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1.
Molecules ; 29(12)2024 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-38930892

RESUMO

The Lamiaceae family, which includes several well-known aromatic plants, is scientifically relevant due to its essential oils (EOs). In this work, four EOs from Mediterranean species, namely Origanum vulgare L., Rosmarinus officinalis L., Salvia officinalis L., and Thymus vulgaris L., were evaluated for their volatile profiles and the biological activity in vitro to assess their potential use in the food and cosmetic sector. GC/MS analysis revealed dominant compounds, such as carvacrol, thymol, and eucalyptol. Regarding biological action, the samples exhibited antioxidant, cytotoxic, anti-inflammatory, antimicrobial, and antifungal activities, with O. vulgare and T. officinalis standing out. T. vulgaris showed the lowest EC50 in the reducing power assay, and O. vulgare had the lowest EC50 in the DPPH assay. Most EOs also displayed excellent anti-inflammatory responses and antifungal properties, with O. vulgare and T. vulgaris also demonstrating antibacterial activity. All EOs from Mediterranean species showed cytotoxicity against tumoral cell lines. Overall, the selected EOs stood out for their interesting bioactivities, with the obtained results underscoring their potential as natural preservatives and bioactive agents in various industrial applications, including food, pharmaceuticals, and cosmetics.


Assuntos
Antioxidantes , Lamiaceae , Óleos Voláteis , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Lamiaceae/química , Antioxidantes/farmacologia , Antioxidantes/química , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Cromatografia Gasosa-Espectrometria de Massas , Origanum/química , Salvia officinalis/química , Linhagem Celular Tumoral , Thymus (Planta)/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Plantas Comestíveis/química , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Timol/farmacologia , Timol/química , Testes de Sensibilidade Microbiana , Cimenos
2.
Molecules ; 29(12)2024 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-38930942

RESUMO

Naturally occurring substances and their derivatives function as vital resources for pesticides that can be used in fields, such as insecticide production and fungicide development. As a botanical entity displaying multifaceted biological functions, wormwood has received thorough scrutiny across multiple sectors. The insect repellency potency combined with antibacterial and antifungal activities of wormwood position it as a potential candidate for prospective development into eco-friendly chemical pesticides. In this research, Wormwood essential oil was procured via ethanol water under ultrasonic scenarios and subsequently diluted with PEG 400 to formulate green chemical pesticides. The defensive efficacy of this green pesticide on plants was validated through 2 weeks of clustered plant growth experiments. Active constituents that exerted their effects were scrutinized by GC-MS. Furthermore, this green pesticide also displays efficacious effects on the prevention and management of aphids, exhibiting a dose-dependent relationship. 4-terpenol, eucalyptol, carvacrol, and L-borneol were identified by GC-MS as the predominant active constituents in this green chemical pesticide. Wormwood can be leveraged to develop green chemical pesticides, which can protect plants without contaminating the environment.


Assuntos
Inseticidas , Óleos Voláteis , Inseticidas/química , Inseticidas/farmacologia , Animais , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Cimenos/química , Cimenos/farmacologia , Química Verde/métodos , Afídeos/efeitos dos fármacos , Eucaliptol/química , Eucaliptol/farmacologia , Canfanos
3.
Sci Rep ; 14(1): 13951, 2024 06 17.
Artigo em Inglês | MEDLINE | ID: mdl-38886531

RESUMO

The thrust of the study was to determine the chemical composition of the essential oils extracted from Thymus pallescens de Noé and Cymbogon citratus Stapf. as well as to evaluate their efficacy in controlling Sitophilus zeamais Motschulsky and Tribolium castaneum (Herbst) in either single or combined populations. Carvacrol (56.04%) and geraniol (20.86%) were identified as the major constituents of T. pallescens and C. citratus respectively. The tested essential oils showed pronounced insecticidal activity against the pest species in relation with the applied doses. T. pallescens EO had the highest efficacy and S. zeamais was found to be more susceptible to both individual and combined treatments. With reference to the contact and fumigation assessments, T. pallescens EO effectuated corrected mortality rates ranging from 42.5-100% to 25-100% in S. zeamais with corresponding lethal concentration (LC50) values of 17.7 µl/ml and 15µL/L air respectively. Whereas, the T. pallescens EO exhibited corrected mortality rates of 42.5-100% and 20-100% with corresponding LC50 values of 18.1 µl/ml and 15.5 µL/L air against T. castaneum in contact and fumigation assessments, respectively. The corrected mortality rates increased for both insect species when using combination treatments, with significant increases in the LC50 values, ranging from 8.59 to 49.9% for both pest species. Analysis of energy biomarkers in the treated insects indicate significantly increased protein and carbohydrate contents and decreased lipids levels. The study therefore demonstrated the bio-insecticidal toxicity of the EOs from T. pallescens and C. citratus against two important maize post-harvest pests, concurrently revealing significant positive and negative insecticidal activity gradients in relation to single or combined populations.


Assuntos
Inseticidas , Óleos Voláteis , Thymus (Planta) , Tribolium , Animais , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Tribolium/efeitos dos fármacos , Inseticidas/farmacologia , Inseticidas/química , Thymus (Planta)/química , Monoterpenos Acíclicos/farmacologia , Monoterpenos Acíclicos/química , Gorgulhos/efeitos dos fármacos , Cimenos/farmacologia , Cimenos/química
4.
Nat Commun ; 15(1): 4943, 2024 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-38858372

RESUMO

The development of Type I photosensitizers (PSs) is of great importance due to the inherent hypoxic intolerance of photodynamic therapy (PDT) in the hypoxic microenvironment. Compared to Type II PSs, Type I PSs are less reported due to the absence of a general molecular design strategy. Herein, we report that the combination of typical Type II PS and natural substrate carvacrol (CA) can significantly facilitate the Type I pathway to efficiently generate superoxide radical (O2-•). Detailed mechanism study suggests that CA is activated into thymoquinone (TQ) by local singlet oxygen generated from the PS upon light irradiation. With TQ as an efficient electron transfer mediator, it promotes the conversion of O2 to O2-• by PS via electron transfer-based Type I pathway. Notably, three classical Type II PSs are employed to demonstrate the universality of the proposed approach. The Type I PDT against S. aureus has been demonstrated under hypoxic conditions in vitro. Furthermore, this coupled photodynamic agent exhibits significant bactericidal activity with an antibacterial rate of 99.6% for the bacterial-infection female mice in the in vivo experiments. Here, we show a simple, effective, and universal method to endow traditional Type II PSs with hypoxic tolerance.


Assuntos
Benzoquinonas , Fotoquimioterapia , Fármacos Fotossensibilizantes , Staphylococcus aureus , Benzoquinonas/química , Benzoquinonas/farmacologia , Benzoquinonas/metabolismo , Fármacos Fotossensibilizantes/farmacologia , Animais , Camundongos , Feminino , Fotoquimioterapia/métodos , Transporte de Elétrons/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Cimenos/farmacologia , Cimenos/química , Antibacterianos/farmacologia , Oxigênio Singlete/metabolismo , Superóxidos/metabolismo , Infecções Estafilocócicas/tratamento farmacológico , Humanos , Luz , Camundongos Endogâmicos BALB C
5.
J Antibiot (Tokyo) ; 77(7): 436-453, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38750249

RESUMO

Mixed vaginitis due to bacterial vaginosis (BV) and vulvovaginal candidiasis (VVC) is the most prevalent form and presents a significant therapeutic challenge globally. Since, the administration of monotherapy leads to subsequent recurrent infections, synergistic therapy that completely eradicates both pathogens is of dire need to manage mixed vaginities scenario and to prevent its recurrence. The current investigation was focused on exploring the synergistic inhibitory efficacy of phytochemicals against the virulence traits of individual and mixed species of C. albicans and G. vaginalis in vitro and in vivo (Galleria mellonella). Out of five phytochemicals (carvacrol, thymol, cinnamaldehyde, eugenol, and borneol) screened for synergism with citral [(Ct) as the prime molecule owing to its myriad therapeutic potential], carvacrol (Ca) in combination with citral exhibited promising synergistic effect. Time-kill kinetics and one-minute contact-killing assays demonstrated the phenomenal microbicidal effect of Ct-Ca combination against both mono and dual-species within 30 min and one-minute time intervals, respectively. Furthermore, the sub-CMICs (synergistic combinatorial MIC) of Ct-Ca have significantly eradicated the mature biofilms and remarkably reduced the virulence attributes of both C. albicans and G. vaginalis (viz., yeast to hyphae transition, filamentation, protease production, and hydrophobicity index), in single and dual species states. The non-toxic nature of Ct-Ca combination was authenticated using in vitro (human erythrocyte cells) and in vivo (Galleria mellonella) models. In addition, the in vivo efficacy evaluation and subsequent histopathological investigation was done using the invertebrate model system G. mellonella, which further ascertained the effectiveness of Ct-Ca combination in fighting off the infection caused by individual and mixed species of C. albicans and G. vaginalis. Concomitantly, the current work is the first of its kind to delineate the in vitro interaction of C. albicans and G. vaginalis mixed species at their growth and biofilm states, together emphasizes the promising therapeutic potential of acclaimed phytochemicals as combinatorial synergistic therapy against mixed vaginitis.


Assuntos
Monoterpenos Acíclicos , Candida albicans , Candidíase Vulvovaginal , Cimenos , Sinergismo Farmacológico , Gardnerella vaginalis , Candida albicans/efeitos dos fármacos , Candida albicans/patogenicidade , Feminino , Cimenos/farmacologia , Animais , Monoterpenos Acíclicos/farmacologia , Gardnerella vaginalis/efeitos dos fármacos , Candidíase Vulvovaginal/tratamento farmacológico , Candidíase Vulvovaginal/microbiologia , Virulência/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Mariposas/microbiologia , Monoterpenos/farmacologia , Antifúngicos/farmacologia , Vaginose Bacteriana/tratamento farmacológico , Vaginose Bacteriana/microbiologia , Humanos , Biofilmes/efeitos dos fármacos
6.
BMC Plant Biol ; 24(1): 483, 2024 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-38822252

RESUMO

BACKGROUND: Zataria multiflora Boiss. is a medicinal and aromatic plant from the Lamiaceae family. It is extensively used in Iranian traditional medicine, mostly as a replacement for Thyme species. This study was focused on the analysis of chemical composition and the distribution and types of trichomes of Z. multiflora grown under different conditions. Equilibrium headspace analysis in combination with GC-FID-MS was used to identify volatile compounds released by aerial parts of Z. multiflora in development stages of 50 and 100% flowering under normal and drought-stress conditions. RESULTS: The main constituents were p-cymene (20.06-27.40%), γ-terpinene (12.44-16.93%), and α-pinene (6.91-16.58%) and thymol (8.52-9.99%). The highest content of p-cymene (27.40%) and thymol (9.99%) was observed in the 50% flowering stage at the 90% field capacity, while the maximum γ-terpinene (16.93%) content was recorded in the 100% flowering stage under normal conditions. Using the SEM method, it was found that peltate glandular and non-glandular trichomes are distributed on the surface of the leaf, stem, and outer side of the calyx. However, capitate trichomes only are detected on the stem and calyx in the 100% flowering and beginning of blooming stages, respectively. The type and structure of trichomes do not vary in different development stages, but they differ in density. The highest number of leaf peltate glandular trichomes was observed in the vegetative and beginning of blooming stages at 50% and 90% field capacity, respectively. Non-glandular trichomes of the stem were observed with high density in both normal and stress conditions, which are more densely in 90% field capacity. CONCLUSIONS: Since this plant has strong potential to be used in the food and pharmacological industries, this study provides valuable information for its cultivation and harvesting at specific phenological stages, depending on desired compounds and their concentrations.


Assuntos
Lamiaceae , Tricomas , Tricomas/crescimento & desenvolvimento , Tricomas/metabolismo , Lamiaceae/crescimento & desenvolvimento , Lamiaceae/metabolismo , Lamiaceae/fisiologia , Lamiaceae/química , Secas , Compostos Orgânicos Voláteis/metabolismo , Compostos Orgânicos Voláteis/análise , Estresse Fisiológico , Monoterpenos Cicloexânicos/metabolismo , Cimenos/metabolismo , Monoterpenos/metabolismo , Monoterpenos Bicíclicos/metabolismo , Timol/metabolismo
7.
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
8.
Exp Eye Res ; 244: 109938, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38789020

RESUMO

Neurodegenerative pathologies affecting the posterior segment of the eye, are characterized by being devastating and responsible for the majority of visual dysfunctions worldwide. These diseases are primarily degenerative, progressing chronically, and can inflict gradual harm to the optic nerve, retinal ganglion cells (RGC), photoreceptors, and other retinal cells. This retinal damage leads to a progressive loss of vision, marking these conditions as a significant health concern worldwide. The intravitreal administration of the phytochemical Carvacrol (CAR) is expected to demonstrate a neuroprotective and antiapoptotic effect on retinal cells, with a specific focus on RGC. This effect will be observed in a retinal degeneration model (RDM) in rabbits induced by cytotoxic and oxidative agents, namely glutamate (GLUT) and L-buthionine-S, R-sulfoximine (BSO). An in vivo study was conducted using New Zealand rabbits in which retinal damage was created to evaluate the effectiveness of CAR. The effectiveness of CAR on the functionality of retinal neuronal cells in RDM was evaluated using pupillary light reflection (PLR). Furthermore, the phytotherapeutic's influence on cell viability was determined through flow cytometry analysis. Finally, the neuroprotective and antiapoptotic capabilities of CAR were specifically scrutinized in RGC through histological studies, quantifying cell survival, and employing immunohistochemical assays to detect the apoptotic index (%) using the TUNEL technique. Our results demonstrated that CAR promoted the recovery of the pupillary contraction profile over time, maintaining the functionality of retinal cells as healthy controls. Additionally, it showed increased cell viability under oxidative and cytotoxic conditions given by GLUT-BSO agents. Finally, we found that CAR protects the survival of RGC and decreases the percentage of apoptotic cells when compared to RDM. CAR demonstrated to have positive effects on the functionality of photoreceptive nerve cells by restoring pupillary contraction. Likewise, it was shown to have neuroprotective and antiapoptotic effects when evaluated in a general and specific way on retinal nerve cells.


Assuntos
Sobrevivência Celular , Cimenos , Modelos Animais de Doenças , Degeneração Retiniana , Células Ganglionares da Retina , Animais , Coelhos , Degeneração Retiniana/prevenção & controle , Degeneração Retiniana/patologia , Degeneração Retiniana/metabolismo , Cimenos/farmacologia , Células Ganglionares da Retina/efeitos dos fármacos , Células Ganglionares da Retina/patologia , Sobrevivência Celular/efeitos dos fármacos , Apoptose/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Injeções Intravítreas , Citometria de Fluxo , Reflexo Pupilar/efeitos dos fármacos , Reflexo Pupilar/fisiologia
9.
Int J Food Microbiol ; 418: 110713, 2024 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-38718617

RESUMO

This research aimed to assess the potential of active food packaging as an innovative approach to enhance the quality of fresh food products. Specifically, our focus was on developing chitosan edible films combined with rosemary nanoemulsion (Ch-RNE) and carvacrol nano-emulsion (Ch-CNE) as effective antibacterial food packaging solutions. The efficacy of these films against artificially inoculated L. monocytogenes (NCTC 13372\ ATCC® 7644) as a Gram-positive bacterium, and S. enterica serovar Typhimurium (ATCC 14028) as a Gram-negative bacterium, in ground meat was investigated. The size of the prepared nano-emulsions was characterized using zeta sizer, FTIR and HRTEM. The MIC of both nano-emulsions against both pathogens was found to be 0.78 % and 1.56 %. Filmogenic mixtures were casted using these concentrations, which were then dried and evaluated for their physical and mechanical properties.


Assuntos
Antibacterianos , Quitosana , Cimenos , Filmes Comestíveis , Emulsões , Embalagem de Alimentos , Listeria monocytogenes , Monoterpenos , Salmonella typhimurium , Cimenos/farmacologia , Quitosana/farmacologia , Quitosana/química , Listeria monocytogenes/efeitos dos fármacos , Listeria monocytogenes/crescimento & desenvolvimento , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/crescimento & desenvolvimento , Emulsões/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Embalagem de Alimentos/métodos , Monoterpenos/farmacologia , Rosmarinus/química , Testes de Sensibilidade Microbiana , Microbiologia de Alimentos , Produtos da Carne/microbiologia , Conservação de Alimentos/métodos
10.
Int J Biol Macromol ; 271(Pt 2): 132488, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38763248

RESUMO

Nanoparticles are used as fillers to improve the properties of biopolymers, and their particle size is an important parameter. This work aims to investigate the effect of particle size of isoreticular metal-organic framework-3 (IRMOF-3) on the mechanical, physical, and release properties of sodium alginate (SA)-based composite active film. In our study, IRMOF-3 with six different particle sizes was synthesized by introducing additives. IRMOF-3 loading with carvacrol (IRMOF-3/CA nanoparticles) was incorporated into the SA matrix to prepare the composite film. The characterization and testing results of films showed that the particle size of nanoparticles affected the physical morphology and chemical structure of the film. Especially smaller nanoparticles uniformly dispersed into the SA matrix more easily, forming a denser and more stable spatial network structure with SA, which could more significantly improve the tensile strength, water vapor barrier, and hydrophobic properties of the film (P < 0.05). In addition, the CA release rate from the active film could be significantly reduced by about 33.90 % even when the smallest particle size of the IRMOF-3/CA nanoparticles was added. Therefore, when IRMOF-3/CA is used as the nano-filler to develop SA-based active film, its particle size has a potential influence on the properties of the film.


Assuntos
Alginatos , Estruturas Metalorgânicas , Nanocompostos , Tamanho da Partícula , Alginatos/química , Nanocompostos/química , Estruturas Metalorgânicas/química , Resistência à Tração , Cimenos/química , Interações Hidrofóbicas e Hidrofílicas , Vapor
11.
Biomed Pharmacother ; 175: 116692, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38701569

RESUMO

CCl4 toxicity is a fatal condition that can cause numerous organ dysfunctions. We evaluated and compared the protective effects of cuminaldehyde (CuA), thymoquinone (TQ), and gallic acid (GA) on CCl4-induced pulmonary and renal toxicity in rats. The impacts of these compounds on CCl4-induced oxidative stress, inflammation, and morphological alterations were examined. The results showed that the compounds under investigation prevented CCl4 from significantly increasing pulmonary and renal lipid peroxidation and NO levels, as well as massively depleting GSH levels and GPX and SOD activities. Moreover, they suppressed the CCl4-induced increase in mucus secretion in the lung and upregulated the gene expression of pulmonary and renal NF-Ò¡B, iNOS, TNF-α, and COX-2. The heatmap cluster plots showed that GA and TQ had better protective potencies than CuA. The external organ morphology, histopathological results, and chest X-ray analysis confirmed the toxicity of CCl4 and the protective influences of the tested compounds in both the lungs and kidneys of rats. These compounds displayed predicted competitive inhibitory effects on iNOS activity and may block the IL-13α2 receptor, as revealed by molecular docking analysis. Thus, CuA, TQ, and GA, particularly the latter two, are prospective protective compounds against the pulmonary and renal toxicity caused by CCl4.


Assuntos
Benzaldeídos , Benzoquinonas , Tetracloreto de Carbono , Ácido Gálico , Rim , Pulmão , NF-kappa B , Estresse Oxidativo , Espécies Reativas de Oxigênio , Transdução de Sinais , Animais , Ácido Gálico/farmacologia , Benzoquinonas/farmacologia , Transdução de Sinais/efeitos dos fármacos , Masculino , NF-kappa B/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Ratos , Tetracloreto de Carbono/toxicidade , Rim/efeitos dos fármacos , Rim/patologia , Rim/metabolismo , Benzaldeídos/farmacologia , Pulmão/efeitos dos fármacos , Pulmão/patologia , Pulmão/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Simulação de Acoplamento Molecular , Cimenos/farmacologia , Substâncias Protetoras/farmacologia , Antioxidantes/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Ratos Wistar , Ratos Sprague-Dawley
12.
Asian Pac J Cancer Prev ; 25(5): 1663-1671, 2024 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-38809638

RESUMO

BACKGROUND: Cancer is a challenge for either the patient or the healthcare manager. Treatment protocols based on chemotherapy or radiotherapy, or both are interfering with the patient's life making him suffer rather than being alleviated. This burden pushed the scientists to search for new regimens that may help ameliorate patient as well as doctor inconvenience. Benefits of plant extracts as medical substitutes in cancer management have been proved. New nano formulated drug delivery systems may help overcoming remedy regimens barriers and obstacles. The present research topic aims to evaluate the anticancer power of two plant extracts in nano emulsion formulation on human melanoma cell line. METHODS: Carvacrol and rosemary essential oils were obtained, and nano emulsions were formulated. NE were characterized using TEM for charge and size distribution. The A375 human melanoma cell line was cultured and propagated then IC50 of prepared NE was added. Assessment of cell cytotoxicity, effect on angiogenesis and apoptosis were tested. RESULTS: After synthesis and characterization, both carvacrol nano emulsion (CNE) and rosemary nano emulsion (RNE) were capable of inhibiting melanoma cell line viability, angiogenesis and they enhanced the expression of caspase-3 proapoptotic marker. CONCLUSION: Rosemary and carvacrol extract nano emulsions could be a new revolutionary agent in human melanoma therapy and these formulations can be applied locally.


Assuntos
Apoptose , Cimenos , Emulsões , Melanoma , Óleos Voláteis , Extratos Vegetais , Humanos , Emulsões/química , Melanoma/tratamento farmacológico , Melanoma/patologia , Extratos Vegetais/farmacologia , Apoptose/efeitos dos fármacos , Cimenos/farmacologia , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Nanopartículas/química , Proliferação de Células/efeitos dos fármacos , Células Tumorais Cultivadas , Sobrevivência Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sistemas de Liberação de Medicamentos
13.
Cell Biochem Funct ; 42(4): e4062, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38807490

RESUMO

Since most solid tumors have a low pH value, a pH-responsive drug delivery system may offer a broad method for tumor-targeting treatment. The present study is used to analyze the anticancer activity of carvacrol-zinc oxide quantum dots (CVC-ZnO QDs) against breast cancer cells (MDA-MB-231). CVC-ZnO QDs demonstrate pH responsive and are specifically released within the acidic pH tumor microenvironment. This property enables targeted drug delivery exclusively to cancer cells while minimizing the impact on normal cells. To the synthesized ZnO QDs, the CVC was loaded and then examined by X-ray diffraction, ultraviolet-visible, Fourier transform infrared spectrophotometer, scanning electron microscopy-energy dispersive X-ray, and transmission electron microscopy. For up to 20 h, CVC release was examined in different pH-buffered solutions. The results showed that carvacrol release was stable in an acidic pH solution. Further, cytotoxicity assay, antioxidant, and lipid peroxidation activity, reactive oxygen species, mitochondrial membrane potential, nuclear damage, and the ability of CVC-ZnO QDs to cause apoptosis were all examined. Apoptosis markers such as Bcl2, Bax, caspase-3, and caspase-9, were also studied. In conclusion, the CVC-ZnO QDs destabilized the MDA-MB-231cells under its acidic tumor microenvironment and regulated apoptosis.


Assuntos
Antineoplásicos , Apoptose , Neoplasias da Mama , Cimenos , Pontos Quânticos , Óxido de Zinco , Humanos , Pontos Quânticos/química , Óxido de Zinco/química , Óxido de Zinco/farmacologia , Óxido de Zinco/síntese química , Cimenos/farmacologia , Cimenos/química , Concentração de Íons de Hidrogênio , Neoplasias da Mama/patologia , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/metabolismo , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Feminino , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Espécies Reativas de Oxigênio/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Potencial da Membrana Mitocondrial/efeitos dos fármacos
14.
Molecules ; 29(10)2024 May 12.
Artigo em Inglês | MEDLINE | ID: mdl-38792138

RESUMO

Cancer is ranked among lethal diseases globally, and the increasing number of cancer cases and deaths results from limited access to effective therapeutics. The use of plant-based medicine has been gaining interest from several researchers. Carvacrol and its isomeric compound, thymol, are plant-based extracts that possess several biological activities, such as antimalarial, anticancer, antifungal, and antibacterial. However, their efficacy is compromised by their poor bioavailability. Thus, medicinal scientists have explored the synthesis of hybrid compounds containing their pharmacophores to enhance their therapeutic efficacy and improve their bioavailability. Hence, this review is a comprehensive report on hybrid compounds containing carvacrol and its isomer, thymol, with potent anticancer and antibacterial agents reported between 2020 and 2024. Furthermore, their structural activity relationship (SAR) and recommended future strategies to further enhance their therapeutic effects will be discussed.


Assuntos
Antibacterianos , Antineoplásicos , Cimenos , Timol , Timol/química , Timol/farmacologia , Cimenos/química , Cimenos/farmacologia , Cimenos/uso terapêutico , Humanos , Antibacterianos/farmacologia , Antibacterianos/química , Antineoplásicos/farmacologia , Antineoplásicos/química , Relação Estrutura-Atividade , Neoplasias/tratamento farmacológico , Animais
15.
Food Res Int ; 187: 114458, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38763690

RESUMO

This study examines the antimicrobial and antibiofilm effectiveness of baicalin and carvacrol against Salmonella enterica ser. Typhimurium on food contact surfaces and chicken meat. The minimum inhibitory concentrations (MIC) for baicalin and carvacrol were found to be 100 µg/mL and 200 µg/mL, respectively, which aligns with findings from previous studies. The compounds exhibited a concentration-dependent decrease in microbial populations and biofilm formation. When used together, they displayed a remarkable synergistic effect, greatly augmenting their antibacterial activity. The assessment of food quality demonstrated that these treatments have no negative impact on the sensory characteristics of chicken meat. The impact of the structure on biofilms was observed through the use of Field Emission Scanning Electron Microscopy (FE-SEM) and Confocal Laser Scanning Microscopy (CLSM), revealing disrupted biofilm architectures and decreased cell viability. Crucially, RT-PCR analysis revealed a marked downregulation of quorum sensing (luxS), virulence (hilA), and stress response (rpoS) genes, highlighting the multifaceted antimicrobial mechanism of action. This gene-specific suppression suggests a targeted disruption of bacterial communication and virulence pathways, offering insight into the comprehensive antibiofilm strategy. This provides further insight into the molecular mechanisms that contribute to their antibiofilm effects.


Assuntos
Antibacterianos , Biofilmes , Galinhas , Cimenos , Flavonoides , Microbiologia de Alimentos , Testes de Sensibilidade Microbiana , Salmonella typhimurium , Biofilmes/efeitos dos fármacos , Cimenos/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Flavonoides/farmacologia , Antibacterianos/farmacologia , Animais , Percepção de Quorum/efeitos dos fármacos , Carne/microbiologia , Monoterpenos/farmacologia , Microscopia Eletrônica de Varredura
16.
Biochim Biophys Acta Biomembr ; 1866(5): 184332, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38740123

RESUMO

The mechanism of chemotherapeutic action of Ru-based drugs involves plasma membrane disruption and valuable insights into this process may be gained using cell membrane models. The interactions of a series of cytotoxic η6-p-cymene ruthenium(II) complexes, [Ru(η6-p-cymene)P(3,5-C(CH3)3-C6H3)3Cl2] (1), [Ru(η6-p-cymene)P(3,5-CH3-C6H3)3Cl2] (2), [Ru(η6-p-cymene)P(4-CH3O-3,5-CH3-C6H2)3Cl2] (3), and [Ru(η6-p-cymene)P(4-CH3O-C6H4)3Cl2] (4), were examined using Langmuir monolayers as simplified healthy and cancerous outer leaflet plasma membrane models. The cancerous membrane (CM1 and CM2) models contained either 40 % 1,2- dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) or 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), 30 % cholesterol (Chol), 20 % 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE), and 10 % 1,2-dipalmitoyl-sn-glycero-3-phospho-l-serine (DPPS). Meanwhile, the healthy membrane (HM1 and HM2) models were composed of 60 % DPPC or DOPC, 30 % Chol and 10 % DPPE. The complexes affected surface pressure isotherms and decreased compressional moduli of cancerous and healthy membrane models, interacting with the monolayers headgroup and tails according to data from polarization-modulated infrared reflection absorption spectroscopy (PM-IRRAS). However, the effects did not correlate with the toxicity of the complexes to cancerous and healthy cells. Multidimensional projection technique showed that the complex (1) induced significant changes in the CM1 and HM1 monolayers, though it had the lowest cytotoxicity against cancer cells and is not toxic to healthy cells. Moreover, the most toxic complexes (2) and (4) were those that least affected CM2 and HM2 monolayers. The findings here support that the ruthenium complexes interact with lipids and cholesterol in cell membrane models, and their cytotoxic activities involve a multifaceted mode of action beyond membrane disruption.


Assuntos
Membrana Celular , Cimenos , Rutênio , Cimenos/química , Cimenos/farmacologia , Membrana Celular/efeitos dos fármacos , Membrana Celular/química , Rutênio/química , Rutênio/farmacologia , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Monoterpenos/química , Monoterpenos/farmacologia , 1,2-Dipalmitoilfosfatidilcolina/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Fosfatidilcolinas/química
17.
Brain Res ; 1836: 148954, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-38649135

RESUMO

Parkinson's disease (PD) is a multifactorial neurodegenerative disorder whose cause is unclear. Neuroinflammation is recognized as one of the major pathogenic mechanisms involved in the development and progression of PD. NLRP3 inflammasome is the most widely studied inflammatory mediator in various diseases including PD. Several phytoconstituents have shown neuroprotective role in PD. Carvacrol is a phenolic monoterpene commonly found in the essential oils derived from plants belonging to Lamiaceae family. It is well known for its anti-inflammatory and antioxidant properties and has been widely explored in several diseases. In this study, we explored the role of Carvacrol in suppressing neuroinflammation by regulating NLRP3 inflammasome through Nrf2/HO-1 axis and subsequently, inflammatory cytokines like IL-1ß, IL-18 in Rotenone induced PD mice model. Three doses (25 mg/kg, 50 mg/kg, 100 mg/kg p.o.) of Carvacrol were administered to, respectively, three groups (LD, MD, HD), one hour after administration of Rotenone (1.5 mg/kg, i.p.), every day, for 21 days. Treatment with Carvacrol ameliorated the motor impairment caused by Rotenone. It alleviated neurotoxicity and reduced inflammatory cytokines. Further, Carvacrol also alleviated oxidative stress and increased antioxidant enzymes. From these results, we show that Carvacrol exerts neuroprotective effects in PD via anti-inflammatory and antioxidant mechanisms and could be a potential therapeutic option in PD.


Assuntos
Cimenos , Modelos Animais de Doenças , Fator 2 Relacionado a NF-E2 , Proteína 3 que Contém Domínio de Pirina da Família NLR , Fármacos Neuroprotetores , Rotenona , Animais , Fator 2 Relacionado a NF-E2/metabolismo , Fator 2 Relacionado a NF-E2/efeitos dos fármacos , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/efeitos dos fármacos , Cimenos/farmacologia , Camundongos , Fármacos Neuroprotetores/farmacologia , Masculino , Inflamassomos/metabolismo , Inflamassomos/efeitos dos fármacos , Heme Oxigenase (Desciclizante)/metabolismo , Doença de Parkinson/tratamento farmacológico , Doença de Parkinson/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Antioxidantes/farmacologia , Proteínas de Membrana , Heme Oxigenase-1
18.
BMC Res Notes ; 17(1): 104, 2024 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-38605312

RESUMO

BACKGROUND: Candida, a common oral microbiota, can cause opportunistic fungal infections. With rising Candida infections and limited effective antifungals, new treatments are needed. This study investigates carvacrol essential oil's effect on oral candidiasis, alone and with nystatin, compared to nystatin alone. MATERIALS AND METHODS: In this study, oral samples were collected from dental clinic patients, especially denture users. The presence of Candida was confirmed and cultured from these samples. Candidiasis was detected by observing Candida colonies. Drug sensitivity was tested on 100 positive samples. The minimum concentration of inhibition and lethality of each isolate was evaluated using nystatin and carvacrol. The results were compared using two-way analysis of variance. Finally, the minimum inhibitory concentration (MIC) of nystatin and carvacrol was calculated individually and in combination. RESULTS: The present study found that Candida albicans and non-albicans species were equally prevalent. Carvacrol showed significant biological activity against all Candida species, with an average MTT of 50.01%. The average MIC value of carvacrol was 24.96 µg/ml, indicating its potential to inhibit Candida growth. The mean Minimum Fungicidal Concentration (MFC) value of carvacrol was 23.48 µg/ml, suggesting its effectiveness in killing the fungi. CONCLUSION: The study's findings reveal that the MIC of carvacrol was significantly lower than that of nystatin and the combination of nystatin and carvacrol. This suggests that carvacrol holds potential as an effective herbal remedy for candidiasis.


Assuntos
Candidíase Bucal , Candidíase , Cimenos , Humanos , Nistatina/farmacologia , Candidíase Bucal/tratamento farmacológico , Candidíase Bucal/microbiologia , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Candida , Candida albicans , Candidíase/tratamento farmacológico , Testes de Sensibilidade Microbiana
19.
J Appl Microbiol ; 135(4)2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38587823

RESUMO

AIM: In this study, it was aimed to examine the antibacterial activity of the essential oil components (EOCs), carvacrol (CAR), cinnamaldehyde (CIN), thymol (TH), alpha pinene (α-PN), eucalyptol (EU), limonene (LIM), and the antibiotics, linezolid (LZD), vancomycin (VAN), gentamicin (GEN), ciprofloxacin (CIP), clindamycin (CLN), and penicillin (PEN) against 50 multidrug resistant Corynebacterium striatum strains, and the synergistic interactions of CAR and CIN with the antibiotics against 10 randomly selected Coryne. striatum strains to explore synergistic interactions to determine if their combined use could enhance antibiotic activity and potentially reduce resistance. METHODS AND RESULTS: The activity of the EOCs and the antibiotics against Coryne. striatum strains isolated from clinical specimens, was examined by broth microdilution method. The synergistic interactions of the EOCs with the antibiotics against 10 randomly selected Coryne. striatum strains were determined by checkerboard method. EOCs, CIN, and CAR and antibiotics, LZD, VAN, GEN, CIP, and CLN were detected to have antibacterial activity against Coryne. striatum strains alone and either synergistic interactions were observed in combinations of the antibiotics with EOCs. CONCLUSIONS: All Coryne. striatum strains were determined to be susceptible to VAN and LZD and resistant to GEN, PEN, CIP, and CLN. Synergistic interactions were observed in all combinations of antibiotics tested with CAR and CIN.


Assuntos
Acroleína , Acroleína/análogos & derivados , Antibacterianos , Corynebacterium , Farmacorresistência Bacteriana Múltipla , Sinergismo Farmacológico , Testes de Sensibilidade Microbiana , Monoterpenos , Óleos Voláteis , Antibacterianos/farmacologia , Corynebacterium/efeitos dos fármacos , Óleos Voláteis/farmacologia , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Acroleína/farmacologia , Monoterpenos/farmacologia , Cimenos/farmacologia , Ciprofloxacina/farmacologia , Gentamicinas/farmacologia , Vancomicina/farmacologia , Linezolida/farmacologia , Limoneno/farmacologia , Eucaliptol/farmacologia , Timol/farmacologia , Clindamicina/farmacologia , Humanos , Penicilinas/farmacologia , Terpenos/farmacologia , Cicloexenos/farmacologia , Infecções por Corynebacterium/microbiologia
20.
Sci Rep ; 14(1): 9218, 2024 04 22.
Artigo em Inglês | MEDLINE | ID: mdl-38649444

RESUMO

For reducing Campylobacter (C.) in the food production chain and thus the risk to the consumer, the combined application of different measures as a multiple-hurdle approach is currently under discussion. This is the first study to investigate possible synergistic activities in vivo, aiming at reducing intestinal C. jejuni counts by administering (i) bacteriophages (phages) in combination with a competitive exclusion (CE) product and (ii) carvacrol combined with organic acids. The combined application of the two selected phages (Fletchervirus phage NCTC 12673 and Firehammervirus phage vB_CcM-LmqsCPL1/1) and the CE product significantly reduced C. jejuni loads by 1.0 log10 in cecal and colonic contents as well as in cloacal swabs at the end of the trial (33 and 34 days post hatch). The proportion of bacterial isolates showing reduced phage susceptibility ranged from 10.9% (isolates from cecal content) to 47.8% (isolates from cloacal swabs 32 days post hatch) for the Fletchervirus phage, while all tested isolates remained susceptible to the Firehammervirus phage. The use of carvacrol combined with an organic acid blend (sorbic acid, benzoic acid, propionic acid, and acetic acid) significantly reduced Campylobacter counts by 1.0 log10 in cloacal swabs on day 30 only.


Assuntos
Bacteriófagos , Galinhas , Cimenos , Cimenos/farmacologia , Animais , Bacteriófagos/fisiologia , Galinhas/microbiologia , Infecções por Campylobacter/prevenção & controle , Infecções por Campylobacter/microbiologia , Doenças das Aves Domésticas/microbiologia , Doenças das Aves Domésticas/prevenção & controle , Doenças das Aves Domésticas/virologia , Campylobacter jejuni/virologia , Campylobacter jejuni/efeitos dos fármacos , Campylobacter/efeitos dos fármacos , Campylobacter/virologia
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