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1.
Int J Mol Sci ; 25(15)2024 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-39125695

RESUMEN

Transparent films with excellent antibacterial properties and strong mechanical properties are highly sought after in packaging applications. In this study, Ag/SiO2 nanoparticles were introduced into a mixed solution of chitosan (CS) and polyvinyl alcohol (PVA) and a Ag/SiO2-CS-PVA transparent film was developed. The excellent properties of the film were confirmed by light transmittance, water contact angle tests and tensile tests. In addition, for the antibacterial test, the antibacterial properties of the sample against Gram-negative bacteria (Escherichia coli) and Gram-positive bacteria (Staphylococcus aureus) were explored, and the average size of the bacteriostatic circle was measured by the cross method. The final results show that Ag/SiO2-CS-PVA transparent film has the advantages of good antibacterial properties, high transparency and high mechanical strength.


Asunto(s)
Antibacterianos , Quitosano , Escherichia coli , Alcohol Polivinílico , Dióxido de Silicio , Plata , Staphylococcus aureus , Quitosano/química , Quitosano/farmacología , Alcohol Polivinílico/química , Antibacterianos/farmacología , Antibacterianos/química , Dióxido de Silicio/química , Plata/química , Plata/farmacología , Escherichia coli/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacos , Resistencia a la Tracción , Pruebas de Sensibilidad Microbiana , Nanopartículas del Metal/química
2.
Polymers (Basel) ; 16(13)2024 Jul 08.
Artículo en Inglés | MEDLINE | ID: mdl-39000804

RESUMEN

The efficient exploitation of planted fast-growing wood is crucial for enhancing wood resource utilization. In this study, the fast-growing poplar wood was modified by in situ impregnation through vacuum impregnation with polyvinyl alcohol and nano-silica sol as impregnation modifiers, combined with delignification-freezing pretreatment. The samples were characterized by FTIR, XRD, SEM, and the universal mechanical testing machine. The results showed that the wrinkle deformation and cracking of the wood blocks were greatly alleviated after the delignification-freezing pretreatment and the polyvinyl alcohol and nano-silica sol were successfully integrated into the wood. The resulting polyvinyl alcohol-silica sol poplar composites exhibited about 216%, 80% and 43% higher compressive strength with respect to delignified wood, natural wood and impregnated natural wood, respectively, thereby demonstrating superior mechanical properties and potential opportunities for value-added and efficient utilization of low-quality wood.

3.
Int J Mol Sci ; 25(9)2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38731960

RESUMEN

Due to a large number of harmful chemicals flowing into the water source in production and life, the water quality deteriorates, and the use value of water is reduced or lost. Biochar has a strong physical adsorption effect, but it can only separate pollutants from water and cannot eliminate pollutants fundamentally. Photocatalytic degradation technology using photocatalysts uses chemical methods to degrade or mineralize organic pollutants, but it is difficult to recover and reuse. Woody biomass has the advantages of huge reserves, convenient access and a low price. Processing woody biomass into biochar and then combining it with photocatalysts has played a complementary role. In this paper, the shortcomings of a photocatalyst and biochar in water treatment are introduced, respectively, and the advantages of a woody biochar-based photocatalyst made by combining them are summarized. The preparation and assembly methods of the woody biochar-based photocatalyst starting from the preparation of biochar are listed, and the water treatment efficiency of the woody biochar-based photocatalyst using different photocatalysts is listed. Finally, the future development of the woody biochar-based photocatalyst is summarized and prospected.


Asunto(s)
Carbono , Carbón Orgánico , Purificación del Agua , Madera , Purificación del Agua/métodos , Carbón Orgánico/química , Catálisis , Madera/química , Carbono/química , Contaminantes Químicos del Agua/química , Procesos Fotoquímicos , Adsorción
4.
PLoS One ; 19(5): e0301617, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38758776

RESUMEN

BACKGROUND: In order to gain a deeper understanding of the relationship between physical activity and adolescent mental health in the post COVID-19 pandemic era, self-esteem and social anxiety were used as mediating variables to explore the potential mechanisms by which physical activity affects adolescent mental health. METHODS: The study used the HELP-II Health Promoting Lifestyle Scale, the SPIN Social Phobia Scale, the Self-Esteem Scale, and the 10-item Kessler Psychological Distress Scale to administer questionnaires to 400 Chinese secondary school students, and SPSS 26.0 and PROCESS 3.3 were used to process the data. RESULTS: The findings showed that (1) physical activity was significantly and positively associated with mental health; (2) self-esteem and social anxiety played a fully mediating role between physical activity and adolescent mental health respectively; (3) self-esteem and social anxiety played a chain mediating role between physical activity and adolescent mental health. CONCLUSION: This study reveals the relationship and influencing mechanism between physical activity and adolescent mental health in the post COVID-19 pandemic era. Appropriate interventions for physical activity, self-esteem, and social anxiety may be beneficial to adolescent mental health. The protective role of self-esteem in adolescent mental health should be the focus of future studies, and further investigations into the association between the COVID-19 and adolescent mental health are warranted.


Asunto(s)
Ansiedad , COVID-19 , Ejercicio Físico , Salud Mental , Autoimagen , Humanos , Adolescente , Femenino , COVID-19/psicología , COVID-19/epidemiología , Masculino , Ejercicio Físico/psicología , Ansiedad/psicología , Encuestas y Cuestionarios , SARS-CoV-2 , Estudiantes/psicología , China/epidemiología , Fobia Social/psicología , Pandemias
5.
Chem Biol Drug Des ; 103(2): e14436, 2024 02.
Artículo en Inglés | MEDLINE | ID: mdl-38395608

RESUMEN

Neuroinflammation contributes to neurological dysfunction in the patients who suffer from subarachnoid hemorrhage (SAH). Isoliquiritigenin (ISL) is a bioactive component extracted from Genus Glycyrrhiza. This work is to investigate whether ISL ameliorates neuroinflammation after SAH. In this study, intravascular perforation of male Sprague-Dawley rats was used to establish a SAH model. ISL was administered by intraperitoneal injection 6 h after SAH in rats. The mortality, SAH grade, neurological score, brain water content, and blood-brain barrier (BBB) permeability were examined at 24 h after the treatment. Expressions of tumor necrosis factor-α, interleukin-6, Iba-1, and MPO were measured by quantitative real-time polymerase chain reaction (qRT-PCR). Besides, the expression levels of NF-κB p65 and NLRP3, ASC, caspase-1, IL-1ß, and IL-18 were analyzed by western blot. The experimental data suggested that ISL treatment could ameliorate neurological impairment, attenuate brain edema, and ameliorate BBB injury after SAH in rats. ISL treatment repressed the expression of proinflammatory cytokines TNF-α and IL-6, and meanwhile inhibited the expression of Iba-1 and MPO. ISL also repressed NF-κB p65 expression as well as the transport from the cytoplasm to the nucleus. In addition, ISL significantly suppressed the expression levels of NLR family pyrin domain containing 3 (NLRP3), ASC, caspase-1, IL-1ß, and IL-18. These findings suggest that ISL inactivates NLRP3 pathway by inhibiting NF-κB p65 translocation, thereby repressing the neuroinflammation after SAH, and it is a potential drug for the treatment of SAH.


Asunto(s)
Lesiones Encefálicas , Chalconas , Hemorragia Subaracnoidea , Humanos , Ratas , Masculino , Animales , FN-kappa B/metabolismo , Hemorragia Subaracnoidea/complicaciones , Hemorragia Subaracnoidea/tratamiento farmacológico , Inflamasomas/metabolismo , Ratas Sprague-Dawley , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Interleucina-18/uso terapéutico , Enfermedades Neuroinflamatorias , Lesiones Encefálicas/tratamiento farmacológico , Lesiones Encefálicas/metabolismo , Lesiones Encefálicas/patología , Factor de Necrosis Tumoral alfa/genética , Caspasas/uso terapéutico
6.
Front Plant Sci ; 14: 1151131, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37615025

RESUMEN

As the most suitable potential clean energy power generation technology, biophotovoltaics (BPV) not only inherits the advantages of traditional photovoltaics, such as safety, reliability and no noise, but also solves the disadvantages of high pollution and high energy consumption in the manufacturing process, providing new functions of self-repair and natural degradation. The basic idea of BPV is to collect light energy and generate electric energy by using photosynthetic autotrophs or their parts, and the core is how these biological materials can quickly and low-loss transfer electrons to the anode through mediators after absorbing light energy and generating electrons. In this mini-review, we summarized the biological materials widely used in BPV at present, mainly cyanobacteria, green algae, biological combinations (using multiple microorganisms in the same BPV system) and isolated products (purified thylakoids, chloroplasts, photosystem I, photosystem II), introduced how researchers overcome the shortcomings of low photocurrent output of BPV, pointed out the limitations that affected the development of BPV' biological materials, and put forward reasonable assumptions accordingly.

7.
Int J Mol Sci ; 24(11)2023 Jun 02.
Artículo en Inglés | MEDLINE | ID: mdl-37298624

RESUMEN

As the focus of architecture, furniture, and other fields, wood has attracted extensive attention for its many advantages, such as environmental friendliness and excellent mechanical properties. Inspired by the wetting model of natural lotus leaves, researchers prepared superhydrophobic coatings with strong mechanical properties and good durability on the modified wood surface. The prepared superhydrophobic coating has achieved functions such as oil-water separation and self-cleaning. At present, some methods such as the sol-gel method, the etching method, graft copolymerization, and the layer-by-layer self-assembly method can be used to prepare superhydrophobic surfaces, which are widely used in biology, the textile industry, national defense, the military industry, and many other fields. However, most methods for preparing superhydrophobic coatings on wood surfaces are limited by reaction conditions and process control, with low coating preparation efficiency and insufficiently fine nanostructures. The sol-gel process is suitable for large-scale industrial production due to its simple preparation method, easy process control, and low cost. In this paper, the research progress on wood superhydrophobic coatings is summarized. Taking the sol-gel method with silicide as an example, the preparation methods of superhydrophobic coatings on wood surfaces under different acid-base catalysis processes are discussed in detail. The latest progress in the preparation of superhydrophobic coatings by the sol-gel method at home and abroad is reviewed, and the future development of superhydrophobic surfaces is prospected.


Asunto(s)
Industrias , Madera , Catálisis , Nanopartículas Capa por Capa , Humectabilidad
8.
Front Plant Sci ; 14: 1154535, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37089635

RESUMEN

Purple corn (Zea mays L.) is a special variety of corn, rich in a large amount of anthocyanins and other functional phytochemicals, and has always ranked high in the economic benefits of the corn industry. However, most studies on the stability of agronomic traits and the interaction between genotype and environment in cereal crops focus on yield. In order to further study the accumulation and stability of special anthocyanins in the growth process of purple corn, this review starts with the elucidation of anthocyanins in purple corn, the biosynthesis process and the gene regulation mechanism behind them, points out the influence of anthocyanin metabolism on anthocyanin metabolism, and introduces the influence of environmental factors on anthocyanin accumulation in detail, so as to promote the multi-field production of purple corn, encourage the development of color corn industry and provide new opportunities for corn breeders and growers.

9.
ACS Appl Mater Interfaces ; 14(49): 54662-54669, 2022 Dec 14.
Artículo en Inglés | MEDLINE | ID: mdl-36459617

RESUMEN

Sodium-sulfur batteries operating at ambient temperature are being extensively studied because of the high theoretical capacity and abundant resources, yet the long-chain polysulfides' shuttle effect causes poor cycling performance of Na-S batteries. We report an annealing/etching method to converse low-cost wheat bran to a 3D honeycomb-like carbon with abundant micropores (WBMC), which is smaller than S8 molecular size (∼0.7 nm). Thus, the microporous structure could only fill small molecular sulfur (S2-4). The micropores made sulfur a one-step reaction without the shuttle effect due to the formed short-chain polysulfides being insoluble. The WBMC@S exhibits an excellent initial capacity (1413 mAh g-1) at 0.2 C, outstanding cycling performance (822 mAh g-1 after 100 cycles at 0.2 C), and high rate performance (483 mAh g-1 at 3.0 C). The electrochemical performance proves that the steric confinement of micropores effectively terminates the shuttle effect.

10.
Front Bioeng Biotechnol ; 10: 1033514, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36324886

RESUMEN

Nature is the source of human design inspiration. In order to adapt to the environment better, creatures in nature have formed various morphological structures during billions of years of evolution, among which the superhydrophobic characteristics of some animal and plant surface structures have attracted wide attention. At present, the preparation methods of bionic superhydrophobic surface based on the microstructure of animal and plant body surface include vapor deposition, etching modification, sol-gel method, template method, electrostatic spinning method and electrostatic spraying method, etc., which have been used in medical care, military industry, shipping, textile and other fields. Based on nature, this paper expounds the development history of superhydrophobic principle, summarizes the structure and wettability of superhydrophobic surfaces in nature, and introduces the characteristics differences and applications of different superhydrophobic surfaces in detail. Finally, the challenge of bionic superhydrophobic surface is discussed, and the future development direction of this field is prospected.

11.
Polymers (Basel) ; 14(16)2022 Aug 17.
Artículo en Inglés | MEDLINE | ID: mdl-36015621

RESUMEN

Compared with other materials, polyethylene terephthalate (PET) has high transparency, excellent physical and mechanical properties in a wide temperature range and good hygiene and safety, so it is widely used in the packaging industry, especially in the packaging of beverages and foods. The optimization of PET bottles is mainly reflected in three aspects: material optimization, structure optimization and process optimization, among which there is much research on material optimization and process optimization, but there is no complete overview on structure optimization. A summary of structural optimization is necessary. Aiming at structural optimization, the finite element method is a useful supplement to the beverage packaging industry. By combining the computer-aided design technology and using finite element software for finite element simulation, researchers can replace the experimental test in the pre-research design stage, predict the effect and save cost. This review summarizes the development of PET bottles for beverage packaging, summarizes various optimization methods for preventing stress cracking in beverage packaging, and especially focuses on comparing and evaluating the effects of several optimization methods for packaging structure. Finally, the future development of all kinds of optimization based on structural optimization in the field of beverage packaging is comprehensively discussed, including personalized design, the combination of various methods and the introduction of actual impact factor calculation.

12.
Front Bioeng Biotechnol ; 10: 958095, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35992341

RESUMEN

As an emerging fringe science, bionics integrates the understanding of nature, imitation of nature, and surpassing nature in one aspect, and it organically combines the synergistic complementarity of function and structure-function integrated materials which is of great scientific interest. By imitating the microstructure of a natural biological surface, the bionic superhydrophobic surface prepared by human beings has the properties of self-cleaning, anti-icing, water collection, anti-corrosion and oil-water separation, and the preparation research methods are increasing. The preparation methods of superhydrophobic surface include vapor deposition, etching modification, sol-gel, template, electrostatic spinning, and electrostatic spraying, which can be applied to fields such as medical care, military industry, ship industry, and textile. The etching modification method can directly modify the substrate, so there is no need to worry about the adhesion between the coating and the substrate. The most obvious advantage of this method is that the obtained superhydrophobic surface is integrated with the substrate and has good stability and corrosion resistance. In this article, the different preparation methods of bionic superhydrophobic materials were summarized, especially the etching modification methods, we discussed the detailed classification, advantages, and disadvantages of these methods, and the future development direction of the field was prospected.

13.
Polymers (Basel) ; 14(15)2022 Aug 03.
Artículo en Inglés | MEDLINE | ID: mdl-35956687

RESUMEN

The polyethylene terephthalate (PET) beverage bottle is one of the most common beverage packages in the world, but the bottom of the PET bottle tends to crack due to excessive stress. In this paper, through numerical simulation and finite element analysis, the mechanical properties of four typical geometric models of bottle bottom are studied, and it is determined that "claw flap bottle bottom (CF-bottom)" has the best structure. Then, the shapes of four bottle bottom structures are fine-tuned by using the automatic optimization method. Under the premise of the same material quality, the surface maximum principal stress, the overall maximum principal stress, and the total elastic strain energy of the bottle bottom are reduced by 46.39-71.81%, 38.16-71.50%, and 38.56-61.38%, respectively, while the deformation displacement is also reduced by 0.63 mm-3.43 mm. In contrast to other papers, this paper dispenses with the manual adjustment of various variables, instead adopting automatic shape optimization to obtain a more accurate model. The percentage of maximum principal stress reduction is remarkable, which provides a feasible theoretical guidance for the structural optimization of PET bottle bottom in the production process.

14.
Polymers (Basel) ; 14(14)2022 Jul 13.
Artículo en Inglés | MEDLINE | ID: mdl-35890620

RESUMEN

PET bottlesare often used as airtight containers for filling carbonated drinks. Because carbonated drinks contain large volumes of CO2 gas, the container needs to bear a tremendous pressure from the inside of the bottle.If the stress exceeds the bearing limit, the material will show the phenomenon of local cracking and liquid overflow.For the structural design, the method of manual adjustment before automatic adjustment was adopted. First, through manual optimization, the initial optimal parameter combination was as follows:the inner diameter of the bottle bottom was 17 mm, the dip angle of the valley bottom was 81°, the deepest part of the valley bottom was 25 mm, and the outer diameter was 27 mm. Comsol software was used for automatic optimization. Compared with the original bottle bottom, the total maximum principal stress and total elastic strain energy in the bottle bottom after manual-automatic double optimization decreased by 69.4% and 40.0%, respectively, and the displacement caused by deformation decreased by 0.60 mm (74.1%). The extremely high reduction ratio was caused by manual-automatic double optimization.

15.
Opt Express ; 28(23): 34337-34345, 2020 Nov 09.
Artículo en Inglés | MEDLINE | ID: mdl-33182906

RESUMEN

The behavior of directly linearly polarized emission was investigated in an isotropic Nd:YAG laser with a weakly anisotropic Fabry-Perot cavity. In order to explore the polarization mechanism, the intracavity eigenmodes were analyzed theoretically. A theoretical model was developed and shown to be suitable for describing the orientation-dependent beam profiles of the polarizer-specific features observed in experiments. This model indicates that the linear polarization emission results from the coherently combined state of intracavity eigenmodes as opposed to an intrinsic polarization state. The coherent combination is attributed to the frequency degeneracy and spontaneous phase locking of polarized eigenmodes. For the first time, the polarization coupling mechanism based on the coherent combination of eigenmodes in an isotropic solid-state laser was demonstrated. Moreover, this study also contributes an effective method to judge different types of linear polarization states.

16.
Eur J Med Chem ; 191: 112134, 2020 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-32088493

RESUMEN

11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) is a key metabolic enzyme that catalyzing the intracellular conversion of inactive glucocorticoids to physiologically active ones. Work over the past decade has demonstrated the aberrant overexpression of 11ß-HSD1 contributed to the pathophysiological process of metabolic diseases like obesity, type 2 diabetes mellitus, and metabolic syndromes. The inhibition of 11ß-HSD1 represented an attractive therapeutic strategy for the treatment of metabolic diseases. Therefore, great efforts have been devoted to developing 11ß-HSD1 inhibitors based on the diverse molecular scaffolds. This review focused on the structural features of the most important 11ß-HSD1 inhibitors and categorized them into natural products derivatives and synthetic compounds. We also briefly discussed the optimization process, binding modes, structure-activity relationships (SAR) and biological evaluations of each inhibitor. Moreover, the challenges and directions for 11ß-HSD1 inhibitors were discussed, which might provide some useful clues to guide the future discovery of novel 11ß-HSD1 inhibitors.


Asunto(s)
11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1/antagonistas & inhibidores , Productos Biológicos/farmacología , Desarrollo de Medicamentos , Inhibidores Enzimáticos/farmacología , Enfermedades Metabólicas/tratamiento farmacológico , 11-beta-Hidroxiesteroide Deshidrogenasa de Tipo 1/metabolismo , Animales , Productos Biológicos/química , Inhibidores Enzimáticos/química , Humanos , Enfermedades Metabólicas/metabolismo , Estructura Molecular
17.
Clin Chim Acta ; 473: 21-25, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-28807540

RESUMEN

BACKGROUND: On an international scale, the necessity of preoperative coagulation screen remains controversial, yet in China, coagulation screen is still a routine test before surgery required by the Ministry of Health of China. METHODS: A retrospective review of 26,807 patients >18y presenting with problems related to the areas of gynecology and obstetrics from March 2013 to July 2015 was performed, and the rate of major bleeding and the amount of blood lost during surgery were compared among groups of patients grouped according to the values of preoperative APTT, the departments the patients belonged to, or the measures for intervention. RESULTS: Groups with increased APTT had higher rates of major bleeding (9.80% & 26.14% vs 2.77%, P<0.001) and more blood loss (862.9 and 1455.6ml vs 194.0ml, P<0.001). And the same conclusion could be induced in both the obstetric and gynecological patients when they were taken into account separately. For obstetric patients, once those with high bleeding risks, e.g., placental abruption, placental implantation, or preoperative massive hemorrhage were excluded, groups with increased APTT would no longer demonstrated the higher rate of major bleeding (0.91% & 2.38% vs 0%, P=0.409 & 0.833) and would even have a lower amount of blood loss (202.76 and 228.09ml vs 322.13ml, P=0.003 and 0.027). In increased APTT patients without bleeding or bleeding tendency, FFP intervention would not make a difference in the rate of major bleeding (7.69% vs 8.37%, P=0.203) and the amount of blood loss (271.35ml vs 306.63, P=0.865). CONCLUSION: For Chinese patients from the Obstetrics and Gynecology Departments, APTT is a good screen test to predict surgical hemorrhage.


Asunto(s)
Pérdida de Sangre Quirúrgica , Ginecología , Obstetricia , Tiempo de Tromboplastina Parcial , Periodo Preoperatorio , Adulto , China , Femenino , Humanos , Estudios Retrospectivos
18.
Sci Rep ; 6: 30106, 2016 07 29.
Artículo en Inglés | MEDLINE | ID: mdl-27471101

RESUMEN

Artemisinin resistance in Plasmodium falciparum threatens global efforts in the elimination or eradication of malaria. Several studies have associated mutations in the PfATP6 gene in conjunction with artemisinin resistance, but the underlying molecular mechanism of the resistance remains unexplored. Associated mutations act as a biomarker to measure the artemisinin efficacy. In the proposed work, we have analyzed the binding affinity and efficacy between PfATP6 and artemisinin in the presence of L263D, L263E and L263K mutations. Furthermore, we performed virtual screening to identify potential compounds to inhibit the PfATP6 mutant proteins. In this study, we observed that artemisinin binding affinity with PfATP6 gets affected by L263D, L263E and L263K mutations. This in silico elucidation of artemisinin resistance enhanced the identification of novel compounds (CID: 10595058 and 10625452) which showed good binding affinity and efficacy with L263D, L263E and L263K mutant proteins in molecular docking and molecular dynamics simulations studies. Owing to the high propensity of the parasite to drug resistance the need for new antimalarial drugs will persist until the malarial parasites are eventually eradicated. The two compounds identified in this study can be tested in in vitro and in vivo experiments as possible candidates for the designing of new potential antimalarial drugs.


Asunto(s)
Antimaláricos/farmacología , Artemisininas/farmacología , ATPasas Transportadoras de Calcio/genética , Resistencia a Medicamentos/efectos de los fármacos , Resistencia a Medicamentos/genética , Malaria Falciparum/tratamiento farmacológico , Mutación/efectos de los fármacos , Humanos , Simulación del Acoplamiento Molecular/métodos , Proteínas Mutantes/genética , Mutación/genética , Plasmodium falciparum/efectos de los fármacos , Plasmodium falciparum/genética , Unión Proteica/efectos de los fármacos , Unión Proteica/genética
19.
Tumour Biol ; 37(8): 10643-52, 2016 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26867766

RESUMEN

The use of cytolytic peptides with potential therapeutic properties is a promising approach to cancer therapy due to their convenient automated synthesis and their capacity for modifications. However, the use of cytolytic peptides is limited due to their nonspecific cytolytic activity. In this study, we designed a tumor-targeting proapoptotic system based on an amphipathic D-amino acid-modified apoptotic peptide, KLA, a variant of (KLAKLAK)2, which is fused with a linear tumor-penetrating homing peptide iRGD through specific cathepsin B (CTSB) cleavage sequences that are overexpressed in many types of tumor tissues. Our data show that the procytotoxic peptide D(KLAKLAKKLAKLA)K-GG-iRGD (m(KLA)-iRGD) is internalized into cultured tumor cells through a neuropilin-1 (NRP1)-activated pathway by iRGD delivery. Once inside the cells, the peptide triggers rapid apoptosis through both the mitochondrial-induced apoptotic pathway and the death receptor pathway in NRP1+/αvß3/CTSB+ tumor cells. Furthermore, m(KLA)-iRGD spread extensively within the tumor tissue when it was injected into 4T1 tumor-bearing mice. The m(KLA)-iRGD peptide inhibited tumor growth to a certain degree, resulting in a significant reduction in tumor volume (P < 0.05) and the total inhibition of metastasis at the end of the treatment. These results suggest that m(KLA)-iRGD has the potential for development as a new antitumor drug.


Asunto(s)
Antineoplásicos/uso terapéutico , Apoptosis/efectos de los fármacos , Catepsina B/metabolismo , Péptidos de Penetración Celular/uso terapéutico , Neoplasias Mamarias Experimentales/tratamiento farmacológico , Oligopéptidos/administración & dosificación , Profármacos/uso terapéutico , Activación Metabólica , Secuencia de Aminoácidos , Animales , Antineoplásicos/administración & dosificación , Antineoplásicos/farmacocinética , Neoplasias de la Mama/patología , División Celular/efectos de los fármacos , Línea Celular Tumoral , Péptidos de Penetración Celular/administración & dosificación , Péptidos de Penetración Celular/farmacocinética , Portadores de Fármacos/administración & dosificación , Ensayos de Selección de Medicamentos Antitumorales , Femenino , Humanos , Neoplasias Mamarias Experimentales/patología , Melanoma Experimental/patología , Ratones , Ratones Endogámicos BALB C , Mitocondrias/efectos de los fármacos , Metástasis de la Neoplasia , Neuropilina-1/fisiología , Profármacos/administración & dosificación , Profármacos/farmacocinética , Receptor fas/fisiología
20.
Bone ; 45(3): 534-44, 2009 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-19501202

RESUMEN

BACKGROUND: Epimedium-derived flavonoids (EFs) have been reported to prevent bone loss in ovariectomized (OVX) rats and late postmenopausal women but the underlying mechanism of the anabolic effect is unknown. OBJECTIVE: This study aimed to investigate the effect of EFs on osteoporotic bone using histomorphometry and on osteoblastogenesis/adipogenesis of bone marrow stromal cells (BMSCs). METHODS: 11-month-old female Wistar rats were divided into Sham, OVX, Sham+soluble vehicle (Sham+SV), OVX+SV and OVX+EFs (10 mg/kg/day) groups. 3 months after surgery, rats from the first two groups were euthanized to verify the establishment of OVX-induced osteoporosis. Other groups were orally treated with either daily SV or EFs for 4 months. At sacrifice, serum was analyzed for the levels of osteocalcin and TRACP 5b, BMD in the proximal femur was measured by pQCT. Static and dynamic bone histomorphometry was performed in proximal tibiae with microCT and undecalcified sections, respectively. The effect of EF treatment on differentiation of rat BMSCs was assessed by colony formation assays and gene expression analysis, respectively. Gene expression, ALP activity and adipocyte numbers were determined in differentiating human BMSCs after exposure to conditioned serum from SV- or EFs-treated OVX rats. RESULTS: The serum level of osteocalcin was higher and TRACP 5b was lower in EFs versus SV-treated OVX rats. BMD, BV/TV, Tb.N and Conn.D in EFs-treated OVX rats were significantly greater than those of SV-treated OVX rats. Bone histomorphometric parameters OS/BS, MAR, and BFR/BS were significantly higher in EFs versus SV-treated OVX rats. EFs significantly increased osteogenesis and decreased adipogenesis of BMSCs, as evidenced by CFU-ALP and CFU-Adipo assays, respectively. The mRNA level of Runx2 and bone sailoprotein was significantly higher while PPARgamma2 was significantly lower in BMSCs from EFs-treated versus SV-treated OVX rats. ALP activity and Runx2 mRNA was significantly higher while adipocyte number and PPARgamma2 mRNA was significantly lower in human BMSCs after exposure to conditioned serum from EFs versus SV-treated OVX rats. CONCLUSION: EFs exerted anabolic effect on osteoporotic bone by concomitantly promoting osteogenic and suppressing adipogenic differentiation of BMSCs.


Asunto(s)
Adipogénesis/efectos de los fármacos , Anabolizantes/farmacología , Células de la Médula Ósea/efectos de los fármacos , Epimedium/química , Flavonoides/farmacología , Osteogénesis/efectos de los fármacos , Osteoporosis/patología , Animales , Biomarcadores/análisis , Células de la Médula Ósea/citología , Diferenciación Celular , Células Cultivadas , Femenino , Osteocalcina/sangre , Osteoporosis/metabolismo , Ovariectomía , Ratas , Ratas Wistar , Células del Estroma/citología , Células del Estroma/efectos de los fármacos
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