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1.
Ultrason Sonochem ; 111: 107093, 2024 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-39395223

RESUMO

Homogenization-circulating ultrasound in combination with an aqueous enzymatic pretreatment microwave-assisted extraction (HCUEPM) technique was successfully applied to extract kernel oil and essential oil from Litsea cubeba fruits. After screening the types and concentrations of enzymes, a 3 % pectinase aqueous solution was chosen. The Plackett-Burman design was used to screen eight parameters that might affect the yield of kernel oil and essential oil to identify significant variables. The best conditions were then predicted by further optimizing statistically significant factors via the Box-Behnken design. The optimal conditions were as follows: stirring speed of 1000 r/min, environmental pH of 5, homogenization time of 4 min, duty cycle of 20 %, ultrasound irradiation power of 400 W, incubation temperature of 52.78 °C, liquid-solid ratio of 9.31 mL/g, and incubation time of 2.53 h. Three parallel experiments were conducted under these conditions, yielding actual kernel oil at 240.56 ± 11.07 mL/kg DW and essential oil at 64.89 ± 3.1 mL/kg DW, which are close to the theoretical values. Compared with the HCUEPM method, the homogenization-microwave-assisted hydrodistillation (HMHD) method yielded 65.63 ± 3.2 mL/kg DW of essential oil but could not extract kernel oil. These findings demonstrate that the HCUEPM used in this study can efficiently extract a significant amount of kernel oil and essential oil from L. cubeba fruits in a short period of time. GC-MS analysis of the kernel oil and essential oil extracted via different methods revealed no significant differences in composition. The main components of the essential oil were D-limonene, trans-citral, cis-citral, and citronellal. The main components of the kernel oil were C10 and C12 medium-chain fatty acids, laying the foundation for the potential application of L. cubeba kernel oil and essential oil in the field of human health.

2.
J Ultrasound Med ; 42(7): 1587-1594, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36637120

RESUMO

OBJECTIVES: To analyze the risk factors of sulfur hexafluoride microbubble contrast agent intravasation during hysterosalpingo-contrast sonography (HyCoSy), and to explore a simple prediction model by the obvious clinical history. METHODS: This was a retrospective study included 299 infertility women who had undergone HyCoSy examination from July 1, 2018 to June 31, 2019. The factors were recorded, including age, endometrial thickness, balloon length, infertility type, history of intrauterine surgery, history of pelvic surgery, and tubal patency. The method of multivariate logistic regression analysis was adopted to analyze the risk factors affecting the contrast agent intravasation, and the receiver operating characteristic curves were plotted to test their efficacy. RESULTS: Secondary infertility, a history of intrauterine surgery, thin endometrial thickness, and tubal obstruction were all risk factors of the occurrence of intravasation (P < .05). And the area under the receiver operating characteristic curves of the multifactor-combined prediction model of the intravasation was significantly larger than that of single-factor. CONCLUSIONS: Sonographers and gynecologists should be familiar with the risk factors of intravasation and select the appropriate timing of HyCoSy toward reducing the occurrence of intravasation and other complications after thoroughly explaining and communicating with the patients.


Assuntos
Meios de Contraste , Infertilidade Feminina , Humanos , Feminino , Meios de Contraste/efeitos adversos , Hexafluoreto de Enxofre , Tubas Uterinas/diagnóstico por imagem , Histerossalpingografia/métodos , Estudos Retrospectivos , Microbolhas , Testes de Obstrução das Tubas Uterinas/métodos , Ultrassonografia/métodos , Fatores de Risco , Infertilidade Feminina/diagnóstico por imagem , Infertilidade Feminina/etiologia
3.
Mol Med Rep ; 26(5)2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36169171

RESUMO

Following the publication of this paper, it was drawn to the Editors' attention by a concerned reader that certain of the cell invasion assay data shown in Figs. 2C and 4C were strikingly similar to data appearing in different form in other articles by different authors. Owing to the fact that the contentious data in the above article had already been published elsewhere, or were already under consideration for publication, prior to its submission to Molecular Medicine Reports, the Editor has decided that this paper should be retracted from the Journal. The authors were asked for an explanation to account for these concerns, but the Editorial Office did not receive a reply. The Editor apologizes to the readership for any inconvenience caused. [Molecular Medicine Reports 18: 1878­1884, 2018; DOI: 10.3892/mmr.2018.9090].

4.
J Biomater Appl ; 37(2): 259-274, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35533369

RESUMO

Amphiphilic polymer micellar carriers are the most commonly used nanocarriers for oral delivery of hydrophobic drugs because their hydrophilic shell can avoid the recognition of the reticuloendothelial system (RES), has excellent drug-carrying capacity, and protect the drug from inactivation in the gastrointestinal fluid. The polymer micelle shell can enter cancer cells by endocytosis, and autophagy in cells, degradation by lysosomal pathway, so as to release drugs, prolong the circulation time of drugs in vivo, and then achieve the effect of drug sustained release. In this study, the glutathione-responsive PLGA-ss-PEG loaded paclitaxel (PTX) micelles (PLGA-ss-PEG-PTX) were developed for anticancer therapy. With its long-term circulation and EPR (enhanced permeability and retention) effect, and the micelle had disulfide bond, which could be used as the recognition group of tumor microenvironment, so that the PLGA-ss-PEG-PTX could specifically accumulate at the tumor site, so as to produce better anti-tumor effect. The PLGA-ss-PEG-PTX was formulated by the emulsification method in this study. The drug loading was about 21.54%, the entrapment efficiency was about 94.2%, and the particle size range was about 90 nm with narrow particle size distribution. Cytotoxicity and embryonic toxicity experiments were carried out using mouse lung cancer cells (LLC) and zebrafish fertilized eggs. It was proved that the low concentration of blank micelles had little cytotoxicity, but high concentration of blank micelles had adverse effects on zebrafish embryonic development, resulting in embryonic malformation. The uptake of drugs by cancer cells was studied by a high connotation cell imaging analysis system. The experiments showed that the drug molecules encapsulated in micelles could achieve higher uptake by cells compared with free drug molecules. In addition, in the in vivo evaluation experiment of drugs, the PLGA-ss-PEG-PTX could significantly enhance the therapeutic effect of the PTX, improve its water solubility, and improve its oral bioavailability.


Assuntos
Micelas , Peixe-Zebra , Animais , Linhagem Celular Tumoral , Portadores de Fármacos/química , Camundongos , Paclitaxel/farmacologia , Paclitaxel/uso terapêutico , Polietilenoglicóis/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico
5.
Nanomedicine (Lond) ; 17(22): 1627-1648, 2022 09.
Artigo em Inglês | MEDLINE | ID: mdl-36636982

RESUMO

Aim: To formulate and assess the anticancer effect of the poly(lactic-co-glycolic acid) (PLGA) copolymer with the thioether groups (diethyl sulfide [Des]) and disulfide bond (cystamine containing disulfide [Cys]), which encapsulated the anticancer drug paclitaxel (PTX) and triggered PTX release in cancer cell H2O2-rich or glutathione-rich surroundings. Methods: PLGA-b-P (Des@Cys) and PLGA-b-P nanoparticles loaded with PTX were prepared and characterized in vitro. The delivery ability of the PLGA-b-P nanoparticles and PLGA-b-P-PTX nanoparticles was assessed on a CT26 (mouse colon cancer cell line) and mouse lung cancer LLC model. Results: The nanoparticles were successfully prepared. Compared with free PTX, the formulated PLGA-b-P nanoparticles loaded with PTX exhibited greater accumulation at the tumor site in the mouse model. Conclusion: PLGA-b-P nanoparticles promote drug accumulation at tumor sites, providing an effective strategy for an intelligent, responsive drug-delivery system.


Assuntos
Nanopartículas , Paclitaxel , Camundongos , Animais , Paclitaxel/farmacologia , Paclitaxel/uso terapêutico , Paclitaxel/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Espécies Reativas de Oxigênio , Preparações de Ação Retardada , Glicóis , Peróxido de Hidrogênio , Linhagem Celular Tumoral , Nanopartículas/química , Oxirredução , Portadores de Fármacos/química
6.
J Mater Chem B ; 9(29): 5785-5793, 2021 07 28.
Artigo em Inglês | MEDLINE | ID: mdl-34190308

RESUMO

Dual phototherapy combining photodynamic therapy (PDT) and photothermal therapy (PTT) is considered to be a more effective therapeutic method against cancer than single treatment. Therefore, the development of a single material with both near-infrared (NIR)-laser-triggered PDT and PTT abilities is highly desirable but remains a great challenge. A design philosophy for photosensitizers for integrated PDT and PTT treatment has been put forward: (1) a high molar extinction coefficient in the NIR region; (2) suitable LUMO and T1 energy levels to regulate intersystem crossing for effective singlet oxygen (1O2) generation for PDT; and (3) the suppression of fluorescence emission to enhance the process of nonradiative transition with appropriate chemical modifications. Herein, an "all-in-one" functional material, di-cyan substituted 5,12-dibutylquinacridone (DCN-4CQA), for diagnosis and therapy was obtained. DCN-4CQA possesses dual-functional phototherapeutic activity and NIR fluorescence and it was produced via a facile synthesis process from the classic organic photoelectric material quinacridone. We then prepared smart water-soluble nanoparticles (NPs), DCN-4CQA/F127, using Pluronic® 127 (F127) as a drug carrier. The NPs exhibited excellent biocompatibility, robust photostability, NIR fluorescence, a high photothermal conversion efficiency (η = 47.3%), and sufficient 1O2 generation (ΦΔ = 24.3%) under NIR laser irradiation. Remarkably, the DCN-4CQA/F127 NPs significantly inhibited tumor growth in mice subjected to NIR laser irradiation. This study provides a new route for the development of highly efficient, low-cytotoxicity photosensitizers for fluorescence-imaging-guided PTT/PDT.


Assuntos
Antineoplásicos/farmacologia , Corantes Fluorescentes/farmacologia , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Imagem Óptica , Fármacos Fotossensibilizantes/farmacologia , Fototerapia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Sobrevivência Celular/efeitos dos fármacos , Teoria da Densidade Funcional , Ensaios de Seleção de Medicamentos Antitumorais , Corantes Fluorescentes/química , Células HeLa , Compostos Heterocíclicos de 4 ou mais Anéis/química , Humanos , Raios Infravermelhos , Neoplasias Mamárias Experimentais/tratamento farmacológico , Neoplasias Mamárias Experimentais/patologia , Camundongos , Estrutura Molecular , Tamanho da Partícula , Fármacos Fotossensibilizantes/síntese química , Fármacos Fotossensibilizantes/química
7.
J Nanobiotechnology ; 19(1): 39, 2021 Feb 06.
Artigo em Inglês | MEDLINE | ID: mdl-33549107

RESUMO

A limitation of current anticancer nanocarriers is the contradiction between multiple functions and favorable biocompatibility. Thus, we aimed to develop a compatible drug delivery system loaded with paclitaxel (PTX) for hepatocellular carcinoma (HCC) therapy. A basic backbone, PTX-loaded poly (3-hydroxybutyrate-co-3-hydroxyvalerate) PHBV nanoparticle (PHBV-PTX-NPs), was prepared by emulsion solvent evaporation. As a gatekeeper, the pH-sensitive coating was formed by self-polymerization of dopamine (PDA). The HCC-targeted arginine-glycine-aspartic acid (RGD)-peptide and PDA-coated nanoparticles (NPs) were combined through the Michael addition. Subsequently, the physicochemical properties of RGD-PDA-PHBV-PTX-NPs were characterized by dynamic light scattering-autosizer, transmission electron microscope, fourier transform infrared spectroscopy, differential scanning calorimetry, thermogravimetry and X-ray spectroscopy. As expected, the RGD-PDA-PHBV-PTX-NPs showed robust anticancer efficacy in a xenograft mouse model. More importantly, they exhibited lower toxicity than PTX to normal hepatocytes and mouse in vitro and in vivo, respectively. Taken together, these results indicate that the RGD-PDA-PHBV-PTX-NPs are potentially beneficial for easing conflict between multifunction and biocompatible characters of nanocarriers.


Assuntos
Antineoplásicos Fitogênicos/administração & dosagem , Carcinoma Hepatocelular/tratamento farmacológico , Preparações de Ação Retardada/química , Neoplasias Hepáticas/tratamento farmacológico , Paclitaxel/administração & dosagem , Poliésteres/química , Animais , Antineoplásicos Fitogênicos/uso terapêutico , Carcinoma Hepatocelular/patologia , Sistemas de Liberação de Medicamentos , Células Hep G2 , Humanos , Concentração de Íons de Hidrogênio , Indóis/química , Neoplasias Hepáticas/patologia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Nanopartículas/química , Oligopeptídeos/química , Paclitaxel/uso terapêutico , Polímeros/química
8.
Zhejiang Da Xue Xue Bao Yi Xue Ban ; 50(5): 614-620, 2021 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-34986528

RESUMO

To construct a hypobaric hypoxia-induced cell injury model. Rat pheochromocytoma PC12 cells were randomly divided into control group, normobaric hypoxia group and hypobaric hypoxia group. The cells in control group were cultured at normal condition, while cells in other two groups were cultured in normobaric hypoxia and hypobaric hypoxia conditions, respectively. CCK-8 method was used to detect cell viability to determine the optimal modeling conditions like the oxygen concentration, atmospheric pressure and low-pressure hypoxia time. The contents of lactate dehydrogenase (LDH), superoxide dismutase (SOD) and malondialdehyde (MDA) were detected by microplate method. The apoptosis ratio and cell cycle were analyzed by flow cytometry. The hypobaric hypoxia-induced cell injury model can be established by culturing for 24 h at 1% oxygen concentration and 41 kPa atmospheric pressure. Compared with the control group and normobaric hypoxia group, the activity of LDH and the content of MDA in hypobaric hypoxia group were significantly increased, the activity of SOD was decreased, the percentage of apoptosis was increased (all <0.05), and the cell cycle was arrested in G0/G1 phase. A stable and reliable cell injury model induced by hypobaric hypoxia has been established with PC12 cells, which provides a suitable cell model for the experimental study on nerve injury induced by hypoxia at high altitude.


Assuntos
Hipóxia , Superóxido Dismutase , Animais , Hipóxia Celular , Malondialdeído , Células PC12 , Ratos , Superóxido Dismutase/metabolismo
9.
J Sci Food Agric ; 101(4): 1314-1322, 2021 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-33245580

RESUMO

BACKGROUND: Pine oil contains a high percentage of polyunsaturated fatty acids, which make it prone to oxidation. Luteolin (LUT) micro-nano particles with antioxidant properties can be used as stabilizers to form an edible oil-in-water Pickering emulsion to improve the oxidative stability of pine nut oil. RESULTS: Under optimal preparation conditions, the LUT micro-nano particles and pine nut oil account for about 0.44 and 90.9 g·kg-1 of the total mass of the emulsion, respectively. The LUT particles in the suspension have a mean particle size of about 479 nm, present a sheet-like structure with a cut surface of 30-50 nm, and can reduce the surface tension of deionized water. In the optimized Pickering emulsion, the emulsion droplets are approximately spherical and have a mean diameter of about 125.6 nm and uniform distribution. The optimized Pickering emulsion droplets can remain stable for up to 2 h in an environment where the pH levels are 7-8.5, ultraviolet B radiation (UVB) irradiation, of less than 5.0 g·kg-1 , and at a temperature of 80 °C. The stability of the emulsion in simulated digestive fluid changed minimally. In the first 7 days of the accelerated oxidation experiment, LUT micro-nano particles not only successfully protected the integrity of emulsion droplets but also fully inhibited the peroxidation of pine oil. CONCLUSION: The strong antioxidant properties of LUT micro-nano particles, and the dense protective layer they formed, stabilized the Pickering emulsion successfully. The particles also improved the oxidation stability of pine nut oil. © 2020 Society of Chemical Industry.


Assuntos
Luteolina/química , Pinus/química , Óleos de Plantas/química , Emulsões/química , Nozes/química , Oxirredução , Tamanho da Partícula
10.
Pharmaceutics ; 12(11)2020 Oct 22.
Artigo em Inglês | MEDLINE | ID: mdl-33105832

RESUMO

Paclitaxel (PTX) is a poor water-soluble antineoplastic drug with significant antitumor activity. However, its low bioavailability is a major obstacle for its biomedical applications. Thus, this experiment is designed to prepare PTX crystal powders through an antisolvent precipitation process using 1-hexyl-3-methylimidazolium bromide (HMImBr) as solvent and water as an antisolvent. The factors influencing saturation solubility of PTX crystal powders in water in water were optimized using a single-factor design. The optimum conditions for the antisolvent precipitation process were as follows: 50 mg/mL concentration of the PTX solution, 25 °C temperature, and 1:7 solvent-to-antisolvent ratio. The PTX crystal powders were characterized via scanning electron microscopy, Fourier transform infrared spectroscopy, high-performance liquid chromatography-mass spectrometry, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Raman spectroscopy, solid-state nuclear magnetic resonance, and dissolution and oral bioavailability studies. Results showed that the chemical structure of PTX crystal powders were unchanged; however, precipitation of the crystalline structure changed. The dissolution test showed that the dissolution rate and solubility of PTX crystal powders were nearly 3.21-folds higher compared to raw PTX in water, and 1.27 times higher in artificial gastric juice. Meanwhile, the bioavailability of PTX crystal increased 10.88 times than raw PTX. These results suggested that PTX crystal powders might have potential value to become a new oral PTX formulation with high bioavailability.

11.
Pharmaceutics ; 11(11)2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31683964

RESUMO

Honokiol (HK), a well-tolerated natural product, has many multiple pharmacological activities. However, its poor water solubility and low bioavailability limit its clinical application and development. The aim of this research was to prepare the solid dispersion (SD) formulation of honokiol (HK) with poloxamer-188 (PLX) as the carrier, thereby improving its solubility and oral bioavailability. Firstly, by investigating the relationship between the addition amount of the PLX and the solubility of HK, and the effects of solid dispersions with different ratios of HK-PLX on the solubility of HK, we determined that the optimum ratio of PLX to HK was (1:4). Then, the HK-PLX (1:4) SD of HK was prepared using the solvent evaporation method. The morphology of the obtained HK-PLX (1:4) SD was different from that of free HK. The HK in the HK-PLX (1:4) SD existed in amorphous form and formed intermolecular hydrogen bonds with PLX. Additionally, the solubility values of the HK-PLX (1:4) SD were about 32.43 ± 0.36 mg/mL and 34.41 ± 0.38 mg/mL in artificial gastric juice (AGJ) and in artificial intestinal juice (AIJ), respectively. Compared with free HK, the release rate and the bioavailability was also substantially improved for HK in its SD form. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that the HK-PLX (1:4) SD showed higher inhibition of HepG2 cells than free HK. Taken together, the present study suggests that the HK-PLX (1:4) SD could become a new oral drug formulation with high bioavailability and could produce a better response for clinical applications of HK.

12.
Int J Biol Macromol ; 138: 207-214, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31306708

RESUMO

In this work, paclitaxel was loaded into porous starch in the form of nanoparticles (PNPS), and the properties of PNPS were investigated by using raw paclitaxel and the system of paclitaxel directly loaded into porous starch (PPS) as control groups. According to the tested results, the drug loading (DL) and encapsulation efficiency (EE) of PNPS were 14.13%±0.27% and 73.92%±0.54%, higher than that of PPS (9.79%±0.31% and 71.17%±0.67%) respectively. Compared with raw paclitaxel and PPS, PNPS exhibited the more prominent dissolution rate and bioavailability, in which the bioavailability of PPS and PNPS were 2.94 and 5.42 times of that of raw paclitaxel respectively. In addition, the IC50 values of raw paclitaxel, PPS and PNPS on Lewis Lung Carcinoma (LLC) cells were 17,703.41±15.76µM, 95.10±5.32µM and 85.68±7.38µM respectively. Furthermore, the residues of acetone in PPS and PNPS were less than the ICH limit for acetone in class III solvents. To summarize, the preparation of PNPS was a potential method to improve the dissolution and bioavailability of paclitaxel.


Assuntos
Portadores de Fármacos/química , Nanopartículas/química , Paclitaxel/química , Paclitaxel/farmacocinética , Amido/química , Disponibilidade Biológica , Linhagem Celular Tumoral , Humanos , Paclitaxel/farmacologia , Tamanho da Partícula , Porosidade , Solubilidade , Solventes/química
13.
Phytomedicine ; 60: 152957, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31128995

RESUMO

BACKGROUND: Inonotus obliquus, namely as Chaga mushroom, is a medicinal and edible fungus, which is widely used in food and medical fields. Inotodiol, a natural lanostane-type triterpenoid with remarkable pharmacological activities, was isolated from Inonotus obliquus, which its potential anti-tumor molecular mechanism was elaborated poorly. PURPOSE: The aim of the present study was to investigate the effect of Inotodiol on HeLa cell migration, invasion and apoptosis through p53-dependent pathway. STUDY DESIGN AND METHODS: The potential mechanisms of Inotodiol on HeLa cell anti-metastatic and pro-apoptosis via wound healing assay, trans-well invasion assay, flow cytometry, caspase-3 activity assay and western blot analysis were studied, as well as the involvement of p53 signaling pathway in anti-metastatic and pro-apoptosis of Inotodiol. Besides, the function of tumor suppressor p53 was further verified by small interfering RNA. RESULTS: Firstly, the cell viability assay showed that low-concentration of Inotodiol had no cytotoxicity to HeLa cells and whereas the concentration above 25 µM significantly inhibited HeLa cell growth and even induced apoptosis. This result was further demonstrated by cell proliferation and morphology assay. Secondly, in vitro wound healing and trans-well invasion assays reported that low-concentration treatment of Inotodiol significantly inhibited cells migration and invasion in a dose-dependent manner, the western blot analysis of matrix mettalloprotinase-2 (MMP2) and matrix mettalloprotinase-9 (MMP9) levels were also decreased. Moreover, Inotodiol notably induced tumor cell apoptosis by Annexin-V-FITC apoptosis assay, which is associated with activation pro-apoptotic proteins of PARP, cleaved caspase-3 and Bax expression, inhibition anti-apoptotic protein Bcl-2 expression. Finally, the anti-tumor activity of Inotodiol was attenuated by silencing p53 tumor suppressor, the result revealed that pre-treatment with p53-specific small interfering RNA (si-p53) markedly inhibited Intodiol-indeuced HeLa cell apoptosis and decreased the caspase-3 activity. What is more, the inhibitory effect of Inotodiol on tumor migration and invasion was blocked under p53 knockdown. CONCLUSION: To sum up, the present study indicated that Inotodiol possessed the potential to prevent malignant tumor migration and invasion, and it might be a natural active compound candidate for clinical treatment of human cervical cancer.


Assuntos
Agaricales/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Lanosterol/análogos & derivados , Proteína Supressora de Tumor p53/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Caspase 3/genética , Caspase 3/metabolismo , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Feminino , Células HeLa , Humanos , Lanosterol/farmacologia , Invasividade Neoplásica , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Transdução de Sinais/efeitos dos fármacos , Proteína Supressora de Tumor p53/genética
14.
Int J Nanomedicine ; 14: 2667-2681, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31043780

RESUMO

BACKGROUND: Lutein ester (LE) is an important carotenoid fatty acid ester. It is a form in which lutein is present in nature and is produced by free non-esterification and fatty acid esterification. LE is one of the safe sources of lutein. Increasing lutein intake can prevent and treat age-related macular degeneration. In addition, it can effectively inhibit gastric cancer, breast cancer, and esophageal cancer. However, the poor aqueous solubility of LE has impeded its clinical applications. OBJECTIVE: The objective of this study was to prepare lutein ester nanoparticles (LE-NPs) by liquid antisolvent precipitation techniques to improve the bioavailability of LE in vivo and improve eye delivery efficiency. MATERIALS AND METHODS: The physical characterization of LE-NPs was performed, and their in vitro dissolution rate, in vitro antioxidant capacity, in vivo bioavailability, tissue distribution, and ocular pharmacokinetics were studied and evaluated. RESULTS: The LE freeze-dried powder obtained under the optimal conditions possessed a particle size of ~164.1±4.3 nm. The physical characterization analysis indicated the amorphous form of LE-NPs. In addition, the solubility and dissolution rate of LE-NPs in artificial gastric juice were 12.75 and 9.65 times that of the raw LE, respectively. The bioavailability of LE-NPs increased by 1.41 times compared with that of the raw LE. The antioxidant capacity of LE-NPs was also superior to the raw LE. The concentration of lutein in the main organs of rats treated with the LE-NPs was higher than that in rats treated with the raw LE. The bioavailability of LE-NPs in rat eyeballs was found to be 2.34 times that of the original drug. CONCLUSION: LE-NPs have potential application as a new oral pharmaceutical formulation and could be a promising eye-targeted drug delivery system.


Assuntos
Precipitação Química , Sistemas de Liberação de Medicamentos/métodos , Ésteres/administração & dosagem , Luteína/administração & dosagem , Solventes/química , Administração Oftálmica , Administração Oral , Animais , Antioxidantes/farmacologia , Disponibilidade Biológica , Ésteres/química , Ésteres/farmacocinética , Luteína/química , Luteína/farmacocinética , Camundongos , Nanopartículas/administração & dosagem , Tamanho da Partícula , Ratos Sprague-Dawley , Solubilidade , Distribuição Tecidual
15.
Food Chem ; 275: 339-345, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30724205

RESUMO

Five novel compounds (Gen-NO2, Gen-2NO2, Gen-NH2, Gen-2NH2 and Gen-6NH2) have been designed via introducing an electron-withdrawing group -NO2 and an electron-donating group -NH2 into the structure of genistein. The effects of -NO2 and -NH2 groups on the antioxidant ability of genistein were investigated via quantum chemistry method in gas and methanol phases. The crucial parameters related to three antioxidant mechanisms were calculated. Moreover, the frontier molecular orbital, natural bond orbital and global descriptive parameters were calculated to evaluate the reactivity of genistein and its derivatives. Calculated results indicate the antioxidant process of genistein and its derivatives inclines to the hydrogen atom transfer (HAT) and sequential proton loss electron transfer (SPLET) mechanisms in gas and methanol phases, respectively. Moreover, introducing -NH2 group into genistein can improve its antioxidant activity owing to the outstanding activities of amino-substituents of genistein, which will provide valuable guidance for the synthesis of new antioxidants experimentally.


Assuntos
Antioxidantes/química , Genisteína/química , Aminas/química , Transporte de Elétrons , Elétrons , Hidrogênio/química , Modelos Químicos , Prótons
16.
J Surg Res ; 237: 12-21, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30694786

RESUMO

BACKGROUND: The obesity epidemic has prompted the need to better understand the impact of adipose tissue on human pathophysiology. However, accurate, efficient, and replicable models of quantifying adiposity have yet to be developed and clinically implemented. We propose a novel semiautomated radiologic method of measuring the visceral fat area (VFA) using computed tomography scan analysis. MATERIALS AND METHODS: We obtained a cohort of 100 patients with rectal adenocarcinoma, with a median age of 60.9 y (age range: 35-87 y) and an average body mass index of 28.8 kg/m2 ± 6.56 kg/m2. The semiautomated quantification method of adiposity was developed using a commercial imaging suite. The method was compared to two manual delineations performed using two different picture archiving communication systems. We quantified VFA, subcutaneous fat area (SFA), total fat area (TFA), and visceral-to-subcutaneous fat ratio (V/S ratio) on computed tomography axial slices that were at the L4-L5 intervertebral level. RESULTS: The semiautomated method was comparable to manual measurements for TFA, VFA, and SFA with intraclass correlation (ICC) of 0.99, 0.97, and 0.96, respectively. However, the ICC for the V/S ratio was only 0.44, which led to the identification of technical outliers that were identified using robust regression. After removal of these outliers, the ICC improved to 0.99 for TFA, VFA, and SFA and 0.97 for the V/S ratio. Measurements from the manual methodology highly correlated between the two picture archiving communication system platforms, with ICC of 0.98 for TFA, 0.98 for VFA, 0.96 for SFA, and 0.95 for the V/S ratio. CONCLUSIONS: This semiautomated method is able to generate precise and reproducible results. In the future, this method may be applied on a larger scale to facilitate risk stratification of patients using measures of abdominal adiposity.


Assuntos
Adenocarcinoma/diagnóstico por imagem , Adiposidade , Processamento de Imagem Assistida por Computador/métodos , Obesidade/diagnóstico , Neoplasias Retais/diagnóstico por imagem , Adenocarcinoma/complicações , Adulto , Idoso , Idoso de 80 Anos ou mais , Algoritmos , Índice de Massa Corporal , Feminino , Humanos , Gordura Intra-Abdominal/diagnóstico por imagem , Masculino , Pessoa de Meia-Idade , Obesidade/complicações , Neoplasias Retais/complicações , Medição de Risco/métodos , Gordura Subcutânea/diagnóstico por imagem , Tomografia Computadorizada por Raios X
17.
Artif Cells Nanomed Biotechnol ; 47(1): 154-165, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30686050

RESUMO

This work investigated the preparation of specific targeted drug delivery systems in cancer chemotherapy by folate conjugated human serum albumin nanoparticles encapsulated resveratrol (RES) nanoparticles (FA-HSA-RESNPs). FA was coupled to HSA, and RES was encapsulated in FA-conjugated HSA by high pressure fluid nano-homogeneous emulsification. The average particle size and polydispersity index of NPs prepared under optimal conditions were 102.1 ± 4.9 nm and 0.001. The drug capsulation efficiency and drug loading efficiency were 98.36 and 14.66%, respectively. The analysis of the results of the physical characterization showed that the RES was present in the FA-HSA-RESNPs in an amorphous state. In vitro drug-release study showed that the NPs can release the drug persistently and slowly. The inhibition rate of FA-HSA-RESNPs and RES was detected using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide method to be 110.8 and 157.2 µM, respectively. The targeting ability of the FA-HSA-RESNPs for the HepG2 cell was measured by fluorescein isothiocyanate-modified albumin techniques. The uptake rate of FA-HSA-RESNPs was higher than that of the original RES. By using near-infrared imaging, in vivo activity was labeled with Cy5 fluorescent FA-HSA-RESNP confirmed FA-HSA-RESNP tumor-targeting ability. The intravenous administration bioavailability of FA-HSA-RESNPs was about 5.95-fold higher than that of the original RES.


Assuntos
Portadores de Fármacos/química , Ácido Fólico/química , Neoplasias Hepáticas/tratamento farmacológico , Nanopartículas/química , Resveratrol/química , Albumina Sérica Humana/química , Animais , Disponibilidade Biológica , Transporte Biológico , Cápsulas , Proliferação de Células/efeitos dos fármacos , Portadores de Fármacos/metabolismo , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/toxicidade , Reposicionamento de Medicamentos , Células Hep G2 , Humanos , Neoplasias Hepáticas/patologia , Camundongos , Ratos , Resveratrol/farmacologia , Resveratrol/uso terapêutico
18.
Pak J Pharm Sci ; 31(5(Special)): 2185-2189, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30463810

RESUMO

The problem of bacterial resistance caused by the irrational use of antibiotics has become a global public health problem. How to improve the rational application of antimicrobial agents is the focus of attention in the global medical industry. In this paper, we analyze the rational application of antibacterial drugs in arthroplasty and nursing intervention. The results showed that the utilization rate of the first generation cephalosporins was the highest, accounting for 43.91%, followed by lincomycin, accounting for 26.59%. At the same time, we analyzed the wound infection and its distribution and drug resistance after artificial joint replacement. In the selection of drug varieties, cleaning surgery should be the first generation of cephalosporins for the prevention of Staphylococcus aureus infection. At the same time, in the process of clinical nursing, the high quality nursing service mode is implemented. The nursing staff should do a good job for the patient's medication guidance after the operation, and charge the attention in the process of drug use.


Assuntos
Antibacterianos/uso terapêutico , Adolescente , Adulto , Idoso , Artroplastia de Substituição/métodos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Enfermagem , Infecções Estafilocócicas/prevenção & controle , Adulto Jovem
19.
Int J Nanomedicine ; 13: 5469-5483, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30271141

RESUMO

BACKGROUND: Honokiol is a bioactive lignanoid and has been utilized in traditional Chinese medicine for a long time. It exhibits several pharmacological properties, such as anticancer effects, anti-inflammatory effects, and antianxiety effects. However, the poor aqueous solubility of honokiol has impeded clinical applications. MATERIALS AND METHODS: In the present study, we adopted the liquid antisolvent precipitation (LAP) technique to prepare nanoparticles of honokiol for enhancement of solubility and bioavailability. Moreover, the honokiol nanoparticles obtained were investigated and evaluated in terms of morphology, physicochemical properties, saturation solubility, dissolution in vitro, bioavailability in vivo, toxicity, and the inhibitory effect on growth of HepG2 cells. RESULTS: The obtained honokiol nanoparticles existed nearly in spherical shape and could be turned into amorphous structure by the LAP method. Moreover, the solubility of the honokiol nanoparticles was extremely higher than that of free honokiol, and the nanoparticle dissolution rate was also higher than that of free honokiol, which was about 20.41 times and 26.2 times than that of free honokiol in artificial gastric juice and in artificial intestinal juice. The area under the curve [AUC(0-t)] value of honokiol nanoparticles was about 6.52 times greater than that of free honokiol; therefore, the honokiol nanoparticles had a higher bioavailability than free honokiol but were innoxious to the organs of rats. Additionally, the honokiol nanoparticles exhibited a higher inhibition of HepG2 cells due to their lower IC50 compared to free honokiol. CONCLUSION: Honokiol nanoparticles have high solubility and bioavailability, and can become a new oral drug formulation and produce a better response for its clinical applications.


Assuntos
Compostos de Bifenilo/farmacologia , Compostos de Bifenilo/farmacocinética , Precipitação Química , Lignanas/farmacologia , Lignanas/farmacocinética , Nanopartículas/química , Solventes/química , Administração Oral , Animais , Disponibilidade Biológica , Compostos de Bifenilo/sangue , Compostos de Bifenilo/química , Varredura Diferencial de Calorimetria , Feminino , Células Hep G2 , Humanos , Lignanas/sangue , Lignanas/química , Nanopartículas/ultraestrutura , Especificidade de Órgãos , Tamanho da Partícula , Ratos Sprague-Dawley , Solubilidade , Termogravimetria , Testes de Toxicidade , Difração de Raios X
20.
Environ Sci Pollut Res Int ; 25(28): 28431-28444, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30088244

RESUMO

Assessing the uptake of trace gases by forests contributes to understanding the mechanisms of gas exchange between vegetation and the atmosphere and to evaluating the potential risk of these pollutant gases to forests. In this study, the multi-timescale characteristics of the stomatal uptake of NO, NO2, SO2 and O3 by Schima superba, Eucalyptus citriodora and Acacia auriculiformis were investigated by continuous sap flow measurements for a 3-year period. The peak canopy stomatal conductance (GC) for these three species appeared between 9:00 and 12:00, which was jointly regulated by the vapour pressure deficit (VPD) and photosynthetically active radiation (PAR). Additionally, annual and seasonal variations in the stomatal uptake of trace gases for these three tree species suggested that there was a combination effect between canopy stomatal conductance and ambient concentration on the uptake of trace gases. Furthermore, the result demonstrated that the trace gas absorption capacities among these three forest types followed the order of S. superba > E. citriodora > A. auriculiformis. The findings of this study have theoretical significance and application value in assessing air purification and the risk of harm to forests in Southern China.


Assuntos
Poluentes Atmosféricos/química , Florestas , Óxidos de Nitrogênio/análise , Ozônio/análise , Dióxido de Enxofre/análise , Árvores/metabolismo , China , Fotossíntese , Transpiração Vegetal , Estações do Ano , Clima Tropical
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