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1.
Exp Parasitol ; 262: 108778, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38735517

RESUMO

Sheep haemonchosis is a disease that causes serious losses in livestock production, particularly with the increase of cases of anthelmintic resistance around the world. This justifies the urgent need of alternative solutions. The aim of this study was to determine the chemical profile, in vitro, and, in vivo, anthelmintic properties of Thymus capitatus essential oil. To evaluate the, in vitro, anthelmintic activity of the T. capitatus EO on Haemonchus contortus, two tests were used: egg hatch assay (EHA) and adult worm motility (AWM) assay. The nematicidal effect of this oil was evaluated, in vivo, in mice infected artificially with Heligmosomoides polygyrus using faecal egg count reduction (FECR) and total worm count reduction (TWCR). Chromatographic characterization of T.capitatus composition using gas chromatography coupled to mass spectrometry (GC-MS) demonstrated the presence of carvacrol (81.16%), as the major constituents. The IC50 values obtained was 1.9 mg/mL in the EHT. In the AWM assay; T. capitatus essential oil achieved 70.8% inhibition at 1 mg/mL after 8 h incubation. The in vivo, evaluation on H. polygyrus revealed a significant nematicidal effect 7 days post-treatment by inducing 49.5% FECR and 64.5% TWCR, using the highest dose (1600 mg/kg). The results of present study, demonstrate that T.capitatus EO possess a significant anthelmintic properties. Furthermore, it could be an alternative source of anthelmintic agents against gastrointestinal infections caused by H. contortus.


Assuntos
Anti-Helmínticos , Fezes , Flores , Cromatografia Gasosa-Espectrometria de Massas , Hemoncose , Haemonchus , Nematospiroides dubius , Óleos Voláteis , Contagem de Ovos de Parasitas , Infecções por Strongylida , Thymus (Planta) , Animais , Haemonchus/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Camundongos , Nematospiroides dubius/efeitos dos fármacos , Thymus (Planta)/química , Hemoncose/veterinária , Hemoncose/tratamento farmacológico , Hemoncose/parasitologia , Infecções por Strongylida/tratamento farmacológico , Infecções por Strongylida/veterinária , Infecções por Strongylida/parasitologia , Anti-Helmínticos/farmacologia , Anti-Helmínticos/isolamento & purificação , Anti-Helmínticos/uso terapêutico , Anti-Helmínticos/química , Fezes/parasitologia , Contagem de Ovos de Parasitas/veterinária , Flores/química , Feminino , Ovinos , Concentração Inibidora 50 , Monoterpenos/farmacologia , Monoterpenos/isolamento & purificação , Monoterpenos/química , Masculino , Doenças dos Ovinos/parasitologia , Doenças dos Ovinos/tratamento farmacológico , Cimenos
2.
Chem Biodivers ; : e202300563, 2024 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-38880770

RESUMO

This study aimed to define the chemical composition of Moroccan Thymus capitatus essential oil, and to investigate its in vitro antioxidant and antifungal activities against human pathogenic fungi. Chemical analysis using GC-FID and GC-MS system revealed 28 constituents, representing 99% of total compounds. Oxygenated monoterpenes represented the highest proportion (79.79%), among which carvacrol (75.73%) was the predominant compound, followed by linalol (2.26%). Monoterpene hydrocarbons represented the second major fraction (16.29%): within them, the predominant constituents were γ-terpinene (5,55%), ρ-cymene (5,50%), and ß-caryophyllene (2.73%). Antioxidant activity was performed by DPPH scavenging, ß-carotene bleaching inhibition, and ferric reducing power. T. capitatus revealed pronounced DPPH radical scavenging activity (IC50=110.53µg.mL-1), strong ferric reducing ability (EC50=644.4µg.mL-1), and a remarkable degree of protection against lipid peroxidation during ß-carotene bleaching inhibition (IC50=251.76µg.mL-1). Antifungal activity was carried out against Candida, Aspergillus, and Rhizopus species by microdilution method.  T. capitatus   exhibited potent anticandidal activity (MIC=125-500µg.mL-1) and strong inhibition against filamentous fungi (MIC=250-500µg.mL-1). Its hemolytic activity against human erythrocytes had a low toxic effect at concentrations lower than 1250µg.mL-1. The useful antioxidant properties and broad antifungal effect of T. capitatus EO confirm its considerable potential for the food industry and for phytopharmaceutical production.

3.
Int J Environ Health Res ; 33(4): 398-412, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35220853

RESUMO

This study investigated composition and toxicity of Thyme EOs against two main stored grain insect pests. Carvacrol was distinguished as a major compound (78.34%). In laboratory tests, EOs applied by both direct contact and fumigant tests was more toxic to L. serricorne than T. castaneum. The EOs were also tested combined with two Tunisian Diatomaceous earths (DEs) against T. castaneum. The LC50 was 6.28 µL/L air for natural preparation EO/R1, 5.90 µL/L air for EO/R2 and 121.17 for crude EOs by fumigant test, respectively. While, contact test revealed that natural DEs; dust act as an insecticide with 'LC50' values of 3.22 and 0.29 µL/cm2f or R1 and R2, respectively. Moreover, a significant difference was noted between crude EO, EO/R1 and EO/R2. Overall, the enhancement of the Tunisian DEs' insecticidal activity by its mix with EOs may be a promising active substance as a stored grain protectant.


Assuntos
Besouros , Inseticidas , Óleos Voláteis , Animais , Inseticidas/farmacologia , Óleos Voláteis/farmacologia , Terra de Diatomáceas/farmacologia , Controle de Pragas
4.
Int J Environ Health Res ; : 1-11, 2023 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-37952172

RESUMO

The objective of the current study was to evaluate the interaction between Tunisian Thymus capitatus essential oil (EO) and cefotaxime against Extended-Spectrum Beta-lactamases (ESBLs) producing Klebsiella pneumoniae hospital strains. GC-MS revealed that the major component of EO was found to be carvacrol (69.28%). The EO exerts an advanced bactericidal effect against all strains. Synergy between EO and cefotaxime was obtained by combined disk diffusion and checkerboard techniques. Combined use of EO and cefotaxime reduced the MIC of imipenem by 8- to 128-fold for all strains (fractional inhibitory concentration index ˂ 0.5, synergy). The time kill curve assay confirmed the advanced activity of combinatory effects of EO and cefotaxime, with total reduce of bacterial number (CFU/mL) after 6 h of culture. Synergistic activity of the combination between EO and cefotaxime constitute an important strategy as therapeutical option to combat infections caused by ESBLs producing Klebsiella pneumoniae.

5.
Can J Microbiol ; 64(10): 647-663, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29746162

RESUMO

Candida glabrata is an opportunistic pathogen, associated with endocarditis, meningitis, and disseminated disease, and also with complicated vaginitis. Essential oils derived from aromatic plants are known in traditional medicine as antimicrobial agents and have antifungal properties. The aim of this work was to evaluate whether 12 tested essential oils (tea tree, laurel, anise, basil, bergamot, lavender, mint, oregano, grapefruit, rosemary, winter savory, and ginger) could have a transverse effect on C. glabrata sensitive strains but above all on strains resistant to the three main azole antifungals used (clotrimazole, fluconazole, itraconazole). For this reason, different strains of C. glabrata, vaginal isolated, were characterized (disk diffusion assay, minimal inhibitory concentration) with respect to their response to such antifungals. Electron microscopy analyses were performed to examine cellular damages in depth. Subsequently, we wanted to evaluate the effect of the oils on human cells to estimate their potential cytotoxicity. Oregano and winter savory were the two most effective essential oils, inducing growth inhibition, cell damage of C. glabrata strains (both sensitive and resistant to azole antifungal drugs), and medium-high level of toxicity against human keratinocytes. The results of this work support the research for new alternatives or complementary therapies against vaginal candidiasis.


Assuntos
Antifúngicos/farmacologia , Azóis/farmacologia , Candida glabrata/efeitos dos fármacos , Óleos Voláteis/farmacologia , Vagina/microbiologia , Células Cultivadas , Feminino , Fluconazol/farmacologia , Humanos , Itraconazol/farmacologia , Testes de Sensibilidade Microbiana
6.
Phytother Res ; 32(8): 1555-1563, 2018 08.
Artigo em Inglês | MEDLINE | ID: mdl-29673001

RESUMO

Thymus capitatus represents 1 of the 5 Tunisian species of the genus Thymus, which has long­standing use for flavouring and preserving several food products. Its constituents have been reported to endow antimicrobial properties, but little is known about their antiviral activities. The aim of this study was to examine the antiviral activity of pure compounds from the most bioactive inhibitory T. capitatus extract in vitro against herpes simplex virus Type 2 (HSV­2) infection and to identify their mechanism of action. Either the extracts or the essential oil exert inhibitory activity against HSV­2 infection, with the ethanolic extract showing the lowest EC50 value (2.3 µg/ml). Three pure compounds were then isolated from the ethanolic extract and investigated for their antiviral activity. ß­sitosterol showed the most favourable selectivity index and both cinnamaldehyde and carvacrol exerted moderate antiviral effect. Investigation of the mechanism of action revealed that all three compounds directly inactivated the infectivity of the virus particles. These findings suggest the use of T. capitatus ethanolic extract as source of anti­HSV­2 pure compounds and warrant further studies to evaluate their therapeutic potential.


Assuntos
Antivirais/farmacologia , Herpesvirus Humano 2/efeitos dos fármacos , Extratos Vegetais/farmacologia , Thymus (Planta)/química , Acroleína/análogos & derivados , Acroleína/farmacologia , Animais , Chlorocebus aethiops , Cimenos , Monoterpenos/farmacologia , Óleos Voláteis/farmacologia , Células Vero , Inativação de Vírus
7.
J Food Sci Technol ; 55(9): 3446-3452, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150803

RESUMO

This work aims to characterize Thymus capitatus essential oil and to investigate its preservative effects on raw milk quality alone or combined to pasteurization heat treatment. To study its preservative effect, 1 mg l-1 of T. capitatus essential oil, characterized by GC-MS, was added to pasteurized or raw milk. The evaluation of milk quality was made by consulting samples total acidities, peroxide values and their total microbial counts, as compared to control milks. Assays were made immediately and after every 48 h of incubation at room temperature throughout 6 days. Results showed that the incorporation of T. capitatus EO to pasteurized milk was the most efficient treatment that inhibited milk deterioration. Combining pasteurization to EO incorporation into raw milk inhibited completely the contaminant bacterial growth to the second day of incubation. Moreover, until the fourth day, no statistical differences have been recorded on the total acidity of incorporated and pasteurized milk samples, while raw milk acidity exceeded 55 g of lactic acid equivalent l-1. Considering milk fat oxidation, adding T. capitatus EO to pasteurized milk has significantly retarded milk peroxide production to day 4. In conclusion, Thymus capitatus essential oil, combined to pasteurization, presents an interesting potency to act as milk stabilizer.

8.
J Food Sci Technol ; 55(10): 4256-4265, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30228424

RESUMO

Chitosan-based coatings and films have been widely studied, demonstrating to be an efficient and eco-friendly approach to extend the shelf life of food products. The effect of incorporating Thymus capitatus essential oil (TCEO) at different concentrations (0.5, 1.0, and 1.5% w/w) on physical, mechanical and antimicrobial properties of chitosan films was studied. The antimicrobial activity of the films was evaluated by agar diffusion method, against 23 spoiling microorganisms isolated from tuna and swordfish (ten Shewanella baltica, one S. morhuae, one S. putrefaciens, two Pseudomonas fluorescens, two P. fragi, five Serratia spp., one Aeromonas molluscorum, and one Acinetobacter radioresistens) and Shewanella putrefaciens ATCC 49138. The films exerted antimicrobial activity against all the tested strain, although not proportional to increasing TCEO concentration. In particular, S. baltica was the most sensitive species and the inhibition was stable after 72 h. In general, TCEO incorporation in chitosan films, significantly (p < 0.05) decreased the water permeability (from 0.577 ± 0.060 gmm/kPahm2 at 61% R.U. for chitosan to 0.487 ± 0.037 gmm/kPahm2 for the film with 1.5% TCEO), the elongation at brake (from 27.322 ± 2.35% for chitosan to 14.695 ± 3.99% for the film with 1.5% TCEO) and increased the tensile strength (from 1.697 ± 0.16% for chitosan to 19.480 ± 2.86% for the film with 1.5% TCEO). Moisture content and water contact angle of the films also showed a similar trend with TCEO introduction, because of crosslinking reaction among the polymer chains and TCEO components. Scanning electron microscopy confirmed structure-properties relationships. These results suggest chitosan films incorporated with TCEO as an alternative treatment to inhibit the growth of degradative bacteria with potential application in the fish industry. The importance of testing more than one strain of the same bacteria species to evaluate the effectiveness of chitosan-essential oils coatings was also demonstrated.

9.
Exp Parasitol ; 183: 231-235, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28916454

RESUMO

Acanthamoeba species are free-living amoebae widely distributed in the environment and which cause serious human infections. The treatment of Acanthamoeba infections is always very difficult and not constantly effective. More efficient drugs against Acanthamoeba must be developed and medicinal plants can be useful in this case. Our research focused on the examination of the anti-Acanthamoeba activity of the essential oil and the ethanolic-aqueous extract from Thymus capitatus L. The essential oil showed best activity with an IC50 of 2.73 µg/ml. The conducted Bio-guided fractionation of thyme extract result to the identification of two active compounds against the trophozoite stage of Acanthamoeba: thymol and 2,3-dihydroxy-p-cymene. The results have clearly shown that the investigated products may be successfully used against Acanthamoeba infections. These molecules that are found in plants may be an alternative for the development of new drugs.


Assuntos
Acanthamoeba/efeitos dos fármacos , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Thymus (Planta)/química , Bioensaio , Fracionamento Químico , Cromatografia Gasosa-Espectrometria de Massas , Concentração Inibidora 50
10.
J Appl Microbiol ; 121(6): 1530-1545, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27568869

RESUMO

AIMS: Candida albicans is an important opportunistic pathogen, responsible for the majority of yeast infections in humans. Essential oils, extracted from aromatic plants, are well-known antimicrobial agents, characterized by a broad spectrum of activities, including antifungal properties. The aim of this work was to assess the sensitivity of 30 different vaginal isolated strains of C. albicans to 12 essential oils, compared to the three main used drugs (clotrimazole, fluconazole and itraconazole). METHODS AND RESULTS: Thirty strains of C. albicans were isolated from vaginal swab on CHROMagar™ Candida. The agar disc diffusion method was employed to determine the sensitivity to the essential oils. The antifungal activity of the essential oils and antifungal drugs (clotrimazole, itraconazole and fluconazole) were investigated using a microdilution method. Transmission and scanning electron microscopy analyses were performed to get a deep inside on cellular damages. Mint, basil, lavender, tea tree oil, winter savory and oregano essential oils inhibited both the growth and the activity of C. albicans more efficiently than clotrimazole. Damages induced by essential oils at the cellular level were stronger than those caused by clotrimazole. CONCLUSIONS: Candida albicans is more sensitive to different essential oils compared to the main used drugs. Moreover, the essential oil affected mainly the cell wall and the membranes of the yeast. SIGNIFICANCE AND IMPACT OF THE STUDY: The results of this work support the research for new alternatives or complementary therapies against vaginal candidiasis.


Assuntos
Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Óleos Voláteis/farmacologia , Candida/efeitos dos fármacos , Candida albicans/isolamento & purificação , Clotrimazol/farmacologia , Feminino , Fluconazol/farmacologia , Humanos , Itraconazol/farmacologia
11.
J Appl Microbiol ; 119(2): 389-99, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-26033505

RESUMO

AIMS: In the present work, the Libyan wild-growing Thymus capitatus essential oil (EO) was evaluated for its biological properties. METHODS AND RESULTS: Carvacrol (68.19%) and thymol (12.29%) were found to be the main compounds of the oil. Antioxidant properties, determined by 2,2-diphenylpicrylhydrazyl (DPPH) assay, revealed that IC50 values were 119, 403 and 105 µg ml(-1) for oil, thymol and carvacrol respectively. Microdilution method showed strong antibacterial and especially antifungal potential. Tetrazolium (MTT) colorimetric assay indicated moderate cytotoxicity towards human cell lines MRC-5, HCT 116 and HT-29 (IC50 = 30-150 µg ml(-1)). In adhesion-inhibition assay oil and main compounds reduced adhesion of Escherichia coli and Listeria monocytogenes on colon cells HT-29 (51 and 39% of inhibition against L. monocytogenes and E. coli respectively). CONCLUSIONS: Essential oil of Th. capitatus showed moderate cytotoxic activity, together with excellent antimicrobial effect, in particular against fungi, and significant potential to reduce pathogen colonization in colon. SIGNIFICANCE AND IMPACT OF THE STUDY: This is the first report that EO of Th. capitatus could protect against colonization of pathogens to colon epithelium. Thymus capitatus from Libya should be recognized as possible new source of natural antioxidants, antimicrobials as well as possible source of new chemotherapeutics.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Aderência Bacteriana/efeitos dos fármacos , Colo/microbiologia , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Thymus (Planta)/química , Anti-Infecciosos/química , Antioxidantes/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Escherichia coli/fisiologia , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Humanos , Listeria monocytogenes/efeitos dos fármacos , Listeria monocytogenes/crescimento & desenvolvimento , Listeria monocytogenes/fisiologia , Óleos Voláteis/química , Extratos Vegetais/química
12.
J Enzyme Inhib Med Chem ; 30(3): 360-5, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25032744

RESUMO

The aim of this study was to examine the bioactivity of the methanol fraction (MF) and n-hexane fraction (HF) of Thymus capitatus leaves in relation to their constituents analysed by gas chromatography and gas chromatography-mass spectrometry. The effects of T. capitatus on the growth of pathogenic bacteria associated with respiratory diseases (13 gram-positive and 4 gram-negative) were determined using a microdilution method. The MF was particularly effective on Streptococcus pneumoniae and Moraxella catarrhalis. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid), ferric-reducing antioxidant power and ß-carotene bleaching assays. A strong activity using ß-carotene bleaching test was observed with the MF (IC50 of 0.7 µg/mL after 30 min of incubation). In the hypoglycaemic test, a selective α-amylase inhibitory activity was detected with the HF begging the most active (IC50 of 422.5 µg/mL). T. capitatus may represent a source of natural bioactive compounds.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Hiperglicemia/tratamento farmacológico , Hipoglicemiantes/farmacologia , Folhas de Planta/química , Thymus (Planta)/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Hiperglicemia/enzimologia , Hiperglicemia/metabolismo , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo
13.
Nat Prod Res ; 37(23): 4038-4041, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36597612

RESUMO

Herpes simplex virus (HSV) can infect millions of people worldwide causing mild to life-threating infections. The current study demonstrates the first comparative anti-HSV type 1 activity and phytochemical investigation of Artemisia herba-alba and Thymus capitatus collected from Egypt and Libya. Liquid chromatography/mass spectrometry (LC/MS) analysis allowed the identification of 56 and 38 compounds in the Egyptian and Libyan Artemisia herba-alba ethanolic extracts, respectively, in addition to 46 and 50 compounds in the Egyptian and Libyan Thymus capitatus ethanolic extracts, respectively. Gas chromatography/mass spectrometry (GC/MS) analysis of their corresponding essential oils revealed the presence of 15, 17, 17 and 8 compounds in Egyptian and Libyan Artemisia herba-alba and Thymus capitatus, respectively. The major chemical classes of the identified compounds were phenolic acids, flavonoids and oxygenated monoterpenes. Evaluation of the anti-HSV1 activities of the studied extracts showed that the Egyptian Thymus capitatus ethanolic extracts were the most potent extract with more than 200-fold reduction in the viral PFU.


Assuntos
Artemisia , Herpesvirus Humano 1 , Lamiaceae , Humanos , África do Norte , Cromatografia Líquida , Egito , Etanol
14.
PeerJ ; 11: e15065, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37077312

RESUMO

Detecting and distinguishing apicultural plants are important elements of the evaluation and quantification of potential honey production worldwide. Today, remote sensing can provide accurate plant distribution maps using rapid and efficient techniques. In the present study, a five-band multispectral unmanned aerial vehicle (UAV) was used in an established beekeeping area on Lemnos Island, Greece, for the collection of high-resolution images from three areas where Thymus capitatus and Sarcopoterium spinosum are present. Orthophotos of UAV bands for each area were used in combination with vegetation indices in the Google Earth Engine (GEE) platform, to classify the area occupied by the two plant species. From the five classifiers (Random Forest, RF; Gradient Tree Boost, GTB; Classification and Regression Trees, CART; Mahalanobis Minimum Distance, MMD; Support Vector Machine, SVM) in GEE, the RF gave the highest overall accuracy with a Kappa coefficient reaching 93.6%, 98.3%, 94.7%, and coefficient of 0.90, 0.97, 0.92 respectively for each case study. The training method used in the present study detected and distinguish the two plants with great accuracy and results were confirmed using 70% of the total score to train the GEE and 30% to assess the method's accuracy. Based on this study, identification and mapping of Thymus capitatus areas is possible and could help in the promotion and protection of this valuable species which, on many Greek Islands, is the sole foraging plant of honeybees.


Assuntos
Criação de Abelhas , Plantas , Tecnologia de Sensoriamento Remoto , Dispositivos Aéreos não Tripulados , Animais , Abelhas , Grécia , Dispersão Vegetal , Plantas/classificação , Tecnologia de Sensoriamento Remoto/métodos , Reprodutibilidade dos Testes
15.
BMC Complement Med Ther ; 23(1): 365, 2023 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-37845669

RESUMO

Non-small-cell lung carcinoma (NSCLC) is a type of epithelial lung cancer accounting for about 85% of all lung cancers. In our research, a novel lupene derivative namely acetoxy-lup-5(6), 20(29)-diene (ALUP), as well as two known triterpenes; lupeol (LUP) and betulinic acid (BA) were isolated through the chromatographic purification of the 95% ethanolic extract of Thymus capitatus. Identification of the compounds was carried out by physicochemical properties as well as spectral 1D and 2D NMR analysis. The anti-cancer activity of the three triterpenes was assessed on non-small cell lung cancer cell line; A549 using MTT assay and cell cycle analysis using annexin V/propidium iodide. The molecular mechanism underlying anti-apoptotic effects was determined by analyzing Let-7 miRNA and miRNA-21 expression, the mRNA gene expression level of Bax, CASP-8, CD95, Bcl2, KRAS, VEGF, Cyclin D1 using qRT-PCR. Our results revealed that the three isolated compounds ALUP, LUP, and BA caused cell cycle arrest at the G2/M phase with an increase in the apoptosis which may be attributed to their significant effect on raising Bax, CASP-8, and CD95 and reducing the mRNA expression levels of Bcl-2, KRAS, VEGF, and Cyclin D1 compared to control cells. RT-PCR results showed that the ALUP, LUP, and BA significantly downregulated miRNA-21 expression. Meanwhile, the three compounds caused significant overexpression of Let-7 miRNA. This is the first report on the anti-cancer activity of acetoxy-lup-5(6), 20(29)-diene (ALUP) in reducing the proliferation and differentiation of the A549 cell line through inducing apoptosis. Finally, by targeting the Let-7 miRNA/Cyclin D1/VEGF cascade, acetoxy-lup-5(6), 20(29)-diene could be a potential therapeutic agent for lung cancer.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , MicroRNAs , Triterpenos , Humanos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Carcinoma Pulmonar de Células não Pequenas/patologia , Neoplasias Pulmonares/genética , Células A549 , Fator A de Crescimento do Endotélio Vascular/metabolismo , Ciclina D1/genética , Ciclina D1/metabolismo , Ciclina D1/farmacologia , Proteína X Associada a bcl-2/metabolismo , Proteínas Proto-Oncogênicas p21(ras)/metabolismo , Proteínas Proto-Oncogênicas p21(ras)/farmacologia , Proteínas Proto-Oncogênicas p21(ras)/uso terapêutico , Linhagem Celular Tumoral , Apoptose , MicroRNAs/genética , Triterpenos/farmacologia , Triterpenos/uso terapêutico , RNA Mensageiro
16.
Vet Sci ; 10(12)2023 Dec 13.
Artigo em Inglês | MEDLINE | ID: mdl-38133253

RESUMO

The most significant ectoparasitic mite of honeybees, Varroa destructor, has a detrimental effect on bee health and honey output. The principal strategy used by the control programs is the application of synthetic acaricides. All of this has resulted in drug resistance, which is now a major worry for beekeeping. As a result, research on alternate products and techniques for mite management is now required. The aim of this study was to determine whether essential oils (EOs) extracted from botanical species of Lamiacae, typical of the Calabria region of Southern Italy, could reduce the population of the mite V. destructor. Among the best-known genera of the Lamiaceae family are oregano, rosemary and thyme, whose EOs were employed in this study. By steam distillation, the EOs were extracted from Origanum vulgare subsp. viridulum (Martrin-Donos) Nyman, Thymus capitatus Hoffmanns. and Link, Thymus longicaulis C.Presl and Salvia rosmarinus Schleid. plant species harvested directly on the Calabrian territory in their balsamic time. Each EO went to the test in vitro (contact toxicity) against V. destructor. Fifty adult female mites, five for each EO and the positive and negative control, were used in each experimental replicate. The positive controls comprised five individuals treated to Amitraz dilute in acetone, and the negative controls included five individuals exposed to acetone alone. To create the working solution to be tested (50 µL/tube), the EOs were diluted (0.5 mg/mL, 1 mg/mL, 2 mg/mL and 4 mg/mL) in HPLC-grade acetone. After 1 h of exposure, mite mortality was manually assessed. Origanum vulgare subsp. viridulum, Thymus capitatus and Thymus longicaulis were the EOs with the highest levels of efficiency at 2 mg/mL, neutralizing (dead + inactivated), 94%, 92% and 94% of parasites, respectively. Salvia rosmarinus EO gave a lower efficacy, resulting in a percentage of 38%. Interestingly, no adverse effects were highlighted in toxicity tests on honeybees. These results show that these OEs of the Lamiaceae family have antiparasitic action on V. destructor. Therefore, they could be used, individually or combined, to exploit the synergistic effect for a more sustainable control of this parasite mite in honeybee farms.

17.
Plants (Basel) ; 11(7)2022 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-35406936

RESUMO

Thymus capitatus and Thymus broussonnetii are two Moroccan endemic medicinal plants used traditionally by the local population. The present study aims to investigate their essential oil chemical composition, antioxidant and antibacterial activities. The chemical composition of the essential oils was determined using the GC-MS analysis, the antioxidant activity assessed using DPPH and FRAP methods while the antimicrobial activity was evaluated against nine bacteria species tested (Enterococcus faecalis, Serratia fonticola, Acinetobacter baumannii, Klebsiella oxytoca, sensitive Klebsiella pneumoniae, sensitive Escherichia coli, resistant Escherichia coli, resistant Staphylococcus aureus and Enterobacter aerogenes). The major identified compounds of T. capitatus essential oil where carvacrol (75%) and p-cymene (10.58%) while carvacrol (60.79%), thymol (12.9%), p-cymene (6.21%) and γ-terpinene (4.47%) are the main compounds in T. broussonnetii essential oil. The bioactivity of the essential oils of the two species of thyme was explained by their richness in oxygenated monoterpenes known for their great effectiveness with an IC50 of 3.48 ± 0.05 and 4.88 ± 0.04 µL/mL and EC50 of 0.12 ± 0.01 and 0.20 ± 0.02 µL/mL in the DPPH and FRAP assays, respectively, with an important antibacterial activity. These results encourage the use of these plants as a source of natural antioxidants, and antibacterial additives, to protect food from oxidative damage and to eliminate bacteria that are responsible for nosocomial infections.

18.
FEBS Open Bio ; 12(6): 1166-1177, 2022 06.
Artigo em Inglês | MEDLINE | ID: mdl-35384415

RESUMO

Kaposi's sarcoma-associated herpesvirus (KSHV), also known as human herpes virus 8 (HHV-8), causes primary effusion lymphoma, multicentric Castleman's disease, and Kaposi's sarcoma. Few antiviral drugs are available to efficiently control KSHV infection, and therefore, the development of novel, effective anti-KSHV treatments is needed. The aim of this study was to determine the antiviral activity of ethanolic and aqueous extracts, essential oils, and certain flavonoids (hesperidin, eupafolin, and vicenin) derived from Thymus capitatus (commonly known as thyme). We assessed the toxicity of these different extracts and components in RPE-1 cell cultures using the MTS test and evaluated their antiviral effect using the TCID50 method. The mechanism of action was determined through time-of-addition tests as well as viral entry, attachment, and virucidal assays. Additionally, western blot analysis was also used to assess their modes of action. Total treatment assay showed that the aqueous extract of T. capitatus has the highest inhibitory effect against KSHVLYT with an EC50 value of 0.2388 µg·mL-1 . Both hesperidin and eupafolin showed the ability to inactivate viral infection in a dose-response manner (EC50 values of 0.2399 and 1.396 µm, respectively). Moreover, they were able to inactivate KSHVLyt postinfection by reducing viral protein expression. In summary, the effective antiviral property of the aqueous extract is likely a result of the inhibition of viral growth within the host cells by both hesperidin and eupafolin.


Assuntos
Herpesvirus Humano 8 , Hesperidina , Sarcoma de Kaposi , Antivirais/farmacologia , Flavonoides/metabolismo , Flavonoides/farmacologia , Herpesvirus Humano 8/metabolismo , Hesperidina/metabolismo , Hesperidina/farmacologia , Humanos , Sarcoma de Kaposi/patologia
19.
Antibiotics (Basel) ; 11(5)2022 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-35625325

RESUMO

Thymus capitatus is a Mediterranean endemic plant commonly known as "Zaïtra" in northern Morocco. As T. capitatus is widely used in traditional medicine and food, this present work aims to investigate the chemical compositions and biological activities of the T. capitatus leaves essential oil (TcLEO), acetonic (TcLAE), and methanolic extract (TcLME). The spectrophotometric determination demonstrated that T. capitatus is a natural source rich in phenolic contents (TPC) and flavonoid contents (TFC) and that TcLME revealed the highest TPC and TFC than TcLAE and TcLEO. The LC-MS analysis of phenolic compounds showed that paraben acid was predominant in both TcLME and TcLAE, followed by cinnamic acid and p-hydroxybenzoic acid. GC-MS analysis of the TcLEO revealed the presence of a total of 10 compounds, which were predominated by carvacrol. The antioxidant activity by ORAC was observed to be significantly higher in TcLEO and TcLAE than in TcLME. All samples used to assess DNA degradation effectively prevented DNA oxidation and, at the same time, had a prooxidant effect. The genotoxicity test showed that the T. capitatus were devoid of any mutagenic activity. Concerning antifungal activity, all samples were able to inhibit the growth of all microorganisms tested at low concentrations. TcLAE showed higher activity than TcLME, and in general, dermatophytes were more susceptible, being Microsporum canis the most sensitive one. Overall, the results obtained from this study confirm the wide uses of T. capitatus. Furthermore, the finding results suggest that the T. capitatus essential oil and extracts can be highly useful for pharmaceutical industries.

20.
Foods ; 11(13)2022 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-35804672

RESUMO

This study aimed to improve the effectiveness of Thymus capitatus and Thymus algeriensis essential oils (EOs), as food preservatives, through their encapsulation in different delivery systems (DSs), namely nanoemulsions and biopolymeric nanoparticles. DSs' preparation is tailored to enhance not only physical stability but also resulting Eos' antioxidant and antibacterial activities through different fabrication methods (high-pressure homogenization emulsification or antisolvent precipitation) and using different emulsifiers and stabilizers. DSs are characterized in terms of droplet size distribution, ζ-potential, and stability over time, as well as antioxidant and antibacterial activities of encapsulated EOs. The antioxidant activity was studied by the FRAP assay; the antibacterial activity was evaluated by the well diffusion method. EOs of different compositions were tested, namely two EOs extracted from Thymus capitatus, harvested from Tunisia during different periods of the year (TC1 and TC2), and one EO extracted from Thymus algeriensis (TA). The composition of TC1 was significantly richer in carvacrol than TC2 and TA. The most stable formulation was the zein-based nanoparticles prepared with TC1 and stabilized with maltodextrins, which exhibit droplet size, polydispersity index, ζ-potential, and encapsulation efficiency of 74.7 nm, 0.14, 38.7 mV, and 99.66%, respectively. This formulation led also to an improvement in the resulting antioxidant (60.69 µg/mg vs. 57.67 µg/mg for non-encapsulated TC1) and antibacterial (inhibition diameters varying between 12 and 33 mm vs. a range between 12 and 28 mm for non-encapsulated TC1) activities of EO. This formulation offers a promising option for the effective use of natural antibacterial bioactive molecules in the food industry against pathogenic and spoilage bacteria.

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