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Poor bioavailability, solubility, and absorption of berberine (Ber) limit its widespread application. Here, we formulated novel chitosan/pectin nanoparticles (NPs) loaded with Ber to address delivery problems and promote the anticancer properties of Ber in AGS gastric cancer cells. The ionic gelification method was used to synthesize NPs-Ber. Physicochemical characterization of NPs-Ber was performed using FE-SEM, DLS, PDI, ζ potential, and FTIR. The cytotoxic effects of NPs-Ber on AGS cells were evaluated using the MTT assay. Apoptosis and cell cycle arrest were examined by flow cytometry. The gene expression levels of miR-185-5p, KLF7, caspase-3, and DNMTs were determined using RT-qPCR. In addition, the 5-methylcytosine level in the genomic DNA was quantified using ELISA. FE-SEM images revealed a denser and more packed matrix for NPs-Ber, and FTIR analysis confirmed the formation of NPs-Ber. The size (550.39 nm), PDI (0.134), and ζ potential (-16.52 mV) confirmed the stability of the prepared NPs-Ber. NPs-Ber showed a continuous release pattern following the Korsmeyer-Peppas model such that 81.36 % of Ber was released from the formulation after 240 min. Compared to NPs and free Ber, NPs-Ber was found to possess higher anticancer activity in AGS cells. This result was indicated by the viability test and further clarified by augmented apoptosis and cell cycle arrest at the G0/G1 phase. The IC50 value of NP-Ber against AGS cells was significantly lower than those of free Ber and NPs. Interestingly, our results showed that NPs-Ber considerably changed the expression levels of miR-185-5p, KLF7, caspase-3, and DNMTs (DNMT1, 3A, and 3B) compared with unloaded NPs and free Ber. Additionally, 5-methylated cytosine (5-mC) levels in cells treated with NPs-Ber were significantly higher than those in cells treated with unloaded NPs or free Ber. In summary, the present study demonstrated that Ber encapsulation in NPs enhances its cytotoxic and epigenetic effects on AGS cells, suggesting the promising potential of NPs-Ber in GC therapy.
Assuntos
Antineoplásicos , Berberina , Quitosana , MicroRNAs , Nanopartículas , Neoplasias Gástricas , Humanos , Neoplasias Gástricas/tratamento farmacológico , Neoplasias Gástricas/genética , Quitosana/química , Berberina/farmacologia , Caspase 3 , Metilação de DNA , Pectinas , Nanopartículas/química , Antineoplásicos/farmacologia , Epigênese Genética , MicroRNAs/genética , Fatores de Transcrição Kruppel-LikeRESUMO
Echinococcosis, or hydatidosis, is one of the most important zoonotic diseases, which is initiated by the larval stage in the clasts of Echinococcus granulosus. For the treatment of hydatidosis, surgery is still the preferred method and the first line of treatment for symptomatic patients. Unfortunately, most of the scolicidal agents that are injected inside cysts during hydatid cyst surgery have side effects, including leaking out of the cyst and adverse effects on the living tissue of the host, such as necrosis of liver cells, which limits their use. This work was carried out to study the lethal effect of green synthesized gold nanoparticles (Au-NCs) against hydatid cyst protoscoleces. Au-NCs were green synthesized using the Saturja khuzestanica extract. Au-NCs were characterized by UV-visible absorbance assay, electron microscopy analysis, X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy. Scolicidal properties of Au-NCs (1-5 mg/mL) were studied against protoscoleces for 10-60 min. The effect of Au-NCs on the expression level of the caspase-3 gene as well as the ultrastructural examination was studied by real-time PCR and scanning electron microscopy (SEM). The cytotoxicity of Au-NCs on hepatocellular carcinoma (HepG2) and normal embryonic kidney (HEK293) cell lines was also studied by the cell viability assay. The obtained Au-NCs are cubes and have an average size of 20-30 nm. The highest scolicidal efficacy was observed at 5 mg/mL with 100% mortality after 20 min of treatment for hydatid cyst protoscoleces. In ex vivo, Au-NCs required more incubation time, indicating more protoscolicidal effects. Au-NCs markedly upregulated the gene level of caspase-3 in protoscoleces; whereas they changed the ultra-structure of protoscoleces by weakening and disintegrating the cell wall, wrinkles, and protrusions due to the formation of blebs. We showed the effective in vitro and ex vivo scolicidal effects of Au-NCs against hydatid cyst protoscoleces by provoking the apoptosis process of caspase-3 activation and changing the ultrastructure of protoscoleces with no significant cytotoxicity against human normal cells. However, additional studies should be conducted to determine the possible harmful side effects and accurate efficacy.
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Echinococcosis is a zoonotic disease caused by larval stages of the Echinococcus genus (metastasis). In this study, salicylate-coated Zinc oxide nanoparticles (SA-ZnO-NPs) were fabricated and characterized by SEM, FTIR and XRD analytical techniques. After that, different doses of SA-ZnO-NPs, SA and ZnO-NPs were taken to assess scolicidal potency. Scanning electron microscopy (SEM) micrographs were also used to evaluate the morphological deformities of treated protoscoleces. Furthermore, Caspase-3&7 inductions were examined in protoscoleces cysts treated with all formulations. Based on SEM and DLS analyses, the size of SA-ZnO-NPs was between 30 and 40 nm, with a spherical shape. The FTIR spectrum verified the presence of SA functional groups on the ZnO coating. At 20 min, SA-ZnO-NPs at 2000 µg/ml exhibited the greatest activity on protoscolices with 100% mortality, followed by ZnO-NPs at 1500 µg/ml at 10 min and SA alone at 2000 µg/ml at 30 min. The activation of Caspase-3&7 apoptotic enzyme was determined for 2000 µg/ml of SA-ZnO-NPs, ZnO-NPs and SA to be 16.4, 31.4, and 35.7%, respectively. The SEM image revealed apoptogenic alterations and the induction of tegument surface wrinkles, as well as abnormalities in rostellum protoscolices. According to the current study, SA-ZnO-NPs have a high mortality rate against hydatid cyst protoscolices. As a result, further studies on the qualitative assessment of these nanoformulations in vivo and preclinical animal trials seem to be required. Furthermore, the adoption of nano-drugs potentially offers alternative therapeutic approaches to combat hydatid cysts.
Assuntos
Equinococose , Echinococcus granulosus , Echinococcus , Nanopartículas Metálicas , Nanopartículas , Óxido de Zinco , Animais , Caspase 3 , Zinco , Óxido de Zinco/farmacologia , Nanopartículas Metálicas/uso terapêutico , Salicilatos/farmacologia , Salicilatos/uso terapêutico , Equinococose/tratamento farmacológicoRESUMO
The harmful compounds in various sources of smoke threaten human health. So far, many studies have investigated the effects of compounds of smoke on transcriptome changes in different human tissues. However, no study has been conducted on the effects of these compounds on transcriptome changes in different human tissues simultaneously. Hence, the present study was conducted to identify smoke-related genes (SRGs) and their response mechanisms to smoke in various human cells and tissues using systems biology based methods. A total of 6,484 SRGs were identified in the studied tissues, among which 4,095 SRGs were up-regulated and 2,389 SRGs were down-regulated. Totally, 459 SRGs were smoke-related transcription factors (SRTFs). Gene regulatory network analysis showed that the studied cells and tissues have different gene regulation and responses to compounds of smoke. The comparison of different tissues revealed no common SRG among the all studied tissues. However, the CYP1B1 gene was common among seven cells and tissues, and had the same expression trend. Network analysis showed that the CYP1B1 is a hub gene among SRGs in various cells and tissues. To the best of our knowledge, for the first time, our results showed that compounds of smoke induce and increase the expression of CYP1B1 key gene in all target and non-target tissues of human. Moreover, despite the specific characteristics of CYP1B1 gene and its identical expression trend in target and non-target tissues, it can be used as a biomarker for diagnosis and prognosis.
Assuntos
Citocromo P-450 CYP1B1/genética , Regulação da Expressão Gênica , Estudo de Associação Genômica Ampla , Fumaça/efeitos adversos , Transcriptoma , Biomarcadores , Redes Reguladoras de Genes , Estudo de Associação Genômica Ampla/métodos , Humanos , Prognóstico , Biologia de Sistemas/métodos , Distribuição TecidualRESUMO
BACKGROUND: Paraquat poisoning leads to lung injury and pulmonary fibrosis. The effect of paraquat encapsulation by previously described Pectin/Chitosan/Tripolyphosphate nanoparticles on its pulmonary toxicity was investigated in present study in a rat model of poison inhalation. MATERIAL AND METHOD: The rats inhaled nebulized different formulation of paraquat (n = 5) for 30 min in various experimental groups. Lung injury and fibrosis scores, Lung tissue enzymatic activities, apoptosis markers were determined compared among groups. RESULTS: Encapsulation of paraquat significantly rescued both lung injury and fibrosis scores. Lung MDA level was reduced by encapsulation. Paraquat poisoning led to lung tissue apoptosis as was evidenced by higher Caspase-3 and Bax/Bcl2 expressions in rats subjected to paraquat inhalation instead of normal saline or free nanoparticles. Again, nanoencapsulation reduced these apoptosis markers significantly. Alpha-SMA expression was also reduced by encapsulation. Nanoparticles per se have no or little toxicity as was evidenced by inflammatory and apoptotic markers and histological scores. CONCLUSION: In a rat model of inhalation toxicity of paraquat, loading of this herbicide on PEC/CS/TPP nanoparticles reduced acute lung injury and fibrosis. The encapsulation also led to lower apoptosis, oxidative stress and alpha-SMA expression in the lung tissue.
Assuntos
Quitosana , Paraquat , Animais , Apoptose , Fibrose , Pulmão/patologia , Paraquat/toxicidade , Pectinas , Polifosfatos , RatosRESUMO
Satureja khuzistanica jamzad (SKJ), which is a member of Lamiaceae, has various proven effects such as antispasmodic and anti-inflammatory, anti-diabetic, antioxidant, and antifungal properties. However, the use of essential oil of plants is limited due to their inherent instability in the environment. Encapsulation with nanoparticles in the nanogel forms is one of their stabilization methods. The aim of this study was to synthesize nano-gel based on chitosan (CS) and extracts of SKJ essential oil, and to evaluate the antibacterial and anticancer activities. SKJ essential oil was extracted using water distillation method. Then, it was loaded on CS particles using two-step process as following: droplets formation and freezing. The Dynamic Light Scattering (DLS), Fourier transform infrared spectroscopy (FTIR), Scanning electron microscopy (SEM), and Zeta potential determination were used to evaluate the physical and chemical properties of CS-SKJ nanogel, which its result was acceptable. After confirmation of the loaded essential oil rate and releasing amount, the antibacterial effects were evaluated on five Gram-positive bacteria and five Gram-negative bacteria using microbroth dilution method. The encapsulation efficiency, size, polydispersity index, and zeta potential of nanoparticles were characterized were 30.74%, 571.00 nm, 0.451 and -67.2 mV, respectively. The results were significant not only on Gram-positive bacteria, but also on Gram-negative bacteria. The MIC range was between 7.8 and 500 µg/ml. The CS-SKJ nanogel has acceptable anticancer activities on KB and A549 tumor cell lines. the IC50 range was between 5.6 and 6.71 µg/ml. The results indicate that both CS particles and SKJ alone, and CS-SKJ nanogel could be considered as the outlook to produce new antimicrobial and anticancer drugs.
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Antibacterianos/administração & dosagem , Antineoplásicos/administração & dosagem , Quitosana/química , Óleos Voláteis/administração & dosagem , Satureja/química , Células A549 , Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Portadores de Fármacos/química , Humanos , Nanopartículas/química , Neoplasias/tratamento farmacológico , Óleos Voláteis/química , Óleos Voláteis/farmacologiaRESUMO
BACKGROUND: Myrtus communis (M. communis) is a wild aromatic plant used for traditional herbal medicine that can be demonstrated in insecticidal, antioxidant, anti-inflammatory, and antimicrobial activity of its essential oils (MCEO). AIM: The present study aimed to evaluate the prophylactic effects of M. communis essential oil (MCEO) against chronic toxoplasmosis induced by the Tehran strain of Toxoplasma gondii in mice. METHODS: Gas chromatography/mass spectrometry (GC/MS) analysis was performed to determine the chemical composition of MCEO. Mice were then orally administrated with MCEO at the doses of 100, 200, and 300 mg/kg/day and also atovaquone 100 mg/kg for 21 days. On the 15th day, the mice were infected with the intraperitoneal inoculation of 20-25 tissue cysts from the Tehran strain of T. gondii. The mean numbers of brain tissue cysts and the mRNA levels of IL-12 and IFN-γ in mice of each tested group were measured. RESULTS: By GC/MS, the major constituents were α-pinene (24.7%), 1,8-cineole (19.6%), and linalool (12.6%), respectively. The results demonstrated that the mean number of T. gondii tissue cysts in experimental groups Ex1 (p < 0.05), Ex2 (p < 0.001) and Ex3 (p < 0.001) was meaningfully reduced in a dose-dependent manner compared with the control group (C2). The mean diameter of tissue cyst was significantly reduced in mice of the experimental groups Ex2 (p < 0.01) and Ex3 (p < 0.001). The results demonstrated that although the mRNA levels of IFN-γ and IL-12 were elevated in all mice of experimental groups, a significant increase (p < 0.001) was observed in tested groups of Ex2 and Ex3 when compared with control groups. CONCLUSION: The findings of the present study demonstrated the potent prophylactic effects of MCEO especially in the doses 200 and 300 mg/kg in mice infected with T. gondii. Although the exceptional anti-Toxoplasma effects of MCEO and other possessions, such as improved innate immunity and low toxicity are positive topics, there is, however, a need for more proof from investigations in this field.
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Antiparasitários/farmacologia , Imunidade Inata/efeitos dos fármacos , Myrtus/química , Óleos Voláteis/farmacologia , Toxoplasmose/imunologia , Animais , Antiparasitários/uso terapêutico , Camundongos , Óleos Voláteis/uso terapêutico , Toxoplasma/efeitos dos fármacos , Toxoplasma/fisiologia , Toxoplasmose/tratamento farmacológicoRESUMO
BACKGROUND: Previous studies have reported that quercetin (Q) has a potential antibacterial and anticancer activity. However, its application is limited by many important factors including high hydrophobicity and low absorption. METHODOLOGY: In the current study, we synthesized and characterized (Patent) a novel chitosan-based quercetin nanohydrogel (ChiNH/Q). Encapsulation efficiency was confirmed by UV/VIS spectrophotometer. Physicochemical characterization of ChiNH/Q was assessed by PDI, DLS, SEM, FTIR, and XRD. The toxicity of the ChiNH/Q against five strains of the pathogen and HepG2 cells was examined. Moreover, the quantification of ChiNH/Q on genomic global DNA methylation and expression of DNMTs (DNMT1/3A/3B) in HepG2 cancer cells were evaluated by ELISA and real-time PCR, respectively. RESULTS: Under the SEM-based images, the hydrodynamic size of the ChiNH/Q was 743.6 nm. The changes in the PDI were 0.507, and zeta potential was obtained as 12.1 mV for ChiNH/Q. The FTIR peak of ChiNH/Q showed the peak at 627 cm-1 corresponded to tensile vibrational of NH2-groups related to Q, and it is the indication of Q loading in the formulation. Moreover, XRD data have detected the encapsulation of ChiNH/Q. The ChiNH/Q showed a potent antimicrobial inhibitory effect and exerted cytotoxic effects against HepG2 cancer cells with IC50 values of 100 µg/mL. Moreover, our data have shown that ChiNH/Q effectively reduced (65%) the average expression level of all the three DNMTs (p<0.05) and significantly increased (1.01%) the 5-methylated cytosine (5-mC) levels in HepG2 cells. CONCLUSION: Our results showed for the first time the bioavailability and potentiality of ChiNH/Q as a potent antimicrobial and anticancer agent against cancer cells. Our result provided evidence that ChiNH/Q could effectively reduce cellular DNMT expression levels and increase genomic global DNA methylation in HepG2 cancer cells. Our results suggest a potential clinical application of nanoparticles as antimicrobial and anticancer agents in combination cancer therapy.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Epigênese Genética/efeitos dos fármacos , Hidrogéis/química , Nanoestruturas/química , Quercetina/farmacologia , Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacocinética , Quitosana/química , DNA (Citosina-5-)-Metiltransferase 1/metabolismo , DNA (Citosina-5-)-Metiltransferases/metabolismo , DNA Metiltransferase 3A , Células Hep G2 , Humanos , Hidrogéis/administração & dosagem , Interações Hidrofóbicas e Hidrofílicas , Testes de Sensibilidade Microbiana , Nanoestruturas/administração & dosagem , Quercetina/administração & dosagem , Quercetina/química , Quercetina/farmacocinética , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
Pesticides exposure can have harmful effects on human health. The liver is the most common organ of pesticides toxicity due to its major metabolic activity. The molecular mechanism of pesticides effect is complex and is controlled by gene regulatory networks. All components of regulatory networks are controlled by transcription factors and other regulatory elements. Therefore, identification of key regulators through system biology approaches and high-throughput techniques can help to provide comprehensive insights into molecular mechanisms of the pesticide effect. In the current study, a microarray data-set was used to potentially identify molecular mechanisms that regulate gene expression profile of rat hepatocyte cell lines in response to pesticides exposure. Results showed that the number of differentially expressed genes (DEGs) and differentially expressed transcription factors (DE-TFs) were dramatically different among pesticides tested. Results also revealed 205 common DEGs and 11 DE-TFs among pesticides tested. Additionally, we found that six DE-TFs (CREB1, CTNNB1, PPARG, SP1, SRF and STAT3) had the highest number of interactions with other DEGs and acted as the key regulatory genes. The results of this study revealed regulator genes that have the key functions in response to pesticides toxicity in rat liver, which can provide the basis for future studies. Furthermore, these regulatory genes can be used as toxicity biomarkers to improve diagnosis and prognosis.
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Biologia Computacional , Redes Reguladoras de Genes/efeitos dos fármacos , Genes Reguladores/genética , Praguicidas/toxicidade , Fatores de Transcrição/genética , Transcriptoma/efeitos dos fármacos , Animais , Linhagem Celular , Perfilação da Expressão Gênica , Hepatócitos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Especificidade de Órgãos , RatosRESUMO
Although many techniques have been devoted to promote therapeutic purposes of drug carrier systems, however, there are still many challenges in this area. Here, we designed co-loaded delivery systems, composed of curcumin loaded cyclodextrin-graphene oxide core (Cur@CD-GO) and gallic acid loaded chitosan shell nanofibers (Cur-Ga NF), which can promote the therapeutic efficiency of drugs. The synthesized nanofibres were fabricated by electrospinning technique with the coaxial system. Results showed that co-loaded delivery systems (Cur-Ga NF) provide better performance over single drug-loaded NFs (Cur@CD-GO). It was demonstrated that the nanofibers were successfully prepared, and the drugs in the core and sell of nanofibers were released in a controlled and sustained manner. The produced Cur-Ga NF, providing improved anti-cancer activity, antimicrobial activity, antioxidant activity and anti-inflammatory outcome as compared to single drug-loaded NFs. Our investigations showed that such co-delivery fiber systems could be employed as a promising nanocarrier for therapeutic applications.
Assuntos
Quitosana/química , Ciclodextrinas/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos , Grafite/química , Nanofibras/química , Anti-Infecciosos , Técnicas de Química Sintética , Curcumina/administração & dosagem , Ciclodextrinas/síntese química , Liberação Controlada de Fármacos , Ácido Gálico/química , Humanos , Estrutura Molecular , Nanofibras/ultraestrutura , Análise EspectralRESUMO
As a potent herbicide capable of contaminating water and soil environments, paraquat, which is still widely used worldwide, is toxic to mammals, algae, aquatic animals, etc. Paraquat was loaded on novel nanoparticles composed of pectin, chitosan, and sodium tripolyphosphate (PEC/CS/TPP). The size, polydispersity index, and ζ potential of nanoparticles were characterized. Further assessments were carried out by SEM, AFM, FT-IR, and DSC. The encapsulation was highly efficient, and there was a delayed release pattern of paraquat. The encapsulated herbicide was less toxic to alveolar and mouth cell lines. Moreover, the mutagenicity of the formulation was significantly lower than those of pure or commercial forms of paraquat in a Salmonella typhimurium strain model. The soil sorption of paraquat and the deep soil penetration of the nanoparticle-associated herbicide were also decreased. The herbicidal activity of paraquat for maize or mustard was not only preserved but also enhanced after encapsulation. It was concluded that paraquat encapsulation with PEC/CS/TPP nanoparticles is highly efficient and the formulation has significant herbicide activity. It is less toxic to human environment and cells, as was evidenced by less soil sorption, cytotoxicity, and mutagenicity. Hence, paraquat-loaded PEC/CS/TPP nanoparticles have potential advantages for future use in agriculture.
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Quitosana/química , Composição de Medicamentos/métodos , Herbicidas/química , Mutagênicos/química , Nanopartículas/química , Paraquat/química , Pectinas/química , Polifosfatos/química , Adsorção , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Portadores de Fármacos/química , Herbicidas/farmacologia , Herbicidas/toxicidade , Humanos , Cinética , Mostardeira/efeitos dos fármacos , Mostardeira/crescimento & desenvolvimento , Mutagênicos/farmacologia , Mutagênicos/toxicidade , Paraquat/farmacologia , Paraquat/toxicidade , Tamanho da Partícula , Solo/química , Poluentes do Solo/química , Poluentes do Solo/farmacologia , Poluentes do Solo/toxicidade , Zea mays/efeitos dos fármacos , Zea mays/crescimento & desenvolvimentoRESUMO
Diabetes mellitus is associated with the development of neuronal tissue damage in different central and peripheral nervous system regions. A common complication of diabetes is painful diabetic peripheral neuropathy. We have explored the antihyperalgesic and neuroprotective properties of Rosmarinus officinalis L. extract (RE) in a rat model of streptozotocin (STZ)-induced diabetes. The nociceptive threshold and motor coordination of these diabetic rats was assessed using the tail-flick and rotarod treadmill tests, respectively. Activated caspase-3 and the Bax:Bcl-2 ratio, both biochemical indicators of apoptosis, were assessed in the dorsal half of the lumbar spinal cord tissue by western blotting. Treatment of the diabetic rats with RE improved hyperglycemia, hyperalgesia and motor deficit, suppressed caspase-3 activation and reduced the Bax:Bcl-2 ratio, suggesting that the RE has antihyperalgesic and neuroprotective effects in this rat model of STZ-induced diabetes. Cellular mechanisms underlying the observed effects may, at least partially, be related to the inhibition of neuronal apoptosis.
Assuntos
Analgésicos/farmacologia , Neuropatias Diabéticas/complicações , Neuroproteção/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Dor/tratamento farmacológico , Extratos Vegetais/farmacologia , Rosmarinus/química , Animais , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/metabolismo , Neuropatias Diabéticas/metabolismo , Hiperalgesia/tratamento farmacológico , Hiperalgesia/metabolismo , Hiperglicemia/tratamento farmacológico , Hiperglicemia/metabolismo , Masculino , Dor/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Ratos , Ratos Wistar , Medula Espinal/efeitos dos fármacos , Medula Espinal/metabolismo , Proteína X Associada a bcl-2/metabolismoRESUMO
This study aims to evaluate the in vitro and in vivo antileishmanial activities of Pistacia vera essential oil and compare their efficacy with a reference drug, meglumine antimoniate (Glucantime®). This essential oil (0-100 µg/mL) was evaluated in vitro against the intracellular amastigote forms of Leishmania tropica (MHOM/IR/2002/Mash2) and then tested on cutaneous leishmaniasis of male BALB/c mice by Leishmania major (MRHO/IR/75/ER). In the in vitro assay, it could be observed that P. vera essential oil significantly (p < 0.05) inhibited the growth rate of amastigote forms (IC50 of 21.3 ± 2.1 µg/mL) in a dose-dependent response compared with the control drug. Meglumine antimoniate also demonstrated antileishmanial effects with an IC50 value of 44.6 ± 2.5 µg/mL for this clinical stage. In the in vivo assay, the results indicated that 30 mg/mL of the essential oil had potent suppression effects on cutaneous leishmaniasis in BALB/c mice (87.5% recovery), while 10 and 20 mg/mL of the essential oil represented the suppression effects as weak to intermediate. The mean diameter of the lesions decreased about 0.11 and 0.27 cm after the treatment of the subgroups with the essential oil concentrations of 10 and 20 mg/mL, respectively. In contrast, in the subgroup treated with the essential oil concentration of 30 mg/mL, the mean diameter of the lesions decreased about 0.56 cm. In the control subgroups, the mean diameter of the lesions increased to 1.01 cm. The main components of P. vera essential oil were limonene (26.21%), α-pinene (18.07%), and α-thujene (9.31%). It was also found that P. vera essential oil had no significant cytotoxic effect on J774 cells. The present study found that P. vera essential oil showed considerable in vitro and in vivo effectiveness against L. tropica and L. major compared to the reference drug. These findings also provided the scientific evidence that natural plants could be used in traditional medicine for the prevention and treatment of cutaneous leishmaniasis.
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Antiprotozoários/uso terapêutico , Leishmania tropica/efeitos dos fármacos , Leishmaniose Cutânea/tratamento farmacológico , Pistacia/química , Animais , Masculino , Meglumina/uso terapêutico , Antimoniato de Meglumina , Camundongos , Camundongos Endogâmicos BALB C , Óleos Voláteis/química , Compostos Organometálicos/uso terapêuticoRESUMO
Current scolicidal agents, which have been used for inactivation of protoscoleces during hydatid cyst surgery are associated with adverse side effects. This study aims to evaluate the in vitro scolicidal effects of Nectaroscordum tripedale L. leave extract against protoscoleces of hydatid cysts and its acute toxicity in mice model. Various concentrations of the extract (12.5-100 mg/mL) were used for 5 to 30 min. Viability of protoscoleces was confirmed using eosin exclusion test (0.1% eosin staining). In addition, the acute toxicity of N. tripedale extract was determined for 2 days in mice model. The results showed that the N. tripedale extract at the concentration of 100 mg/mL after 5 min of exposure killed 100% protoscoleces. Similarly, the mean of mortality rate of protoscoleces after 10 min of exposure to concentration of 50 mg/mL was 100%. The LD50 values of intraperitoneal injection of the N. tripedale extract was 3.36 g/kg body wt. and the maximum nonfatal doses were 2.98 g/kg body wt. The results showed the potential of N. tripedale extract as a natural source for the production of new scolicidal agent for use in hydatid cyst surgery.
Assuntos
Allium/química , Antiparasitários/farmacologia , Equinococose/tratamento farmacológico , Echinococcus/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Antiparasitários/isolamento & purificação , Antiparasitários/toxicidade , Relação Dose-Resposta a Droga , Equinococose/parasitologia , Echinococcus/crescimento & desenvolvimento , Dose Letal Mediana , Masculino , Camundongos , Fitoterapia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/química , Plantas MedicinaisRESUMO
A green synthetic approach by using oak fruit hull (Jaft) extract for preparation of silver nanoparticles (AgNPs) was developed and optimized. Parameters affecting the synthesis of AgNPs, such as temperature, extract pH, and concentration of extract (ratio of plant sample to extraction solvent), were investigated and optimized. Optimum conditions for the synthesis of silver nanoparticles are as follows: Ag(+) concentration, 1 mM; extract concentration, 40 g/L (4% w/v); pH = 9 and temperature, 45°C. Biosynthesized silver nanoparticles were characterized using UV-visible absorption spectroscopy (UV-Vis), Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), dynamic light scattering (DLS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). TEM and DLS analyses have shown the synthesized AgNPs were predominantly spherical in shape with an average size of 40 nm. The cytotoxic activity of the synthesized AgNPs and Jaft extract containing AgNPs against human breast cancer cell (MCF-7) was investigated and the half maximal inhibitory concentrations (IC50) were found to be 50 and 0.04 µg/mL at 24 h incubation, respectively. This eco-friendly and cost-effective synthesis method can be potentially used for large-scale production of silver nanoparticles.
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Matrix solid-phase dispersion (MSPD) method coupled with gas chromatography flame ionisation detector as a quick and easy extraction technique has been developed to extract carvacrol from plants and herbal medicines. Influence of important parameters on the MSPD method efficiency, such as the sorbent material, the ratio of sample to sorbent material, elution solvent and volume of the elution solvent has been evaluated and optimised. Carvacrol was successfully extracted by diatomaceous earth as sorbent with 350 µL of dichloromethane as elution solvent. The calibration curve showed good linearity (r(2) = 0.9965) and precision (RSD < 8.16%) in the concentration range of 0.5-100 µg mL(-1) for carvacrol. The limit of detection and limit of quantification were 0.1 and 0.5 µg mL(-1), respectively. The recoveries were in the range of 74.4-80.5% with relative standard deviation (RSD) values ranging from 8.4% to 9.8%. The reported MSPD extraction method revealed to be simpler and faster than conventional methods used to quantify carvacrol from plants and herbal medicines.
Assuntos
Ionização de Chama/métodos , Monoterpenos/análise , Preparações de Plantas/química , Plantas Medicinais/química , Cimenos , SolventesRESUMO
OBJECTIVE: To determine the chemical composition, antioxidant activity and antibacterial properties of essential oils of the aerial parts of Salvia sclareoides (S. sclareoides). METHODS: The essential oil of the areal parts of S. sclareoides was obtained by using hydrodistillation method and the composition of the volatile components analyzed by gas chromatography method coupled with mass spectrometry detector. The antimicrobial capacity of the essential oil of S. sclareoides was investigated by microdilution technique. The antioxidant activities were determined employing inhibition of 2,2-diphenyl-1-picrylhydrazyl hydrate radical method. RESULTS: Mass spectra were searched against mass spectrometry databases and sixty components were recognized. Non-terpenoids (41.6%) and sesquiterpenes (39.7%) were determined as the main components of the essential oil. The main identified components were, linalool (27.6%), trans-caryophyllene (16.6%), beta.-trans-ocimene (11.831%), germacrene-D (10%), bicyclogermacrene (3.3%) and caryophyllene oxide (2.8%). Two monoterpens (13.2%) and three oxygenated sesquiterpenes (5.5%) were also obtained from the essential oil of the S. sclareoides CONCLUSIONS: Results indicated that essential oil of S. sclareoides includes rather higher proportions of non-terpenoid and sesquiterpenes compounds with good antioxidant and antibacterial properties.