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1.
Sci Rep ; 14(1): 10650, 2024 05 09.
Artigo em Inglês | MEDLINE | ID: mdl-38724532

RESUMO

Avoiding fatigue is a long-standing challenge in both healthy and diseased individuals. Establishing objective standard markers of fatigue is essential to evaluate conditions in spatiotemporally different locations and individuals and identify agents to fight against fatigue. Herein, we introduced a novel method for evaluating fatigue using nervous system markers (including dopamine, adrenaline, and noradrenaline), various cytokine levels (such as interleukin [IL]-1ß, tumor necrosis factor [TNF]-α, IL-10, IL-2, IL-5 and IL-17A), and oxidative stress markers (such as diacron-reactive oxygen metabolites [d-ROMs] and biological antioxidant potential [BAP]) in a rat fatigue model. Using this method, the anti-fatigue effects of methyl dihydrojasmonate (MDJ) and linalool, the fragrance/flavor compounds used in various products, were assessed. Our method evaluated the anti-fatigue effects of the aforementioned compounds based on the changes in levels of the nerves system markers, cytokines, and oxidative stress markers. MDJ exerted more potent anti-fatigue effects than linalool. In conclusion, the reported method could serve as a useful tool for fatigue studies and these compounds may act as effective therapeutic agents for abrogating fatigue symptoms.


Assuntos
Monoterpenos Acíclicos , Citocinas , Modelos Animais de Doenças , Fadiga , Estresse Oxidativo , Animais , Estresse Oxidativo/efeitos dos fármacos , Monoterpenos Acíclicos/farmacologia , Ratos , Fadiga/tratamento farmacológico , Fadiga/metabolismo , Citocinas/metabolismo , Masculino , Ciclopentanos/farmacologia , Antioxidantes/farmacologia , Biomarcadores , Monoterpenos/farmacologia , Oxilipinas/farmacologia , Ratos Sprague-Dawley
2.
Pak J Pharm Sci ; 37(1(Special)): 223-229, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38747273

RESUMO

In this study, the anti-osteogenic properties of the volatile oil extracted from Homalomena gigantea rhizome using ethyl acetate (EtOAc) and methanol (MeOH) were examined. Gas chromatography-mass spectrometry (GC-MS) was employed for the identification of volatile components. Following this, bioassays were performed to evaluate their effects on osteogenesis, encompassing parameters like cell viability, osteoblast differentiation, collagen synthesis and mineralization. The GC-MS analysis revealed 19 compounds in the EtOAc extract and 36 compounds in the MeOH extract. In the MeOH extract, major constituents included bis(2-ethylhexyl) terephthalate (13.83%), linalool (9.58%), palmitic acid (6.55%) and stearic acid (4.29%). The EtOAc extract contained bis(2-ethylhexyl) terephthalate (16.64%), palmitic acid (5.60%) and stearic acid (3.11%) as the predominant components. Both the EtOAc and MeOH extracts of H. gigantea exhibited promising potential for further investigation in anti-osteoporosis research. These findings contribute to the exploration of natural compounds with potential anti-osteoporotic properties, expanding our understanding of their therapeutic potential.


Assuntos
Cromatografia Gasosa-Espectrometria de Massas , Óleos Voláteis , Osteogênese , Extratos Vegetais , Rizoma , Osteogênese/efeitos dos fármacos , Rizoma/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Animais , Sobrevivência Celular/efeitos dos fármacos , Osteoblastos/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Camundongos , Ácido Palmítico/farmacologia , Monoterpenos Acíclicos/farmacologia
3.
Bol. latinoam. Caribe plantas med. aromát ; 23(3): 382-389, mayo 2024. ilus, tab, graf
Artigo em Inglês | LILACS | ID: biblio-1538151

RESUMO

The extraction of geraniol from palmarosa oil using hydrotropic solvents was investigated. Palmarosa oil possesses an appealing rose aroma and properties like anti - inflammatory, antifungal, and antioxidant due to the presence of geraniol. The extraction of geraniol from palmarosa oil by using distillation methods like steam dis tillation and fractional distillation was a laborious process. So hydrotropes were tried for extraction. The geraniol yield and purity depend on parameters like concentration of hydrotrope, solvent volume ratio, and time period. Using the Box Benkhem Desig n (BBD), the extraction process was optimized. One of the major advantages of using hydrotropic solvents is that they were classified as green solvents, and recovery of solvents is also possible. To reduce the extraction time probe sonication is carried ou t. Different hydrotropic solvents with probe sonication are done on palmarosa oil by altering various process parameters to study the separation, yield, and purity.


Se investigó la extracción de geraniol del aceite de palmarosa utilizando solventes hidrotrópicos. El aceite de palmarosa posee un atractivo aroma a rosa y propiedades antiinflamatorias, antifúngicas y antioxidantes debido a la pr esencia de geraniol. La extracción de geraniol del aceite de palmarosa mediante métodos de destilación como la destilación por vapor y la destilación fraccionada ha sido un proceso laborioso. Por lo tanto, se probaron los hidrotropos para la extracción. El rendimiento y la pureza del geraniol dependen de parámetros como la concentración del hidrotropo, la relación de volumen del solvente y el período de tiempo. Se optimizó el proceso de extracción usando el diseño Box Benkhem (BBD). Una de las principales v entajas de usar solventes hidrotrópicos es que se clasifican como solventes verdes y también es posible recuperar los solventes. Para reducir el tiempo de extracción, se lleva a cabo una sonda de ultrasonido. Se realizan diferentes solventes hidrotropos co n sonda de ultrasonido en el aceite de palmarosa alterando varios parámetros del proceso para estudiar la separación, el rendimiento y la pureza.


Assuntos
Cymbopogon/química , Monoterpenos Acíclicos/farmacologia , Monoterpenos Acíclicos/química , Óleos de Plantas/farmacologia , Óleos de Plantas/química
4.
Parasit Vectors ; 17(1): 194, 2024 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-38664829

RESUMO

BACKGROUND: Sarcoptic mange is a serious animal welfare concern in bare-nosed wombats (Vombatus ursinus). Fluralaner (Bravecto®) is a novel acaricide that has recently been utilised for treating mange in wombats. The topical 'spot-on' formulation of fluralaner can limit treatment delivery options in situ, but dilution to a volume for 'pour-on' delivery is one practicable solution. This study investigated the in vitro acaricidal activity of Bravecto, a proposed essential oil-based diluent (Orange Power®), and two of its active constituents, limonene and citral, against Sarcoptes scabiei. METHODS: Sarcoptes scabiei were sourced from experimentally infested pigs. In vitro assays were performed to determine the lethal concentration (LC50) and survival time of the mites when exposed to varying concentrations of the test solutions. RESULTS: All compounds were highly effective at killing mites in vitro. The LC50 values of Bravecto, Orange Power, limonene and citral at 1 h were 14.61 mg/ml, 4.50%, 26.53% and 0.76%, respectively. The median survival times of mites exposed to undiluted Bravecto, Orange Power and their combination were 15, 5 and 10 min, respectively. A pilot survival assay of mites collected from a mange-affected wombat showed survival times of < 10 min when exposed to Bravecto and Orange Power and 20 min when exposed to moxidectin. CONCLUSIONS: These results confirm the acaricidal properties of Bravecto, demonstrate acaricidal properties of Orange Power and support the potential suitability of Orange Power and its active constituents as a diluent for Bravecto. As well as killing mites via direct exposure, Orange Power could potentially enhance the topical delivery of Bravecto to wombats by increasing drug penetration in hyperkeratotic crusts. Further research evaluating the physiochemical properties and modes of action of Orange Power and its constituents as a formulation vehicle would be of value.


Assuntos
Acaricidas , Isoxazóis , Óleos de Plantas , Sarcoptes scabiei , Escabiose , Animais , Sarcoptes scabiei/efeitos dos fármacos , Acaricidas/farmacologia , Isoxazóis/farmacologia , Escabiose/tratamento farmacológico , Escabiose/parasitologia , Óleos de Plantas/farmacologia , Óleos de Plantas/química , Monoterpenos Acíclicos/farmacologia , Suínos , Limoneno/farmacologia , Limoneno/química , Terpenos/farmacologia , Terpenos/química , Cicloexenos/farmacologia , Cicloexenos/química , Dose Letal Mediana
5.
Pestic Biochem Physiol ; 201: 105886, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38685252

RESUMO

This study evaluates the pediculicidal activity of nanoformulations containing different binary essential oil component mixtures (eugenol:linalool, 1,8 -cineole:linalool, and eugenol:thymol) using immersion bioassays. These have allowed us to evaluate the knockdown time affecting 50% of the individuals (KT50). In addition, the type of interaction between the components in each mixture was established in terms of the combination index (IC). The KT50 values were 6.07; 8.83; 7.17 and 27.23 h for linalool, 1,8 -cineole, eugenol, and thymol, respectively. For the eugenol:linalool mixtures, the efficacy was lower or equal to that obtained for the nanoformulations of the pure compounds, with values of KT50 about 13.33, 8.16 and 6.71 h for mixtures with ratios 3:1, 1:1 and 1:3, respectively. These mixtures present IC > 1, evidencing antagonistic interaction, which is enhanced with eugenol content. In the case of the binary mixtures of 1,8 -cineole: linalool, KT50 values were similar to those obtained for eugenol:linalool mixtures with similar ratios. In this case, IC assumes values close to unity, suggesting additive interactions independently of the mixture composition. On the other side, mixtures of eugenol:thymol with 1:1 and 1:3 ratios showed values of 9.40 and 32.93 h, while the mixture with a 3:1 ratio showed the greatest effectiveness (KT50 of 4.42 h). Eugenol:thymol mixtures show synergistic interaction (IC < 1) for combinations 3:1 and 1:1, while no interaction was observed for 1:3 combination. This indicates that eugenol enhances thymol activity. These results must be considered an important step forward to the development of effective pediculicidal nanoformulations based on botanical compounds.


Assuntos
Monoterpenos Acíclicos , Eucaliptol , Eugenol , Monoterpenos , Monoterpenos/farmacologia , Monoterpenos/química , Animais , Eugenol/farmacologia , Eugenol/química , Eucaliptol/farmacologia , Monoterpenos Acíclicos/farmacologia , Monoterpenos Acíclicos/química , Pediculus/efeitos dos fármacos , Inseticidas/farmacologia , Inseticidas/química , Timol/farmacologia , Timol/química , Micelas , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Nanopartículas/química , Infestações por Piolhos/tratamento farmacológico
6.
Int J Biol Macromol ; 266(Pt 2): 131344, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38574923

RESUMO

In this study, we obtained triple-layer films based on furcellaran and gelatin, in which the middle layer was enriched with extract of Curcuma longa in citral. This newly developed material underwent a comprehensive characterisation process to identify significant improvements in its functional properties. Both SEM, XRD and FTIR analyzes indicated the formation of interactions not only between the components but also between the film layers. Notably, the incorporation of the natural extract led to a significant reduction in solubility, decreasing it from 74.79 % to 57.25 %, while enhancing thermal stability expressed as a melting point elevating it from 147.10 °C in the control film to 158.80 °C in the film with the highest concentration of the active ingredient. Simultaneously, the addition of this active ingredient resulted in decreased water contact angle (WCA) values, rendering the film more hydrophilic. The produced films exhibit great promise as packaging materials, particularly within the food industry, and the conducted research is marked by its forward-looking and developmental approach.


Assuntos
Monoterpenos Acíclicos , Alginatos , Curcuma , Gelatina , Extratos Vegetais , Gomas Vegetais , Curcuma/química , Gelatina/química , Extratos Vegetais/química , Monoterpenos Acíclicos/química , Monoterpenos Acíclicos/farmacologia , Solubilidade , Embalagem de Alimentos/métodos , Interações Hidrofóbicas e Hidrofílicas , Água/química , Espectroscopia de Infravermelho com Transformada de Fourier
7.
Food Chem ; 449: 139240, 2024 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-38599109

RESUMO

The study reports the efficacy of nanofabricated citronellal inside the chitosan biopolymer (NeCn) against Aspergillus flavus growth, aflatoxin B1 (AFB1) production, and active ingredient biodeterioration (Piperine) in Piper longum L. The prepared NeCn was characterized by Scanning Electron Microscopy (SEM), Dynamic Light Scattering (DLS), and Fourier Transform Infrared Spectroscopy (FTIR). The results revealed that the NeCn exhibited distantly improved antifungal (1.25 µL/mL) and AFB1 inhibition (1.0 µL/mL) compared to free Cn. The perturbances in membrane function, mitochondrial membrane potential, antioxidant defense system, and regulatory genes (Ver-1 and Nor-1) of AFB1 biosynthesis were reported as probable modes of action of NeCn. The NeCn (1.25 µL/mL) effectively protects the P. longum from A. flavus (78.8%), AFB1 contamination (100%), and deterioration of Piperine (62.39%), thus demonstrating its potential as a promising novel antifungal agent for food preservation.


Assuntos
Monoterpenos Acíclicos , Aflatoxina B1 , Aspergillus flavus , Quitosana , Piper , Aflatoxina B1/metabolismo , Aspergillus flavus/efeitos dos fármacos , Aspergillus flavus/crescimento & desenvolvimento , Aspergillus flavus/metabolismo , Quitosana/química , Quitosana/farmacologia , Piper/química , Biopolímeros/química , Biopolímeros/farmacologia , Monoterpenos Acíclicos/farmacologia , Monoterpenos Acíclicos/química , Aldeídos/farmacologia , Aldeídos/química , Antifúngicos/farmacologia , Antifúngicos/química , Conservação de Alimentos/métodos , Monoterpenos/farmacologia , Monoterpenos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia
8.
Insect Sci ; 31(1): 134-146, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37358042

RESUMO

Monochamus alternatus is the primary carrier of pine wood nematodes, which pose a serious threat to Pinus spp. in many countries. Newly emerging M. alternatus adults feed on heathy host pines, while matured adults transfer to stressed host pines for mating and oviposition. Several odorant-binding proteins (OBPs) of M. alternatus have been proved to aid in the complex process of host location. To clarify the corresponding relations between OBPs and pine volatiles, more OBPs need to be studied. In this research, MaltOBP19 showed a specific expression in the antennae and mouthparts of M. alternatus, and it was marked in 4 types of antenna sensilla by immunolocalization. Fluorescence binding assays demonstrated the high binding affinity of MaltOBP19 with camphene and myrcene in vitro. In Y-tube olfactory experiments, M. alternatus adults were attracted by camphene and RNAi of OBP19 via microinjection significantly decreased their attraction index. Myrcene induced phobotaxis, but RNAi had no significant effect on this behavior. Further, we found that ingesting dsOBP19 produced by a bacteria-expressed system with a newly constructed vector could lead to the knockdown of MaltOBP19. These results suggest that MaltOBP19 may play a role in the process of host conversion via the recognition of camphene, which has been identified to be strongly released in stressed host pines. In addition, it is proved that knockdown of OBP can be achieved by oral administration of bacteria-expressed double-stranded RNA in M. alternatus adults, providing a new perspective in the control of M. alternatus.


Assuntos
Alcenos , Besouros , Pinus , Receptores Odorantes , Feminino , Animais , Besouros/genética , Monoterpenos Acíclicos/farmacologia , Monoterpenos Bicíclicos/farmacologia
9.
Phytomedicine ; 120: 155070, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37729771

RESUMO

BACKGROUND: Antimicrobial peptides (AMPs) are considered as the most potential alternatives to antibiotics, but they have several drawbacks, including high cost, medium antimicrobial efficacy, poor cell selectivity, which limit clinical application. To overcome the above problems, combination therapy of AMPs with adjuvants might maximize the effectiveness of AMPs. We found that citronellal can substantially potentiate the ZY4R peptide efficacy against Escherichia coli ATCC25922. However, it is unclear whether ZY4R/citronellal combination poses synergistic antimicrobial effects against most bacteria, and their synergy mechanism has not been elucidated. PURPOSE: To investigate synergistic antimicrobial efficacies, biosafety, and synergy mechanism of ZY4R/citronellal combination. METHOD: Checkerboard, time-kill curves, cytotoxicity assays, and in vivo animal models were conducted to assess synergistic antimicrobial effects and biosafety of the ZY4R/citronellal combination. To evaluate their synergy mechanism, a series of cell-based assays and transcriptome analysis were performed. RESULTS: ZY4R/citronellal combination exhibited synergistic antimicrobial effects against 20 clinically significant pathogens, with the fractional inhibitory concentration index (FICI) ranging from 0.313 to 0.047. Meanwhile, ZY4R/citronellal combination enhanced antimicrobial efficacies without compromising cell selectivity, contributing to decreasing drug dosage and improving biosafety. Compared with ZY4R (4 mg/kg) and citronellal (25 mg/kg) alone, ZY4R (4 mg/kg)/citronellal (25 mg/kg) combination significantly decreased the bacterial load in peritoneal fluid, liver, and kidney (P < 0.05) and alleviated pathological damage of the organs of mice. Mechanistic studies showed that ZY4R allowed citronellal to pass through the outer membrane rapidly and acted on the inner membrane together with citronellal, causing more potent membrane damage. The membrane damage prompted the continuous accumulation of citronellal in cells, and citronellal further induced energy breakdown and inhibited exopolysaccharide (EPS) production, which aggravated ZY4R-induced outer membrane damage, thereby resulting in bacterial death. CONCLUSIONS: ZY4R/citronellal combination exhibited broad-spectrum synergy with a low resistance development and high biosafety. Their synergy mechanism acted on two important cellular targets (energy metabolism and membrane integrity). Combination therapy of ZY4R with citronellal may be a promising mixture to combat bacterial infections facing an antibiotic-resistance crisis.


Assuntos
Adjuvantes Imunológicos , Peptídeos Antimicrobianos , Animais , Camundongos , Monoterpenos Acíclicos/farmacologia , Resistência a Múltiplos Medicamentos
10.
Sci Rep ; 13(1): 11063, 2023 07 08.
Artigo em Inglês | MEDLINE | ID: mdl-37422493

RESUMO

Several Eurydema species (Hemiptera: Pentatomidae) are considered as pests, however, reports on their chemical ecology are scarce. In the current study we focused on Eurydema ornata (Linnaeus) a pentatomid pest of several brassicaceous crops. Since the species is known to feed preferably on generative parts of plants, a series of floral and green leaf volatiles were tested by electroantennography and compounds eliciting remarkable responses were also tested in the field. Three compounds elicited the most outstanding responses from antennae of E. ornata: allyl isothiocyanate, phenylacetaldehyde and ± linalool. Field experiments were conducted in Hungary between 2017 and 2021 to test the potential attractive effects of the compounds. Three Eurydema species were caught in the experiments E. ornata, E. oleracea (Linnaeus) and E. ventralis Kolenati. In the experiments combinations containing allyl isothiocyanate attracted both males and females of E. ornata. The compound was also attractive on its own, in a positive, dose-dependent manner. When presented alone, neither phenylacetaldehyde nor ± linalool was attractive to the species, furthermore, addition of these compounds to allyl isothiocyanate did not affect attraction considerably. To our knowledge this is the first demonstration of field attration of an Eurydema species to a semiochemical and one of the few reports on trapping of a pentatomid species with a synthetic plant volatile in the field. Perspectives regarding research and potential practical applications are discussed in the paper.


Assuntos
Hemípteros , Heterópteros , Compostos Orgânicos Voláteis , Animais , Masculino , Feminino , Heterópteros/fisiologia , Monoterpenos Acíclicos/farmacologia , Compostos Orgânicos Voláteis/farmacologia
11.
J Pharm Pharmacol ; 75(8): 1130-1139, 2023 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-37379815

RESUMO

OBJECTIVES: Breast cancer is the most diagnosed cancer in females worldwide. Phytochemicals are among the recent compelling approaches showing anticancer activity. Geraniol is a monoterpenoid showing anti-tumoral potential in cell lines. However, its exact mechanism in breast cancer has not been elucidated. In addition, the possible chemosenstizing effect of geraniol when combined with chemotherapeutic drugs in breast carcinoma has not been previously addressed. METHODS: Therefore, the aim of the current work is to investigate the potential therapeutic as well as chemosensitizing effects of geraniol on breast carcinoma induced in mice through examination of tumour biomarkers and histopathology profile. KEY FINDINGS: Results showed a prominent suppression of tumour growth following geraniol treatment. This was accompanied with miR-21 downregulation that subsequently upregulated PTEN and suppressed mTOR levels. Geraniol was also able to activate apoptosis and inhibit autophagy. Histopathological examination revealed high necrosis areas separating malignant cells in the geraniol-treated group. Combined geraniol and 5-fluorouracil treatment induced more than 82% inhibition of tumour rate, surpassing the effect of each drug alone. CONCLUSIONS: It can be concluded that geraniol could represent a promising avenue for breast cancer treatment as well as a potential sensitizing agent when combined with chemotherapeutic drugs.


Assuntos
Fluoruracila , MicroRNAs , Feminino , Animais , Camundongos , Fluoruracila/farmacologia , Monoterpenos Acíclicos/farmacologia , Transdução de Sinais , Linhagem Celular Tumoral , MicroRNAs/genética , MicroRNAs/farmacologia , Proliferação de Células , Apoptose , Regulação Neoplásica da Expressão Gênica
12.
Molecules ; 28(9)2023 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-37175079

RESUMO

Geraniol (GNL), a natural monoterpene, is found in many essential oils of fruits, vegetables, and herbs, including lavender, citronella, lemongrass, and other medicinal and aromatic plants. GNL is commonly used by the cosmetic and food industries and has shown a wide spectrum of pharmacological activities including anti-inflammatory, anticancer, antimicrobial, antioxidant, and neuroprotective activities. It represents a potential anti-inflammatory agent and a promising cancer chemopreventive agent, as it has been found to be effective against a broad range of cancers, including colon, prostate, breast, lung, skin, kidney, liver, and pancreatic cancer. Moreover, GNL scavenges free radicals and preserves the activity of antioxidant enzymes. In addition, GNL induces apoptosis and cell cycle arrest, modulates multiple molecular targets, including p53 and STAT3, activates caspases, and modulates inflammation via transcriptional regulation. In the present study, different modes of action are described for GNL's activity against cancer and inflammatory diseases. This compound protects various antioxidant enzymes, such as catalase, glutathione-S-transferase, and glutathione peroxidase. Experiments using allergic encephalomyelitis, diabetes, asthma, and carcinogenesis models showed that GNL treatment had beneficial effects with low toxicity. GNL has been shown to be effective in animal models and tumor cell lines, but there have not been any clinical studies carried out for it. The aim of the present review is to provide updated data on the potential effects of GNL on cancer and inflammation, and to enhance our understanding of molecular targets, involved pathways, and the possible use of GNL for clinical studies and therapeutic purposes in the treatment of cancer and inflammation-related diseases.


Assuntos
Antioxidantes , Neoplasias , Masculino , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Fígado , Monoterpenos Acíclicos/farmacologia , Inflamação/tratamento farmacológico , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Neoplasias/tratamento farmacológico
13.
Eur J Pharmacol ; 951: 175714, 2023 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-37054939

RESUMO

Alzheimer's disease (AD) is the most progressive and irreversible neurodegenerative disease that leads to synaptic loss and cognitive decline. The present study was designed to evaluate the effects of geraniol (GR), a valuable acyclic monoterpene alcohol, with protective and therapeutic effects, on passive avoidance memory, hippocampal synaptic plasticity, and amyloid-beta (Aß) plaques formation in an AD rat model induced by intracerebroventricular (ICV) microinjection of Aß1-40. Seventy male Wistar rats were randomly into sham, control, control-GR (100 mg/kg; P.O. (orally), AD, GR-AD (100 mg/kg; P.O.; pretreatment), AD-GR (100 mg/kg; P.O.; treatment), and GR-AD-GR (100 mg/kg; P.O.; pretreatment & treatment). Administration of GR was continued for four consecutive weeks. Training for the passive avoidance test was carried out on the 36th day and a memory retention test was performed 24 h later. On day 38, hippocampal synaptic plasticity (long-term potentiation; LTP) was recorded in perforant path-dentate gyrus (PP-DG) synapses to assess field excitatory postsynaptic potentials (fEPSPs) slope and population spike (PS) amplitude. Subsequently, Aß plaques were identified in the hippocampus by Congo red staining. The results showed that Aß microinjection increased passive avoidance memory impairment, suppressed of hippocampal LTP induction, and enhanced of Aß plaque formation in the hippocampus. Interestingly, oral administration of GR improved passive avoidance memory deficit, ameliorated hippocampal LTP impairment, and reduced Aß plaque accumulation in the Aß-infused rats. The results suggest that GR mitigates Aß-induced passive avoidance memory impairment, possibly through alleviation of hippocampal synaptic dysfunction and inhibition of Aß plaque formation.


Assuntos
Doença de Alzheimer , Doenças Neurodegenerativas , Ratos , Masculino , Animais , Doença de Alzheimer/induzido quimicamente , Doença de Alzheimer/tratamento farmacológico , Monoterpenos Acíclicos/farmacologia , Ratos Wistar , Hipocampo , Plasticidade Neuronal , Potenciação de Longa Duração , Peptídeos beta-Amiloides/farmacologia , Transtornos da Memória/induzido quimicamente , Transtornos da Memória/tratamento farmacológico , Modelos Animais de Doenças , Fragmentos de Peptídeos/farmacologia
14.
Chem Biol Drug Des ; 102(3): 523-535, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37118873

RESUMO

Geraniol (GE), an acyclic monoterpene, is a chief constituent of essential oils of herbs and fruits. It possesses diverse pharmacological actions like antioxidant, anti-inflammatory, anti-apoptotic, and anti-parkinson. However, its neuroprotective potential in stroke is yet to be explored at large. The present study evaluated the neuroprotective potential of GE against the global model of cerebral ischemia/reperfusion (I/R)-injury in rats. Bilateral common carotid artery (BCCA) occlusion for 30 min followed by 7 days of reperfusion caused varied biochemical/enzymatic alterations viz. increase in levels of lipid peroxidation (LPO), nitric oxide (NO), xanthine oxidase (XO), and decrease in the levels of cerebroprotectives like superoxide dismutase (SOD), catalase (CAT), total thiols, and glutathione (GSH). GE-pretreatment markedly reversed these changes and restored the levels of protective enzymatic and non-enzymatic antioxidants near to normal compared to I/R group. Besides, GE treatment showed marked improvement in anxiety-related behavior and neuronal deficits in animals subjected to I/R injury. Moreover, 2,3,5-triphenyl tetrazolium chloride (TTC)-stained rat brain coronal sections and histopathological studies revealed neuronal protection against I/R-injury, as evidenced by a reduction in infarct area (%) and an increase in hippocampal CA1 neuronal density in the GE-treated groups. The results of this study revealed that GE exhibited potential neuroprotective activity by reducing oxidative stress and infarction area, and protecting hippocampal CA1 neurons against I/R-injury in the global stroke model in rats.


Assuntos
Isquemia Encefálica , Fármacos Neuroprotetores , Traumatismo por Reperfusão , Acidente Vascular Cerebral , Ratos , Animais , Monoterpenos Acíclicos/uso terapêutico , Monoterpenos Acíclicos/farmacologia , Acidente Vascular Cerebral/tratamento farmacológico , Acidente Vascular Cerebral/prevenção & controle , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Estresse Oxidativo , Glutationa/metabolismo , Traumatismo por Reperfusão/tratamento farmacológico , Hipocampo/metabolismo , Hipocampo/patologia , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Isquemia Encefálica/tratamento farmacológico
15.
Food Res Int ; 164: 112337, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36737930

RESUMO

Escherichia coli (E. coli) is a Gram-negative bacterium and some pathogenic types may cause serious diseases, foods or food environments were the primary routes for its infection. Citrus aurantium L. var. amara Engl., a variety of sour orange, were used as a kind of non-conventional edible plant in China, but its antimicrobial activity and mechanisms were not well studied. Thus, in this study, EO from the flower of Citrus aurantium L. var. amara Engl. (CAEO) were studied as a kind of natural antimicrobial agent to control E. coli, our results showed that both of CAEO and its main component (linalool) exhibited strong antibacterial efficacy. Further, transcriptomic and proteomic analysis were carried out to explore cell response under linalool treatment and the main results included: (1) The synthesis and modification of lipopolysaccharide (LPS) was significantly influenced. (2) Ribosomal assembly and protein synthesis were significantly inhibited. (3) The expression of proteins related to the uptake of several essential substances was significantly changed. In all, our results would supply a theoretical basis for the proper use of CAEO and linalool as a promising antimicrobial agent to prevent and control E. coli infection in the future.


Assuntos
Monoterpenos Acíclicos , Escherichia coli , Lipopolissacarídeos , Proteínas de Transporte , Escherichia coli/efeitos dos fármacos , Escherichia coli/metabolismo , Lipopolissacarídeos/biossíntese , Proteômica , Ribossomos , Monoterpenos Acíclicos/farmacologia
16.
Biochem Pharmacol ; 210: 115467, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36849063

RESUMO

Geraniol (Ger), a natural acyclic monoterpene alcohol, has been reported to exert protective effects through anti-inflammation in Acute liver failure (ALF). However, its specific roles and precise mechanisms underlying anti-inflammatory effects in ALF have not yet fully explored. We aimed to investigated the hepatoprotective effects and mechanisms of Ger against ALF induced by lipopolysaccharide (LPS)/D-galactosamine (GaIN). In this study, the liver tissue and serum of LPS/D-GaIN-induced mice were collected. The degree of liver tissue injury was evaluated by HE and TUNEL staining. Serum levels of liver injury markers (ALT and AST) and inflammatory factors were measured by ELISA assays. PCR and western blotting were conducted to determine the expression of inflammatory cytokines, NLRP3 inflammasome-related proteins, PPAR-γ pathway-related proteins, DNA Methyltransferases and M1/M2 polarization cytokines. Immunofluorescence staining was used to assess the localization and expression of macrophage markers (F4/80 and CD86), NLRP3 and PPAR-γ. In vitro experiments were performed in macrophages stimulated with LPS with or without IFN-γ. Purification of macrophages and cell apoptosis was analyzed using flow cytometry. We found that Ger effectively alleviated ALF in mice, specified by the attenuation of liver tissue pathological damage, inhibition of ALT, AST and inflammatory factor levels, and inactivation of NLRP3 inflammasome. Meanwhile, downregulation M1 macrophage polarization may involve in the protective effects of Ger. In vitro, Ger reduced the activation of NLRP3 inflammasome and apoptosis through regulating PPAR-γ methylation by inhibiting M1 macrophage polarization. In conclusion, Ger protects against ALF through suppressing NLRP3 inflammasome-mediated inflammation and LPS-induced macrophage M1 polarization via modulating PPAR-γ methylation.


Assuntos
Inflamassomos , Falência Hepática Aguda , Camundongos , Animais , Inflamassomos/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Lipopolissacarídeos/toxicidade , Monoterpenos Acíclicos/metabolismo , Monoterpenos Acíclicos/farmacologia , Galactosamina/toxicidade , Galactosamina/metabolismo , Metilação , PPAR gama/genética , PPAR gama/metabolismo , Transdução de Sinais , Falência Hepática Aguda/induzido quimicamente , Falência Hepática Aguda/tratamento farmacológico , Falência Hepática Aguda/metabolismo , Citocinas/metabolismo , Macrófagos , Camundongos Endogâmicos C57BL
17.
J Neurophysiol ; 129(1): 41-55, 2023 01 01.
Artigo em Inglês | MEDLINE | ID: mdl-36448682

RESUMO

Retinoic acid, the active metabolite of vitamin A, is important for vertebrate cognition and hippocampal plasticity, but few studies have examined its role in invertebrate learning and memory, and its actions in the invertebrate central nervous system are currently unknown. Using the mollusc Lymnaea stagnalis, we examined operant conditioning of the respiratory behavior, controlled by a well-defined central pattern generator (CPG), and used citral to inhibit retinoic acid signaling. Both citral- and vehicle-treated animals showed normal learning, but citral-treated animals failed to exhibit long-term memory at 24 h. Cohorts of citral- or vehicle-treated animals were dissected into semi-intact preparations, either 1 h after training, or after the memory test 24 h later. Simultaneous electrophysiological recordings from the CPG pacemaker cell (right pedal dorsal 1; RPeD1) and an identified motorneuron (VI) were made while monitoring respiratory activity (pneumostome opening). Activity of the CPG pneumostome opener interneuron (input 3 interneuron; IP3) was also monitored indirectly. Vehicle-treated conditioned preparations showed significant changes in network parameters immediately after learning, such as reduced motorneuron bursting activity (from IP3 input), delayed pneumostome opening, and decoupling of coincident IP3 input within the network. However, citral-treated preparations failed to exhibit these network changes and more closely resembled naïve preparations. Importantly, these citral-induced differences were manifested immediately after training and before any overt changes in the behavioral response (memory impairment). These studies shed light on where and when retinoid signaling might affect a central pattern-generating network to promote memory formation during conditioning of a homeostatic behavior.NEW & NOTEWORTHY We provide novel evidence for how conditioning-induced changes in a CPG network are disrupted when retinoid signaling is inhibited. Inhibition of retinoic acid signaling prevents long-term memory formation following operant conditioning, but has no effect on learning. Simultaneous electrophysiological and behavioral analyses indicate network changes immediately following learning, but these changes are prevented with inhibition of retinoid signaling, before any overt changes in behavior. These data suggest sites for retinoid actions during memory formation.


Assuntos
Memória de Longo Prazo , Retinoides , Animais , Retinoides/farmacologia , Monoterpenos Acíclicos/farmacologia , Condicionamento Operante/fisiologia , Tretinoína , Lymnaea/fisiologia
18.
Ultrason Sonochem ; 92: 106269, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36571884

RESUMO

In this study, a novel citral nanoemulsion (CLNE) was prepared by ultrasonic emulsification. The synergistic antibacterial mechanism of ultrasound combined with CLNE against Salmonella Typhimurium and the effect on the physicochemical properties of purple kale were investigated. The results showed that the combined treatment showed obviously inactivate effect of S. Typhimurium. Treatment with 0.3 mg/mL CLNE combined with US (20 kHz, 253 W/cm2) for 8 min reduced S. Typhimurium populations in phosphate-buffered saline (PBS) by 9.05 log CFU/mL. Confocal laser scanning microscopy (CLSM), flow cytometry (FCM), protein and nucleic acid release assays showed that the US combination CLNE disrupt the integrity of S. Typhimurium membranes. Reactive oxygen species (ROS) and malondialdehyde (MDA) detection indicated that US+CLNE exacerbated oxidative stress and lipid peroxidation in cell membranes. The morphological changes of cells after different treatments by field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM) illustrated that the synergistic effect of US+CLNE treatment changed the morphology and internal microstructure of the bacteriophage cells. Application of US+CLNE on purple kale leaves for 6 min significantly (P < 0.05) reduced the number of S. Typhimurium, but no changes in the physicochemical properties of the leaves were detected. This study elucidates the synergistic antibacterial mechanism of ultrasound combined with CLNE and provides a theoretical basis for its application in food sterilization.


Assuntos
Brassica , Salmonella typhimurium , Monoterpenos Acíclicos/farmacologia , Antibacterianos/farmacologia
19.
Naunyn Schmiedebergs Arch Pharmacol ; 396(2): 301-309, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36322162

RESUMO

Citral, a monoterpene which is a part of the essential oil of several medicinal plants, is generally regarded as safe for human and animal consumption. Studies have introduced citral as a functional component of some essential oils in anxiolytic and antidepressant therapies; however, the neuropharmacological characteristics of citral have not yet been reported. In the present study, we evaluated the anxiolytic activities of citral in comparison to two standard anxiolytics, diazepam and buspirone, in Swiss albino mice by intraperitoneal administration of 1, 2, 5, 10, and 20 mg/kg using elevated plus maze (EPM) and open-field test (OFT). Moreover, we also examined whether the GABAA-benzodiazepine and 5-HT1A receptor are involved in the anxiolytic-like effects of citral by pretreatment with flumazenil and WAY-100635, respectively. Citral dose-dependently decreased the number of border crossings and time spent in borders, and also the number of grooming and rearing in OFT without altering the exploratory behavior of mice. In the EPM, this monoterpene led to a significant increase in number of entries in open arms and time spent in open arms, as well as a decrease in time spent in closed arms. Pretreatment with flumazenil and WAY-100635 both could reverse the anxiolytic effects of the citral in the EPM. These results suggest that anxiolytic activity of citral occurs via the GABAA and 5-HT1A receptor modulation.


Assuntos
Ansiolíticos , Animais , Camundongos , Monoterpenos Acíclicos/farmacologia , Ansiolíticos/farmacologia , Ansiolíticos/uso terapêutico , Ansiedade/tratamento farmacológico , Comportamento Animal , Teste de Labirinto em Cruz Elevado , Flumazenil/farmacologia , Ácido gama-Aminobutírico/farmacologia , Aprendizagem em Labirinto , Receptor 5-HT1A de Serotonina
20.
Org Biomol Chem ; 21(3): 632-638, 2023 01 18.
Artigo em Inglês | MEDLINE | ID: mdl-36562351

RESUMO

Geraniol, a monoterpene, and furan are structural motifs that exhibit antifouling activity. In this study, monoterpene-furan hybrid molecules with potentially enhanced antifouling activity were designed and synthesized. The nine synthetic hybrids showed antifouling activity against the cypris larvae of the barnacle Balanus (Amphibalanus) amphitrite with EC50 values of 1.65-4.70 µg mL-1. This activity is higher than that of geraniol and the reference furan compound. This hybridization approach to increase antifouling activity is useful and can also be extended to other active structural units.


Assuntos
Incrustação Biológica , Thoracica , Animais , Monoterpenos/farmacologia , Incrustação Biológica/prevenção & controle , Monoterpenos Acíclicos/farmacologia , Furanos/farmacologia , Larva
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