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1.
Molecules ; 26(14)2021 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-34299656

RESUMO

Chemical composition, antioxidant capacity, and antimicrobial activity of lavender essential oils (LEOs) extracted from three different varieties of Lavandula angustifolia Mill. (1-Moldoveanca 4, 2-Vis magic 10, and 3-Alba 7) have been determined. These plants previously patented in the Republic of Moldova were cultivated in an organic agriculture system in the northeastern part of Romania and then harvested in 3 consecutive years (2017-2019) to obtain the essential oils. From the inflorescences in the complete flowering stage, the LEOs were extracted by hydrodistillation. Then, their composition was analyzed by gas chromatography coupled with mass spectrometry (GC-MS) and by Fourier Transformed Infrared spectroscopy (FT-IR). The major identified constituents are as follows: linalool (1: 32.19-46.83%; 2: 29.93-30.97%; 3: 31.97-33.77%), linalyl acetate (1: 17.70-35.18%; 2: 27.55-37.13%; 3: 28.03-35.32%), and terpinen-4-ol (1: 3.63-7.70%; 2: 3.06-7.16%; 3: 3.10-6.53%). The antioxidant capacity as determined by ABTS and DPPH assays indicates inhibition, with the highest activity obtained for LEO var. Alba 7 from 2019. The in vitro antimicrobial activities of the LEOs and combinations were investigated as well, by using the disk diffusion method and minimum inhibitory concentration (MIC) against the Gram-positive bacterial strain Staphylococcus aureus (ATCC 6538), Gram-negative Pseudomonas aeruginosa (ATCC 27858), Escherichia coli (ATCC 25922), the yeast Candida albicans (ATCC 10231), and clinical isolates. Our results have shown that LEOs obtained from the three studied varieties of L. angustifolia manifest significant bactericidal effects against tested microorganisms (Staphylococcus aureus and Escherichia coli), and antifungal effects against Candida albicans. The mixture of LEOs (Var. Alba 7) and geranium, respectively, in tea tree EOs, in different ratios, showed a significant enhancement of the antibacterial effect against all the studied strains, except Pseudomonas aeruginosa.


Assuntos
Anti-Infecciosos , Antioxidantes , Bactérias/crescimento & desenvolvimento , Candida albicans/crescimento & desenvolvimento , Lavandula/química , Óleos Voláteis , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Óleos Voláteis/farmacologia
2.
Molecules ; 26(13)2021 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-34279380

RESUMO

Cannabis sativa L. (hemp) is a plant used in the textile industry and green building material industry, as well as for the phytoremediation of soil, medical treatments, and supplementary food products. The synergistic effect of terpenes, flavonoids, and cannabinoids in hemp extracts may mediate the biogenic synthesis of metal nanoparticles. In this study, the chemical composition of aqueous leaf extracts of three varieties of Romanian hemp (two monoecious, and one dioecious) have been determined by Fourier-Transformed Infrared spectroscopy (FT-IR), high-performance liquid chromatography, and mass spectrometry (UHPLC-DAD-MS). Then, their capability to mediate the green synthesis of silver nanoparticles (AgNPs) and their pottential antibacterial applications were evaluated. The average antioxidant capacity of the extracts had 18.4 ± 3.9% inhibition determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH•) and 78.2 ± 4.1% determined by 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS™) assays. The total polyphenolic content of the extracts was 1642 ± 32 mg gallic acid equivalent (GAE) L-1. After this, these extracts were reacted with an aqueous solution of AgNO3 resulting in AgNPs, which were characterized by UV-VIS spectroscopy, FT-IR, scanning electron microscopy (SEM-EDX), and dynamic light scattering (DLS). The results demonstrated obtaining spherical, stable AgNPs with a diameter of less than 69 nm and an absorbance peak at 435 nm. The mixture of extracts and AgNPs showed a superior antioxidant capacity of 2.3 ± 0.4% inhibition determined by the DPPH• assay, 88.5 ± 0.9% inhibition as determined by the ABTS•+ assay, and a good antibacterial activity against several human pathogens: Escherichia coli, Klebsiella pneumoniae, Pseudomonas fluorescens, and Staphylococcus aureus.


Assuntos
Antibacterianos/química , Cannabis/química , Química Verde/métodos , Nanopartículas Metálicas/química , Extratos Vegetais/química , Antioxidantes/química , Folhas de Planta/química , Polifenóis/análise , Prata/química
3.
Sci Rep ; 10(1): 21322, 2020 12 07.
Artigo em Inglês | MEDLINE | ID: mdl-33288856

RESUMO

Satureja hortensis is one of the representative plants from the Lamiaceae family, and its essential oil has been used in various applicative fields, from the food industry to aromatherapy. The changes that occur in heated samples at different temperatures (160, 175, 190 ºC) over different periods (0.5 and 2.5 h) in Satureja hortensis essential oil composition and chemical properties were evaluated. The results showed that the major chemical composition constituents of the investigated essential oil are γ-terpinene + α-terpinolene and carvacrol + p-cymene and the thermal behavior is dependent on the content. This composition drastically changes through the heating of the samples and causes significant changes in thermal behavior. The present study demonstrated that the concentration of carvacrol in S. hortensis essential oil is increasing after heating treatment, and the sample heated at 190 ºC for 2.5 h contained more than 91% carvacrol. This simple treatment is a rapid way to obtain carvacrol from the essential oil that has high potential as a natural preservative suitable for the food industry and alternative and complementary medicine.

4.
PLoS One ; 13(7): e0200314, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29995918

RESUMO

The aim of the present study was to establish the influence of high-temperature heating on the composition and thermal behavior of coffee oils obtained from Arabica green and roasted coffee beans, respectively. Morphological studies performed using scanning electron microscopy revealed the oil bodies uniformly distributed within the cells in both types of coffee beans analyzed. The obtained oils have a fatty acid composition rich in linoleic acid, palmitic acid, oleic acid, stearic acid, arachidic acid and linolenic acid. The total content of saturated fatty acids of investigated oils was 49.38 and 46.55%, the others being unsaturated fatty acids. The thermal behavior and thermo-oxidative stability of coffee oils extracted from green coffee beans and roasted coffee beans, the coffee oil high-temperature heated up to 200 °C, were investigated using simultaneous thermal analysis TG/DTG/DTA, in an oxidizing atmosphere. The data obtained for the analyzed samples depend mainly on the nature and compositions of fatty acids, and to a lesser extent on the roasting process of the coffee beans and the high-temperature heating process of the extracted oil. The chromatographic and TG/DTG/DTA data suggest that Arabica coffee oil has great potential for use in technological processes which require high-temperature heating (e.g. food industry or pastries).


Assuntos
Café/química , Extratos Vegetais/química , Óleos Vegetais/química , Café/ultraestrutura , Ácidos Graxos/análise , Cromatografia Gasosa-Espectrometria de Massas , Temperatura Alta , Microscopia Eletrônica de Varredura , Oxirredução , Sementes/química , Sementes/ultraestrutura
5.
ACS Nano ; 8(3): 1972-94, 2014 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-24559246

RESUMO

The intrinsic property of cell-penetrating peptides (CPPs) to deliver therapeutic molecules (nucleic acids, drugs, imaging agents) to cells and tissues in a nontoxic manner has indicated that they may be potential components of future drugs and disease diagnostic agents. These versatile peptides are simple to synthesize, functionalize, and characterize yet are able to deliver covalently or noncovalently conjugated bioactive cargos (from small chemical drugs to large plasmid DNA) inside cells, primarily via endocytosis, in order to obtain high levels of gene expression, gene silencing, or tumor targeting. Typically, CPPs are often passive and nonselective yet must be functionalized or chemically modified to create effective delivery vectors that succeed in targeting specific cells or tissues. Furthermore, the design of clinically effective systemic delivery systems requires the same amount of attention to detail in both design of the delivered cargo and the cell-penetrating peptide used to deliver it.


Assuntos
Peptídeos Penetradores de Células/síntese química , Peptídeos Penetradores de Células/metabolismo , Portadores de Fármacos/síntese química , Portadores de Fármacos/metabolismo , Desenho de Fármacos , Sequência de Aminoácidos , Animais , Peptídeos Penetradores de Células/química , Portadores de Fármacos/química , Humanos , Dados de Sequência Molecular , Nanopartículas/química , Nanopartículas/metabolismo , Transporte Proteico
6.
Hum Reprod ; 28(7): 1874-89, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23585561

RESUMO

STUDY QUESTION: Do cell penetrating peptides (CPPs) translocate into spermatozoa and, if so, could they be utilized to deliver a much larger protein cargo? SUMMARY ANSWER: Chemically diverse polycationic CPPs rapidly and efficiently translocate into spermatozoa. They exhibit differential accumulation within intracellular compartments without detrimental influences upon cellular viability or motility but they are relatively ineffective in transporting larger proteins. WHAT IS ALREADY KNOWN: Endocytosis, the prevalent route of protein internalization into eukaryotic cells, is severely compromised in mature spermatozoa. Thus, the translocation of many bioactive agents into sperm is relatively inefficient. However, the delivery of bioactive moieties into mature spermatozoa could be significantly improved by the identification and utility of an efficient and inert vectorial delivery technology. STUDY DESIGN: CPP translocation efficacies, their subsequent differential intracellular distribution and the influence of peptides upon viability were determined in bovine spermatozoa. Temporal analyses of sperm motility in the presence of exogenously CPPs utilized normozoospermic human donor samples. MATERIALS AND METHODS: CPPs were prepared by manual, automated and microwave-enhanced solid phase synthesis. Confocal fluorescence microscopy determined the intracellular distribution of rhodamine-conjugated CPPs in spermatozoa. Quantitative uptake and kinetic analyses compared the translocation efficacies of chemically diverse CPPs and conjugates of biotinylated CPPs and avidin. 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) conversion assays were employed to analyse the influence of CPPs upon sperm cell viability and sperm class assays determined the impact of CPPs on motility in capacitated and non-capacitated human samples. MAIN RESULTS: Chemically heterogeneous CPPs readily translocated into sperm to accumulate within discrete intracellular compartments. Mitoparan (INLKKLAKL(Aib)KKIL), for example, specifically accumulated within the mitochondria located in the sperm midpiece. The unique plasma membrane composition of sperm is a critical factor that directly influences the uptake efficacy of structurally diverse CPPs. No correlations in efficacies were observed when comparing CPP uptake into sperm with either uptake into fibroblasts or direct translocation across a phosphatidylcholine membrane. These comparative investigations identified C105Y (CSIPPEVKFNKPFVYLI) as a most efficient pharmacokinetic modifier for general applications in sperm biology. Significantly, CPP uptake induced no detrimental influence upon either bovine sperm viability or the motility of human sperm. As a consequence of the lack of endocytotic machinery, the CPP-mediated delivery of much larger protein complexes into sperm is relatively inefficient when compared with the similar process in fibroblasts. LIMITATIONS, REASONS FOR CAUTION: It is possible that some CPPs could directly influence aspects of sperm biology and physiology that were not analysed in this study. WIDER IMPLICATIONS OF THE FINDINGS: CPP technologies have significant potential to deliver selected bioactive moieties and so could modulate the biology and physiology of human sperm biology both prior- and post-fertilization.


Assuntos
Peptídeos Penetradores de Células/metabolismo , Motilidade Espermática , Espermatozoides/metabolismo , Animais , Bovinos , Permeabilidade da Membrana Celular , Endocitose , Humanos , Masculino , Camundongos , Células NIH 3T3 , Transporte Proteico
7.
Bioconjug Chem ; 24(3): 305-13, 2013 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-23350661

RESUMO

Gliomas are therapeutically challenging cancers with poor patient prognosis. New drug delivery strategies are needed to achieve a more efficient chemotherapy-based approach against brain tumors. The current paper demonstrates development of a tumor-targeted delivery vector that is based on a cell-penetrating peptide pVEC and a novel glioma-targeting peptide sequence gHo. The unique tumor-homing peptide gHo was identified using in vitro phage display technology. The novel delivery vector, which we designated as gHoPe2, was constructed by a covalent conjugation of pVEC, gHo, and a cargo; the latter could be either a labeling moiety (such as a fluorescent marker) or a cytostatic entity. Using a fluorescent marker, we demonstrate efficient uptake of the vector in glioma cells and selective labeling of glioma xenograft tumors in a mouse model. This is the first time that we know where in vitro phage display has yielded an efficient, in vivo working vector. We also demonstrate antitumor efficacy of the delivery vector gHoPe2 using a well-characterized chemotherapeutic drug doxorubicin. Vectorized doxorubicin proved to be more efficient than the free drug in a mouse glioma xenograft model after systemic administration of the drugs. In conclusion, we have characterized a novel glioma-homing peptide gHo, demonstrated development of a new and potential glioma-targeted drug delivery vector gHoPe2, and demonstrated the general feasibility of the current approach for constructing cell-penetrating peptide-based targeted delivery systems.


Assuntos
Neoplasias Encefálicas/tratamento farmacológico , Peptídeos Penetradores de Células/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Vetores Genéticos/administração & dosagem , Glioma/tratamento farmacológico , Sequência de Aminoácidos , Animais , Neoplasias Encefálicas/genética , Linhagem Celular Tumoral , Peptídeos Penetradores de Células/genética , Feminino , Vetores Genéticos/genética , Glioma/genética , Células HEK293 , Células HeLa , Humanos , Camundongos , Camundongos Nus , Dados de Sequência Molecular , Ensaios Antitumorais Modelo de Xenoenxerto/métodos
8.
Biochim Biophys Acta ; 1828(5): 1365-73, 2013 May.
Artigo em Inglês | MEDLINE | ID: mdl-23357356

RESUMO

Harnessing of a branched structure is a novel approach in the design of cell-penetrating peptides and it has provided highly efficient transfection reagents for intracellular delivery of nucleic acids. The new stearylated TP10 analogs, NickFects, condense plasmid DNA, splice correcting oligonucleotides and short interfering RNAs into stable nanoparticles with a size of 62-160nm. Such nanoparticles have a negative surface charge (-11 to -18mV) in serum containing medium and enable highly efficient gene expression, splice correction and gene silencing. One of the novel peptides, NickFect51 is capable of transfecting plasmid DNA into a large variety of cell lines, including refractory suspension and primary cells and in several cases exceeds the transfection level of commercially available reagent Lipofectamine™ 2000 without any cytotoxic side effects. Additionally we demonstrate the advantages of NickFect51 in a protein production system, QMCF technology, for expression and production of recombinant proteins in hardly transfectable suspension cells.


Assuntos
Peptídeos Penetradores de Células/química , Técnicas de Transferência de Genes , Vetores Genéticos/genética , Ácidos Nucleicos/genética , Sequência de Aminoácidos , Animais , Células CHO , Linhagem Celular Tumoral , Membrana Celular/metabolismo , Membrana Celular/ultraestrutura , Células Cultivadas , Cricetinae , Cricetulus , Vetores Genéticos/química , Células HEK293 , Células HeLa , Humanos , Células Jurkat , Luciferases/genética , Microscopia Eletrônica de Transmissão , Nanopartículas/química , Nanopartículas/ultraestrutura , Oligonucleotídeos/genética , Plasmídeos/química , Plasmídeos/genética , RNA Interferente Pequeno/genética , Ácidos Esteáricos/química , Transfecção/métodos
9.
Bioconjug Chem ; 22(11): 2255-62, 2011 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-21978260

RESUMO

Cell-penetrating peptide based vehicles have been developed for the delivery of different payloads into the cells in culture and in animals. However, several biological features, among which is the tendency to trigger innate immune response, limit the development of highly efficient peptide-based drug delivery vectors. This study aims to evaluate the influence of transportan 10 (TP10) and its chemically modified derivatives, PepFects (PFs), on the innate immune response of the host system. PFs have shown high efficiency in nucleic acid delivery in vitro and in vivo; hence, the estimation of their possible toxic side effects would be of particular interest. In this study, we analyzed cytotoxic and immunogenic response of PF3, PF4, and PF6 peptides in monocytic leukemia and peripheral blood mononuclear cell lines. In comparison with amphipathic PFs, TP10, TAT, stearyl-(RxR)(4) peptides, and the most widely used transfection reagents Lipofectamine 2000 and Lipofectamine RNAiMAX were also analyzed in this study. IL-1ß, IL-18, and TNF-α cytokine release was detected using highly sensitive enzyme-linked immunosorbent assay (ELISA). Cell viability was detected by measuring the activity of cellular enzymes that reduce water-soluble tetrazolium salts to formazan dyes and apoptosis was evaluated by measuring the levels of caspase-1 and caspase-3/7 over untreated cells. All peptides were found to be nontoxic and nonimmunogenic in vitro at the concentrations of 10 µM and 5 µM, respectively, and at a dose of 5 mg/kg in vivo, suggesting that these CPPs exhibit a promising potential in the delivery of therapeutic molecules into the cell without risks of toxicity and inflammatory reactions.


Assuntos
Peptídeos Penetradores de Células/imunologia , Peptídeos Penetradores de Células/toxicidade , Portadores de Fármacos/toxicidade , Galanina/imunologia , Galanina/toxicidade , Proteínas Recombinantes de Fusão/imunologia , Proteínas Recombinantes de Fusão/toxicidade , Venenos de Vespas/imunologia , Venenos de Vespas/toxicidade , Animais , Caspases/metabolismo , Linhagem Celular Tumoral/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Peptídeos Penetradores de Células/química , Peptídeos Penetradores de Células/genética , Células Cultivadas , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Ensaio de Imunoadsorção Enzimática/métodos , Feminino , Galanina/química , Humanos , Interleucina-18/imunologia , Interleucina-1beta/imunologia , Leucócitos Mononucleares/citologia , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/imunologia , Lipopeptídeos/química , Lipopeptídeos/imunologia , Lipopeptídeos/toxicidade , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Proteínas Recombinantes de Fusão/química , Transfecção , Fator de Necrose Tumoral alfa/imunologia , Venenos de Vespas/química
10.
Mol Ther ; 19(8): 1457-67, 2011 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-21343913

RESUMO

Finding suitable nonviral delivery vehicles for nucleic acid-based therapeutics is a landmark goal in gene therapy. Cell-penetrating peptides (CPPs) are one class of delivery vectors that has been exploited for this purpose. However, since CPPs use endocytosis to enter cells, a large fraction of peptides remain trapped in endosomes. We have previously reported that stearylation of amphipathic CPPs, such as transportan 10 (TP10), dramatically increases transfection of oligonucleotides in vitro partially by promoting endosomal escape. Therefore, we aimed to evaluate whether stearyl-TP10 could be used for the delivery of plasmids as well. Our results demonstrate that stearyl-TP10 forms stable nanoparticles with plasmids that efficiently enter different cell-types in a ubiquitous manner, including primary cells, resulting in significantly higher gene expression levels than when using stearyl-Arg9 or unmodified CPPs. In fact, the transfection efficacy of stearyl-TP10 almost reached the levels of Lipofectamine 2000 (LF2000), however, without any of the observed lipofection-associated toxicities. Most importantly, stearyl-TP10/plasmid nanoparticles are nonimmunogenic, mediate efficient gene delivery in vivo, when administrated intramuscularly (i.m.) or intradermally (i.d.) without any associated toxicity in mice.


Assuntos
Peptídeos Penetradores de Células/metabolismo , Técnicas de Transferência de Genes , Vetores Genéticos , Plasmídeos/metabolismo , Transfecção/métodos , Animais , Transporte Biológico , Linhagem Celular , Cricetinae , Cricetulus , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Endossomos/metabolismo , Terapia Genética/métodos , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Ácidos Nucleicos/metabolismo
11.
J Control Release ; 141(1): 42-51, 2010 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-19744531

RESUMO

In recent years, oligonucleotide-based molecules have been intensely used to modulate gene expression. All these molecules share the common feature of being essentially impermeable over cellular membranes and they therefore require efficient delivery vectors. Cell-penetrating peptides are a group of delivery peptides that has been readily used for nucleic acid delivery. In particular, polyarginine and derivates thereof, i.e. the (RxR)(4) peptide, have been applied with success both in vitro and in vivo. A major problem, however, with these arginine-rich peptides is that they frequently remain trapped in endosomal compartments following internalization. The activity of polyarginine has previously been improved by conjugation to a stearyl moiety. Therefore, we sought to investigate what impact such modification would have on the pre-clinically used (RxR)(4) peptide for non-covalent delivery of plasmids and splice-correcting oligonucleotides (SCOs) and compare it with stearylated Arg9 and Lipofectamine 2000. We show that stearyl-(RxR)(4) mediates efficient plasmid transfections in several cell lines and the expression levels are significantly higher than when using unmodified (RxR)(4) or stearylated Arg9. Although the transfection efficiency is lower than with Lipofectamine 2000, we show that stearyl-(RxR)(4) is substantially less toxic. Furthermore, using a functional splice-correction assay, we show that stearyl-(RxR)(4) complexed with 2'-OMe SCOs promotes significant splice correction whereas stearyl-Arg9 fails to do so. Moreover, stearyl-(RxR)(4) promotes dose-dependent splice correction in parity with (RxR)(4)-PMO covalent conjugates, but at least 10-times lower concentration. These features make this stearic acid modified analog of (RxR)(4) an intriguing vector for future in vivo experiments.


Assuntos
Portadores de Fármacos/química , Ácidos Nucleicos/administração & dosagem , Peptídeos/química , Oligonucleotídeos Fosforotioatos/administração & dosagem , Ácidos Esteáricos/química , Processamento Alternativo/efeitos dos fármacos , Processamento Alternativo/genética , Animais , Células CHO , Permeabilidade da Membrana Celular , Proliferação de Células , Cricetinae , Cricetulus , Citometria de Fluxo , Expressão Gênica , Células HeLa , Humanos , Lipídeos , Luciferases/genética , Ácidos Nucleicos/química , Ácidos Nucleicos/genética , Oligonucleotídeos Fosforotioatos/química , Oligonucleotídeos Fosforotioatos/genética , Plasmídeos , Transfecção
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