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1.
Int J Mol Sci ; 25(10)2024 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-38791403

RESUMO

Nowadays, there is an increasing interest in the study of medicinal and aromatic plants, due to their therapeutic properties that correlate with the presence of different active compounds. Agastache species (sp.) are aromatic plants that belong to the Lamiaceae family, originating from North America and East Asia. The present study aimed to evaluate the composition of essential oils (EOs) obtained from different Romanian cultivated Agastache sp. and to investigate their antibacterial and cytotoxic activities. The gas chromatography-mass spectrometry (GC-MS) screening revealed that menthone was the dominant constituent of A. foeniculum (31.58%), A. rugosa (39.60%) and A. rugosa 'After Eight' (39.76%) EOs, while estragole was the major constituent of A. foeniculum "Aromat de Buzau" (63.27%) and A. mexicana (41.66%) EOs. The investigation of the antiproliferative effect showed that A. rugosa and A. foeniculum "Aromat de Buzau" EOs had significant cytotoxic activity on MDA-MB-231 and HEPG2 tumour cell lines, with the most promising effect on the MDA-MB-231 breast cancer cell line for A. foeniculum "Aromat de Buzau" EO (IC50 = 203.70 ± 0.24 µg/mL). Regarding the antibacterial activity, A. rugosa EO was most active against E. coli (8.91 ± 3.27 µL/mL) and S. aureus (10.80 ± 0.00 µL/mL). To the best of our knowledge, this is the first report on the cytotoxic effect of Agastache sp. EOs on MDA-MB-231, HCT116 and HEPG2 tumour cell lines. The results of our study provide new and promising information for the subsequent in vivo study of the pharmacological properties of Agastache sp. essential oils.


Assuntos
Agastache , Antibacterianos , Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis , Humanos , Antibacterianos/farmacologia , Antibacterianos/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Agastache/química , Linhagem Celular Tumoral , Células Hep G2 , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/química , Testes de Sensibilidade Microbiana , Proliferação de Células/efeitos dos fármacos , Compostos Orgânicos Voláteis/farmacologia , Compostos Orgânicos Voláteis/análise , Compostos Orgânicos Voláteis/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química
2.
Molecules ; 29(9)2024 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-38731442

RESUMO

Two series, "a" and "b", each consisting of nine chemical compounds, with 2,3-disubstituted quinazolin-4(3H)-one scaffold, were synthesized and evaluated for their anticonvulsant activity. They were investigated as dual potential positive allosteric modulators of the GABAA receptor at the benzodiazepine binding site and inhibitors of carbonic anhydrase II. Quinazolin-4(3H)-one derivatives were evaluated in vivo (D1-3 = 50, 100, 150 mg/kg, administered intraperitoneally) using the pentylenetetrazole (PTZ)-induced seizure model in mice, with phenobarbital and diazepam, as reference anticonvulsant agents. The in silico studies suggested the compounds act as anticonvulsants by binding on the allosteric site of GABAA receptor and not by inhibiting the carbonic anhydrase II, because the ligands-carbonic anhydrase II predicted complexes were unstable in the molecular dynamics simulations. The mechanism targeting GABAA receptor was confirmed through the in vivo flumazenil antagonism assay. The pentylenetetrazole experimental anticonvulsant model indicated that the tested compounds, 1a-9a and 1b-9b, present a potential anticonvulsant activity. The evaluation, considering the percentage of protection against PTZ, latency until the onset of the first seizure, and reduction in the number of seizures, revealed more favorable results for the "b" series, particularly for compound 8b.


Assuntos
Anticonvulsivantes , Pentilenotetrazol , Receptores de GABA-A , Convulsões , Anticonvulsivantes/farmacologia , Anticonvulsivantes/síntese química , Anticonvulsivantes/química , Animais , Camundongos , Convulsões/tratamento farmacológico , Convulsões/induzido quimicamente , Receptores de GABA-A/metabolismo , Quinazolinonas/farmacologia , Quinazolinonas/química , Quinazolinonas/síntese química , Simulação de Acoplamento Molecular , Masculino , Relação Estrutura-Atividade , Simulação de Dinâmica Molecular , Simulação por Computador , Modelos Animais de Doenças , Estrutura Molecular , Sítio Alostérico
3.
Molecules ; 28(4)2023 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-36838592

RESUMO

The aim of the present study was to correlate the antioxidant, antimicrobial, and cytotoxic activities of hydroalcoholic extracts obtained from the aerial parts of three Dracocephalum moldavica L. cultivars with their polyphenolic compositions. The polyphenols were identified and quantified using spectrophotometrical methods and LC-MS analysis. Their antioxidant capacities were assessed using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods. Their in vitro antimicrobial efficacies were assessed using the agar well diffusion and broth microdilution methods. Their cytotoxicity was investigated on normal diploid foreskin fibroblasts (BJ) and on colorectal adenocarcinoma (DLD-1) cell lines. The results pointed out significant amounts of polyphenolic compounds in the compositions of the tested cultivars, with rosmarinic acid as the main compound (amounts ranging between 5.337 ± 0.0411 and 6.320 ± 0.0535 mg/mL). All three cultivars displayed significant antioxidant (IC50 ranging between 35.542 ± 0.043 and 40.901 ± 0.161 µg/mL for the DPPH assay, and for the FRAP assay 293.194 ± 0.213 and 330.165 ± 0.754 µmol Trolox equivalent/mg dry vegetal material) and antimicrobial potential (especially towards the Gram-positive bacteria), as well as a selective toxicity towards the tumoral line. A significant positive correlation was found between antioxidant activity and the total phenolic acids (r2 = 0.987) and polyphenols (r2 = 0.951). These findings bring further arguments for strongly considering D. moldavica cultivars as promising vegetal products, which warrants further investigation.


Assuntos
Anti-Infecciosos , Antineoplásicos , Antioxidantes/química , Extratos Vegetais/química , Polifenóis/farmacologia , Anti-Infecciosos/farmacologia
4.
Molecules ; 27(8)2022 Apr 18.
Artigo em Inglês | MEDLINE | ID: mdl-35458796

RESUMO

Considering the important damage caused by the reactive oxygen (ROS) and nitrogen (RNS) species in the human organism, the need for new therapeutic agents, with superior efficacy to the known natural and synthetic antioxidants, is crucial. Quinazolin-4-ones are known for their wide range of biological activities, and phenolic compounds display an important antioxidant effect. Linking the two active pharmacophores may lead to an increase of the antioxidant activity. Therefore, we synthesized four series of new hybrid molecules bearing the quinazolin-4-one and phenol scaffolds. Their antioxidant potential was evaluated in vitro, considering different possible mechanisms of action: hydrogen atom transfer, ability to donate electrons and metal ions chelation. Theoretical quantum and thermodynamical calculations were also performed. Some compounds, especially the ortho diphenolic ones, exerted a stronger antioxidant effect than ascorbic acid and Trolox.


Assuntos
Antioxidantes , Fenóis , Antioxidantes/farmacologia , Ácido Ascórbico , Humanos , Relação Estrutura-Atividade
5.
Molecules ; 27(13)2022 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-35807229

RESUMO

Rosmarinus officinalis L. is a species that is widely known for its culinary and medicinal uses. The purpose of the present study consisted of the evaluation of the antiproliferative and antimicrobial effects of R. officinalis-loaded liposomes (L-R). Characterization of the liposomes was performed by establishing specific parameters. The load of the obtained liposomes was analyzed using an LC-MS method, and antiproliferative assays evaluated the cell viability on a liver adenocarcinoma cell line and on a human hepatic stellate cell line. Antimicrobial assays were performed by agar-well diffusion and by broth microdilution assays. The obtained liposomes showed high encapsulation efficiency, suitable particle size, and good stability. High amounts of caffeic (81.07 ± 0.76), chlorogenic (14.10 ± 0.12), carnosic (20.03 ± 0.16), rosmarinic (39.81 ± 0.35), and ellagic (880.02 ± 0.14) acids were found in their composition, together with other polyphenols. Viability and apoptosis assays showed an intense effect on the cancerous cell line and a totally different pattern on the normal cells, indicating a selective toxicity towards the cancerous ones and an anti-proliferative mechanism. Antimicrobial potential was noticed against all tested bacteria, with a better efficacy towards Gram-positive species. These results further confirm the biological activities of R. officinalis leaf extract, and proposes and characterizes novel delivery systems for their encapsulation, enhancing the biological activities of polyphenols, and overcoming their limitations.


Assuntos
Anti-Infecciosos , Rosmarinus , Anti-Infecciosos/farmacologia , Humanos , Lipossomos , Extratos Vegetais/farmacologia , Polifenóis/farmacologia
6.
Molecules ; 26(6)2021 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-33804618

RESUMO

Rosmarinus officinalis L. is a widely known species for its medicinal uses, that is also used as raw material for the food and cosmetic industry. The aim of the present study was to offer a novel perspective on the medicinal product originating from this species and to test its hepatoprotective activity. The tested sample consisted in a tincture obtained from the fresh young shoots. Compounds that are evaluated for this activity are polyphenols and terpenoids, that are identified and quantified by HPLC-UV-MS and GC-MS. Antioxidant activity was assessed in vitro, using the DPPH, FRAP and SO assays. Hepatoprotective activity was tested in rats with experimentally-induced hepatotoxicity. In the chemical composition of the tincture, phenolic diterpenes (carnosic acid, carnosol, rosmanol, rosmadial) and rosmarinic acid were found to be the majority compounds, alongside with 1,8-cineole, camphene, linalool, borneol and terpineol among monoterpenes. In vitro, the tested tincture proved significant antioxidant capacity. Results of the in vivo experiment showed that hepatoprotective activity is based on an antioxidant mechanism. In this way, the present study offers a novel perspective on the medicinal uses of the species, proving significant amounts of polyphenols and terpenes in the composition of the fresh young shoots tincture, that has proved hepatoprotective activity through an antioxidant mechanism.


Assuntos
Antioxidantes/farmacologia , Doença Hepática Induzida por Substâncias e Drogas , Estresse Oxidativo/efeitos dos fármacos , Brotos de Planta/química , Rosmarinus/química , Animais , Antioxidantes/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cinamatos/química , Cinamatos/farmacologia , Depsídeos/química , Depsídeos/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Monoterpenos/química , Monoterpenos/farmacologia , Ratos , Ácido Rosmarínico
7.
Molecules ; 26(11)2021 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-34067400

RESUMO

Syringa vulgaris L. (common lilac) is one of the most popular ornamental species, but also a promising not comprehensively studied source of bioactive compounds with important therapeutic potential. Our study was designed to characterize the chemical composition and to assess the antioxidant and cytotoxic properties of ethanolic extracts obtained from S. vulgaris L. flowers, leaves, bark, and fruit. The chemical profile of the ethanolic extracts was investigated using chromatographic (HPLC-DAD-ESI+, GC-MS) and spectral (UV-Vis, FT-IR) methods, while the protective effect against free radicals was evaluated in vitro by different chemical assays (DPPH, FRAP, CUPRAC). The cytotoxic activity was tested on two tumoral cell lines, HeLa, B16F10, using the MTT assay. Significant amounts of free or glycosylated chemical components belonging to various therapeutically important structural classes, such as phenyl-propanoids (syringin, acteoside, echinacoside), flavonoids (quercetin, kaempferol derivatives) and secoiridoids (secologanoside, oleuropein, 10-hydroxy oleuropein, demethyloleuropein, syringalactone A, nuzhenide, lingstroside) were obtained for the flowers, leaves and bark extracts, respectively. Furthermore, MTT tests pointed out a significant cytotoxic potential expressed in a non-dose-dependent manner toward the tumoral lines. The performed methods underlined that S. vulgaris extracts, in particular belonging to flowers and leaves, represent valuable sources of compounds with antioxidant and antitumoral potential.


Assuntos
Antioxidantes/química , Flores/química , Estresse Oxidativo , Extratos Vegetais/química , Folhas de Planta/química , Syringa/química , Animais , Linhagem Celular Tumoral , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Cromatografia Gasosa-Espectrometria de Massas , Glucosídeos , Glicosídeos , Células HeLa , Humanos , Melanoma Experimental , Camundongos , Fenóis , Fenilpropionatos , Folhas de Planta/metabolismo , Quercetina/análise , Espectroscopia de Infravermelho com Transformada de Fourier
8.
Molecules ; 24(14)2019 Jul 23.
Artigo em Inglês | MEDLINE | ID: mdl-31340530

RESUMO

Solidago species are often used in traditional medicine as anti-inflammatory, diuretic, wound-healing and antimicrobial agents. Still, the bioactive compounds and biological activities of some species have not been studied. The present work aimed to investigate the polyphenolic profile and the biological properties of Solidago graminifolia L. Salisb., a poorly explored medicinal plant. The hydroalcoholic extracts from aerial parts were evaluated for total phenolic content (TPC), total flavonoid content (TFC) and the polyphenolic compounds were investigated by HPLC-MS. The antioxidant potential in vitro was determined using DPPH and FRAP assays. Antibacterial and antifungal effects were evaluated by dilution assays and MIC, MBC and MFC were calculated. The results showed that Solidago graminifolia aerial parts contain an important amount of total phenolics (192.69 mg GAE/g) and flavonoids (151.41 mg RE/g), with chlorogenic acid and quercitrin as major constituents. The hydroalcoholic extracts showed promising antioxidant and antimicrobial potential, with potent antibacterial activity against Staphylococcus aureus and important antifungal effect against Candida albicans and C. parapsilosis. The obtained results indicated that the aerial parts of Solidago graminifolia could be used as novel resource of phytochemicals in herbal preparations with antioxidant and antimicrobial activities.


Assuntos
Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Ácido Clorogênico/isolamento & purificação , Flavonoides/isolamento & purificação , Fenóis/isolamento & purificação , Quercetina/análogos & derivados , Solidago/química , Anti-Infecciosos/classificação , Anti-Infecciosos/farmacologia , Antioxidantes/classificação , Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Candida parapsilosis/efeitos dos fármacos , Candida parapsilosis/crescimento & desenvolvimento , Clorofórmio/química , Ácido Clorogênico/farmacologia , Etanol/química , Flavonoides/classificação , Flavonoides/farmacologia , Metanol/química , Testes de Sensibilidade Microbiana , Fenóis/classificação , Fenóis/farmacologia , Picratos/antagonistas & inibidores , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Quercetina/isolamento & purificação , Quercetina/farmacologia , Solventes/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimento
9.
Molecules ; 24(8)2019 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-31018502

RESUMO

Several Ajuga species are used in Romanian folk medicine for their antioxidant, antimicrobial and anti-inflammatory properties, to treat pain, fever or arthritis. Still, the active compounds responsible for these effects and their mechanism of action are scarcely known. This research was designed to investigate the phytochemical profile (e.g. iridoids, polyphenolic compounds, phytosterols), as well as the biological potential (antioxidant, antibacterial, antifungal, anti-inflammatory properties) of two selected Ajuga species collected from different regions of Romanian spontaneous flora. The main compounds identified in A. reptans aerial parts extracts were 8-O-acetylharpagide, isoquercitrin and ß-sitosterol, whilst in A. genevensis were 8-O-acetylharpagide, luteolin and campesterol. The extracts were screened for their antioxidant potential using different methods (DPPH, TEAC, EPR) and the results showed a good activity, in accordance with the polyphenol content (18-26 mg GAE/g dw). The antifungal activity on the tested strains was good. The determination of few parameters linked with the inflammatory mechanism allowed the assessment of in vivo anti-inflammatory potential. Ajuga reptans and A. genevensis ethanol extracts had anti-inflammatory activity through lowering the oxidative stress, phagocytosis, PMN and total leukocytes. The best anti-oxidative and anti-inflammatory activity was observed for the Ajuga reptans 100 mg dw/mL extract when compared with diclofenac, thus the dose could be correlated with the pharmacological effect. These findings provide substantial evidence that both selected Ajuga species have the potential to be valued as sources of phytochemicals in effective anti-inflammatory herbal preparations.


Assuntos
Ajuga/química , Iridoides/farmacologia , Fitosteróis/farmacologia , Fitoterapia/métodos , Polifenóis/farmacologia , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Compostos de Bifenilo/antagonistas & inibidores , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Humanos , Inflamação/tratamento farmacológico , Iridoides/química , Iridoides/isolamento & purificação , Testes de Sensibilidade Microbiana , Neutrófilos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Fagocitose/efeitos dos fármacos , Fitosteróis/química , Fitosteróis/isolamento & purificação , Picratos/antagonistas & inibidores , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Plantas Medicinais , Polifenóis/química , Polifenóis/isolamento & purificação , Ratos , Ratos Wistar , Romênia
10.
Molecules ; 24(17)2019 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-31455036

RESUMO

Thymus marschallianus Willd. is a Lamiaceae species spread in a large variety of habitats worldwide. The aim of the present research was to analyse two different samples belonging to this species, one obtained from the spontaneous flora and one from culture. The total polyphenols, flavonoids, and phenolic acid contents were spectrophotometrically determined. Qualitative and quantitative analysis of polyphenols was performed by an HPLC-DAD-ESI (+)-MS method. For the antibacterial assay, the well-diffusion and the broth microdilution methods were used. Analysis of polyphenols revealed for both samples the presence of flavonoids like luteolin, quercetin, apigenin and their derivatives, but also of rosmarinic acid and methyl-rosmarinate. Differences regarding the amount of these compounds were emphasized. Significantly larger amounts of flavonoids were found for the sample harvested in the spontaneous flora, while for the rosmarinic acid, larger amounts were found for the cultured sample. Both samples displayed promising antibacterial activity, particularly towards Gram positive organisms. T. marschallianus represents, therefore, a rich source of polyphenolic compounds that prove its promising potential as a medicinal species.


Assuntos
Anti-Infecciosos/farmacologia , Compostos Fitoquímicos/farmacologia , Thymus (Planta)/química , Anti-Infecciosos/química , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Flavonoides/química , Flavonoides/farmacologia , Bactérias Gram-Positivas/efeitos dos fármacos , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacologia , Compostos Fitoquímicos/química , Polifenóis/química , Polifenóis/farmacologia
11.
BMC Complement Altern Med ; 18(1): 226, 2018 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-30053845

RESUMO

BACKGROUND: Although Galanthus nivalis L. (snowdrop) is known for the galanthamine content, used in the treatment of Alzheimer disease, the polyphenolic compounds of Amaryllidaceae species are less studied. Proper understanding of the polyphenolics in these extracts and of their antioxidant and antimicrobial properties may allow a reconsideration of their medicinal uses. METHODS: The polyphenolic content of four selected Amaryllidaceae species harvested from Romania (Galanthus nivalis L., Narcissus pseudonarcissus L., N. poeticus L. and Leucojum vernum L.) was determined by spectrophotometric methods; the identification of phenolic compounds was performed by a HPLC-MS method, in order to establish their polyphenolic fingerprints. For the evaluation of the antioxidant potential the following methods were employed: DPPH radical scavenging, FRAP, hemoglobin ascorbate peroxidase activity inhibition (HAPX), inhibition of lipid peroxidation catalyzed by cytochrome c, and electron paramagnetic resonance (EPR) spectroscopy assays. Antimicrobial activity was assessed using the disc diffusion method. RESULTS: Qualitative and quantitative analyses highlight important amount of polyphenols (over 15 mg/g); the main identified compounds are chlorogenic and p-coumaric acids in all species. Only G. nivalis shows antioxidant activity by all the used methods. G. nivalis and L. vernum strongly inhibits the growth of S. aureus, while N. poeticus shows a very good antifungal activity. CONCLUSIONS: The results of this study provide a new approach to the properties and therapeutic uses of some Romanian widespread Amaryllidaceae species that could be considered sources of developing new medicinal products with anti anti-staphylococcal and antifungal activity.


Assuntos
Amaryllidaceae/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Antioxidantes/química , Bactérias/efeitos dos fármacos , Compostos de Bifenilo , Peroxidação de Lipídeos/efeitos dos fármacos , Picratos , Extratos Vegetais/química , Polifenóis/química , Polifenóis/farmacologia , Romênia
12.
Molecules ; 23(8)2018 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-30126246

RESUMO

The biological properties and main phenolic compounds of the O. vulgare L. ssp. vulgare extract are described in the present paper. The polyphenolic compounds were analyzed by chromatographic and spectrophotometric techniques. The antioxidant potential was evaluated using several methods: CUPRAC (cupric ion reducing antioxidant capacity), FRAP (ferric reducing ability of plasma), inhibition of lipid peroxidation catalyzed by cytochrome c, and superoxide (SO) scavenging assays. The antimicrobial activity of the oregano extract was evaluated by means of agar-well diffusion assay. The hepatoprotective effect of the O. vulgare extract on CCl4-induced hepatotoxicity was evaluated in rats. Liver injury was estimated by determination of alanine aminotransaminase (ALT), aspartate aminotransaminase (AST), gamma-glutamyl transferase GGT, total protein and albumin concentrations, glutathione peroxidase (GPx), catalase (CAT), superoxide dismutase (SOD) and malondialdehyde (MDA). These values were improved by the administration of oregano extract. A specific phenolic profile was evidenced by these data, with large amounts of rosmarinic and chlorogenic acids. The oregano extract showed very strong antioxidant activity in good agreement with the phenolic content. Antimicrobial activity was good, especially against Salmonella enteritidis and Aspergillus niger strains. The high hepatoprotective, antioxidant and antimicrobial activity, along with polyphenol-rich content, can support the use of O. vulgare in therapy. We also expect our results to open new research directions for designing important new drug products, using indigenous plant material.


Assuntos
Origanum/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cromatografia Líquida de Alta Pressão , Feminino , Fungos/efeitos dos fármacos , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Polifenóis/química , Polifenóis/farmacologia , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia
13.
Molecules ; 21(8)2016 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-27529204

RESUMO

This study aims to evaluate the phenolic profile, and antioxidant and antimicrobial activity of Achillea schurii Sch.-Bip., an endemic species from Romania that has not been investigated yet. The chromatographic profile of the phenolic components was obtained using the HPLC-MS method, while the total polyphenol, flavonoid, caffeic acid derivative contents were quantified using spectrophotometric methods. The antioxidant activity was evaluated using different methods: DPPH radical scavenging, hemoglobin ascorbate peroxidase activity inhibition (HAPX), inhibition of lipid peroxidation catalyzed by cytochrome c, and direct detection of plant-derived free radicals using electron paramagnetic resonance (EPR). The antimicrobial test was performed using the disk diffusion assay. The phenolic profile has revealed high amounts of isoquercitrin, rutin, luteolin, and apigenin. The A. schurii extract exhibited a good antioxidant capacity, and high phenolic contents (76.93 mg/g polyphenols, 18.61 mg/g flavonoids and 41.48 mg/g caffeic acid derivatives, respectively). The antimicrobial tests reveal a remarkable inhibitory activity against Listeria monocytogenes, Staphylococcus aureus, and Salmonella typhimurium. Considering the above, A. schurii may be deemed to offer good perspectives for pharmaceutical and industrial applications.


Assuntos
Achillea/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Flores/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Bactérias/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Citocromos c/química , Radicais Livres/antagonistas & inibidores , Fungos/efeitos dos fármacos , Peroxidação de Lipídeos , Testes de Sensibilidade Microbiana , Fenóis/química , Fenóis/farmacologia
14.
Pak J Pharm Sci ; 29(1 Suppl): 261-72, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27005495

RESUMO

Various thiosemicarbazones (TSCs) and their heterocyclic thiadiazolines (TDZ) possess important biological effects. In addition, chromenyl derivatives exhibit a wide range of pharmacological activities. Based on these findings and as a continuation of our research on nitrogen and sulfur containing compounds, we investigated a series of previously reported chromenyl-TSCs (1a-j) and chromenyl-TDZs (2a-j) for their in vitro antimicrobial activities against two bacterial and four fungal strains. MIC and MBC/MFC (µg/mL) values of these compounds were evaluated and compared to those of Spectinomycin, Moxifloxacin and Fluconazole, used as reference drugs. For a better understanding of the drug-receptor interactions, all the compounds were further subjected to molecular docking against four targets that were chosen based on the specific mechanism of action of the reference drugs used in the antimicrobial screening. All compounds tested showed equal or higher antibacterial/antifungal activities relative to the used reference drugs. In silico studies (molecular docking) revealed that all the investigated compounds showed good binding energies towards four receptor protein targets and supported their antimicrobial properties.


Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Benzopiranos/química , Benzopiranos/farmacologia , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Simulação por Computador , Fungos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Modelos Moleculares , Simulação de Acoplamento Molecular , RNA/efeitos dos fármacos , RNA/metabolismo , Receptores de Droga/química , Receptores de Droga/efeitos dos fármacos , Relação Estrutura-Atividade , Tiazóis/química , Tiazóis/farmacologia , Tiossemicarbazonas/química , Tiossemicarbazonas/farmacologia
15.
Pak J Pharm Sci ; 29(1 Suppl): 301-7, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-27005507

RESUMO

The aim of this study was focused on the polyphenolic composition and antioxidant capacity of Genista tinctoria L. and Genistella sagittalis (L.) Gams. A qualitative and quantitative characterization of the main phenolic compounds from the extracts were carried out using a HPLC-MS method. The total polyphenolic and flavonoid content was spectrophotometrically determined. The antioxidant activity towards various radicals generated in different systems was evaluated usingDPPH bleaching method, Trolox equivalent antioxidant capacity assay (TEAC) and Oxygen radical absorbance capacity (ORAC), and all indicated that G. tinctoria extract was more antioxidant than G. sagittalis extract.That was in good agreement with the total polyphenolic and flavonoidic content.Chlorogenic acid, p-coumaric acid, isoquercitrin and apigenin were identified in bothspecies. Caffeic acid, ferulic acid, hyperoside, rutin, quercitrin and luteolin were found only in G. tinctoria, while quercetin was determined in G. sagittalis.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Fabaceae/química , Genista/química , Polifenóis/química , Polifenóis/farmacologia , Compostos de Bifenilo/química , Cromanos/farmacologia , Cromatografia Líquida de Alta Pressão , Flavonas/química , Flavonas/farmacologia , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Radicais Livres/metabolismo , Espectrometria de Massas , Picratos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/química
16.
Pak J Pharm Sci ; 28(6 Suppl): 2297-303, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-26687747

RESUMO

In the present study, six indigenous species of Lamiaceae family (Origanum vulgare L., Melissa officinalis L., Rosmarinus officinalis L., Ocimum basilicum L., Salvia officinalis L. and Hyssopus officinalis L.), have been analyzed to assess the rosmarinic acid, phenyl propane derivatives and polyphenolic contents and their antioxidant and antimicrobial potential. HPLC-MS method has been used for the analysis ofrosmarinicacid. The phenyl propane derivatives and total phenolic contents were determined using spectrophotometric method. The ethanolic extracts were screened for antioxidant activities by DPPH radical scavenging, HAPX (hemoglobin ascorbate per oxidase activity inhibition), and EPR (electron paramagnetic resonance) methods. The ethanolic extracts revealed the presence of rosmarinic acid in the largest amount in O. vulgare (12.40mg/g) and in the lowest in R. officinalis (1.33 mg/g). O. vulgare extracts exhibited the highest antioxidant capacity, in line with the rosmarinic acid and polyphenolic contents. The antimicrobial testing showed a significant activity against L. monocytogenes, S. aureus and C. albicans for all six extracts.

17.
Molecules ; 19(7): 9240-56, 2014 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-24991757

RESUMO

Nineteen bisthiazoles were tested in order to assess their anti-inflammatory and antioxidant properties. First, we evaluated the in vitro direct antioxidant capacity of the bisthiazoles using the DPPH radical scavenging method. Then, the anti-inflammatory effect was tested in acute rat experimental inflammation by measuring the acute phase bone marrow response, the phagocytic capacity and the serum nitro-oxidative stress status. Although none of the substances showed significant direct antioxidant potential in the DPPH assay, most of them improved serum oxidative status, when administered to rats with inflammation. Four of the bisthiazoles proved to have good anti-inflammatory properties, similar or superior to that of equal doses meloxicam.


Assuntos
Anti-Inflamatórios/farmacologia , Estresse Oxidativo , Fagocitose/efeitos dos fármacos , Espécies Reativas de Nitrogênio/sangue , Tiazóis/farmacologia , Animais , Anti-Inflamatórios/química , Medula Óssea/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Sequestradores de Radicais Livres/química , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Masculino , Meloxicam , Ratos Wistar , Espécies Reativas de Nitrogênio/fisiologia , Tiazinas/farmacologia , Tiazóis/química , Terebintina
18.
Pharmaceutics ; 16(1)2024 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-38258100

RESUMO

Antimicrobial resistance is an increasing problem for global public health. One of the strategies to combat this issue is the synthesis of novel antimicrobials through rational drug design based on extensive structure-activity relationship studies. The thiazole nucleus is a prominent feature in the structure of many authorized antimicrobials, being clubbed with different heterocycles. The purpose of this review is to study the structure-activity relationship in antimicrobial thiazoles clubbed with various heterocycles, as reported in the literature between 2017 and 2023, in order to offer an overview of the last years in terms of antimicrobial research and provide a helpful instrument for future research in the field.

19.
Biomolecules ; 14(2)2024 Feb 12.
Artigo em Inglês | MEDLINE | ID: mdl-38397456

RESUMO

Considering the pivotal role of angiogenesis in solid tumor progression, we developed a novel series of quinazoline-thiazole hybrids (SA01-SA07) as antiproliferative and anti-angiogenic agents. Four out of the seven compounds displayed superior antiproliferative activity (IC50 =1.83-4.24 µM) on HepG2 cells compared to sorafenib (IC50 = 6.28 µM). The affinity towards the VEGFR2 kinase domain was assessed through in silico prediction by molecular docking, molecular dynamics studies, and MM-PBSA. The series displayed a high degree of similarity to sorafenib regarding the binding pose within the active site of VEGFR2, with a different orientation of the 4-substituted-thiazole moieties in the allosteric pocket. Molecular dynamics and MM-PBSA evaluations identified SA05 as the hybrid forming the most stable complex with VEGFR2 compared to sorafenib. The impact of the compounds on vascular cell proliferation was assessed on EA.hy926 cells. Six compounds (SA01-SA05, SA07) displayed superior anti-proliferative activity (IC50 = 0.79-5.85 µM) compared to sorafenib (IC50 = 6.62 µM). The toxicity was evaluated on BJ cells. Further studies of the anti-angiogenic effect of the most promising compounds, SA04 and SA05, through the assessment of impact on EA.hy296 motility using a wound healing assay and in ovo potential in a CAM assay compared to sorafenib, led to the confirmation of the anti-angiogenic potential.


Assuntos
Antineoplásicos , Sorafenibe/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/química , Simulação de Acoplamento Molecular , Quinazolinas/farmacologia , Quinazolinas/química , Inibidores de Proteínas Quinases/farmacologia , Inibidores de Proteínas Quinases/química , Inibidores da Angiogênese/farmacologia , Proliferação de Células , Estrutura Molecular
20.
Nutrients ; 16(6)2024 Mar 14.
Artigo em Inglês | MEDLINE | ID: mdl-38542742

RESUMO

Nutraceuticals represent an emerging and dynamic scientific field due to their important potential in integrated healthcare through nutritional and medicinal approaches that interact and complement each other mutually. In an attempt to find new sources for such preparations, the present research focuses on the species Craterellus cornucopioides (L.) Pers. (Cantharellaceae), also known as the black trumpet. This wild mushroom species is renowned for its culinary excellence and unique taste and is used especially in a dehydrated state. However, beyond its gastronomic value, recent scientific investigations have revealed its potential as a source of bioactive compounds with pharmaceutical and therapeutic significance. Our study aimed, therefore, to review the current data regarding the morphology, chemical profile, and medicinal potential of the black trumpet mushroom, highlighting its unique attributes. By conducting a comprehensive literature analysis, this paper contributes to the broader understanding of this remarkable fungal species as a potential functional food and its promising applications in the field of therapeutics.


Assuntos
Agaricales , Basidiomycota , Basidiomycota/química , Agaricales/química , Suplementos Nutricionais
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