RESUMO
Enzymatic kinetic resolution is a promising way to produce l-menthol. However, the properties of the reported biocatalysts are still unsatisfactory and far from being ready for industrial application. Herein, a para-nitrobenzylesterase (pnbA) gene from Bacillus subtilis was cloned and expressed to produce l-menthol from d,l-menthyl acetate. The highest enantiomeric excess (ee) value of the product generated by pnbA was only approximately 80%, with a high conversion rate (47.8%) of d,l-menthyl acetate with the help of a cosolvent, indicating high catalytic activity but low enantioselectivity (E = 19.95). To enhance the enantioselectivity and catalytic efficiency of pnbA to d,l-menthyl acetate in an organic solvent-free system, site-directed mutagenesis was performed based on the results of molecular docking. The F314E/F315T mutant showed the best catalytic properties (E = 36.25) for d,l-menthyl acetate, with 92.11% ee and 30.58% conversion of d,l-menthyl acetate. To further improve the properties of pnbA, additional mutants were constructed based on the structure-guided triple-code saturation mutagenesis strategy. Finally, four mutants were screened for the best enantioselectivity (ee > 99%, E > 300) and catalytic efficiency at a high substrate concentration (200 g/L) without a cosolvent. This work provides several generally applicable biocatalysts for the industrial production of l-menthol.
Assuntos
Esterases , Mentol , Esterases/genética , Esterases/química , Mentol/química , Bacillus subtilis/genética , Simulação de Acoplamento Molecular , Extratos Vegetais , AcetatosRESUMO
Three-phase crystallization (TPC) was introduced in this study to purify L-menthol from menthol enantiomer mixtures in consideration of the formation of solid solutions. TPC is a new separation technology, which combines melt crystallization and vaporization to result in the desired crystalline product from a liquid mixture along with the unwanted components vaporized via the three-phase transformation by reducing temperature and pressure. The three-phase transformation conditions for the liquid menthol enantiomer mixtures were determined based on the thermodynamic calculations to direct the TPC experiments. A new model was proposed based on the mass and energy balances in consideration of the formation of the solid solutions to predict the yield and purity of the final L-menthol product during TPC. The yield and purity obtained from the TPC experiments were compared with those predicted by the model.
Assuntos
Anestésicos , Mentol , Cristalização , Mentol/química , Terpenos , Temperatura , Termodinâmica , Extratos VegetaisRESUMO
This research was conducted to explore the influence of cold shock on the firmness, a quality marker in chili pepper during 0-21 d storage and determine mechanism by cold shock impacted pectin. Chili peppers were exposed to cold shock precooling (0 ± 2 °C water/ice mixture) for 0-, 30-, 90- and 150-min, respectively. Results showed that cold shock alleviated loss of firmness throughout storage. Firmness was positively associated with sodium carbonate-soluble pectin content (r = 0.44), methylation degree of CDTA-soluble pectin (r = 0.82) and water-soluble pectin (WSP, r = 0.87), but negatively associated with WSP content (r = -0.76), and the activities of ß-galactosidase (r = -0.72) and pectinlyase (r = -0.74). Cold shock for 90 min was determined to be optimal. This study confirms the applicability of cold shock precooling to maintain firmness and thereby to extend the shelf life of chili pepper.
Assuntos
Capsicum , Pectinas , Capsicum/química , Cânfora , Mentol/química , Resposta ao Choque Frio , ÁguaRESUMO
Cancer remains a major health problem worldwide, with colorectal cancer (CRC) being the third most incident and the second most lethal. Inflammation, on the other hand, has been highly associated with cancer development and maintenance, therefore, the reduction of the inflammatory microenvironment represents a promising therapeutic strategy. Deep eutectic systems (DES) are based on the combination of different components which together, at a certain molar ratio, present a deep decrease in their melting point compared with the individual compounds. When an active pharmaceutical ingredient is part of a DES it is designated by therapeutic deep eutectic system (THEDES). New THEDES combining terpenes with anticancer properties, such as safranal, menthol and linalool, with nonsteroidal anti-inflammatory drugs (NSAIDs), like ibuprofen, ketoprofen and flurbiprofen were produced. To evaluate THEDES anti-CRC therapeutic potential, their physico-chemical properties, bioavailability and bioactivity, were explored. Our results show that safranal:ibuprofen (3:1), safranal:ibuprofen (4:1) and menthol:ibuprofen (3:1) present promising therapeutic activity towards CRC cells due to a selective cytotoxic action towards cancer cells. menthol:ibuprofen (3:1) anti-proliferative action seems to be related with cell membrane disruption, reduction of the inflammation through the reduction of reactive oxygen species (ROS) production, and induction of apoptosis via caspase-3. On the other hand, safranal:ibuprofen (3:1) and safafranal:ibuprofen (4:1) seem to prevent tumour expansion only through the induction of apoptosis via caspase-3. Besides, these systems present an increase in ibuprofen permeability, with menthol:ibuprofen (3:1) increasing also ibuprofen's solubility thus its overall bioavailability. Knowing that cancer is a huge problematic situation that requires alternative therapies with less side effects, improved efficacy, associated with less costs and environmentally friendly, a new opportunity emerges for DES to be part of the pharmaceutical industry.
Assuntos
Neoplasias Colorretais , Ibuprofeno , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Caspase 3 , Neoplasias Colorretais/tratamento farmacológico , Humanos , Ibuprofeno/química , Inflamação , Mentol/química , Mentol/farmacologia , Terpenos/farmacologia , Microambiente TumoralRESUMO
An ecofriendly and efficient ultrasound-assisted deep eutectic solvents dispersive liquid-phase microextraction by solidifying the deep eutectic solvents-rich phase was developed to determine azoxystrobin, fludioxonil, epoxiconazole, cyprodinil, and prochloraz in fruit juices and tea drinks by high-performance liquid chromatography. A varieties of environmental hydrophobic deep eutectic solvents serving as extraction agents were prepared using L-menthol and decanoic acid as hydrogen-bond acceptor and hydrogen-bond donor, respectively. The deep eutectic solvents were ultrasonically dispersed in sample solutions, solidified in a freezer and easily harvested. The main variables were optimized by one-factor-at-a-time and response surface test. The new method performs well with relative recovery of 71.75-109.40%, linear range of 2.5-5000 µg/L (r ≥ 0.9968), detection limit of 0.75-8.45 µg/L, quantification limit of 2.5-25 µg/L,, and inter- and intraday relative standard deviations below 13.53 and 14.84%, respectively. As for the extraction mechanism, deep eutectic solvents were disposed into many fine particles in the solution and captured the analytes based on the changes of particle size and quantity in deep eutectic solvents droplets after extraction. The environmental method can successfully detect fungicide residues in real fruit juices and tea drinks.
Assuntos
Ácidos Decanoicos/química , Sucos de Frutas e Vegetais/análise , Fungicidas Industriais/análise , Microextração em Fase Líquida , Mentol/química , Chá/química , Ondas Ultrassônicas , Interações Hidrofóbicas e Hidrofílicas , Solventes/químicaRESUMO
CONTEXT: Psidium guajava L. (Myrtaceae) leaf contains a wide variety of bioactive compounds that contribute valuable effects on human well-being. OBJECTIVE: This study investigates the influence of guava leaf extract-menthol toner on thermoregulation, including perspiration, skin temperature, and recovery heart rate. MATERIALS AND METHODS: This randomised, placebo-controlled clinical trial assessed the effects of the guava leaf extract-menthol toner and placebo with a 1-week washout period. Sixty-four participants were enrolled. The participants exercised on a treadmill until a 75% heart rate reserve was achieved for 5 min, followed by a 5 min post-exercise rest period. The skin temperature and heart rate were then measured before 5 mL of the testing product was sprayed to specific areas of the body, left it for 30 sec before wiped off. Post-exercise perspiration and skin temperatures were collected by sweat patches and measured by the Skin-thermometer ST500, respectively. A 20 min heart rate monitoring period started 10 min after the exercise and measured every 2 min intervals. RESULTS: Use of the toner significantly reduced post-exercise perspiration to approximately half of the baseline and placebo use values (p < 0.05). Furthermore, relative heart rate changes showed no significant differences among the tests (p > 0.05). Skin temperature was also unaffected (p > 0.05). DISCUSSION AND CONCLUSION: Guava leaf extract-menthol toner reduced perspiration by astringent effects but did not influence heat dissipation and did not affect cardiovascular mechanism compared to the controls. Additional cleaning with guava leaf extract-menthol toner could offer better hygiene after a workout.
Assuntos
Regulação da Temperatura Corporal/efeitos dos fármacos , Exercício Físico/fisiologia , Extratos Vegetais/farmacologia , Psidium/química , Adolescente , Estudos Cross-Over , Teste de Esforço , Feminino , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Mentol/química , Folhas de Planta , Método Simples-Cego , Temperatura Cutânea/efeitos dos fármacos , Sudorese/efeitos dos fármacos , Adulto JovemRESUMO
Various essential oils from plants and fragrance components such as monoterpenes have been discovered to reduce spontaneous movements in mice; thus, it has been made clear that the odor itself has the sedative activity. In the present study, we examined the sedative activity of the odors of fragrance components added to eye drops; l-menthol, d-camphor, phenylethyl alcohol, and geraniol, which are often used as refreshers or preservatives. Each fragrance component was administered by the inhalation route to mice, and the sedative effects were evaluated using an open field test. The results showed that four components administered via inhalation to mice significantly decreased the amount of spontaneous motor activity in a dose-dependent manner, indicating that all four components have a sedative effect. The optimal concentrations at which l-menthol, d-camphor, phenylethyl alcohol, and geraniol showed the highest sedative activity were 4 × 10-2 mg per cage, 4 × 10-4 mg per cage, 4 × 10-2 mg per cage, and both 4 × 10-4 and 4 × 10-2 mg per cage, respectively. The AUC graph of geraniol was represented as a W-shaped curve, suggesting that the sedative action of geraniol was biphasic. The present finding demonstrates a new perspective on a possible pharmacological property of eye drop additives used with no expected pharmacological functions.
Assuntos
Monoterpenos Acíclicos/química , Cânfora/química , Mentol/química , Monoterpenos/química , Álcool Feniletílico/química , Extratos Vegetais/química , Animais , Hipnóticos e Sedativos , Masculino , CamundongosRESUMO
Our study evaluated the in vitro antioxidant properties, antibacterial and antifungal activities, anti-inflammatory properties, and chemical composition of the essential oils (EOs), total phenol, and total flavonoid of wild Mentha pulegium L. This study also determined the mineral (nutritional and toxic) elements in the plant. The EOs were extracted using three techniques-hydro distillation (HD), steam distillation (SD), and microwave-assisted distillation (MAD)-and were analyzed using chromatography coupled with flame ionization (GC-FID) and gas chromatography attached with mass spectrometry detector (GC-MS). The antioxidant effects of the EOs were tested with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), while the antibacterial and antifungal activities of the EO and methanolic extract were tested using Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans. Twenty-six compounds were identified in the essential oil, representing 97.73% of the total oil, with 0.202% yield. The major components were pulegone (74.81%), menthone (13.01%) and piperitone (3.82%). Twenty-one elements, including macro- and micro-elements (Ba, Br, Ca, Cl, Co, Cr, Cs, Eu, Fe, K, Mg, Mn, Mo, Na, Rb, Sb, Sc, Sr, Th, U and Zn), were detected using neutron activation analysis (INAA) and inductively coupled plasma optical emission spectrometry (ICP-OES), with the concentration of mineral element close to the FAO recommendation. The results show that the EOs and extracts from Mentha pulegium L. had significant antimicrobial activities against the microorganisms, including five human pathogenic bacteria, one yeast (Candida albicans), and one phytopathogenic fungi. The in vivo anti-inflammatory activities of the leaf extracts were confirmed. The results indicate that the EOs and extracts from Mentha pulegium L. have promising applications in the pharmaceutical industries, clinical applications, and in medical research.
Assuntos
Flavonoides/química , Mentha pulegium/química , Minerais/química , Óleos Voláteis/química , Extratos Vegetais/química , Polifenóis/química , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Monoterpenos Cicloexânicos/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Masculino , Mentol/química , Camundongos , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologiaRESUMO
Vitamin D deficiency has been linked to various diseases, but could be rectified via fortified food stuffs or supplementation. In this study 39 different hydrophobic deep eutectic solvents were evaluated for green extraction of ergosterol from mushroom. Extraction parameters (e.g. time, solvent volume) were optimized using response surface methodology (RSM) and a maximum extraction yield of 6995.00 µg ergosterol/g dry weight mushroom was attained with menthol: pyruvic acid. The extracted ergosterol was purified using a novel methodology and the extraction solvent was reused for six cycles, while retaining extraction efficiency (up to 28%). The ergosterol was exposed to ultra-violet radiation for conversion to ergocalciferol (vitamin D2) resulting in a yield of ergocalciferol that was equivalent to 2142.01 µg/g dry weight mushroom.
Assuntos
Agaricus/química , Ergosterol/isolamento & purificação , Mentol/química , Fracionamento Químico/métodos , Ergocalciferóis/química , Ergosterol/química , Indústria de Processamento de Alimentos/métodos , Interações Hidrofóbicas e Hidrofílicas , Solventes/química , Raios UltravioletaRESUMO
: The present work evaluates for the first time two Lavandin (Lavandula × intermedia Emeric ex Loisel.) aromatic waters obtained from different plant organs, the flowers and the stems. Both extracts were analysed by GC-MS, which indicates semi-quantitative differences between the major metabolites including linalool, 1,8-cineole, camphor, linalyl acetate and 4-terpineol. 1H-NMR and LC-MS investigation confirmed the presence of these compounds. Moreover, behavioural tests with the food insect pest Tribolium confusum (Coleoptera Tenebrionidae) showed a good repellency for both hydrosols extracts with RD50 values of 3.6 and 3.3 µL cm-2 for the flowers and stems, respectively; at the higher concentrations, however, the hydrosol extract from the flowers is expected to be more effective than the one from the stems. The effect of the flowers and stems aromatic water of Lavandin on seed germination of Raphanus sativus was also evaluated. Results showed that seed germination was completely inhibited by flowers hydrolate, having a possible application as natural herbicide. The overall experience with these Lavandin extracts indicates the potential of improved hydrolates to become the main distillation products, rather than by-products, of the aromatic plants manufacturing; this stimulates further discussions about the potential positive impacts that such a shift could have in the context of ecopharmacognosy.
Assuntos
Repelentes de Insetos/farmacologia , Lavandula/química , Extratos Vegetais/farmacologia , Tribolium/fisiologia , Monoterpenos Acíclicos/química , Monoterpenos Acíclicos/farmacologia , Animais , Cânfora/química , Cânfora/farmacologia , Eucaliptol/química , Eucaliptol/farmacologia , Flores/química , Cromatografia Gasosa-Espectrometria de Massas , Germinação , Repelentes de Insetos/química , Itália , Mentol/análogos & derivados , Mentol/química , Mentol/farmacologia , Monoterpenos/química , Monoterpenos/farmacologia , Óleos Voláteis , Extratos Vegetais/química , Óleos de Plantas , Caules de Planta/química , Raphanus/fisiologiaRESUMO
Herbal treatments are often used as a treatment for migraine. Therefore, an evaluation of their safety and efficacy is important. Based on the Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines, and Cochrane Collaboration's tool for assessing the risk of bias, a systematic literature review of randomised, controlled human trials assessing the effects of herbal treatments delivered as a single ingredient for the acute or prophylactic treatment of migraine were conducted. Studies were identified through electronic database searches on Medline (Pubmed), Cochrane Library, Scopus, and CINAHL. Nineteen studies were identified examining the effects on migraine of feverfew, butterbur, curcumin, menthol/peppermint oil, coriander, citron, Damask rose, chamomile, and lavender. Overall, findings on the efficacy of feverfew were mixed and there was positive, albeit limited evidence for butterbur. There were positive, preliminary findings on curcumin, citron, and coriander as a prophylactic treatment for migraine, and the use of menthol and chamomile as an acute treatment. However, the risk of bias was high for many studies. The results of this systematic review suggest that several herbal medicines, via their multifactorial physiological influences, present as potential options to enhance the treatment of migraine. However, further high-quality research is essential to examine their efficacy and safety as a treatment for migraine.
Assuntos
Transtornos de Enxaqueca/tratamento farmacológico , Fitoterapia/métodos , Extratos Vegetais/uso terapêutico , Plantas Medicinais/fisiologia , Ensaios Clínicos Controlados Aleatórios como Assunto/estatística & dados numéricos , Terapia por Acupuntura , Camomila/fisiologia , Quimioprevenção/métodos , Citrus/fisiologia , Terapia Combinada , Coriandrum/fisiologia , Humanos , Mentol/química , Mentol/uso terapêutico , Transtornos de Enxaqueca/epidemiologia , Musicoterapia , Plantas Medicinais/química , Ensaios Clínicos Controlados Aleatórios como Assunto/métodos , Tanacetum parthenium/química , Tanacetum parthenium/fisiologiaRESUMO
This review article discusses the active constituents and potential of two menthol mint oils, Mentha piperita (MPEO) and Mentha arvensis (MAEO), as natural sources for botanical pesticides. The biological activities of these menthol mint oils, which can be useful in agriculture, have been broadly researched, especially toward phytotoxic microorganisms. To a lesser extent, the insecticidal and herbicidal activities of mint EOs have also been studied. It is apparent that the prospect of using menthol mint oils in agriculture is increasing in popularity. A number of investigations showed that the in vitro efficacy of MPEO and MAEO, as well as that of their main constituent, menthol, is pronounced. The results of in vitro research are useful for choosing EOs for further investigations. However, it is clear that in situ experiments are crucial and should be more extensively developed. At the same time, known techniques are to be applied to this area and new methods should be worked out, aiming at the improvement of EOs' pesticidal efficacy and cost-effectiveness, for future implementation in agricultural pest control.
Assuntos
Mentha piperita/química , Mentol/química , Óleos Voláteis/química , Óleos de Plantas/química , Mentha/química , Extratos Vegetais/químicaRESUMO
Deep eutectic solvents have been recently reported as an interesting alternative to improve the therapeutic efficacy of conventional drugs, hence called therapeutic deep eutectic solvents (THEDES). The main objective of this work was to evaluate the potential of limonene (LIM) based THEDES as new possible systems for cancer treatment. LIM is known to have antitumor activity, however it is highly toxic and cell viability is often compromised, thus this compound is not selective towards cancer cells. Different THEDES based on LIM were developed to unravel the anticancer potential of such systems. THEDES were prepared by gently mixing saturated fatty acids menthol or ibuprofen (IBU) with LIM. Successful THEDES were obtained for Menthol:LIM (1:1), CA:LIM (1:1), IBU:LIM (1:4) and IBU:LIM(1:8). The results indicate that all the THEDES present antiproliferative properties, but IBU:LIM (1:4) was the only formulation able to inhibit HT29 proliferation without comprising cell viability. Therefore, IBU:LIM (1:4) was the formulation selected for further assessment of anticancer properties. The results suggest that the mechanism of action of LIM:IBU (1:4) is different from isolated IBU and LIM, which suggest the synergetic effect of DES. In this work, we unravel a methodology to tune the selectivity of LIM towards HT29 cell line without compromising cell viability of healthy cells. We demonstrate furthermore that coupling LIM with IBU leads also to an enhancement of the anti-inflammatory activity of IBU, which may be important in anti-cancer therapies.
Assuntos
Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Líquidos Iônicos/farmacologia , Limoneno/farmacologia , Neoplasias/tratamento farmacológico , Antineoplásicos/química , Antineoplásicos/uso terapêutico , Células CACO-2 , Sobrevivência Celular/efeitos dos fármacos , Ácidos Decanoicos/química , Ácidos Decanoicos/farmacologia , Ácidos Decanoicos/uso terapêutico , Composição de Medicamentos/métodos , Ensaios de Seleção de Medicamentos Antitumorais , Células HT29 , Humanos , Ibuprofeno/química , Ibuprofeno/farmacologia , Ibuprofeno/uso terapêutico , Líquidos Iônicos/química , Líquidos Iônicos/uso terapêutico , Limoneno/química , Limoneno/uso terapêutico , Mentol/química , Mentol/farmacologia , Mentol/uso terapêutico , Ácido Mirístico/química , Ácido Mirístico/farmacologia , Ácido Mirístico/uso terapêutico , Neoplasias/patologiaRESUMO
This study aims at investigating p-menthane, a novel bio-based solvent resulting from the hydrogenation of d-limonene, as a green alternative to n-hexane or toluene for the extraction and solubilization of natural substances. First, conductor-like combination of quantum chemistry (COSMO) coupled with statistical thermodynamics (RS) calculations show a comparable solubilization profile of p-menthane and n-hexane for carotene, volatile monoterpenes such as carvone and limonene, and model triglycerides. Other data obtained experimentally in solid/liquid extraction conditions further indicate that p-menthane showed similar performances to n-hexane for extracting carotenes from carrots, aromas from caraway seeds, and oils from rapeseeds, as these products showed a comparable composition. p-Menthane was also tested using common analytical extraction procedures such as Soxhlet for determination of oil content via multiple extraction stages, and Dean-Stark for determination of water content via azeotropic distillation. For both systems, yields were comparable, but for Dean-Stark, the distillation curve slope was higher when using p-menthane, and the time needed to attain 100% water recovery was 55% shorter than for toluene. Taken together, these results reveal the potential of p-menthane as a green replacer for petroleum-based solvents such as n-hexane or toluene.
Assuntos
Produtos Biológicos/química , Citrus sinensis/química , Química Verde/métodos , Mentol/química , Solventes/química , Carotenoides/isolamento & purificação , Carum/química , Daucus carota/química , Destilação , Ácidos Graxos/análise , Cinética , Odorantes/análise , Óleo de Brassica napus , Sementes/química , Solubilidade , Tolueno/química , Água/químicaRESUMO
Photothermal therapy (PTT) as an emerging technique for cancer treatment has drawn great attention owing to its minimally invasive nature. However, it is difficult to achieve a complete tumor regression due to the heterogeneous heat distribution over the tumor. Application of photothermal conversion agents may enhance PTT efficiency, and a multifunctional imaging may provide guidance for the implementation of PTT. Herein, an L-menthol/IR-780 loaded liposome (MIL) is prepared to achieve NIR-triggered cavitation for enhancing photothermal ablation. The synthesized MIL possesses outstanding colloidal stability and photoacoustic/near infrared fluorescence/ultrasound (PA/NIRF/US) imaging contrast to offer multimodal imaging-guided photothermal therapy of cancer. Upon irradiation, the IR-780 acts as the photoabsorber to convert NIR light into heat energy. More importantly, the produced hyperthermia can not only induce ablation of tumor cells but also trigger vaporization and bubbling of encapsulated L-menthol (menthol). Consequently, the generated menthol bubbles obviously enhance the US imaging signal and promote photothermal ablation of the tumor.
Assuntos
Mentol/química , Fototerapia/métodos , Nanomedicina Teranóstica/métodos , Animais , Linhagem Celular Tumoral , Humanos , Hipertermia Induzida/métodos , Nanopartículas/químicaRESUMO
The time-temperature superposition principle (TTSP) was applied to the destabilization kinetics of a pharmaceutical emulsion. The final goal of this study is to predict precisely the emulsion stability after long-term storage from the short-period accelerated test using TTSP. As the model emulsion, a cream preparation that is clinically used for the treatment of pruritus associated with chronic kidney disease was tested. After storage at high temperatures ranging from 30 to 45⯰C for designated periods, the emulsion state was monitored using magnetic resonance imaging, and then the phase separation behaviors observed were analyzed according to the Arrhenius approach applying TTSP. The Arrhenius plot showed a biphasic change around 35⯰C, indicating that the separation behaviors of the sample were substantially changed between the lower (30-35⯰C) and higher (35-45⯰C) temperature ranges. This study also monitored the coalescence behavior using a backscattered light measurement. The experiment verified that the destabilization was initiated by coalescence of oil droplets and then it eventually led to obvious phase separation via creaming. Furthermore, we note the coalescence kinetics agreed well with the phase separation kinetics. Therefore, in the case of the sample emulsion, the coalescence behavior has a dominant influence on the destabilization process. This study offers a profound insight into the destabilization process of pharmaceutical emulsions and demonstrates the promising applicability of TTSP to pharmaceutical research.
Assuntos
Emulsões/química , Creme para a Pele/química , Cânfora/química , Difenidramina/química , Estabilidade de Medicamentos , Etanol/química , Cinética , Mentha , Mentol/química , Óleos de Plantas/química , Temperatura , Timol/química , Fatores de TempoRESUMO
The incorporation of chemo/photothermal/photodynamic therapy in subcellular organelles such as mitochondria has attracted extensive attention recently. Here, we designed mitochondria-targeted hollow mesoporous silica nanoparticles (THMSNs) loaded biocompatible phase-change material L-menthol (LM) via a facile method. Meanwhile, antitumor drug doxorubicin (DOX) and near-infrared (NIR) dye indocyanine green (ICG) approved by FDA were simultaneously encapsulated into THMSNs, denoted as THMSNs@LMDI, which showed NIR radiation triggered capacity for cancer treatment. With the mitochondria-targeted ability of triphenylphosphine, the resulting THMSNs@LMDI showed evidently improved cellular internalization and specific accumulation in mitochondria. Under NIR irradiation, the versatile ICG would be bound to simultaneously produce photodynamic and photothermal therapy. Meanwhile, in view of the solid-liquid phase transition feature of gatekeeper LM, THMSNs@LMDI provided a platform for NIR-mediated temperature-responsive DOX release. As a matter of course, these smart subcellular organelle-THMSNs could serve as an effective drug delivery platform for site-specific on-demand chemo/photothermal/photodynamic therapy of cancer.
Assuntos
Raios Infravermelhos , Mitocôndrias/metabolismo , Nanopartículas/química , Dióxido de Silício/química , Materiais Biocompatíveis/química , Materiais Biocompatíveis/metabolismo , Materiais Biocompatíveis/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Doxorrubicina/química , Doxorrubicina/metabolismo , Doxorrubicina/farmacologia , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Humanos , Verde de Indocianina/química , Verde de Indocianina/metabolismo , Verde de Indocianina/farmacologia , Mentol/química , Mentol/metabolismo , Mentol/farmacologia , Mitocôndrias/efeitos dos fármacos , Nanopartículas/toxicidade , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Fotoquimioterapia , Fototerapia , Porosidade , Oxigênio Singlete/metabolismoRESUMO
This study was conducted to investigate effects of dietary peppermint leaves and menthol supplementations on performance, survivability rate, cost economics, meat physicochemical properties, and carcass characteristics of broiler chicks. A total of 384 1-day-old, unsexed Ross 308 broiler chicks, were divided into 2 experiments. Each experiment included 192 birds that were assigned to 4 dietary treatments that included peppermint leaves at concentrations of 0, 5, 10, or 15 g/kg in the first experiment or menthol at concentrations of 0, 26, 52, or 78 mg/kg in the second experiment. Each treatment had 6 replicate pens with 8 birds. The experiments lasted for 35 D. The peppermint leaves contained 1.48% essential oil that contained 35.1% menthol, and the levels of menthol were selected based on the concentrations in peppermint leaf levels. Body weight and body-weight gain increased with the increase in dietary peppermint leaves (linear, P < 0.01) and menthol concentrations (linear, quadratic, P < 0.01) during the trial periods. In addition, the feed intake linearly increased (P < 0.01) with increasing peppermint leaves or menthol levels and, in turn, caused linear improvements (P < 0.01) in feed conversion values. Interestingly, a lower mortality rate was recorded in the supplementation groups and, therefore, a higher net return was observed. However, pH values and drip loss percentage of breast and leg muscles were not affected by either dietary peppermint levels or menthol levels. Increasing peppermint or menthol levels decreased (P < 0.001) cook-loss percentage of breast and leg muscles. On the other hand, dietary supplementation of peppermint leaves or menthol had no effect (P ≥ 0.05) on the relative weights of dressing, breast, leg, liver, heart, gizzard, spleen, or pancreas. Interestingly, abdominal fat percentage was decreased by either supplemental peppermint or menthol. Hence, the present investigation demonstrates that peppermint leaves can be used as an effective novel nutritional bio-agent up to 15 g/kg to improve the performance of broiler chicks, mainly due to its active component.
Assuntos
Carne/análise , Mentha piperita/química , Mentol/metabolismo , Ração Animal/análise , Ração Animal/economia , Animais , Galinhas/crescimento & desenvolvimento , Galinhas/fisiologia , Dieta/veterinária , Suplementos Nutricionais/análise , Suplementos Nutricionais/economia , Mentol/administração & dosagem , Mentol/química , Folhas de Planta/química , Distribuição AleatóriaRESUMO
Various nanoformulations of perfluorocarbon have been developed thus far, to achieve ultrasound imaging of tumors and tumor-targeted therapy. However, their application has been greatly limited by their short sonographic duration and large size distribution. A novel theranostic agent was constructed based on gold nanoshell cerasome-encapsulated L-menthol (GNC-LM). Owing to the sustained and controllable generation of L-menthol bubbles under near-infrared laser irradiation, GNC-LM showed good performance in contrast enhancement of ultrasound imaging in vivo. GNC-LM could be imaged for 30 min, which is much longer than the imaging time of SonoVue (commercially used microbubbles). Moreover, photothermal therapy (PTT) based on the light-to-heat conversion of the nanosystem effectively ablated the tumor. Our study demonstrated the promising potential of the obtained GNC-LM to serve as a therapeutic nanoprobe for ultrasound contrast imaging and PTT of tumors.
Assuntos
Meios de Contraste/química , Ouro/química , Hipertermia Induzida , Lipídeos/química , Mentol/química , Nanoconchas/química , Neoplasias/terapia , Fototerapia , Animais , Morte Celular , Camundongos Endogâmicos BALB C , Nanoconchas/ultraestrutura , Neoplasias/diagnóstico por imagem , Neoplasias/patologia , UltrassonografiaRESUMO
INTRODUCTION: Lip plumpers are topical agents that offer immediate, but temporary, volumization of the lips. While these products are becoming increasingly popular and are available at multiple retailers, there is a lack of clinical studies to evaluate the efficacy, longevity, and safety of the lip plumping products. METHODS: This is a prospective, single center, clinical trial to evaluate the duration, efficacy, and safety of a lip plumping agent in two clinical visits. Lip volume and adverse event were assessed by two clinicians at various time points: 15 minutes, 1 hour, 2 hours, 3 hours, and 4 hours. RESULTS: Twenty-two subjects were enrolled in the study, and eighteen completed the study. Investigator assessments of global improvement 15 minutes after application of the lip plumping product demonstrated improvement in lip fullness in 100% of the subjects (18/18), and 1 hour post-application 67% (12/18) showed an improvement in lip fullness that was statistically significant compared to the 2-hour assessment (P less than 0.05). Subject evaluations noted improvement in lip fullness 15 minutes post-application in 94.4% (17/18) of subjects, and 1 hour post-application, 89% (16/18) of the subjects who completed the trial noted some improvement in the volume of their lips that was statistically significant compared to the 2-hour post-application time point (P less than 0.0001). Subjects noted that they did experience a tingling and heat sensation, but a majority noted that that this sensation lasted less than 15 minutes. DISCUSSION: Our study demonstrated that the lip plumping product increased lip volume in almost all patients 15 minutes post-application and showed a continued improvement in lip fullness per investigator assessments 1 hour after application. Adverse events of a tingling or heat sensation were expected and observed as the topical product contained capsaicin, cinnamon, and menthol, all of which can induce this sensation by the release of substance P. J Drugs Dermatol. 2018;17(9):999-1004.