Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 17 de 17
Filtrar
Más filtros











Base de datos
Intervalo de año de publicación
1.
Heliyon ; 10(17): e36918, 2024 Sep 15.
Artículo en Inglés | MEDLINE | ID: mdl-39286159

RESUMEN

Objective: Based on the visualization and analysis of the CiteSpace software, we aimed to explore the current research status and development trend of depression caused by external therapies in traditional Chinese medicine (TCM) and to provide a reference for further research in this field. Methods: In the China National Knowledge Infrastructure, Wanfang, Web of Science, and PubMed databases, relevant articles on external therapies in TCM for depression were selected as the research objects, and CiteSpace performed the bibliometric analysis. Results: In total, 1672 Chinese and 441 English articles were included after CiteSpace was used to remove duplicate articles and perform manual screening. The Chinese articles were analyzed, and the overall issuance showed an upward trend; the core author was Tu Ya, and the institution with the highest article production was Heilongjiang University of Traditional Chinese Medicine. The English articles were analyzed, and the overall issuance showed an upward trend; the core author was Macpherson, Hugh, and the institution with the highest article production was Guangzhou University of Traditional Chinese Medicine. China ranked first in terms of number and centrality of publications, followed by the United States. The keywords of Chinese and English articles were analyzed to conclude that the research trends in this field were an exploration of therapeutic mechanisms, acupoint application therapy, and assessment of sleep quality, and the research hotspots were the clinical application of external therapies in TCM and the types of underlying diseases. Conclusion: This study comprehensively and objectively summarized the relevant literature on external therapies in TCM for depression. It highlights the direction for further exploration by revealing and analyzing the research hotspots and trends in this field.

2.
Br J Cancer ; 131(7): 1212-1223, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39174739

RESUMEN

BACKGROUND: Liver cancer stem cells (LCSCs) significantly impact chemo-resistance and recurrence in liver cancer. Dopamine receptor D4 (DRD4) is known to enhance the cancer stem cell (CSC) phenotype in glioblastoma and correlates with poor prognosis in some non-central nervous system tumors; however, its influence on LCSCs remains uncertain. METHODS: To investigate the gene and protein expression profiles of DRD4 in LCSCs and non-LCSCs, we utilized transcriptome sequencing and Western blotting analysis. Bioinformatics analysis and immunohistochemistry were employed to assess the correlation between DRD4 expression levels and the pathological characteristics of liver cancer patients. The impact of DRD4 on LCSC phenotypes and signaling pathways were explored using pharmacological or gene-editing techniques. Additionally, the effect of DRD4 on the protein expression and intracellular localization of ß-catenin were examined using Western blotting and immunofluorescence. RESULTS: DRD4 expression is significantly elevated in LCSCs and correlates with short survival in liver cancer. The expression and activity of DRD4 are positive to resistance, self renewal and tumorigenicity in HCC. Mechanistically, DRD4 stabilizes ß-catenin and promotes its entry into the nucleus via activating the PI3K/Akt/GSK-3ß pathway, thereby enhancing LCSC phenotypes. CONCLUSIONS: Inhibiting DRD4 expression and activation offers a promising targeted therapy for eradicating LCSCs and relieve chemo-resistance.


Asunto(s)
Resistencia a Antineoplásicos , Neoplasias Hepáticas , Células Madre Neoplásicas , Proteínas Proto-Oncogénicas c-akt , Receptores de Dopamina D4 , Transducción de Señal , beta Catenina , Humanos , Células Madre Neoplásicas/metabolismo , Células Madre Neoplásicas/patología , Neoplasias Hepáticas/patología , Neoplasias Hepáticas/genética , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/tratamiento farmacológico , Resistencia a Antineoplásicos/genética , beta Catenina/metabolismo , beta Catenina/genética , Receptores de Dopamina D4/genética , Receptores de Dopamina D4/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Ratones , Animales , Línea Celular Tumoral , Fenotipo , Masculino , Regulación Neoplásica de la Expresión Génica , Carcinoma Hepatocelular/patología , Carcinoma Hepatocelular/genética , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/tratamiento farmacológico , Femenino , Ratones Desnudos
3.
Front Neurol ; 14: 1194441, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37426434

RESUMEN

Background: Tension-type headache (TTH) is one of the most common primary headaches. Several studies have confirmed the efficacy of acupuncture therapies for TTH, but it is uncertain which treatment is most effective. Objective: This study aimed to compare the effectiveness and safety of different acupuncture therapies for TTH using Bayesian Network Meta-analysis to provide new ideas for treating TTH. Methods: Nine databases were searched for randomized controlled trials (RCTs) about different acupuncture therapies for TTH up to December 1, 2022. The outcome indicators analyzed in our study were total effective rate, visual analog scale (VAS), headache frequency, and safety. Pairwise meta-analysis and risk of bias assessment were performed using Review Manager 5.4. Stata 15.0 generated a network evidence plot and detected publication bias. Finally, a Bayesian network meta-analysis of the data was used by RStudio. Results: The screening process resulted in 30 RCTs that met the inclusion criteria, including 2,722 patients. Most studies failed to report details of trials and were therefore assessed as unclear risks. Two studies were considered high risk because they did not report on all pre-specified outcome indicators or had incomplete data on outcome indicators. The NMA results showed that for total effective rate, bloodletting therapy had the most considerable SUCRA value (0.93156136), for VAS, head acupuncture combined with Western medicine ranked first (SUCRA = 0.89523571), and acupuncture combined with herbal medicine was the most effective in improving headache frequency (p > 0.05). Conclusion: Acupuncture can be used as one of the complementary or alternative therapies for TTH; bloodletting therapy better improves the overall symptoms of TTH, head acupuncture combined with Western medicine is more effective in reducing VAS scores, and acupuncture combined with herbal medicine seems to reduce headache frequency, but the difference is not statistically significant. Overall, acupuncture for TTH is effective with mild side effects, but future high-quality studies are still necessary. Systematic review registration: https://www.crd.york.ac.uk/prospero/, PROSPERO [CRD42022368749].

4.
Medicine (Baltimore) ; 101(39): e30659, 2022 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-36181083

RESUMEN

BACKGROUND: Rotator cuff injury is a common clinical disorder of the musculoskeletal system. It is one of the most common causes of shoulder pain and shoulder joint dysfunction. Intra-articular injection therapy is one of the common conservative treatments for rotator cuff injury in clinical practice, but scholars have been controversial about the different drugs used for injection therapy and their clinical effectiveness, and there is no complete agreement on the choice of different injectables, and the existing original studies are mostly direct comparisons in 1 arm, lacking indirect comparisons, making it difficult to have a clear and comprehensive understanding. OBJECTIVE: A network Meta-analysis was used to comprehensively compare the effectiveness of drug injection therapies for rotator cuff injuries. METHODS: The PubMed, The Cochrane Library, EMbase, Chinese national knowledge infrastructure, Chinese BioMedical Literature on disc, China Science and Technology Journal Database, and Wan-Fang databases were searched for randomized controlled trials on the effectiveness of steroid injections for the comparative treatment of rotator cuff injury for the period April 19, 2013 to April 19, 2022 (the last decade). Two investigators independently screened the literature, extracted data according to inclusion and exclusion criteria, and evaluated the quality of the literature in parallel. Statistical analysis was performed using Stata 16.0 software to compare the differences in efficacy of each treatment measure and rank the efficacy using the ratio and 95% confidence interval (CI) as the effect indicator. RESULTS: 10 RCTs with a total of 861 patients with rotator cuff injury were included, involving 4 therapeutic measures: corticosteroid injection therapy (COR), platelet-rich plasma injection therapy (PRP), Hyaluronic acid injection therapy (HA), and prolotherapy therapy (PRO).Meta-analysis results showed that the ranking results of the 4 therapeutic measures were: corticosteroid injection + hyaluronic acid injection > platelet-rich plasma injection + corticosteroid injection > corticosteroid injection > platelet-rich plasma injection > PRO > platelet-rich plasma injection + hyaluronic acid injection > hyaluronic acid injection. CONCLUSION: we recommend that corticosteroid injections combined with hyaluronic acid injections can be used for the non-surgical conservative clinical management of rotator cuff injuries.


Asunto(s)
Plasma Rico en Plaquetas , Lesiones del Manguito de los Rotadores , Articulación del Hombro , Corticoesteroides/uso terapéutico , Humanos , Ácido Hialurónico/uso terapéutico , Inyecciones Intraarticulares , Metaanálisis en Red , Lesiones del Manguito de los Rotadores/tratamiento farmacológico , Esteroides , Resultado del Tratamiento
5.
NPJ Biofilms Microbiomes ; 8(1): 72, 2022 09 19.
Artículo en Inglés | MEDLINE | ID: mdl-36123373

RESUMEN

Indoor surfaces are paradoxically presumed to be both colonized by pathogens, necessitating disinfection, and "microbial wastelands." In these resource-poor, dry environments, competition and decay are thought to be important drivers of microbial community composition. However, the relative contributions of these two processes have not been specifically evaluated. To bridge this knowledge gap, we used microcosms to evaluate whether interspecies interactions occur on surfaces. We combined transcriptomics and traditional microbiology techniques to investigate whether competition occurred between two clinically important pathogens, Acinetobacter baumannii and Klebsiella pneumoniae, and a probiotic cleaner containing a consortium of Bacillus species. Probiotic cleaning seeks to take advantage of ecological principles such as competitive exclusion, thus using benign microorganisms to inhibit viable pathogens, but there is limited evidence that competitive exclusion in fact occurs in environments of interest (i.e., indoor surfaces). Our results indicate that competition in this setting has a negligible impact on community composition but may influence the functions expressed by active organisms. Although Bacillus spp. remained viable on surfaces for an extended period of time after application, viable colony forming units (CFUs) of A. baumannii recovered following exposure to a chemical-based detergent with and without Bacillus spp. showed no statistical difference. Similarly, for K. pneumoniae, there were small statistical differences in CFUs between cleaning scenarios with or without Bacillus spp. in the chemical-based detergent. The transcriptome of A. baumannii with and without Bacillus spp. exposure shared a high degree of similarity in overall gene expression, but the transcriptome of K. pneumoniae differed in overall gene expression, including reduced response in genes related to antimicrobial resistance. Together, these results highlight the need to fully understand the underlying biological and ecological mechanisms for community assembly and function on indoor surfaces, as well as having practical implications for cleaning and disinfection strategies for infection prevention.


Asunto(s)
Antiinfecciosos , Probióticos , Detergentes/farmacología , Desinfección/métodos , Klebsiella pneumoniae/genética , Transcriptoma
7.
Sci Total Environ ; 807(Pt 2): 150532, 2022 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-34606868

RESUMEN

Circulating saltwater aquariums hosting marine animals contain a wide range of microorganisms, which have strong implications on promoting animal health. In this study, we investigated the degradation of chloroquine phosphate, an anti-parasitic bath pharmaceutical used in saltwater quarantine and exhibition systems, and attributed the reduction in drug concentration to microbial degradation of chloroquine associated with pipeline microbial communities. To advance our knowledge on chloroquine degradation in aquatic systems, we conducted microbial and chemical analyses on three tropical saltwater systems. Our findings show that aquarium microbiome composition is shaped by sampling location (i.e., tank water and pipeline; PERMANOVA R2 = 0.09992, p = 0.0134), chloroquine dosing (PERMANOVA R2 = 0.05700, p = 0.0030), and whether the aquarium is occupied by marine animals (PERMANOVA R2 = 0.07019, p = 0.0009). Several microbial taxa belonging to the phyla Actinobacteria, Bacteroidetes, Chloroflexi, and Proteobacteria, along with functional genes related to pathways such as phenylethylamine degradation and denitrification, appeared to have differential (relative) abundance between samples where chloroquine degradation was observed and those without degradation (Benjamini-Hochberg adjusted p-value <0.05). Together, these results provide practical mitigation options to prevent or delay the development of chloroquine-degrading microbial communities in saltwater aquariums. Our results further demonstrate the need to improve our understanding of the interactions between nitrogen availability and microbial activity in saltwater systems.


Asunto(s)
Cloroquina
8.
J Org Chem ; 86(18): 12676-12682, 2021 Sep 17.
Artículo en Inglés | MEDLINE | ID: mdl-34472854

RESUMEN

Sulfonyl oxime ethers undergo facile radical substitutions with various amines to yield the corresponding oxime ethers. An efficient arylation of sulfonyl oxime ethers was accomplished under ambient temperature and metal-free conditions, with a wide range of functional group tolerance. Mechanistic investigations indicate that a phenyl radical is involved in the catalytic cycle.

9.
Microb Biotechnol ; 14(3): 798-802, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-33037788

RESUMEN

Humans spend the vast majority of their time indoors where complex interactions occur among indoor anthropogenic chemicals, indoor microbiomes and human occupants. This paper summarizes previous work addressing interactions between anthropogenic chemicals associated with indoor household products and building materials, and microorganisms found within the built environment. Water availability seems to determine the extent to which microbes are impacted by anthropogenic chemicals, since desiccation remains one of the primary stressors regulating microbial viability indoors. Several lines of evidence suggest that both fungi and bacteria are capable of transforming biodegradable ingredients originating from various products used indoors when water is present. Previous research also establishes positive and significant correlations between anthropogenic chemicals that are antimicrobial and antibiotic resistance gene abundance. As researchers move towards understanding complex indoor environments as well as the role of anthropogenic chemicals in shaping microbiomes, in situ activities associated with the viable indoor microbial population merit more attention.


Asunto(s)
Hongos , Microbiota , Bacterias/genética , Materiales de Construcción , Farmacorresistencia Microbiana , Humanos
10.
J Hazard Mater ; 396: 122445, 2020 09 05.
Artículo en Inglés | MEDLINE | ID: mdl-32298860

RESUMEN

Over the past two decades, Ag and Zn nanoparticles have been integrated into various consumer products as a biocide. While some nano-enabled consumer products have been shown to have antibacterial properties, their antibacterial efficacy as well as the human and environmental health outcomes are not fully known. In this study, we examine a nanoparticle-enabled product that also serves as a conduit for human exposure to bacteria: toothbrushes. We utilize a combination of chemical analyses, laboratory experiments, and microscopy to characterize the nano-enabled toothbrush bristles. Our analysis showed the majority of measured Ag and Zn particles ranged from approximately 50 to 100 nm in size and were located on the surface and within bristles. During simulated brushing, antimicrobial bristles released both Ag and Zn, the majority of which was released in particulate form. While our results demonstrate that antimicrobial bristles have enhanced bactericidal properties compared to control samples, we also show that the surface topography influences nanoparticle retention, microbial adhesion, and bactericidal activity. We thus conclude that Ag or Zn content alone is insufficient to predict antimicrobial properties, which are further governed by the bioavailability of Ag or Zn at the bristle surface.


Asunto(s)
Antiinfecciosos , Cepillado Dental , Antibacterianos/farmacología , Diseño de Equipo , Humanos , Microscopía
11.
Trials ; 21(1): 77, 2020 Jan 14.
Artículo en Inglés | MEDLINE | ID: mdl-31937335

RESUMEN

BACKGROUND: Acupoint selection is a key factor in the treatment of diseases and has not been well studied. The aim of this trial is to explore the differences in efficacy between compatible acupoints and a single acupoint for patients with functional dyspepsia (FD). METHODS: This randomized controlled trial will be conducted in the First Affiliated Hospital of Changchun University of Chinese Medicine in China. Two hundred and sixteen FD patients will be randomly assigned to the compatible acupoints group, single acupoint group, or sham acupuncture group. This trial will include a 1-week baseline period, a 4-week treatment period, and a 4-week follow-up period. During the 4-week treatment period, patients will receive 20 sessions of acupuncture (weekly cycles of one session per day for 5 consecutive days followed by a 2-day break). The primary outcome will be a change in the Nepean Dyspepsia Life Quality Index from baseline to after the 4-week treatment period. Secondary outcome measures will include the dyspeptic symptom sum score, Overall Treatment Effect questionnaire, and 36-item Short Form survey. Adverse events also will be recorded. Ultraweak photon emission and metabolomics tests will be performed at baseline and at the end of treatment to explore the mechanisms of the differences between compatible acupoints and a single acupoint. DISCUSSION: The results of this trial will allow us to compare the difference in efficacy between compatible acupoints and a single acupoint. The findings from this trial will be published in peer-reviewed journals. TRIAL REGISTRATION: Acupuncture-Moxibustion Clinical Trial Registry, AMCTR-IPC-18000176, registered on 4 March 2019; Chinese Clinical Trial Registry, ChiCTR1900023983, registered on 23 June 2019.


Asunto(s)
Puntos de Acupuntura/clasificación , Terapia por Acupuntura/métodos , Dispepsia/fisiopatología , Dispepsia/terapia , Terapia por Acupuntura/efectos adversos , Adolescente , Adulto , Estudios de Casos y Controles , China/epidemiología , Dispepsia/psicología , Femenino , Humanos , Masculino , Metabolómica/métodos , Persona de Mediana Edad , Fotones , Calidad de Vida , Proyectos de Investigación , Encuestas y Cuestionarios , Resultado del Tratamiento , Adulto Joven
12.
PLoS Pathog ; 16(1): e1008211, 2020 01.
Artículo en Inglés | MEDLINE | ID: mdl-31971995

RESUMEN

The decades-long global trend of urbanization has led to a population that spends increasing amounts of time indoors. Exposure to microbes in buildings, and specifically in dust, is thus also increasing, and has been linked to various health outcomes and to antibiotic resistance genes (ARGs). These are most efficiently screened using DNA sequencing, but this method does not determine which microbes are viable, nor does it reveal whether their ARGs can actually disseminate to other microbes. We have thus performed the first study to: 1) examine the potential for ARG dissemination in indoor dust microbial communities, and 2) validate the presence of detected mobile ARGs in viable dust bacteria. Specifically, we integrated 166 dust metagenomes from 43 different buildings. Sequences were assembled, annotated, and screened for potential integrons, transposons, plasmids, and associated ARGs. The same dust samples were further investigated using cultivation and isolate genome and plasmid sequencing. Potential ARGs were detected in dust isolate genomes, and we confirmed their placement on mobile genetic elements using long-read sequencing. We found 183 ARGs, of which 52 were potentially mobile (associated with a putative plasmid, transposon or integron). One dust isolate related to Staphylococcus equorum proved to contain a plasmid carrying an ARG that was detected metagenomically and confirmed through whole genome and plasmid sequencing. This study thus highlights the power of combining cultivation with metagenomics to assess the risk of potentially mobile ARGs for public health.


Asunto(s)
Contaminación del Aire Interior , Farmacorresistencia Microbiana/genética , Polvo , Genes Bacterianos , Microbiota/genética , Microbiología Ambiental , Transferencia de Gen Horizontal , Genoma Bacteriano , Metagenómica
13.
J Expo Sci Environ Epidemiol ; 30(1): 1-15, 2020 01.
Artículo en Inglés | MEDLINE | ID: mdl-31591493

RESUMEN

The indoor environment is an important source of microbial exposures for its human occupants. While we naturally want to favor positive health outcomes, built environment design and operation may counter-intuitively favor negative health outcomes, particularly with regard to antibiotic resistance. Indoor environments contain microbes from both human and non-human origins, providing a unique venue for microbial interactions, including horizontal gene transfer. Furthermore, stressors present in the built environment could favor the exchange of genetic material in general and the retention of antibiotic resistance genes in particular. Intrinsic and acquired antibiotic resistance both pose a potential threat to human health; these phenomena need to be considered and controlled separately. The presence of both environmental and human-associated microbes, along with their associated antibiotic resistance genes, in the face of stressors, including antimicrobial chemicals, creates a unique opportunity for the undesirable spread of antibiotic resistance. In this review, we summarize studies and findings related to various interactions between human-associated bacteria, environmental bacteria, and built environment conditions, and particularly their relation to antibiotic resistance, aiming to guide "healthy" building design.


Asunto(s)
Farmacorresistencia Microbiana/fisiología , Antibacterianos/farmacología , Bacterias/genética , Farmacorresistencia Microbiana/genética , Ecología , Transferencia de Gen Horizontal , Humanos
14.
Indoor Air ; 29(6): 880-894, 2019 11.
Artículo en Inglés | MEDLINE | ID: mdl-31429989

RESUMEN

Since the advent of soap, personal hygiene practices have revolved around removal, sterilization, and disinfection-both of visible soil and microscopic organisms-for a myriad of cultural, aesthetic, or health-related reasons. Cleaning methods and products vary widely in their recommended use, effectiveness, risk to users or building occupants, environmental sustainability, and ecological impact. Advancements in science and technology have facilitated in-depth analyses of the indoor microbiome, and studies in this field suggest that the traditional "scorched-earth cleaning" mentality-that surfaces must be completely sterilized and prevent microbial establishment-may contribute to long-term human health consequences. Moreover, the materials, products, activities, and microbial communities indoors all contribute to, or remove, chemical species to the indoor environment. This review examines the effects of cleaning with respect to the interaction of chemistry, indoor microbiology, and human health.


Asunto(s)
Contaminación del Aire Interior , Entorno Construido , Desinfección , Humanos , Microbiota
15.
Indoor Air ; 29(4): 551-562, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-30980566

RESUMEN

Microbes in indoor environments are constantly being exposed to antimicrobial surface finishes. Many are rendered non-viable after spending extended periods of time under low-moisture, low-nutrient surface conditions, regardless of whether those surfaces have been amended with antimicrobial chemicals. However, some microorganisms remain viable even after prolonged exposure to these hostile conditions. Work with specific model pathogens makes it difficult to draw general conclusions about how chemical and physical properties of surfaces affect microbes. Here, we explore the survival of a synthetic community of non-model microorganisms isolated from built environments following exposure to three chemically and physically distinct surface finishes. Our findings demonstrated the differences in bacterial survival associated with three chemically and physically distinct materials. Alkaline clay surfaces select for an alkaliphilic bacterium, Kocuria rosea, whereas acidic mold-resistant paint favors Bacillus timonensis, a Gram-negative spore-forming bacterium that also survives on antimicrobial surfaces after 24 hours of exposure. Additionally, antibiotic-resistant Pantoea allii did not exhibit prolonged retention on antimicrobial surfaces. Our controlled microcosm experiment integrates measurement of indoor chemistry and microbiology to elucidate the complex biochemical interactions that influence the indoor microbiome.


Asunto(s)
Microbiología Ambiental , Viabilidad Microbiana , Propiedades de Superficie , Actinobacteria/crecimiento & desarrollo , Contaminación del Aire Interior/prevención & control , Antiinfecciosos/farmacología , Bacillus/crecimiento & desarrollo , Enterococcus hirae/crecimiento & desarrollo , Microbacterium , Microbiota , Micrococcaceae/crecimiento & desarrollo , Noroeste de Estados Unidos , Pintura/microbiología , Pantoea/crecimiento & desarrollo
16.
Bioorg Med Chem Lett ; 27(2): 147-151, 2017 01 15.
Artículo en Inglés | MEDLINE | ID: mdl-27956344

RESUMEN

12 novel scopoletin-isoxazole and scopoletin-pyrazole hybrids were designed, synthesized and their chemical structures were confirmed by HR-MS, IR, 1H NMR and 13C NMR spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including HCT-116, Hun7 and SW620 by MTT assay. The screening results showed that six compounds (9a, 9c, 9d, 12a, 18b and 18d) exhibited potent cytotoxic activities with IC50 values below 20µM. Besides, we have further evaluated the growth inhibitory activities of six compounds against the human normal tissue cell lines HFL-1. Especially, compound 9d displayed significant anti-proliferative activity with IC50 values ranging from 8.76µM to 9.83µM and weak cytotoxicity with IC50 value of 90.9µM on normal cells HFL-1, which suggested that isoxazole-based hybrids of scopoletin were an effective chemical modification to improve the anticancer activity of scopoletin.


Asunto(s)
Antineoplásicos/farmacología , Isoxazoles/farmacología , Pirazoles/farmacología , Escopoletina/análogos & derivados , Escopoletina/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/toxicidad , Línea Celular Tumoral , Humanos , Indoles/farmacología , Isoxazoles/síntesis química , Isoxazoles/toxicidad , Pirazoles/síntesis química , Pirazoles/toxicidad , Pirroles/farmacología , Escopoletina/síntesis química , Escopoletina/toxicidad , Sunitinib
17.
Eur J Med Chem ; 93: 300-7, 2015 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-25703298

RESUMEN

A series of hybrids of scopoletin and substituted cinnamic acid were designed, synthesized and evaluated in vitro and in vivo against five human tumor cell lines [MCF-7, MDA-MB-231, A549, HCT-116, and HeLa] with doxorubicin as the positive control. Compounds 17a, 17b, 17c and 17g exhibited potent cytotoxic activity. Especially, compound 17b displayed broad spectrum activity with IC50 values ranging from 0.249 µM to 0.684 µM. Moreover, in a preliminary pharmacological study, 17b not only remarkably induced cellular apoptosis, but also clearly induced A549 cells cycle arrest at S phase. In vivo study showed that 17b significantly suppressed tumor growth in a dose-dependent manner without causing the loss of the mean body weight of mice, which was superior to doxorubicin. These preliminary results indicate that 17b is an optimal anti-cancer leading compound and merit further structural modification.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Cinamatos/química , Escopoletina/química , Escopoletina/farmacología , Animales , Antineoplásicos/síntesis química , Apoptosis/efectos de los fármacos , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Técnicas de Química Sintética , Femenino , Humanos , Ratones , Escopoletina/síntesis química , Ensayos Antitumor por Modelo de Xenoinjerto
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA