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1.
Clin Oral Investig ; 28(7): 413, 2024 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-38965139

RESUMO

OBJECTIVES: This study compares the biofilm inhibition effects of denture cleaning tablets, carvacrol, and their combined use against Candida albicans on denture bases produced with different techniques. Additionally, the surface roughness and contact angles of these denture bases were evaluated. MATERIALS AND METHODS: Test samples were prepared from four different denture base materials (cold-polymerized, heat-polymerized, CAD/CAM milling, and 3D-printed). The surface roughness and contact angles of the test samples were measured using a profilometer and goniometer, respectively. For the evaluation of biofilm inhibition, samples were divided into 5 subgroups: Corega and carvacrol, separately and combined treatments, positive (inoculated with C. albicans) and negative control (non-inoculated with C. albicans, only medium). Biofilm mass was determined using the crystal violet method. An additional prepared test sample for each subgroup was examined under scanning electron microscopy (SEM). RESULTS: The surface roughness values of the 3D-printed test samples were found to be statistically higher than the other groups (P < .001). The water contact angle of all test materials was not statistically different from each other (P > .001). Corega and carvacrol, separately and combined, significantly decreased the amount of biofilm on all surfaces (P < .0001). Treatment of corega alone and in combination with carvacrol to the 3D-printed material caused less C. albicans inhibition than the other groups (P < .001; P < .05). CONCLUSIONS: The surface roughness values of all test groups were within the clinically acceptable threshold. Although Corega and carvacrol inhibited C. albicans biofilms, their combined use did not show a synergistic effect. CLINICAL RELEVANCE: Carvacrol may be used as one of the disinfectant agents for denture cleaning due to its biofilm inhibition property.


Assuntos
Biofilmes , Candida albicans , Cimenos , Bases de Dentadura , Higienizadores de Dentadura , Teste de Materiais , Microscopia Eletrônica de Varredura , Propriedades de Superfície , Biofilmes/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Bases de Dentadura/microbiologia , Cimenos/farmacologia , Higienizadores de Dentadura/farmacologia , Impressão Tridimensional , Comprimidos
2.
Int J Mol Sci ; 25(13)2024 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-39000327

RESUMO

Microbial biofilms pose severe problems in the medical field and food industry, as they are the cause of many serious infections and food-borne diseases. The extreme biofilms' resistance to conventional anti-microbial treatments presents a major challenge to their elimination. In this study, the difference in resistance between Staphylococcus aureus DSMZ 12463 biofilms, biofilm-detached cells, and planktonic cells against microcapsules containing carvacrol was assessed. The antimicrobial/antibiofilm activity of low pH disinfection medium containing the microencapsulated carvacrol was also studied. In addition, the effect of low pH on the in vitro carvacrol release from microcapsules was investigated. The minimum inhibitory concentration of microencapsulated carvacrol was 0.625 mg mL-1. The results showed that biofilms exhibited greater resistance to microencapsulated carvacrol than the biofilm-detached cells and planktonic cells. Low pH treatment alone, by hydrochloric acid addition, showed no bactericidal effect on any of the three states of S. aureus strain. However, microencapsulated carvacrol was able to significantly reduce the planktonic cells and biofilm-detached cells below the detection limit (no bacterial counts), and the biofilm by approximatively 3 log CFU mL-1. In addition, results showed that microencapsulated carvacrol combined with low pH treatment reduced biofilm by more than 5 log CFU mL-1. Thus, the use of microencapsulated carvacrol in acidic environment could be a promising approach to combat biofilms from abiotic surfaces.


Assuntos
Antibacterianos , Biofilmes , Cimenos , Testes de Sensibilidade Microbiana , Staphylococcus aureus , Biofilmes/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/fisiologia , Cimenos/farmacologia , Concentração de Íons de Hidrogênio , Antibacterianos/farmacologia , Plâncton/efeitos dos fármacos , Cápsulas , Composição de Medicamentos/métodos , Farmacorresistência Bacteriana/efeitos dos fármacos
3.
BMC Complement Med Ther ; 24(1): 265, 2024 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-38992651

RESUMO

BACKGROUND: Origanum species have been used in various commercial constructions as a remedy against burns and wounds, agriculture, alcoholic drinks, fragrance, and flavoring substances of food products. The essential oil of Origanum onites L. (EOOO) and its component carvacrol (CV) possesses a wide range of biological activities including anti-cancer activity. PURPOSE: The purpose of this study was to investigate the growth inhibitory activity of the essential oil and its major component CV and then hepatotoxicity pathway-related genes in HepG2 cells. METHODS: The effects of the EOOO and CV on cell growth and mRNA expressions of 84 hepatotoxicity pathway-related genes were investigated in HepG2, using trypan blue exclusion/ bromodeoxyuridine (BrdU) incorporation tests and real-time-polymerase chain reaction (RT-PCR) array, respectively. RESULTS: The EOOO and CV inhibited cell growth with IC50 values of 0.08 µg/mL and 45 µg/mL, respectively, after 24 h. Real-time, reverse-transcription-polymerase chain reaction (RT2-PCR) array analysis revealed that expressions of 32 genes out of 84 were changed at least 2-fold or more in the EOOO-treated cells. Among them, expression levels of 17 genes were elevated, while expression levels of 15 genes were diminished. Furthermore, after exposure of cells to 45 µg/mL of CV, the expression of 8 genes was increased while the other 8 genes were decreased. Both the EOOO and carvacrol affected the expression of 48 genes of HepG2 cells which are involved in the hepatotoxicity pathway, indicating their hepatoprotective and possible anti-hepatocarcinogenic effects. CONCLUSION: The present study demonstrates that the essential oil of Origanum onites and carvacrol can be used in various applications such as anticancer or herbal drugs, since its non-hepatotoxicity.


Assuntos
Cimenos , Monoterpenos , Óleos Voláteis , Origanum , Humanos , Cimenos/farmacologia , Óleos Voláteis/farmacologia , Origanum/química , Células Hep G2 , Monoterpenos/farmacologia , Proliferação de Células/efeitos dos fármacos
4.
Molecules ; 29(13)2024 Jul 06.
Artigo em Inglês | MEDLINE | ID: mdl-38999167

RESUMO

Organometallic complexes of the formula [Ru(N^N)(p-cymene)Cl][X] (N^N = bidentate polypyridyl ligands, p-cymene = 1-methyl-4-(1-methylethyl)-benzene, X = counter anion), are currently studied as possible candidates for the potential treatment of cancer. Searching for new organometallic compounds with good to moderate cytotoxic activities, a series of mononuclear water-soluble ruthenium(II)-arene complexes incorporating substituted pyridine-quinoline ligands, with pending -CH2OH, -CO2H and -CO2Me groups in the 4-position of quinoline ring, were synthesized, for the first time, to study their possible effect to modulate the activity of the ruthenium p-cymene complexes. These include the [Ru(η6-p-cymene)(pqhyme)Cl][X] (X = Cl- (1-Cl), PF6- (1-PF6), pqhyme = 4-hydroxymethyl-2-(pyridin-2-yl)quinoline), [Ru(η6-p-cymene)(pqca)Cl][Cl] ((2-Cl), pqca = 4-carboxy-2-(pyridin-2-yl)quinoline), and [Ru(η6-p-cymene)(pqcame)Cl][X] (X = Cl- (3-Cl), PF6- (3-PF6), pqcame = 4-carboxymethyl-2-(pyridin-2-yl)quinoline) complexes, respectively. Identification of the complexes was based on multinuclear NMR and ATR-IR spectroscopic methods, elemental analysis, conductivity measurements, UV-Vis spectroscopic, and ESI-HRMS techniques. The solid-state structures of 1-PF6 and 3-PF6 have been elucidated by single-crystal X-ray diffraction revealing a three-legged piano stool geometry. This is the first time that the in vitro cytotoxic activities of these complexes are studied. These were conducted in HEK293T (human embryonic kidney cells) and HeLa cells (cervical cancer cells) via the MTT assay. The results show poor in vitro anticancer activities for the HeLa cancer cell lines and 3-Cl proved to be the most potent (IC50 > 80 µΜ). In both cell lines, the cytotoxicity of the ligand precursor pqhyme is significantly higher than that of cisplatin.


Assuntos
Antineoplásicos , Complexos de Coordenação , Cimenos , Piridinas , Quinolinas , Rutênio , Humanos , Rutênio/química , Quinolinas/química , Quinolinas/síntese química , Quinolinas/farmacologia , Ligantes , Cimenos/química , Cimenos/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Piridinas/química , Piridinas/síntese química , Piridinas/farmacologia , Complexos de Coordenação/química , Complexos de Coordenação/farmacologia , Complexos de Coordenação/síntese química , Estrutura Molecular , Linhagem Celular Tumoral , Cristalografia por Raios X , Sobrevivência Celular/efeitos dos fármacos
5.
ACS Appl Mater Interfaces ; 16(28): 36017-36029, 2024 Jul 17.
Artigo em Inglês | MEDLINE | ID: mdl-38975983

RESUMO

Oral infectious diseases have a significant impact on the health of oral and maxillofacial regions, as well as the overall well-being of individuals. Carvacrol and thymol, two isomers known for their effective antibacterial and anti-inflammatory properties, have gained considerable attention in the treatment of oral infectious diseases. However, their application as topical drugs for oral use is limited due to their poor physical and chemical stability. UiO-66, a metal-organic framework based on zirconium ion (Zr4+), exhibits high drug loading capability. Carvacrol and thymol were efficiently loaded onto UiO-66 with loading rates of 79.60 ± 0.71% and 79.65 ± 0.76%, respectively. The release rates of carvacrol and thymol were 77.82 ± 0.87% and 76.51 ± 0.58%, respectively, after a period of 72 h. Moreover, Car@UiO-66 and Thy@UiO-66 demonstrated excellent antibacterial properties against Candida albicans, Escherichia coli, and Staphylococcus aureus with minimum bactericidal concentrations (MBC) of 0.313 mg/mL, 0.313 mg/mL, and 1.25 mg/mL, respectively. Furthermore, based on the results of the CCK8 cytotoxicity assay, even at concentrations as high as 1.25 mg/mL, Car@UiO-66 and Thy@UiO-66 exhibited excellent biocompatibility with a relative cell survival rate above 50%. These findings suggest that Car@UiO-66 and Thy@UiO-66 possess favorable biocompatibility properties without significant toxicity towards periodontal membrane cells. Additionally, in vivo studies confirmed the efficacy of Car@UiO-66and Thy@UiO-66 in reducing inflammation, promoting bone formation through inhibition of TNF-a and IL6 expression, enhancement of IL10 expression, and acceleration of bone defect healing. Therefore, the unique combination of antibacterial, anti-inflammatory, and osteogenic properties make Car@UiO-66 and Thy@Ui O-66 promising candidates for the treatment of oral infectious diseases and repairing bone defects.


Assuntos
Antibacterianos , Anti-Inflamatórios , Candida albicans , Cimenos , Escherichia coli , Estruturas Metalorgânicas , Staphylococcus aureus , Timol , Timol/química , Timol/farmacologia , Cimenos/química , Cimenos/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Estruturas Metalorgânicas/química , Estruturas Metalorgânicas/farmacologia , Camundongos , Testes de Sensibilidade Microbiana , Ratos , Osteogênese/efeitos dos fármacos , Humanos
6.
Turkiye Parazitol Derg ; 48(2): 72-76, 2024 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-38958374

RESUMO

Objective: Trichomonas vaginalis is a sexually transmitted protozoan parasite that usually causes infections in women. Metronidazole is used as the first choice in the treatment of this parasitic disease, but there is a need for new drugs since 1980's with increasing numbers of reported resistance. In this study, it was aimed to determine the antitrichomonal activity of the major components of Cinnamomum zeylanicum (cinnamon) and Thymus vulgaris (thyme) essential oils, cinnamaldehyde, carvacrol and thymol against metronidazole resistant and susceptible T. vaginalis strains, and to determine their interaction with metronidazole by checkerboard method. Methods: Cinnamaldehyde, carvacrol, thymol and metronidazole were obtained commercially. Two clinical isolates and one metronidazole resistant T. vaginalis reference strain were used in the study. MIC50 and MLC values of essential oil components and metronidazole were determined by broth microdilution method. The combinations of essential oil components with metronidazole were determined by the checkerboard method. Results: According to in vitro activity tests, cinnamaldehyde was determined to be most effective essential oil component. Clinical isolates were susceptible to metronidazole. In combination study, metronidazole showed synergy with cinnamaldehyde and carvacrol, and partial synergy with thymol. Conclusion: It was determined that cinnamaldehyde, carvacrol and thymol, which are known to have high antimicrobial activity, also have strong activity against T. vaginalis isolates and show a synergistic interaction with metronidazole. The use of metronidazole at lower doses in the synergistic interaction may contribute to the literature in terms of reducing drug side effects, creating a versatile antimicrobial target, and reducing the rate of resistance development.


Assuntos
Acroleína , Cimenos , Sinergismo Farmacológico , Metronidazol , Monoterpenos , Óleos Voláteis , Timol , Thymus (Planta) , Trichomonas vaginalis , Acroleína/análogos & derivados , Acroleína/farmacologia , Timol/farmacologia , Cimenos/farmacologia , Metronidazol/farmacologia , Humanos , Óleos Voláteis/farmacologia , Thymus (Planta)/química , Trichomonas vaginalis/efeitos dos fármacos , Monoterpenos/farmacologia , Feminino , Cinnamomum zeylanicum/química , Antiprotozoários/farmacologia , Testes de Sensibilidade Microbiana , Resistência a Medicamentos
7.
Phytopathology ; 114(7): 1502-1514, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-39023506

RESUMO

Late blight, caused by the notorious pathogen Phytophthora infestans, poses a significant threat to potato (Solanum tuberosum) crops worldwide, impacting their quality as well as yield. Here, we aimed to investigate the potential use of cinnamaldehyde, carvacrol, and eugenol as control agents against P. infestans and to elucidate their underlying mechanisms of action. To determine the pathogen-inhibiting concentrations of these three plant essential oils (PEOs), a comprehensive evaluation of their effects using gradient dilution, mycelial growth rate, and spore germination methods was carried out. Cinnamaldehyde, carvacrol, and eugenol were capable of significantly inhibiting P. infestans by hindering its mycelial radial growth, zoospore release, and sporangium germination; the median effective inhibitory concentration of the three PEOs was 23.87, 8.66, and 89.65 µl/liter, respectively. Scanning electron microscopy revealed that PEOs caused the irreversible deformation of P. infestans, resulting in hyphal shrinkage, distortion, and breakage. Moreover, propidium iodide staining and extracellular conductivity measurements demonstrated that all three PEOs significantly impaired the integrity and permeability of the pathogen's cell membrane in a time- and dose-dependent manner. In vivo experiments confirmed the dose-dependent efficacy of PEOs in reducing the lesion diameter of potato late blight. Altogether, these findings provide valuable insight into the antifungal mechanisms of PEOs vis-à-vis late blight-causing P. infestans. By utilizing the inherent capabilities of these natural compounds, we could effectively limit the harmful impacts of late blight on potato crops, thereby enhancing agricultural practices and ensuring the resilience of global potato food production.


Assuntos
Cimenos , Eugenol , Óleos Voláteis , Phytophthora infestans , Doenças das Plantas , Solanum tuberosum , Phytophthora infestans/efeitos dos fármacos , Phytophthora infestans/fisiologia , Solanum tuberosum/microbiologia , Óleos Voláteis/farmacologia , Doenças das Plantas/microbiologia , Doenças das Plantas/prevenção & controle , Eugenol/farmacologia , Cimenos/farmacologia , Monoterpenos/farmacologia , Micélio/efeitos dos fármacos , Micélio/crescimento & desenvolvimento , Óleos de Plantas/farmacologia , Hifas/efeitos dos fármacos , Hifas/crescimento & desenvolvimento , Esporos/efeitos dos fármacos , Esporos/fisiologia , Acroleína/análogos & derivados
8.
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
9.
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
10.
Arch Biochem Biophys ; 758: 110062, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38880320

RESUMO

Carvacrol (CV) is an organic compound found in the essential oils of many aromatic herbs. It is nearly unfeasible to analyze all the current human proteins for a query ligand using in vitro and in vivo methods. This study aimed to clarify whether CV possesses an anti-diabetic feature via Docking-based inverse docking and molecular dynamic (MD) simulation and in vitro characterization against a set of novel human protein targets. Herein, the best poses of CV docking simulations according to binding energy ranged from -7.9 to -3.5 (kcal/mol). After pathway analysis of the protein list through GeneMANIA and WebGestalt, eight interacting proteins (DPP4, FBP1, GCK, HSD11ß1, INSR, PYGL, PPARA, and PPARG) with CV were determined, and these proteins exhibited stable structures during the MD process with CV. In vitro application, statistically significant results were achieved only in combined doses with CV or metformin. Considering all these findings, PPARG and INSR, among these target proteins of CV, are FDA-approved targets for treating diabetes. Therefore, CV may be on its way to becoming a promising therapeutic compound for treating Diabetes Mellitus (DM). Our outcomes expose formerly unexplored potential target human proteins, whose association with diabetic disorders might guide new potential treatments for DM.


Assuntos
Cimenos , Hipoglicemiantes , Metformina , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Monoterpenos , Humanos , Cimenos/farmacologia , Cimenos/química , Metformina/farmacologia , Metformina/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/uso terapêutico , Monoterpenos/farmacologia , Monoterpenos/química , Hiperglicemia/tratamento farmacológico , Hiperglicemia/metabolismo , Receptor de Insulina/metabolismo , PPAR gama/metabolismo , PPAR gama/química , Ligação Proteica , Simulação por Computador , Antígenos CD
11.
Bioorg Med Chem Lett ; 109: 129826, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-38830427

RESUMO

Carvacrol, called CA, is a dynamic phytoconstituent characterized by a phenol ring abundantly sourced from various natural reservoirs. This versatile scaffold serves as a pivotal template for the design and synthesis of novel drug molecules, harboring promising biological activities. The active sites positioned at C-4, C-6, and the hydroxyl group (-OH) of CA offer fertile ground for creating potent drug candidates from a pharmacological standpoint. In this comprehensive review, we delve into diverse synthesis pathways and explore the biological activity of CA derivatives. We aim to illuminate the potential of these derivatives in discovering and developing efficacious treatments against a myriad of life-threatening diseases. By scrutinizing the structural modifications and pharmacophore placements that enhance the activity of CA derivatives, we aspire to inspire the innovation of novel therapeutics with heightened potency and effectiveness.


Assuntos
Cimenos , Descoberta de Drogas , Cimenos/química , Cimenos/farmacologia , Cimenos/síntese química , Humanos , Estrutura Molecular , Animais , Relação Estrutura-Atividade , Monoterpenos/química , Monoterpenos/farmacologia , Monoterpenos/síntese química
12.
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
13.
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
14.
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
15.
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
16.
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
17.
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
18.
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
19.
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
20.
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
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