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1.
J Agric Food Chem ; 67(40): 11066-11076, 2019 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-31508948

RESUMO

The electrospinning of nanofibers (NFs) of cinnamaldehyde inclusion complexes (ICs) with two different hydroxypropylated cyclodextrins (CDs), hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and hydroxypropyl-γ-cyclodextrin (HP-γ-CD), was successfully performed in order to produce cinnamaldehyde/CD-IC NFs without using an additional polymer matrix. The inclusion complexation between cinnamaldehyde and hydroxypropylated CDs was studied by computational molecular modeling, and the results suggested that HP-ß-CD and HP-γ-CD can be inclusion complexed with cinnamaldehyde at 1:1 and 2:1 (cinnamaldehyde/CD) molar ratios. Additionally, molecular modeling and phase solubility studies showed that water solubility of cinnamaldehyde dramatically increases with cyclodextrin inclusion complex (CD-IC) formation. The HP-ß-CD has shown slightly stronger binding with cinnamaldehyde when compared to HP-γ-CD for cinnamaldehyde/CD-IC. Although cinnamaldehyde is a highly volatile compound, it was effectively preserved with high loading by the cinnamaldehyde/CD-IC NFs. It was also observed that cinnamaldehyde has shown much higher temperature stability in cinnamaldehyde/CD-IC NFs compared to uncomplexed cinnamaldehyde because of the inclusion complexation state of cinnamaldehyde within the hydroxypropylated CD cavity. Moreover, cinnamaldehyde still has kept its antibacterial activity in cinnamaldehyde/CD-IC NF samples when tested against Escherichia coli. In addition, cinnamaldehyde/CD-IC NF mats were fast-dissolving in water, even though pure cinnamaldehyde has a water-insoluble nature. In brief, self-standing nanofibrous mats of electrospun cinnamaldehyde/CD-IC NFs are potentially applicable in food, oral-care, healthcare, and pharmaceutics because of their fast-dissolving character, enhanced water solubility, stability at elevated temperature, and promising antibacterial activity.


Assuntos
Acroleína/análogos & derivados , Antibacterianos/química , Antibacterianos/farmacologia , Composição de Medicamentos/métodos , Acroleína/química , Acroleína/farmacologia , Ciclodextrinas/química , Composição de Medicamentos/instrumentação , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Nanofibras/química , Solubilidade , Temperatura Ambiente
2.
Int J Nanomedicine ; 14: 5713-5728, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31413571

RESUMO

Purpose: The levels of reactive oxygen species (ROS) in tumor cells are much higher than that in normal cells, and rise rapidly under the influence of exogenous or endogenous inducing factors, eventually leading to the apoptosis of tumor cells. Therefore, this study prepared a dual pH/reducing-responsive poly (N-isopropylacrylamide-co-Cinnamaldehyde-co-D-α-tocopheryl polyethylene glycol 1000 succinate, PssNCT) nanogels, which employed two exogenous ROS inducers, cinnamaldehyde (CA) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), to selectively induce apoptosis by regulating ROS levels in tumor cells. Methods: The PssNCT nanogels were prepared by the free radical precipitation polymerization under the crosslink between pH-sensitive hydrazone and reducing-sensitive disulfide bonds, followed by the physicochemical and morphological characteristics investigations. Plasma stability, dual pH/reducing responsive degradation and in vitro release were also assessed. In cell experiments, cytotoxicity in different cells were first detected. The intracellular ROS levels and mitochondrial functions of tumor cells were then evaluated. Moreover, the apoptosis and western-blot assays were employed to verify the association between ROS levels elevation and apoptosis in tumor cells. Results: The nanogels exhibited a round-like hollow structure with the diameter smaller than 200nm. The nanogels were stable in plasma, while showed rapid degradation in acidic and reducing environments, thus achieving significant release of CA and TPGS in these media. Furthermore, the sufficient amplification of ROS signals was induced by the synergistically function of CA and TPGS on mitochondria, which resulted in the opening of the mitochondrial apoptotic pathway and enhanced cytotoxicity on MCF-7 cells. However, nanogels barely affected L929 cells owing to their lower intracellular ROS basal levels. Conclusion: The specific ROS regulation method achieved by these nanogels could be explored to selectively kill tumor cells according to the difference of ROS signals in different kinds of cells.


Assuntos
Apoptose , Espaço Intracelular/química , Polietilenoglicóis/farmacologia , Polietilenoimina/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Acroleína/análogos & derivados , Acroleína/farmacologia , Animais , Apoptose/efeitos dos fármacos , Doxorrubicina/farmacologia , Liberação Controlada de Fármacos , Humanos , Concentração de Íons de Hidrogênio , Células MCF-7 , Camundongos , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Vitamina E/síntese química , Vitamina E/química
3.
Int Braz J Urol ; 45(5): 1033-1042, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31408283

RESUMO

Cinnamomum cassia (Cinnamon) is a well-known traditional medicine with therapeutic benefits for centuries. We evaluated the effects of cinnamon essential oil (CEO) and its main component cinnamaldehyde (CA) on human corpus cavernosum (HCC) and rat CC. The essential oil of cinnamon was analyzed for the confirmation of the oil profile. HCC specimens from patients undergoing penile prosthesis surgery (age 48-69 years) were utilized for functional studies. In addition, erectile responses in anesthetized control and diabetic rats were evaluated in vivo after intracavernosal injection of CEO and CA, and rat CC strips were placed in organ baths. After precontraction with phenylephrine (10µM), relaxant responses to CEO and CA were investigated. CA (96.9%) was found as the major component. The maximum relaxation responses to CEO and CA were 96.4±3.5% and 96.0±5.0% in HCC and 97.5±5.5% and 96.8±4.8% in rat CC, respectively. There was no difference between control and diabetic rats in relaxation responses to CEO and CA. The relaxant responses obtained with essential oil and CA were not attenuated in the presence of nitric oxide synthase (NOS) inhibitor, and soluble guanylate cyclase inhibitor (sGS) in CC. In vivo, erectile responses in diabetic rats were lower than in control rats, which was restored after intracavernosal injection of CEO and CA. CEO and CA improved erectile function and relaxation of isolated strips of rat CC and HCC by a NO/cGMP-independent mechanism. Further investigations are warranted to fully elucidate the restorative effects of CEO and CA on diabetic erectile dysfunction.


Assuntos
Acroleína/análogos & derivados , Cinnamomum zeylanicum/química , Relaxamento Muscular/efeitos dos fármacos , Óleos Voláteis/farmacologia , Pênis/efeitos dos fármacos , Acroleína/farmacologia , Idoso , Análise de Variância , Animais , Disfunção Erétil/tratamento farmacológico , Disfunção Erétil/fisiopatologia , Humanos , Masculino , Pessoa de Meia-Idade , Relaxamento Muscular/fisiologia , Ereção Peniana/efeitos dos fármacos , Ereção Peniana/fisiologia , Pênis/fisiopatologia , Fenilefrina/farmacologia , Inibidores da Fosfodiesterase 5/farmacologia , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Citrato de Sildenafila/farmacologia , Vasoconstritores/farmacologia
4.
Artigo em Inglês | MEDLINE | ID: mdl-31294650

RESUMO

The present study examines the influence of the natural preservatives carvacrol, eugenol, trans-cinnamaldehyde and the essential oil (EO) Origanum vulgare on ochratoxin A (OTA) production and the mycelial growth of two food-related moulds, Penicillium verrucosum and Aspergillus westerdijkiae, by broth macro-dilution assay for 21 days. With the addition of ½ minimum inhibitory concentration (MIC) carvacrol, eugenol and O. vulgare EO, the mycelial dry weight of both moulds decreased significantly over the whole incubation period of 7, 14 and 21 days. Trans-cinnamaldehyde slightly stimulated the growth of A. westerdijkiae and P. verrucosum at 14 and 21 days of incubation. Growth inhibition did not accompany inhibition of OTA production. Although the growth of both moulds was inhibited after the addition of ½ MIC carvacrol, eugenol and O. vulgare EO, the OTA production of the strong mycotoxin producer A. westerdijkiae was stimulated. Only trans-cinnamaldehyde inhibited the production of OTA with the addition of ½ MIC. P. verrucosum produced significantly less OTA than A. westerdijkiae, and its mycotoxin production was almost completely inhibited by the addition of ½ MIC of the natural preservatives.


Assuntos
Aspergillus/efeitos dos fármacos , Microbiologia de Alimentos , Conservantes de Alimentos/farmacologia , Micélio/efeitos dos fármacos , Ocratoxinas/biossíntese , Penicillium/efeitos dos fármacos , Acroleína/análogos & derivados , Acroleína/química , Acroleína/farmacologia , Aspergillus/química , Eugenol/química , Eugenol/farmacologia , Conservantes de Alimentos/química , Monoterpenos/química , Monoterpenos/farmacologia , Micélio/crescimento & desenvolvimento , Ocratoxinas/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Penicillium/química
5.
J Chem Ecol ; 45(8): 667-672, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31313134

RESUMO

Agriotes ustulatus is an economically important click beetle in Europe. A female-produced pheromone, (E,E)-farnesyl acetate, has been identified and is used for monitoring and detecting males. More recently, a floral lure targeting females with modest, but significant, activity has been described. Based on preliminary data, we hypothesized, that similar to the effects on the congeneric A. brevis, addition of the pheromone to the floral lure should improve female A. ustulatus catches. Also, as click beetles have been reported to respond to white light, we studied possible interactions between visual and chemical cues. In field trials, the addition of the synthetic pheromone to the floral lure resulted in a dramatic increase in the number of females trapped, whereas male catches remained unaffected and equal to those in traps baited with pheromone only. A white visual cue did not influence trap catches. Maximum catches of both sexes of A. ustulatus can be achieved using the pheromone and the floral lure inside the same trap. Furthermore, the compounds can be formulated in a single polyethylene bag dispenser, making handling of the trap easier. Due to a much larger proportion of females in the catch, this improved trap may be a promising tool for semiochemical-based, environmentally sound agricultural practice against this important pest.


Assuntos
Besouros/fisiologia , Feromônios/química , Acroleína/análogos & derivados , Acroleína/química , Acroleína/farmacologia , Animais , Anisóis/química , Anisóis/farmacologia , Comportamento Animal/efeitos dos fármacos , Farneseno Álcool/análogos & derivados , Farneseno Álcool/química , Farneseno Álcool/farmacologia , Feminino , Flores/química , Flores/metabolismo , Controle de Insetos , Masculino , Feromônios/farmacologia , Estereoisomerismo
6.
Zhonghua Xin Xue Guan Bing Za Zhi ; 47(6): 465-470, 2019 Jun 24.
Artigo em Chinês | MEDLINE | ID: mdl-31262131

RESUMO

Objective: To investigate the effect of cinnamaldehyde (CIN) on the inflammation and apoptosis on human umbilical vein endothelial cells (HUVECs) induced by lipopolysaccharide (LPS), and to explore the potential mechanisms. Methods: HUVECs were divided in to 8 groups: blank control group, LPS group, LPS+(low, medium, high) dose CIN groups and (low, medium, high) CIN groups. Cell cytotoxicity was determined by trypan blue staining, mRNA expression of the inflammatory factors was determined by RT-PCR,apoptosis was determined by TUNEL staining,the signal pathway was determined by Western blot. Results: (1) Cell viability:compared with the control group,cell survival rate was significantly lower in the LPS group (P<0.01), while the survival rates were all significantly higher in the 3 LPS+CIN groups than in the LPS group (all P<0.01) in a concentration-dependent manner. (2) The mRNA expression of the inflammation factors: compared with the control group, mRNA expression of the inflammation factors were all increased in the LPS group (all P<0.01),while the effect of LPS could be significantly reversed by cotreatment with CIN in a concentration-dependent manner (all P<0.01). Compared with control group, the mRNA expression of the inflammation factors in the LPS group were all enhanced in a time-dependent manner (0,6,12,24 h),which could be significantly downregulated by cotreatment with LPS+CIN (high dose) in a time-dependent manner. (3) Cell apoptosis: compared with the control group, the apoptosis rate was significantly higher in the LPS group (P<0.01), while this effect could be significantly reversed by the cotreatment with CIN (high dose) (P<0.01). (4) Signaling pathway: compared with the control group, the phosphorylation of iκBα, p65 in HUVECs treated with LPS were rapidly up-regulated compared with their corresponding total proteins and the expression of TLR4 (all P<0.01), while the degree of p-iκBα/iκBα, p-p65/p65 and TLR4 could be significantly suppressed by cotreatment with CIN (high dose) (all P<0.01). Conclusion: CIN can attenuate LPS induced inflammation and apoptosis in HUVECs, possibly by inhibiting the activation of NF-κB signaling pathway.


Assuntos
Inflamação , Acroleína/análogos & derivados , Apoptose , Células Endoteliais da Veia Umbilical Humana , Humanos , Lipopolissacarídeos , NF-kappa B
7.
Eur J Med Chem ; 178: 131-140, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31195168

RESUMO

Cancer is known as a leading cause of death worldwide. In the last two decades, the incidence of cancer has been dramatically increased mostly due to lifestyle changes. The importance of this issue has attracted further attention to discover novel therapies to prevent and treat cancers. According to previous studies, drugs used to treat cancer have shown significant limitations. Therefore, the role of herbal medicines alone or in combination with chemotherapy drugs has been extensively studied in cancer treatment. Cinnamon is a natural component showing a wide range of pharmacological functions including anti-oxidant, anti-microbial and anti-cancer activities. Impaired apoptosis plays critical roles in the initiation and progression of cancer. Increasing evidence indicates that cinnamon, as a therapeutic agent, has anti-cancer effects via affecting numerous apoptosis-related pathways in cancer cells. Here, we highlighted anticancer properties of cinnamon, particularly through targeting apoptosis-related mechanisms.


Assuntos
Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Cinnamomum zeylanicum/química , Eugenol/uso terapêutico , Extratos Vegetais/uso terapêutico , Acroleína/análogos & derivados , Acroleína/farmacologia , Animais , Antineoplásicos/farmacologia , Benzoatos/farmacologia , Linhagem Celular Tumoral , Eugenol/farmacologia , Humanos , Extratos Vegetais/farmacologia
8.
Food Chem ; 295: 671-679, 2019 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-31174811

RESUMO

The aim of this work was to develop and optimize a pH-responsive nanoparticle based on poly(D,L-lactide-co-glycolide) (PLGA) and chitosan (CHIT) for delivery of natural antimicrobial using trans-cinnamaldehyde (TCIN) as a model compound. The optimization was performed using a central composite design and the desirability function approach. The optimized levels of variables considering all significant responses were 4% (w/w) of TCIN and 6.75% (w/w) of CHIT. After, optimized nanoparticles were produced and characterized according to their physicochemical properties and their antimicrobial activity against Salmonella Typhimurium and Staphylococcus aureus. Optimized nanoparticles characterization indicated a satisfactory TCIN encapsulation (33.20 ±â€¯0.85%), spherical shape, pH-responsive controlled release, with faster release in the presence of CHIT at low pH, and enhanced antimicrobial activity against both pathogens. TCIN encapsulation using PLGA coated with CHIT enhanced its antimicrobial activity and generated a delivery system with pH-sensitivity for controlled release with promising properties for food safety applications.


Assuntos
Anti-Infecciosos/química , Quitosana/sangue , Nanopartículas/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Acroleína/análogos & derivados , Acroleína/química , Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Varredura Diferencial de Calorimetria , Quitosana/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio , Testes de Sensibilidade Microbiana , Tamanho da Partícula , Salmonella/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos
9.
J Photochem Photobiol B ; 196: 111513, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31136885

RESUMO

Photobiomodulation (PBM) is a therapy suggested for the treatment of pain and inflammation. Different mechanisms have been proposed to explain the analgesic and inflammatory effects of photobiomodulation, but there are still gaps on the mechanisms underlying. The objective was to investigate the analgesic and anti-inflammatory effect of red LED, as well as to investigate the possible mechanism of action in acute nociception models. Radiation was applied with red LED (660 nm, 215 mW, 84.64 mW/cm2, 2.531 J/cm2 (30s); 5.07 J/cm2 (60s) 7.61 J/cm2 (90s) and 10.15 J/cm2 (120 s)). The red LED applied 60 s before the experiments, promoted reduction of the nociceptive neurogenic (1st phase) and inflammatory pain (2nd phase) induced by intraplantar (i.pl.) injection of formalin. This effect duration in the second phase was 180 min after pretreatment of the LED. Red LED also reduced nociception induced by intraperitoneal injection of acetic acid. Furthermore, red LED prevented nociception induced by i.pl. injection of cinnamaldehyde, capsaicin, menthol and acidified saline. It was demonstrate the involvement of glutamatergic system with the reduction the nociception induced by glutamate. The red LED was able to prevent nociception induced by intracellular signaling cascades activators, phorbol 12-myristate 13-acetate (PMA), bradykinin, forskolin and prostaglandin. In addition, red LED, respectively, from 30 to 90s demonstrated an antiedematogenic effect on ear edema and reduction the migration of inflammatory cells induced by single application of croton oil. Thus, the new findings in this study support some underlying mechanism by which red LED phototherapy reduces acute pain. However, need further clarification regarding analgesic and anti-inflammatory effect of the photobiomodulation in preclinical studies.


Assuntos
Dor Aguda/radioterapia , Inflamação/radioterapia , Terapia com Luz de Baixa Intensidade , Acroleína/análogos & derivados , Acroleína/farmacologia , Dor Aguda/patologia , Animais , Dinoprostona/farmacologia , Orelha/patologia , Edema/patologia , Edema/radioterapia , Inflamação/patologia , Luz , Masculino , Camundongos , Nociceptividade/efeitos dos fármacos , Nociceptividade/efeitos da radiação
10.
J Appl Microbiol ; 127(1): 99-108, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31050849

RESUMO

AIMS: The antimicrobial activity of cinnamon essential oil and cinnamaldehyde against bacterial and fungal pathogens associated with canine otitis externa, as well as the effect of their combination with EDTA were investigated. METHODS AND RESULTS: Antimicrobial susceptibility testing was performed using the broth microdilution method while spot-plating technique was used to determine their bactericidal activity. Time-kill kinetics and checkerboard assays were performed to confirm the bactericidal activity and combination effects of the compounds. Cinnamon oil and cinnamaldehyde exhibited antimicrobial activity against Gram-positive and Gram-negative pathogens, as well as Malassezia pachydermatis. Synergistic interaction was shown when EDTA (672 µg ml-1 ) was combined with cinnamon oil (41 µg ml-1 ) and cinnamaldehyde (22 µg ml-1 ) against Pseudomonas aeruginosa. Cinnamaldehyde exhibited significantly stronger antimicrobial activity than cinnamon bark oil. CONCLUSIONS: Cinnamon essential oil and cinnamaldehyde, either used alone or in combination with EDTA, were effective against the causative micro-organisms of canine otitis externa. The data suggest that cinnamaldehyde could be a promising antimicrobial agent against canine otitis externa. SIGNIFICANCE AND IMPACT OF THE STUDY: This study shows that cinnamon essential oil and cinnamaldehyde, especially the latter, could be used in combination with EDTA as novel treatment for sensitive and resistant bacterial and fungal pathogens involved in canine otitis externa.


Assuntos
Acroleína/análogos & derivados , Anti-Infecciosos/farmacologia , Ácido Edético/farmacologia , Óleos Voláteis/farmacologia , Otite Externa/veterinária , Acroleína/farmacologia , Animais , Antibacterianos/farmacologia , Cães , Sinergismo Farmacológico , Testes de Sensibilidade Microbiana/estatística & dados numéricos , Otite Externa/microbiologia
11.
J Mycol Med ; 29(2): 154-157, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30956064

RESUMO

Candida rugosa (recently reclassified Diutina rugosa) is an emerging pathogen affecting humans and animals. Candida resistance to existing drugs is an important factor to be monitored, as well as the need of researching alternatives to conventional antifungals. Here, we evaluated the in vitro effects of some antifungals and major components of essential oils by the broth microdilution method (CLSI M27-A3) against fifteen C. rugosa strains from animals isolated and molecular identificated. The results showed MIC90 of: 0.125µg/mL to ketoconazole and voriconazole, 0.25µg/mL to micafungin, 0.5µg/mL to anidulafungin, 1µg/mL to caspofungin, 2µg/mL to amphotericin B, itraconazole and flucytosin, 8µg/mL to fluconazole, 16µg/mL to nystatin and >128µg/mL to terbinafine. The compounds carvacrol (MIC90 320µg/mL), thimol (MIC90 320µg/mL) and cinnamaldehyde (MIC90 160µg/mL) demonstrated antifungal activity against the samples tested.


Assuntos
Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Óleos Voláteis/farmacologia , Acroleína/análogos & derivados , Acroleína/farmacologia , Anidulafungina/farmacologia , Animais , Caspofungina/farmacologia , Bovinos/microbiologia , Cães/microbiologia , Cavalos/microbiologia , Micafungina/farmacologia , Testes de Sensibilidade Microbiana , Óleos Voláteis/química
12.
Molecules ; 24(8)2019 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31027179

RESUMO

Wound healing can be delayed following colonization and infection with the common bacterium Pseudomonas aeruginosa. While multiple therapies are used for their treatment, these are ineffective, expensive, and labour-intensive. Thus, there is an enormous unmet need for the treatment of infected wounds. Cinnamaldehyde, the major component of cinnamon oil, is well known for its antimicrobial properties. Herein, we investigated the effects of sub-inhibitory concentrations of cinnamaldehyde in the virulence of P. aeruginosa. We also assessed its healing potential in P. aeruginosa-infected mouse skin wounds and the mechanisms involved in this response. Sub-inhibitory concentrations of cinnamaldehyde reduced P. aeruginosa metabolic rate and its ability to form biofilm and to cause haemolysis. Daily topical application of cinnamaldehyde on P. aeruginosa-infected skin wounds reduced tissue bacterial load and promoted faster healing. Lower interleukin-17 (IL-17), vascular endothelial growth factor (VEGF) and nitric oxide levels were detected in cinnamaldehyde-treated wound samples. Blockage of transient receptor potential ankyrin 1, the pharmacological target of cinnamaldehyde, abrogated its healing activity and partially reversed the inhibitory actions of this compound on VEGF and IL-17 generation. We suggest that topical application of sub-inhibitory concentrations of cinnamaldehyde may represent an interesting approach to improve the healing of P. aeruginosa-infected skin wounds.


Assuntos
Acroleína/análogos & derivados , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/patogenicidade , Pele/microbiologia , Cicatrização/efeitos dos fármacos , Acroleína/uso terapêutico , Animais , Anti-Infecciosos/uso terapêutico , Biofilmes/efeitos dos fármacos , Modelos Animais de Doenças , Feminino , Interleucina-17/metabolismo , Camundongos , Infecções por Pseudomonas/tratamento farmacológico , Canal de Cátion TRPA1/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo
13.
Parasit Vectors ; 12(1): 89, 2019 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-30867033

RESUMO

BACKGROUND: Pyrethroid and organophosphate resistance in the malaria vector Anopheles gambiae has led to the search for not only alternative insecticides, but also repellent chemical compounds. However, little is known about the potential actions of repellents and the cross-resistance risk between insecticide and repellent compounds. METHODS: Here we show the action of permethrin, DEET, geraniol, carvacrol, culminaldehyde and cinnamaldehyde against three A. gambiae strains: 'Kis' (Kisumu susceptible strain), 'KdrKis' (pyrethroid resistant strain) and 'AcerKis' (organophosphate resistant strain), the last two differing from the first by a mutation on the kdr and ace1 genes, respectively. CONCLUSIONS: Results from the DEET assays show it induced repellency for the resistant KdrKis and AcerKis strains but maintained irritancy for the susceptible strain. More generally, we show resistance genes modify the behavior of An. gambiae, increasing or decreasing the effectiveness of DEET and natural compounds, depending on the mutation. These findings offer a new avenue for research on the target and mechanism of repellent compounds. We discuss these findings in the context of vector control strategies.


Assuntos
Anopheles/efeitos dos fármacos , DEET/farmacologia , Repelentes de Insetos/farmacologia , Resistência a Inseticidas , Malária/prevenção & controle , Controle de Mosquitos , Acroleína/análogos & derivados , Acroleína/farmacologia , Animais , Anopheles/genética , Feminino , Humanos , Inseticidas/farmacologia , Masculino , Monoterpenos/farmacologia , Mosquitos Vetores/efeitos dos fármacos , Mutação , Permetrina/farmacologia , Piretrinas/farmacologia , Terpenos/farmacologia
14.
Int J Food Microbiol ; 296: 1-7, 2019 May 02.
Artigo em Inglês | MEDLINE | ID: mdl-30818250

RESUMO

Salmonella enterica is a major human pathogen that is responsible for 23,000 hospitalizations annually in the United States. Contact with contaminated pet food and infected companion animals can transmit salmonellosis to humans. Recent multistate human outbreaks of salmonellosis linked to commercial contaminated dry dog foods underscore the need for controlling the pathogen in pet foods for protecting pet and public health. In this study, the efficacy of five Generally Recognized as Safe (GRAS) status, plant-derived antimicrobials (PDAs), namely trans-cinnamaldehyde (TC), carvacrol (CR), thymol (TY), eugenol (EG), and caprylic acid (CA) applied as a vegetable oil or chitosan based antimicrobial spray on dry pet food for reducing Salmonella Schwarzengrund was investigated. Three hundred gram portions of a commercial dry dog food were inoculated with a two-strain mixture of nalidixic acid (NA) resistant S. Schwarzengrund (~6 log CFU/g), followed by a spray treatment with 0%, 0.5%, 1% or 2% of TC, CR, TY, EG or CA in combination with 5% vegetable oil or 1% chitosan as a carrier. The control and treated dog food samples were stored at 25 °C for 28 days. On days 0, 1, 3, 5, 7, 14, 21, and 28, Salmonella on pet food was enumerated by serial dilution and plating on xylose lysine desoxycholate (XLD) agar. All PDAs at 1% and 2% applied in vegetable oil or chitosan reduced S. Schwarzengrund by at least ~2 log CFU/g on day 3 of storage when compared to control (P < 0.05). No significant reductions in Salmonella were observed on feed sprayed with only vegetable oil or chitosan (P > 0.05). Overall, 2% TC in vegetable oil or chitosan was the most effective treatment, where at least 3 to 3.5 log CFU/g reduction in bacterial populations was observed during storage (P < 0.05). Results suggest that the aforementioned PDAs could potentially be used as an antimicrobial spray to reduce S. Schwarzengrund on dry dog food. However, further studies on the acceptance of PDA-treated dry food by dogs are needed.


Assuntos
Ração Animal/microbiologia , Antibacterianos/farmacologia , Quitosana/farmacologia , Óleos Vegetais/farmacologia , Intoxicação Alimentar por Salmonella/prevenção & controle , Infecções por Salmonella/prevenção & controle , Salmonella enterica/efeitos dos fármacos , Soja/química , Acroleína/análogos & derivados , Acroleína/farmacologia , Animais , Surtos de Doenças/prevenção & controle , Eugenol/farmacologia , Microbiologia de Alimentos , Humanos , Monoterpenos/farmacologia , Animais de Estimação/microbiologia , Intoxicação Alimentar por Salmonella/microbiologia , Infecções por Salmonella/microbiologia
15.
Int J Nanomedicine ; 14: 1597-1618, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30880968

RESUMO

Objective: Nanoparticles can efficiently carry and deliver anticancer agents to tumor sites. Mounting evidence indicates that many types of cancer cells, including colon cancer, have a weakly acidic microenvironment and increased levels of reactive oxygen species. The construction of nano drug delivery vehicles "activatable" in response to the tumor microenvironment is a new antitumor therapeutic strategy. Methods: Cinnamaldehyde (CA) was designed to link directly with dextran to form a polymer through an acid cleavable acetal bond. Herein, a novel pH-sensitive drug delivery system was constructed with co-encapsulated 10-hydroxy camptothecin (HCPT). Dynamic light scattering (DLS) analysis, transmission electron microscopy (TEM) analysis, and release kinetics analysis of HCPT-CA-loaded nanoparticles (PCH) were conducted to investigate the physical and chemical properties. The cellular uptake signatures of the nanoparticles were observed by confocal microscopy and flow cytometry. Cell viability, cell scratch assay, apoptosis assay, and colony formation assay were performed to examine the potent antiproliferative and apoptotic effects of the PCH. The antitumor mechanism of the treatment with PCH was evaluated by Western blotting, flow cytometry, and TEM analysis. The pharmacokinetics of PCH were examined in healthy Sprague Dawley rats within 6 hours after sublingual vein injection. We lastly examined the biodistribution and the in vivo anticancer activity of PCH using the xenograft mouse models of HCT116 cells. Results: Both HCPT and CA were quickly released by PCH in an acidic microenvironment. PCH not only induced cancer cell death through the generation of intracellular reactive oxygen species in vitro but also facilitated the drug uptake, effectively prolonged drug circulation, and increased accumulation of drug in tumor sites. More attractively, PCH exhibited excellent therapeutic performance and better in vivo systemic safety. Conclusion: Overall, PCH not only utilized the tumor microenvironment to control drug release, improve drug pharmacokinetics, and passively target the drug to the tumor tissue, but also exerted a synergistic anticancer effect. The acid-responsive PCH has enormous potential as a novel anticancer therapeutic strategy.


Assuntos
Ácidos/química , Antineoplásicos/uso terapêutico , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/patologia , Nanopartículas/química , Estresse Oxidativo , Acroleína/análogos & derivados , Acroleína/química , Animais , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Camptotecina/farmacocinética , Camptotecina/farmacologia , Camptotecina/uso terapêutico , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Dextranos/química , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Retículo Endoplasmático/efeitos dos fármacos , Retículo Endoplasmático/metabolismo , Retículo Endoplasmático/ultraestrutura , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Feminino , Humanos , Concentração de Íons de Hidrogênio , Camundongos Endogâmicos BALB C , Camundongos Nus , Nanopartículas/ultraestrutura , Espectroscopia de Prótons por Ressonância Magnética , Ratos Sprague-Dawley , Espécies Reativas de Oxigênio/metabolismo
16.
Meat Sci ; 153: 66-74, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30913410

RESUMO

The aim of this study was to compare the effects of corn starch films containing Zataria multiflora essential oil (ZEO) and cinnamaldehyde (CIN) in conventional, nanoemulsion (NZEO) and fortified nanoemulsion (NZEOC) forms, on pH value, oxidative stability and sensory properties of ground beef patties during 20 days of storage at 4 ±â€¯1 °C. Results of mechanical evaluation indicated that all treated films exhibited lower tensile strength (P ≤ .05) and higher elongation at break (P ≥ .05) than control samples. Also, film containing NZEO showed the best results at the end of storage with the following scores: Peroxide value (3.70 meq/kg of lipid), thiobarbituric acid reactive substance (1.03 mg MDA/kg sample), carbonyl content (0.83 nmol/mg protein) and sensory analysis (overall acceptibility: 5.85). Furthermore, NZEOC had no positive effect on the antioxidant activity compared with NZEO+CIN. The results of the study can be applied to food packaging industry for particularly meat and meat products.


Assuntos
Acroleína/análogos & derivados , Lamiaceae/química , Produtos da Carne/análise , Amido/química , Acroleína/química , Animais , Antioxidantes/química , Bovinos , Embalagem de Alimentos/métodos , Humanos , Nanoestruturas/química , Óleos Voláteis/química , Paladar
17.
Appl Microbiol Biotechnol ; 103(8): 3521-3535, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30852658

RESUMO

At present, anti-virulence drugs are being considered as potential therapeutic alternatives and/or adjuvants to currently failing antibiotics. These drugs do not kill bacteria but inhibit virulence factors essential for establishing infection and pathogenesis through targeting non-essential metabolic pathways reducing the selective pressure to develop resistance. We investigated the effect of naturally isolated plant compounds on the repression of the quorum sensing (QS) system which is linked to virulence/pathogenicity in Pseudomonas aeruginosa. Our results show that trans-cinnamaldehyde (CA) and salicylic acid (SA) significantly inhibit expression of QS regulatory and virulence genes in P. aeruginosa PAO1 at sub-inhibitory levels without any bactericidal effect. CA effectively downregulated both the las and rhl QS systems with lasI and lasR levels inhibited by 13- and 7-fold respectively compared to 3- and 2-fold reductions with SA treatment, during the stationary growth phase. The QS inhibitors (QSI) also reduced the production of extracellular virulence factors with CA reducing protease, elastase and pyocyanin by 65%, 22% and 32%, respectively. The QSIs significantly reduced biofilm formation and concomitantly with repressed rhamnolipid gene expression, only trace amount of extracellular rhamnolipids were detected. The QSIs did not completely inhibit virulence factor expression and production but their administration significantly lowered the virulence phenotypes at both the transcriptional and extracellular levels. This study shows the significant inhibitory effect of natural plant-derived compounds on the repression of QS systems in P. aeruginosa.


Assuntos
Acroleína/análogos & derivados , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/genética , Percepção de Quorum/efeitos dos fármacos , Ácido Salicílico/farmacologia , Fatores de Virulência/genética , Acroleína/farmacologia , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Biofilmes/efeitos dos fármacos , Biofilmes/crescimento & desenvolvimento , Espaço Extracelular/metabolismo , Pseudomonas aeruginosa/crescimento & desenvolvimento , Pseudomonas aeruginosa/patogenicidade , Percepção de Quorum/genética , Virulência/efeitos dos fármacos , Fatores de Virulência/metabolismo
18.
Lett Appl Microbiol ; 68(6): 562-572, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30861569

RESUMO

Streptococcus suis is a major swine pathogen. Different strategies to reduce the antimicrobial resistance to conventional antimicrobials (AMBs) have been proposed, including the combined use with essential oils (EOs). The objective of this work was to evaluate the effectiveness of the combination of cinnamon, oregano, common thyme and red thyme EOs and their main components (cinnamaldehyde, carvacrol and thymol) with conventional AMBs (oxytetracycline, trimethoprim-sulfamethoxazole, gentamicin and penicillin) against field resistant S. suis strains. The checkerboard method was used to assess the interaction, by the fractional inhibitory concentration index (FICindex ) determination. All the AMBs showed synergistic (FICindex  ≤ 0·5) or additive (0·5 < FICindex  ≤ 1) effect with at least one of the four essential oils. In general, the combination of the AMBs with the EOs showed better results than combination the AMBs with the main components, although no antagonist effects were detected in any case. The results obtained would support the combined use of AMBs agents with EOs for the treatment of S. suis. SIGNIFICANCE AND IMPACT OF THE STUDY: Streptococcus suis is an important pig pathogen and a zoonosis. Control is based on antimicrobials; however, there is pressure to reduce the use of antimicrobials and new products or combination therapies are of considerable interest. We have evaluated the combined interaction of four essential oils or their main components with conventional antimicrobials against resistant S. suis strains. A positive interaction between gentamicin and oxytetracycline with cinnamon, oregano or thyme was observed, suggesting that a combination of conventional antimicrobials with EOs is a promising alternative for the control of S. suis infections.


Assuntos
Acroleína/análogos & derivados , Antibacterianos/farmacologia , Monoterpenos/farmacologia , Óleos Voláteis/farmacologia , Streptococcus suis/efeitos dos fármacos , Doenças dos Suínos/tratamento farmacológico , Timol/farmacologia , Acroleína/farmacologia , Animais , Cinnamomum zeylanicum/química , Farmacorresistência Bacteriana Múltipla , Testes de Sensibilidade Microbiana , Origanum/química , Streptococcus suis/crescimento & desenvolvimento , Suínos , Doenças dos Suínos/microbiologia , Thymus (Planta)/química
19.
J Neurooncol ; 143(1): 69-77, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30887242

RESUMO

INTRODUCTION: Glioblastoma (GBM) is the most common and aggressive human primary brain malignancy. The key properties of GBM, stemness and invasiveness, are known to be associated with a highly unfavorable prognosis. Notably, the process of epithelial-mesenchymal transition (EMT) is closely related to the progression of GBM. On the basis of reports that 2'-hydroxycinnamaldehyde (HCA) and its derivative, 2'-benzoyloxycinnamaldehyde (BCA), suppresses EMT in several human cancer cells, we sought to evaluate the therapeutic efficacy of HCA and BCA, alone and in combination with temozolomide (TMZ), on GBM tumorspheres (TSs). METHODS: Two human GBM TSs were treated with HCA, BCA, or TMZ. Therapeutic effects were evaluated by measuring ATP levels, neurosphere formation, 3D-invasion in collagen matrix, and viability. Protein expression profiles after drug treatment were evaluated by western blotting. In vivo anticancer efficacy of drugs was examined in a mouse orthotopic xenograft model. RESULTS: Combined treatment of GBM TSs with HCA or BCA and TMZ significantly reduced cell viability, stemness, and invasiveness. Expression levels of stemness-, invasiveness-, and mesenchymal transition-associated markers, Zeb1, N-cadherin, and ß-catenin, were also substantially decreased by the combined treatment. The combined treatment also reduced tumor growth in a mouse orthotopic xenograft model. CONCLUSION: Our findings suggest that HCA and BCA, combined with TMZ, are potential therapeutic agents in the treatment of GBM.


Assuntos
Antineoplásicos/farmacologia , Cinamatos/farmacologia , Glioblastoma/tratamento farmacológico , Invasividade Neoplásica , Células-Tronco Neoplásicas/efeitos dos fármacos , Temozolomida/farmacologia , Acroleína/análogos & derivados , Acroleína/farmacologia , Trifosfato de Adenosina/metabolismo , Animais , Benzoatos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Quimioterapia Combinada , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Glioblastoma/patologia , Glioblastoma/fisiopatologia , Humanos , Camundongos Nus , Invasividade Neoplásica/patologia , Invasividade Neoplásica/fisiopatologia , Transplante de Neoplasias , Células-Tronco Neoplásicas/patologia , Células-Tronco Neoplásicas/fisiologia , Tecidos Suporte
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