Dano ao DNA/efeitos dos fármacos , Sinergismo Farmacológico , Células HCT116 , Células HT29 , Humanos , Peróxido de Hidrogênio/toxicidade , Irinotecano/análogos & derivados , Linfócitos/efeitos dos fármacos , Mutagênicos/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Própole/farmacologia , Inibidores da Topoisomerase I/farmacologia
15.
Reprod Domest Anim ; 55(3): 325-332, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31926029

RESUMO

The aim of the present study was to evaluate the effect of the addition of two olive oil-derived antioxidants, hydroxytyrosol (3,4-dihydroxyphenylethanol, HT) and 3,4-dihydroxyphenylglycol (DHPG), on ovine semen during liquid storage at 5°C and 15°C. Semen was collected, pooled, diluted and then divided into aliquots supplemented with different concentrations (5 µg/ml, 10 µg/ml, 50 µg/ml and 100 µg/ml) of HT, DHPG and a mixture (MIX) of both antioxidants. Sperm motility characteristics were assessed in the different samples at 0, 6, 24, 48, 72 and 96 hr after cooling, and a fertility trial was also conducted. The results showed that the antioxidant addition did not significantly improve total and progressive motility in ovine cooled sperm maintained at 15° or 5°C. However, in samples stored at 5°C, LIN (48, 72, 96 hr), STR (0 hr) and WOB (0, 48, 72, 96 hr) values significantly decreased in comparison with control treatment when high antioxidant concentrations were added (MIX100 or HT100). When samples were maintained at 15°C, MIX50 showed significantly higher VCL values than the control treatment after 6 hr cooling, and MIX100 showed significantly lower VCL values at 96 hr after cooling. According to the artificial insemination trial, no significant differences were observed when antioxidants were added. In conclusion, the use of HT and DHPG showed small impact in sperm motility and fertility was not affected (nor detrimentally nor positively) when insemination was carried out using antioxidant-supplemented liquid sperm.


Assuntos
Antioxidantes/farmacologia , Metoxi-Hidroxifenilglicol/análogos & derivados , Álcool Feniletílico/análogos & derivados , Preservação do Sêmen/veterinária , Motilidade Espermática/efeitos dos fármacos , Animais , Feminino , Fertilidade/efeitos dos fármacos , Inseminação Artificial/veterinária , Masculino , Metoxi-Hidroxifenilglicol/farmacologia , Olea/química , Álcool Feniletílico/farmacologia , Sêmen/efeitos dos fármacos , Preservação do Sêmen/métodos , Carneiro Doméstico , Espermatozoides/efeitos dos fármacos , Temperatura
16.
Nanotechnology ; 31(17): 175705, 2020 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-31931488

RESUMO

Due to the resistance to drugs, studies involving the combination and controlled release of different agents are gradually increasing. In this study, two different active ingredients, known to have antibacterial and antiparasitic activities, were encapsulated into single polymeric nanoparticles. After co-encapsulation their antibacterial and antileishmanial activity was enhanced approximately 5 and 250 times, respectively. Antibacterial and antileishmanial activities of caffeic acid phenethyl ester and juglone loaded, multifunctional nanoformulations (CJ4-CJ6-CJ8) were also evaluated for the first time in the literature comparatively with their combined free formulations. The antibacterial activity of the multifunctional nanoformulation (CJ8) were found to have a much higher activity (MIC values 6.25 and 12.5 µg ml-1 for S. aureus and E. coli, respectively) than all other formulations. Similar efficacy for CJ8 was obtained in the antiparasitic study against the Leishmania promastigotes and the IC50 was reduced to 0.1263 µg ml-1. The high activity of multifunctional nanoparticles is not only due to the synergistic effect of the active molecules but also by the encapsulation into polymeric nanoparticles. Therefore, it has been shown in the literature for the first time that the biological activity of molecules whose activity is increased by the synergistic effect can be improved with nanosystems.


Assuntos
Antibacterianos/farmacologia , Antiparasitários/farmacologia , Ácidos Cafeicos/farmacologia , Naftoquinonas/farmacologia , Álcool Feniletílico/análogos & derivados , Antibacterianos/química , Antiparasitários/química , Ácidos Cafeicos/química , Escherichia coli/efeitos dos fármacos , Leishmania/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Nanopartículas , Naftoquinonas/química , Tamanho da Partícula , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Staphylococcus aureus/efeitos dos fármacos
17.
Biomed Res Int ; 2020: 1315202, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31998777

RESUMO

Oleuropein and hydroxytyrosol, as major compounds of olive leaves, have been reported to exert numerous pharmacological properties, including anticancer, antidiabetic, and anti-inflammatory activities. The purpose of this study is to evaluate and compare the protective effect of oleuropein- and hydroxytyrosol-rich extracts, derived from olive leaves, on high-fat diet-induced lipid metabolism disturbance and liver injury in rats. In this respect, four groups of male rats (8 per group) were used: control group (Control), group treated with high-fat diet (HFD), group treated with HFD and oleuropein (HFD + OLE), and group treated with HFD and hydroxytyrosol (HFD + HYD). The current research showed that the treatment with the HFD increased the body weight and adipose tissue mass in male rats. Moreover, the plasma levels of triglycerides, total cholesterol, LDL-cholesterol, AST, ALT, LDH, and TNF-α were also raised. The hepatic immunohistochemical analysis revealed a significant increase in the expression of inflammatory genes (COX-2, NF-κB, and TNF-α). Equally, it showed a rise of the apoptotic markers (a decrease in the expression of the Bcl-2 and an increase of the P53). In addition, the oral administration of oleuropein- and hydroxytyrosol-rich olive leaf extracts at 16 mg/kg similarly reduced the body weight and adipose tissue mass and improved the lipid profile. Moreover, these extracts, mainly the hydroxytyrosol-rich extract, reduced the elevated liver enzymes, enhanced the antioxidant status, and attenuated the liver inflammation and apoptosis. These findings suggest that the oleuropein- and hydroxytyrosol-rich olive leaf extracts possessed hypolipidemic and hepatoprotective effects against the HFD-induced metabolic disorders by enhancing the antioxidative defense system and blocking the expression of the proteins involved in inflammation and liver damage.


Assuntos
Gorduras na Dieta/efeitos adversos , Iridoides/farmacologia , Hepatopatias , Fígado , Olea/química , Álcool Feniletílico/análogos & derivados , Extratos Vegetais/farmacologia , Folhas de Planta/química , Animais , Gorduras na Dieta/farmacologia , Iridoides/química , Metabolismo dos Lipídeos , Fígado/lesões , Fígado/metabolismo , Fígado/patologia , Hepatopatias/tratamento farmacológico , Hepatopatias/metabolismo , Hepatopatias/patologia , Masculino , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Extratos Vegetais/química , Ratos
18.
Cell Tissue Res ; 380(1): 173-189, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31838605

RESUMO

Male reproductive dysfunction represents one of the overlooked consequences of diabetes that still deserve more scientific attention. We designed this study to explore the therapeutic potential of hydroxytyrosol (HT) on diabetic testicular damage and to investigate its relationship with adenosine monophosphate-activated protein kinase (AMPK) expression. In this context, 30 adult male Wistar rats were utilized and subdivided into control, diabetic and HT-treated diabetic groups. Testicular sections were prepared for histopathological examination and immunohistochemical detection of 8-hydroxy-2'-deoxyguanosine, Sertoli cell vimentin, myoid cell α-SMA, androgen receptors and caspase-3. We also assessed oxidative enzymatic and lipid peroxidation biochemical profiles, sperm count, morphology and motility. Real-time PCR of AMPK expression in tissue homogenate was performed. We observed that HT restored testicular histopathological structure and significantly reduced oxidative DNA damage and the apoptotic index. The HT-treated group also exhibited significantly higher Sertoli cell vimentin, myoid cell α-SMA and androgen receptor immune expression than the diabetic group. A rescue of the oxidative enzymatic activity, lipid peroxidation profiles, sperm count, morphology and motility to control levels was also evident in the HT-treated group. Significant upregulation of AMPK mRNA expression in the HT-treated group clarified the role of AMPK as an underlying molecular interface of the ameliorative effects of HT. We concluded that HT exhibited tangible antioxidant and antiapoptotic impacts on the testicular cytomorphological and immunohistochemical effects of experimentally induced diabetes. Furthermore, AMPK has an impactful role in the molecular machinery of these effects.


Assuntos
Proteínas Quinases Ativadas por AMP/biossíntese , Antioxidantes/farmacologia , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/tratamento farmacológico , Álcool Feniletílico/análogos & derivados , Doenças Testiculares/tratamento farmacológico , Doenças Testiculares/enzimologia , 8-Hidroxi-2'-Desoxiguanosina/metabolismo , Proteínas Quinases Ativadas por AMP/metabolismo , Animais , Diabetes Mellitus Experimental/enzimologia , Diabetes Mellitus Experimental/patologia , Masculino , Álcool Feniletílico/farmacologia , Ratos , Ratos Wistar , Doenças Testiculares/etiologia , Testículo/efeitos dos fármacos , Testículo/enzimologia , Testículo/patologia
19.
J Biotechnol ; 308: 82-86, 2020 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-31794783

RESUMO

Lymphedema is a chronic accumulation of interstitial fluid due to inefficient lymph drainage. Major causes of lymphedema are malformations of lymphatic vessels, trauma, toxic damage and surgery. The swelling typically affects the limbs. Lymphedema may be primary, caused by genetic mutations and relatively rare, or secondary (acquired), due to external causes such as infections or surgery. Fluid accumulation induces pathological changes: activation of the inflammatory cascade, immune cell infiltration, tissue fibrosis, adipose accumulation. We focused on the inflammatory phenotype mediated by leukotriene B4, a lipid mediator of the inflammatory pathway, and the potential therapeutic effect of hydroxytyrosol. We conducted an electronic search in PubMed using "lymphedema", "lymphedema pathway", "hydroxytyrosol" as keywords. We found that lymphedema deregulates at least six molecular pathways and that hydroxytyrosol, a compound with antioxidant activity, can improve endothelial dysfunction, hemostatic and lipid profiles, and decrease oxidative stress and inflammation through inhibition of leukotriene B4 activity. This review is the first to highlight the possibility of using hydroxytyrosol to treat the secondary effects of lymphedema, especially inflammation. The possible effects of hydroxytyrosol on lymphedema should be tested in vitro and in vivo to find the best way to treat patients with lymphedema in order to improve their health status.


Assuntos
Antioxidantes/farmacologia , Linfedema/metabolismo , Redes e Vias Metabólicas/efeitos dos fármacos , Álcool Feniletílico/análogos & derivados , Animais , Antioxidantes/uso terapêutico , Regulação da Expressão Gênica/efeitos dos fármacos , Hemostasia , Humanos , Leucotrieno B4/metabolismo , Linfedema/tratamento farmacológico , Linfedema/etiologia , Olea/química , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Álcool Feniletílico/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
20.
J Biotechnol ; 309: 29-33, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31884046

RESUMO

Hydroxytyrosol is a phenolic phytochemical with antioxidant properties in vitro. It is a natural compound that can be found in olive leaves and oil. The main dietary source of hydroxytyrosol is extra virgin olive oil. Due to its bioavailability, chemical properties and easy formulation along with its lack of toxicity, hydroxytyrosol is considered an excellent food supplement by the nutraceutical and food industries. The purpose of this review is to discuss the potential therapeutic effects of hydroxytyrosol in vivo. To do so, we conducted an electronic search in PubMed and other literature databases using "hydroxytyrosol", "beneficial effect/s", "pharmacology" as key-words. From this search, we found that hydroxytyrosol has anti-inflammatory, anti-tumor, antiviral, antibacterial and antifungal properties. Hydroxytyrosol also improves endothelial dysfunction, decreases oxidative stress, and is neuro- and cardio-protective. Due to all these biological properties, hydroxytyrosol is currently the most actively investigated natural phenol. The evidence presented in this review suggests that hydroxytyrosol has great pharmacological potential.


Assuntos
Antioxidantes/farmacologia , Azeite de Oliva/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/análogos & derivados , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Humanos , Olea/química , Azeite de Oliva/química , Fenóis/química , Fenóis/farmacologia , Álcool Feniletílico/química , Álcool Feniletílico/farmacologia , Folhas de Planta/química
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