RÉSUMÉ
Food contamination by mycotoxigenic fungi is one of the principal factors that cause food loss and economic losses in the food industry. The objective of this work was to incorporate the essential oil from Corymbia citriodora Hook and its constituents citronellal and ß-citronellol into poly(lactic acid) nanofibers; to characterize the nanofibers by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy and differential scanning calorimetry; to evaluate the antifungal activity by the fumigation method; to evaluate the antimycotoxigenic activity against Aspergillus carbonarius, Aspergillus ochraceus, Aspergillus westerdijkiae, Aspergillus flavus, and Aspergillus parasiticus; and to evaluate the morphology of these microorganisms. All the nanofibers had a regular, smooth, and continuous morphology. FTIR analyses confirmed that the active ingredients were incorporated into the polymer matrix. All samples exhibited antifungal and ochratoxigenic inhibitory activities of up to 100% and 99%, respectively, with the best results observed for (PLA + 30 wt% ß-citronellol) nanofibers and (PLA + 30 wt% citronellal) nanofibers. However, 100% inhibition of the production of aflatoxin B1 and B2 was not observed. The images obtained by SEM indicated that the nanofibers caused damage to the hyphae, caused a decrease in the production of spores, and caused deformation, rupture, and non-formation of the conid head, might be an alternative for the control of mycotoxigenic fungi.
Sujet(s)
Monoterpènes acycliques , Antifongiques , Aspergillus , Nanofibres , Huile essentielle , Polyesters , Nanofibres/composition chimique , Polyesters/composition chimique , Polyesters/pharmacologie , Huile essentielle/pharmacologie , Huile essentielle/composition chimique , Antifongiques/pharmacologie , Antifongiques/composition chimique , Monoterpènes acycliques/pharmacologie , Monoterpènes acycliques/composition chimique , Aspergillus/effets des médicaments et des substances chimiques , Aldéhydes/pharmacologie , Aldéhydes/composition chimique , Tests de sensibilité microbienne , Monoterpènes/pharmacologie , Monoterpènes/composition chimiqueRÉSUMÉ
Acute myelogenous leukemia (AML) is one of the most lethal cancers, lacking a definitive curative therapy due to essential constraints related to the toxicity and efficacy of conventional treatments. This study explores the co-adjuvant potential of Lippia alba essential oils (EO) for enhancing the effectiveness and selectivity of two chemotherapy agents (cytarabine and clofarabine) against AML cells. EO derived from L. alba citral chemotype were produced using optimized and standardized environmental and extraction protocols. Rational fractionation techniques were employed to yield bioactive terpene-enriched fractions, guided by relative chemical composition and cytotoxic analysis. Pharmacological interactions were established between these fractions and cytarabine and clofarabine. The study comprehensively evaluated the cytotoxic, genotoxic, oxidative stress, and cell death phenotypes induced by therapies across AML (DA-3ER/GM/EVI1+) cells. The fraction rich in citral (F2) exhibited synergistic pharmacological interactions with the studied chemotherapies, intensifying their selective cytotoxic, genotoxic, and pro-oxidant effects. This shift favored transitioning from necrosis to a programmed cell death phenotype (apoptotic). The F2-clofarabine combination demonstrated remarkable synergistic anti-leukemic performance while preserving cell integrity in healthy cells. The observed selective antiproliferative effects may be attributed to the potential dual prooxidant/antioxidant behavior of citral in L. alba EO.
Sujet(s)
Monoterpènes acycliques , Lippia , Huile essentielle , Huile essentielle/pharmacologie , Huile essentielle/composition chimique , Lippia/composition chimique , Monoterpènes acycliques/pharmacologie , Humains , Lignée cellulaire tumorale , Antinéoplasiques/pharmacologie , Cytarabine/pharmacologie , Leucémie aigüe myéloïde/traitement médicamenteux , Clofarabine/pharmacologie , Apoptose/effets des médicaments et des substances chimiques , Synergie des médicaments , Stress oxydatif/effets des médicaments et des substances chimiques , Prolifération cellulaire/effets des médicaments et des substances chimiquesRÉSUMÉ
This is a nonclinical, controlled, and triple-blind study to investigate the effects of codeine-associated geraniol on the modulation of orofacial nociception and its potential central nervous system depressing effect in an animal model. The orofacial antinociceptive activity of geraniol in combination with codeine was assessed through the following tests: (i) formalin-induced pain, (ii) glutamate-induced pain, and (iii) capsaicin-induced pain. Six animals were equally distributed into six groups and received the following treatments, given intraperitoneally (i.p.) 30 minutes before the experiments: a) geraniol/codeine 50/30 mg/kg; b) geraniol/codeine 50/15 mg/kg; c) geraniol/codeine 50/7.5 mg/kg; d) geraniol 50 mg/kg; e) codeine 30 mg/kg (positive control); or f) 0.9% sodium chloride (negative control). We performed pain behavior analysis after the injection of formalin (20 µL, 20%), glutamate (20 µL, 25 µM), and capsaicin (20 µL, 2.5 µg) into the paranasal region. Rubbing time of the paranasal region by the hind or front paw was used as a parameter. In the neurogenic phase of the formalin test, the geraniol/codeine at 50/7.5 mg/kg was able to promote the maximum antinociceptive effect, reducing nociception by 71.9% (p < 0.0001). In the inflammatory phase of the formalin test, geraniol/codeine at 50/30 mg/kg significantly reduced orofacial nociception (p < 0.005). In the glutamate test, geraniol/codeine at 50/30 mg/kg reduced the rubbing time by 54.2% and reduced nociception in the capsaicin test by 66.7% (p < 0.005). Geraniol alone or in combination does not promote nonspecific depressing effects on the central nervous system. Based on our findings, we suggest the possible synergy between geraniol and codeine in the modulation of orofacial pain.
Sujet(s)
Monoterpènes acycliques , Analgésiques , Capsaïcine , Codéine , Algie faciale , Mesure de la douleur , Terpènes , Animaux , Codéine/pharmacologie , Algie faciale/induit chimiquement , Algie faciale/traitement médicamenteux , Monoterpènes acycliques/pharmacologie , Mâle , Mesure de la douleur/effets des médicaments et des substances chimiques , Capsaïcine/pharmacologie , Terpènes/pharmacologie , Analgésiques/pharmacologie , Souris , Facteurs temps , Modèles animaux de maladie humaine , Reproductibilité des résultats , Formaldéhyde , Acide glutamique , Résultat thérapeutique , Nociception/effets des médicaments et des substances chimiques , Analyse de variance , Statistique non paramétrique , Comportement animal/effets des médicaments et des substances chimiquesRÉSUMÉ
PURPOSE: The flea Ctenocephalides felis (Siphonaptera: Pulicidae), parasitizes dogs and cats globally, acting as a vector for various pathogens affecting both animals and humans. Growing interest in environmentally friendly, plant-based products prompted this study. The aim of the study was to determine the chemical composition of essential oils (EOs) from Copaifera reticulata, Citrus paradisi, Lavandula hybrida and Salvia sclarea, assessing their insecticidal and repellent properties, determining lethal concentrations (LC50 and LC90), and evaluating residual efficacy in vitro against Ctenocephalides felis felis. METHODS: Gas Chromatography with Flame Ionization Detector analyzed EO composition. In vitro tests involved preparing EO solutions at various concentrations. Ten specimens from each life stage (egg, larva, pupa, adult) were used for insecticidal activity assessment. Adulticidal activity was assessed using 10 cm2 filter paper strip, each treated with 0.200 mL of the test solution. Immature stages activities were evaluated using 23.76 cm2 discs of the same filter paper, each treated with 0.470 mL of the test solution. Mortality percentage was calculated using (number of dead insects × 100) / number of incubated insects. Probit analysis calculated LC50 values with a 95% confidence interval. RESULTS: Major EO constituents were ß-caryophyllene (EOCR), linalool (EOLH), linalyl acetate (EOSS), and limonene (EOCP). LC50 values were obtained for all stages except for the essential oil of C. paradisi. All oils showed repellent activity at 800 µg/cm2. OECR exhibited greater residual efficacy. CONCLUSION: Each EO demonstrated superior insecticidal activity against specific C. felis felis stages.
Sujet(s)
Ctenocephalides , Insectifuges , Insecticides , Huile essentielle , Salvia , Animaux , Huile essentielle/pharmacologie , Huile essentielle/composition chimique , Salvia/composition chimique , Insectifuges/pharmacologie , Insectifuges/composition chimique , Insecticides/pharmacologie , Insecticides/composition chimique , Ctenocephalides/effets des médicaments et des substances chimiques , Fabaceae/composition chimique , Lavandula/composition chimique , Larve/effets des médicaments et des substances chimiques , Pupe/effets des médicaments et des substances chimiques , Citrus/composition chimique , Monoterpènes acycliques/pharmacologie , Monoterpènes/pharmacologie , Monoterpènes/composition chimique , Huiles végétales/pharmacologie , Huiles végétales/composition chimique , Dose létale 50RÉSUMÉ
BACKGROUND: Growing concerns about sustainability have driven the search for eco-friendly pest management solutions. Combining natural and synthetic compounds within controlled release systems is a promising strategy. This study investigated the co-encapsulation of the natural compound citral (Cit) and the synthetic antifungal cyproconazole (CPZ) using two water-based nanocarriers: solid lipid nanoparticles (SLNs) and chitosan nanoparticles (CSNPs). RESULTS: Both CSNPs and SLNs loaded with Cit + CPZ displayed superior antifungal activity against Botrytis cinerea compared to free compounds. Notably, CSNPs with a 2:1 Cit:CPZ ratio exhibited the highest efficacy, achieving a minimum inhibitory concentration (MIC100) of < 1.56 µg mL-1, lower than the 12.5 µg mL-1 of non-encapsulated compounds. This formulation significantly reduced the required synthetic CPZ while maintaining efficacy, highlighting its potential for environmentally friendly pest control. CONCLUSION: The successful co-encapsulation of Cit + CPZ within CSNPs, particularly at a 2:1 ratio, demonstrates a promising approach for developing effective and sustainable antifungal formulations against B. cinerea. © 2024 Society of Chemical Industry.
Sujet(s)
Monoterpènes acycliques , Botrytis , Fongicides industriels , Nanoparticules , Botrytis/effets des médicaments et des substances chimiques , Monoterpènes acycliques/pharmacologie , Nanoparticules/composition chimique , Fongicides industriels/pharmacologie , Fongicides industriels/composition chimique , Triazoles/pharmacologie , Triazoles/composition chimique , Tests de sensibilité microbienne , Chitosane/pharmacologie , Chitosane/composition chimique , Vecteurs de médicaments/composition chimique , Antifongiques/pharmacologie , Antifongiques/composition chimique , Lipides/composition chimique , Préparation de médicament , Maladies des plantes/prévention et contrôle , Maladies des plantes/microbiologieRÉSUMÉ
Linalool-rich Rosewood oil (Aniba rosaeodora Ducke) is a natural compound widely used in perfumery industry. Evidence suggests that linalool exerts antidepressant and anxiolytic effects. Conversely, ethanol binge drinking (i.e., intermittent and episodic consumption) during adolescence elicits neurobehavioral alterations associated with brain damage. Here, we investigated whether linalool-rich Rosewood oil administration can improve the emotional and molecular impairments associated with ethanol binge-like exposure during adolescence in female rats. Rosewood oil was obtained by hydrodistillation and posteriorly analyzed. Adolescent female Wistar rats received four-cycles of ethanol binge-like pattern (3â¯g/kg/day, 3 days on/4 days off) and daily Rosewood oil (35â¯mg/kg, intranasally) for 28 days. Twenty-four hours after treatments, it was evaluated the impact of ethanol exposure and Rosewood oil treatment on the putative emotional impairments assessed on the splash and forced swimming tests, as well as the levels of brain-derived neurotrophic factor (BDNF), S100B, oxidative parameters, and inflammatory cytokines in prefrontal cortex and hippocampus. Results indicated that Rosewood oil intranasal administration mitigated emotional impairments induced by ethanol exposure accompanied by a marked increase in BDNF, S100B, glutathione (GSH), and antioxidant activity equivalent to Trolox (TEAC) levels in brain areas. Rosewood oil treatment also prevented the ethanol-induced increase of interleukin-1ß, interleukin-6, tumor necrosis factor α (TNF-α), and neurofilament light chain (NFL) levels. These findings provide the first evidence that Rosewood oil intranasal administration exerts protective effects against emotional and molecular impairments associated with adolescent ethanol binge-like exposure, possibly due to linalool actions triggering neurotrophic factors, rebalancing antioxidant status, and attenuating proinflammatory process.
Sujet(s)
Monoterpènes acycliques , Éthanol , Huile essentielle , Rat Wistar , Animaux , Femelle , Huile essentielle/pharmacologie , Huile essentielle/isolement et purification , Monoterpènes acycliques/pharmacologie , Rats , Hyperalcoolisation rapide/traitement médicamenteux , Antioxydants/pharmacologie , Stress oxydatif/effets des médicaments et des substances chimiques , Émotions/effets des médicaments et des substances chimiques , Comportement animal/effets des médicaments et des substances chimiques , Hippocampe/effets des médicaments et des substances chimiques , Hippocampe/métabolisme , Cytokines/métabolisme , Facteur neurotrophique dérivé du cerveau/métabolisme , Cortex préfrontal/effets des médicaments et des substances chimiques , Cortex préfrontal/métabolismeRÉSUMÉ
Sodium chloride (NaCl) can cause oxidative stress in plants, which represents a potential obstacle to the development of monocultures worldwide. Onion (Allium cepa L.) is a famous vegetable consumed and used in world cuisine. In the present study, we analyzed the influence of soil physicochemical profile and the remedial capacity of linalool on seed emergence, roots, and leaf growth in onions subjected to salt stress, as well as its in vivo and in vitro antioxidant potential, Fe2+chelating activity, and reducing power of Fe3+. The outcome of the soil analysis established the following order of abundance: sulfur (S) > calcium (Ca) > potassium (K) > magnesium (Mg) > sodium (Na). NaCl (150 mM) significantly reduced the emergence speed index (ESI), leaf and root length, while increasing the peroxidation content. The length of leaves and roots significantly increased after treatment with linalool (300 and 500 µg/mL). Our data showed negative correlations between seed emergence and K+ concentration, which was reversed after treatments. Linalool (500 µg/mL) significantly reduced oxidative stress, but increased Fe2+ concentration and did not show potential to reduce Fe3+. The in vivo antioxidant effect of linalool is thought to primarily result from an enzymatic activation process. This mechanism underscores its potential as a therapeutic agent for oxidative stress-related conditions. Further investigation into this process could unveil new avenues for antioxidant therapy.
Sujet(s)
Monoterpènes acycliques , Antioxydants , Oignons , Oignons/effets des médicaments et des substances chimiques , Monoterpènes acycliques/pharmacologie , Stress salin/effets des médicaments et des substances chimiques , Monoterpènes/pharmacologie , Stress oxydatif/effets des médicaments et des substances chimiquesRÉSUMÉ
ETHNOPHARMACOLOGICAL RELEVANCE: In Brazilian popular medicine, Lippia alba leaves are used in teas to treat pain and inflammatory diseases. AIM OF THE STUDY: to evaluate the chemical composition, antinociceptive, and anti-inflammatory activities of Lippia alba essential oil and its major compound geraniol. MATERIAL AND METHODS: Lippia alba leaves were collected in Pará state, Brazil. The leaf essential oil was obtained using a modified Clevenger-type extractor. Then, the oil was analyzed by GC and GC-MS analyses. To evaluate the toxicity of LaEO and geraniol, the doses of 50, 300, and 2000 mg/kg were used in a mouse model. For antinociception tests, abdominal contortion, hot plate, and formalin tests were used; all groups were treated with LaEO and geraniol at doses of 25, 50, and 100 mg/kg; and to evaluate inflammation using the ear edema model. RESULTS: The constituents identified in the highest content were oxygenated monoterpenes: geraniol (37.5%), geranial (6.7%) and neral (3.8%). The animals treated with LaEO and geraniol demonstrated atypical behaviors with aspects of lethargy and drowsiness, characteristics of animals in a state of sedation; the relative weights showed no significant difference compared to the controls. In the abdominal contortion test, LaEO at 25 mg/kg, 50 mg/kg doses, and 100 mg/kg reduced the number of contortions, representing a percentage reduction of 84.64%, 81.23%, and 66.21% respectively. In the hot plate test, LaEO and geraniol increased the latency time at doses of 25, 50, and 100 mg/kg in all test periods; there was no statistical difference between LaEO and geraniol. In the first phase of the formalin test, only doses of 25 mg/kg and 100 mg/kg of LaEO showed significant activity, reducing the latency time by 53.40% and 58.90%. LaEO at doses of 25 mg/kg and 100 mg/kg reduced the size of the edema, demonstrating an anti-inflammatory activity of 59.38% (25 mg/kg) and 50% (100 mg/kg). CONCLUSION: Lippia alba essential oil and geraniol showed central/peripheral analgesic and anti-inflammatory potential and can be used as an alternative or complementary treatment to conventional drugs. More studies are needed to evaluate its action mechanisms and its analgesic effects.
Sujet(s)
Monoterpènes acycliques , Analgésiques , Anti-inflammatoires , Oedème , Lippia , Huile essentielle , Feuilles de plante , Animaux , Lippia/composition chimique , Huile essentielle/pharmacologie , Huile essentielle/composition chimique , Brésil , Analgésiques/pharmacologie , Analgésiques/isolement et purification , Souris , Anti-inflammatoires/pharmacologie , Anti-inflammatoires/isolement et purification , Mâle , Feuilles de plante/composition chimique , Oedème/traitement médicamenteux , Oedème/induit chimiquement , Monoterpènes acycliques/pharmacologie , Plantes médicinales/composition chimique , Douleur/traitement médicamenteux , Comportement animal/effets des médicaments et des substances chimiques , Relation dose-effet des médicaments , Mesure de la douleur/effets des médicaments et des substances chimiquesRÉSUMÉ
INTRODUCTION: Citral is a low-toxicity monoterpene that has a vasodilator effect on various smooth muscles, and The present study aimed to evaluate its vasorelaxant effect on umbilical vessels of normotensive parturients (NTP) and with preeclampsia parturients (PEP). METHOD: Segments of human umbilical artery (HUA) and vein (HUV) of NTP or PEP were mounted in a bath to record the force of contraction, under tension of 3.0 gf and contracted with the contracting agents: K+ (60 mM), 5 -HT (10 µM) and Ba2+ (1-30 mM). Next, the effect of citral (1-3000 µM) on these contractions and on basal tone was evaluated. RESULTS: In HUA and HUV, citral (1-1000 µM), in NTP condition, inhibited contractions evoked by K+ (IC50 of 413.5 and 271.3, respectively) and by 5-HT (IC50 of 164.8 and 574.3). In the PEP condition, in HUA and HUV, citral also inhibited the contractions evoked by K+ (IC50 of 363.3 and 218.3, respectively) and 5-HT (IC50 of 432.1 and 520.4). At a concentration of 1000 µM, citral completely or almost completely (>90 %) inhibited all contractions. At a concentration of 100-1000 µM, citral, in general, was already able to reduce the contraction induced by 1-3 mM Ba2+ in both AUH and VUH, under NTP and PEP conditions. DISCUSSION: Citral has been shown to be an effective HUA and HUV vasodilator in NTP and PEP. As its toxicity is low, it suggests that this substance can be considered a potential therapeutic agent.
Sujet(s)
Monoterpènes acycliques , Monoterpènes , Pré-éclampsie , Artères ombilicales , Vasodilatateurs , Humains , Femelle , Grossesse , Pré-éclampsie/physiopathologie , Monoterpènes acycliques/pharmacologie , Monoterpènes/pharmacologie , Artères ombilicales/effets des médicaments et des substances chimiques , Adulte , Vasodilatateurs/pharmacologie , Veines ombilicales/effets des médicaments et des substances chimiques , Vasodilatation/effets des médicaments et des substances chimiquesRÉSUMÉ
Tetrahydrolinalool (THL) is an acyclic monoterpene alcohol, produced during linalol metabolism and also a constituent of essential oils. As described in the literature, many monoterpenes present anticonvulsant properties, and thus we became interested in evaluating the anticonvulsant activity of Tetrahydrolinalool using in mice model as well as in silico approaches. Our results demonstrated that THL increased latency to seizure onset and also reduced the mortality, in picrotoxin induced seizure tests. The results may be related to GABAergic regulation, which was also suggested in seizure testing induced by 3-mercapto-propionic acid. In the strychnine-induced seizure testing, none of the groups pretreated with THL modulated the parameters indicative of anticonvulsant effect. The electrophysiological results revealed that THL treatment reduces seizures induced by pentylenetetrazole. The in silico molecular docking studies showed that the interaction between THL and a GABAA receptor model formed a stable complex, in comparison to the crystaligraphic structure of diazepam, a structurally related ligand. In conclusion, all the evidences showed that THL presents effective anticonvulsant activity related to the GABAergic pathway, being a candidate for treatment of epileptic syndromes.
Sujet(s)
Monoterpènes acycliques , Anticonvulsivants , Simulation de docking moléculaire , Monoterpènes , Pentétrazol , Crises épileptiques , Anticonvulsivants/pharmacologie , Anticonvulsivants/composition chimique , Anticonvulsivants/synthèse chimique , Animaux , Souris , Crises épileptiques/traitement médicamenteux , Monoterpènes/pharmacologie , Monoterpènes/composition chimique , Monoterpènes/synthèse chimique , Monoterpènes acycliques/pharmacologie , Monoterpènes acycliques/composition chimique , Monoterpènes acycliques/synthèse chimique , Mâle , Récepteurs GABA-A/métabolisme , Récepteurs GABA-A/composition chimique , Relation structure-activité , Comportement animal/effets des médicaments et des substances chimiques , Picrotoxine/pharmacologieRÉSUMÉ
Pain is characterized by the unpleasant sensory and emotional sensation associated with actual or potential tissue damage, whereas nociception refers to the mechanism by which noxious stimuli are transmitted from the periphery to the CNS. The main drugs used to treat pain are nonsteroidal anti-inflammatory drugs (NSAIDs) and opioid analgesics, which have side effects that limit their use. Therefore, in the search for new drugs with potential antinociceptive effects, essential oils have been studied, whose constituents (monoterpenes) are emerging as a new therapeutic possibility. Among them, linalool and its metabolites stand out. The present study aims to investigate the antinociceptive potential of linalool and its metabolites through a screening using an in silico approach. Molecular docking was used to evaluate possible interactions with important targets involved in antinociceptive activity, such as α2-adrenergic, GABAergic, muscarinic, opioid, adenosinergic, transient potential, and glutamatergic receptors. The compounds in the investigated series obtained negative energies for all enzymes, representing satisfactory interactions with the targets and highlighting the multi-target potential of the L4 metabolite. Linalool and its metabolites have a high likelihood of modulatory activity against the targets involved in nociception and are potential candidates for future drugs.
Sujet(s)
Monoterpènes acycliques , Analgésiques , Simulation de docking moléculaire , Monoterpènes acycliques/composition chimique , Monoterpènes acycliques/pharmacologie , Monoterpènes acycliques/métabolisme , Analgésiques/composition chimique , Analgésiques/pharmacologie , Analgésiques/métabolisme , Humains , Simulation numérique , Animaux , Douleur/traitement médicamenteux , Douleur/métabolisme , Monoterpènes/composition chimique , Monoterpènes/pharmacologieRÉSUMÉ
The current study was conducted to determine the neuroprotective role and mechanism of action of Linalool (LIN) in SCI. The SCI in Sprague-Dawley (SD) rats was induced by weight-drop contusion model. Results of the suggested that LIN showed improvement in the locomotor function of SCI rats in a BBB scoring analysis. It was found in agreement with histopathological analysis of spinal cord tissue where LIN improves the neuronal architecture of spinal cord tissues, and protect neurons from degeneration. It also reduces oxidative stress via modulating endogenous antioxidants (MDA, SOD, and GSH) and inhibits the generation of pro-inflammatory cytokines (TNF-α, IL-1ß, and IL-6). In western blot analysis, LIN showed dose-dependent reduction of expression of toll-like receptor (TLR-4) and nuclear factor-kappa B (NF-ĸB). Our study demonstrated that administration of Linalool alleviated spinal cord injury via anti-inflammatory and antioxidant activities in spinal cord tissues possibly due to inhibition of TLR4/NF-κB activation.
El estudio actual se realizó para determinar el papel neuroprotector y el mecanismo de acción de Linalool (LIN) en SCI. La LIN en ratas Sprague-Dawley (SD) se indujo mediante el modelo de contusión de caída de peso. Los resultados sugirieron que LIN mostró una mejora en la función locomotora de ratas SCI en un análisis de puntuación BBB. De acuerdo con el análisis histopatológico del tejido de la médula espinal se encontró que LIN mejora la arquitectura neuronal de los tejidos de la médula espinal y protege a las neuronas de la degeneración. También reduce el estrés oxidativo mediante la modulación de antioxidantes endógenos (MDA, SOD y GSH) e inhibe la generación de citocinas proinflamatorias (TNF-α, IL-1ß e IL-6). En el análisis de Western blot, LIN mostró una reducción dependiente de la dosis de la expresión del receptor tipo toll (TLR-4) y el factor nuclear kappa B (NF-ĸB). Nuestro estudio demostró que la administración de Linalool alivió la lesión de la médula espinal a través de actividades antiinflamatorias y antioxidantes en los tejidos de la médula espinal, posiblemente debido a la inhibición de la activación de TLR4/NF-κB.
Sujet(s)
Animaux , Mâle , Rats , Traumatismes de la moelle épinière/traitement médicamenteux , Monoterpènes acycliques/administration et posologie , Test ELISA , Transduction du signal/effets des médicaments et des substances chimiques , Technique de Western , Facteur de transcription NF-kappa B/antagonistes et inhibiteurs , Rat Sprague-Dawley , Stress oxydatif/effets des médicaments et des substances chimiques , Récepteur de type Toll-4/antagonistes et inhibiteurs , Monoterpènes acycliques/pharmacologie , InflammationRÉSUMÉ
BACKGROUND: Geraniol (GE) is dietary acyclic monoterpene alcohol found in essential oils from aromatic plants with therapeutic value against gastric ulcers already described. HYPOTHESIS/PURPOSE: To assess whether oral GE accelerates gastric healing or prevents ulcer recurrence, and to evaluate the hypothesis that GE promotes antiulcer effects by the inhaled route and that promotes changes in the behavior of ulcerated rodents. METHODS: Gastric healing effects, underlining mechanisms, and behavioral changes were measured in80% acetic acid-induced gastric ulcer model in rats receiving GE by oral (30 mg/kg) or inhaled route (1 mg/L of air/min); whereas the effects of GE to avoid ulcer recurrence was evaluated in mice submitted to 10% acetic acid plus IL-1ß ulcer. RESULTS: GE administered by both routes accelerates gastric healing, increasing mucin and GSH levels, CAT, and GST activities, and reducing MPO activity. Moreover, oral, and inhaled GE minimized ulcer recurrence reducing gastric TNF and IL-6 levels and preserving mucin levels. Interestingly, the inhalation or oral intake of GE promotes anxiolytic-like effects in ulcerated rats. CONCLUSION: Data altogether suggest that the GE accelerates gastric healing through the strengthening of protective factors of the gastric mucosa, promoting a quality healing that reduces the recurrence of the lesion. Besides, the anxiolytic-like effect of GE may also contribute to its gastric healing action since anxiety is recognized as one of the etiologic agents of ulcers.
Sujet(s)
Monoterpènes acycliques , Anxiolytiques , Antiulcéreux , Ulcère gastrique , Animaux , Souris , Rats , Acide acétique , Monoterpènes acycliques/pharmacologie , Anxiolytiques/pharmacologie , Antiulcéreux/pharmacologie , Muqueuse gastrique , Mucines , Rat Wistar , Ulcère gastrique/induit chimiquement , Ulcère gastrique/traitement médicamenteuxRÉSUMÉ
Staphylococcus aureus is a Gram-positive bacterium that is considered an important human pathogen. Due to its virulence and ability to acquire mechanisms of resistance to antibiotics, the clinical severity of S. aureus infection is driven by inflammatory responses to the bacteria. Thus, the present study aimed to investigate the modulating role of citral in inflammation caused by S. aureus infection. For this, we used an isolate obtained from a nasal swab sample of a healthy child attending a day-care centre in Vitória da Conquista, Bahia, Brazil. The role of citral in modulating immunological factors against S. aureus infection was evaluated by isolating and cultivating human peripheral blood mononuclear cells. The monocytes were treated with 4%, 2%, and 1% citral before and after inoculation with S. aureus. The cells were analysed by immunophenotyping of monocyte cell surface molecules (CD54, CD282, CD80, HLA-DR, and CD86) and cytokine dosage (IL-1ß, IL-6, IL-10, IL-12p70, IL-23, IFN-γ, TGF-ß, and TNF-α), and evaluated for the expression of 84 genes related to innate and adaptive immune system responses. GraphPad Prism software and variables with P values < 0.05, were used for statistical analysis. Our data demonstrated citral's action on the expression of surface markers involved in recognition, presentation, and migration, such as CD14, CD54, and CD80, in global negative regulation of inflammation with inhibitory effects on NF-κB, JNK/p38, and IFN pathways. Consequently, IL-1ß, IL-6, IL-12p70, IL-23, IFN-γ, and TNF-α cytokine expression was reduced in groups treated with citral and groups treated with citral at 4%, 2%, and 1% and infected, and levels of anti-inflammatory cytokines such as IL-10 were increased. Furthermore, citral could be used as a supporting anti-inflammatory agent against infections caused by S. aureus. There are no data correlating citral, S. aureus, and the markers analysed here; thus, our study addresses this gap in the literature.
Sujet(s)
Monoterpènes acycliques/pharmacologie , Facteurs immunologiques/pharmacologie , Monocytes/effets des médicaments et des substances chimiques , Infections à staphylocoques/immunologie , Staphylococcus aureus/immunologie , Adulte , Brésil , Cellules cultivées , Enfant , Humains , Inflammation/complications , Inflammation/traitement médicamenteux , Inflammation/immunologie , Mâle , Monocytes/immunologie , Infections à staphylocoques/complications , Infections à staphylocoques/traitement médicamenteux , Staphylococcus aureus/effets des médicaments et des substances chimiques , Jeune adulteRÉSUMÉ
Essential oils (EOs) are widely recognized as efficient and safe alternatives for controlling pest insects in foods. However, there is a lack of studies evaluating the toxicological stability of botanical insecticides in stored grains in order to establish criteria of use and ensure your efficiency. The objective of this work was to evaluate the toxicological stability of basil essential oil (O. basilicum) and its linalool and estragole components for Sitophilus zeamais (Motschulsky) adults in corn grains by fumigation. The identification of the chemical compounds of the essential oil was performed with a gas chromatograph coupled to a mass selective detector. Mortality of insects was assessed after 24 h exposure. After storage for six (EO) and two months (linalool and estragole) under different conditions of temperature (5, 20, and 35 °C) and light (with and without exposure to light), its toxicological stability was evaluated. Studies revealed that the essential oil of O. basilicum and its main components exhibited insecticidal potential against adults of S. zeamais. For greater toxicological stability, suitable storage conditions for them include absence of light and temperatures equal to or less than 20 °C.
Sujet(s)
Coléoptères/effets des médicaments et des substances chimiques , Lutte contre les insectes , Insecticides/pharmacologie , Ocimum basilicum/composition chimique , Huile essentielle/pharmacologie , Huiles végétales/pharmacologie , Monoterpènes acycliques/composition chimique , Monoterpènes acycliques/pharmacologie , Animaux , Stabilité de médicament , Insecticides/composition chimique , Dose létale 50 , Huile essentielle/composition chimique , Huiles végétales/composition chimique , Tests de toxicitéRÉSUMÉ
The objective of this study was to evaluate the possible relaxing effect of essential oils (EOs) (Aloysia triphylla and Lippia alba) and phytochemicals (citral and linalool) in the gastropod Pomacea canaliculata. Animals were exposed to compounds at the concentrations range of 25-750 µL L-1. Magnesium chloride (MgCl2, 10-50 g L-1) and control group (ethanol 6.75 mL L-1, highest concentration used for treatment dilution) were also tested. The EOs, citral and MgCl2 had no relaxing effect at the concentrations range tested, and citral caused aversive behavior (closure of the operculum) from 90 µL L-1. Exposure to linalool at 25, 50, 100, 200 and 400 µL L-1 relaxed 28, 76, 88, 96 and 100% of the animals, respectively. The concentrations of 25, 50 and 400 µL L-1 differed statistically from each other, while 100 and 200 µL L-1 were equal to 50 and 400 µL L-1. All animals recovered up to 40 min, except at of 400 µL L-1. Linalool is effective for relaxing P. canaliculata and can be useful in management techniques that require relaxation. However, further studies are needed to certify whether linalool is appropriate for maintaining animal welfare in invasive procedures that require total insensitivity.
Sujet(s)
Monoterpènes acycliques/pharmacologie , Lippia , Escargots/effets des médicaments et des substances chimiques , Verbenaceae , AnimauxRÉSUMÉ
AIMS: Anti-inflammatory molecules, such as rose oxide (RO), are likely to exert therapeutic effects in systemic arterial hypertension (SAH), a disease associated with abnormal immune responses. We aimed to investigate acute autonomic effects of RO on hemodynamic parameters of Wistar and spontaneously hypertensive rats (SHR). METHODS: Rats were anesthetized and femoral artery and veins were cannulated. Next day, blood pressure (BP) and heart rate (HR) were recorded. Acute effects of RO (1.25, 2.5, or 5.0 mg/kg; iv) on BP, HR, and variability of systolic arterial pressure (SAP) and pulse interval (PI) were assessed. The effects of RO were also investigated in SHR, which received atropine (2 mg/kg), propranolol (4 mg/kg), or hexamethonium (20 mg/kg) 15 min before receiving RO. Vasorelaxant effects of RO (10-10 to 10-4 M) on aortic rings of rats were also assessed. KEY FINDINGS: In Wistar rats, none of the RO doses evoked significant changes in BP, HR, and variability of SAP and PI. On the other hand, in SHR, RO elicited reduction in mean arterial pressure (MAP), and prevented the increase in the low frequency power (LF) of the SAP spectra. Pretreatment with atropine or propranolol did not alter hypotension, but attenuated RO-induced bradycardia. Hexamethonium prevented RO-induced hypotension and bradycardia. RO exerted vasorelaxant effects on aortic rings with (Wistar and SHR) or without functional endothelium (SHR only). SIGNIFICANCE: Rose oxide, a monoterpene with anti-inflammatory properties, acts as an antihypertensive molecule due to its ability to acutely promote hypotension and bradycardia in spontaneously hypertensive rats.
Sujet(s)
Monoterpènes acycliques/usage thérapeutique , Anti-inflammatoires non stéroïdiens/usage thérapeutique , Antihypertenseurs/usage thérapeutique , Pression sanguine/effets des médicaments et des substances chimiques , Rythme cardiaque/effets des médicaments et des substances chimiques , Hypertension artérielle/traitement médicamenteux , Monoterpènes acycliques/pharmacologie , Animaux , Anti-inflammatoires non stéroïdiens/pharmacologie , Antihypertenseurs/pharmacologie , Baroréflexe/effets des médicaments et des substances chimiques , Baroréflexe/physiologie , Pression sanguine/physiologie , Relation dose-effet des médicaments , Rythme cardiaque/physiologie , Hypertension artérielle/physiopathologie , Mâle , Rats , Rats de lignée SHR , Rat Wistar , Spécificité d'espèce , Vasodilatation/effets des médicaments et des substances chimiques , Vasodilatation/physiologieRÉSUMÉ
Methicillin-resistant Staphylococcus aureus (MRSA) is responsible for high morbidity and mortality rates. Citral has been studied in the pharmaceutical industry and has shown antimicrobial activity. This study aimed to analyze the antimicrobial activity of citral in inhibiting biofilm formation and modulating virulence genes, with the ultimate goal of finding a strategy for treating infections caused by MRSA strains. Citral showed antimicrobial activity against MRSA isolates with minimum inhibitory concentration (MIC) values between 5 mg/mL (0.5%) and 40 mg/mL (4%), and minimum bactericidal concentration (MBC) values between 10 mg/mL (1%) and 40 mg/mL (4%). The sub-inhibitory dose was 2.5 mg/mL (0.25%). Citral, in an antibiogram, modulated synergistically, antagonistically, or indifferent to the different antibiotics tested. Prior to evaluating the antibiofilm effects of citral, we classified the bacteria according to their biofilm production capacity. Citral showed greater efficacy in the initial stage, and there was a significant reduction in biofilm formation compared to the mature biofilm. qPCR was used to assess the modulation of virulence factor genes, and icaA underexpression was observed in isolates 20 and 48. For icaD, seg, and sei, an increase was observed in the expression of ATCC 33,591. No significant differences were found for eta and etb. Citral could be used as a supplement to conventional antibiotics for MRSA infections.
Sujet(s)
Monoterpènes acycliques/pharmacologie , Antibactériens/pharmacologie , Staphylococcus aureus résistant à la méticilline/effets des médicaments et des substances chimiques , Biofilms/effets des médicaments et des substances chimiques , Staphylococcus aureus résistant à la méticilline/pathogénicité , Tests de sensibilité microbienne , Microscopie confocale , Facteurs de virulence/antagonistes et inhibiteursRÉSUMÉ
Essential oils' active compounds present great potential as a bactericidal agent in active packaging. The encapsulation in polymeric walls promotes their protection against external agents besides allowing controlled release. This work produced PLA capsules with three different active compounds, Cinnamomum cassia essential oil (CEO), eugenol (EEO), and linalool (LEO), by emulsion solvent evaporation method. Characterizations included SEM, Zeta potential, FTIR, TGA, and bactericidal activity against E. coli, S. aureus, L. monocytogenes, and Salmonella. The active compounds showed microbiological activity against all pathogens. CEO capsules showed superior colloidal stability. The active compounds' presence in all capsules was confirmed by FTIR analysis, with possible physical interaction between CEO, EEO, and the polymeric matrix, while LEO had a possible chemical interaction with PLA. TGA analysis showed a plasticizing effect of active compounds, and the loading efficiency was 39.7%, 50.7%, and 22.3% for CEO-PLA, EEO-PLA, and LEO-PLA, respectively. The capsules presented two release stages, sustaining activity against pathogens for up to 28 days, indicating a satisfactory internal morphology. This study presented methodology for encapsulation of antimicrobial compounds that can be suitable for active food packaging. CEO-PLA capsules regarding stability and antibacterial activity achieved the best results.
Sujet(s)
Antibactériens/pharmacologie , Bactéries/effets des médicaments et des substances chimiques , Maladies d'origine alimentaire/prévention et contrôle , Huile essentielle/pharmacologie , Huiles végétales/pharmacologie , Polyesters/composition chimique , Monoterpènes acycliques/composition chimique , Monoterpènes acycliques/pharmacologie , Antibactériens/composition chimique , Bactéries/croissance et développement , Capsules , Cinnamomum aromaticum , Colloïdes , Préparation de médicament , Libération de médicament , Stabilité de médicament , Eugénol/composition chimique , Eugénol/pharmacologie , Microbiologie alimentaire , Emballage alimentaire , Maladies d'origine alimentaire/microbiologie , Tests de sensibilité microbienne , Huile essentielle/composition chimique , Huiles végétales/composition chimique , Facteurs tempsRÉSUMÉ
Essential oils and their main components, monoterpenes, have been proven to be important alternatives for the control of pathogenic and spoiling microorganisms, but the mode of action of these compounds is poorly understood. This work aimed to determine the mode of action of citral and geraniol on the model yeast Saccharomyces cerevisiae using a flow cytometry approach. Exponentially growing yeast cells were treated with different concentrations of citral and geraniol for 3 h, and evaluated for cell wall susceptibility to glucanase, membrane integrity, reactive oxygen species (ROS) accumulation, mitochondrial membrane potential, and metacaspase activity. Results provide strong evidence that citral and geraniol acute fungicidal activity against Saccharomyces cells involves the loss of membrane and cell wall integrity resulting in a dose-dependent apoptotic/necrotic cell death. However, yeast cells that escape this first cell membrane disruption, particularly evident on sub-lethal concentration, die by metacaspase-mediated apoptosis induced by the accumulation of intracellular ROS. The deleted mutant on the yca1 gene showed high tolerance to citral and geraniol.