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1.
PeerJ ; 12: e17111, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38525272

RESUMO

Background: Lymph node involvement significantly impacts the survival of gastric cancer patients and is a crucial factor in determining the appropriate treatment. This study aimed to evaluate the potential of enhanced computed tomography (CT)-based radiomics in predicting lymph node metastasis (LNM) and survival in patients with gastric cancer before surgery. Methods: Retrospective analysis of clinical data from 192 patients diagnosed with gastric carcinoma was conducted. The patients were randomly divided into a training cohort (n = 128) and a validation cohort (n = 64). Radiomic features of CT images were extracted using the Pyradiomics software platform, and distinctive features were further selected using a Lasso Cox regression model. Features significantly associated with LNM were identified through univariate and multivariate analyses and combined with radiomic scores to create a nomogram model for predicting lymph node involvement before surgery. The predictive performance of radiomics features, CT-reported lymph node status, and the nomogram model for LNM were compared in the training and validation cohorts by plotting receiver operating characteristic (ROC) curves. High-risk and low-risk groups were identified in both cohorts based on the cut-off value of 0.582 within the radiomics evaluation scheme, and survival rates were compared. Results: Seven radiomic features were identified and selected, and patients were stratified into high-risk and low-risk groups using a 0.582 cut-off radiomics score. Univariate and multivariate analyses revealed that radiomics features, diabetes mellitus, Nutrition Risk Screening (NRS) 2002 score, and CT-reported lymph node status were significant predictors of LNM in patients with gastric cancer. A predictive nomogram model was developed by combining these predictors with the radiomics score, which accurately predicted LNM in gastric cancer patients before surgery and outperformed other models in terms of accuracy and sensitivity. The AUC values for the training and validation cohorts were 0.82 and 0.722, respectively. The high-risk and low-risk groups in both the training and validation cohorts showed significant differences in survival rates. Conclusion: The radiomics nomogram, based on contrast-enhanced computed tomography (CECT ), is a promising non-invasive tool for preoperatively predicting LNM in gastric cancer patients and postoperative survival.


Assuntos
Neoplasias Gástricas , Humanos , Metástase Linfática/diagnóstico por imagem , Nomogramas , Radiômica , Estudos Retrospectivos , Neoplasias Gástricas/diagnóstico por imagem , Tomografia Computadorizada por Raios X
2.
Sci Rep ; 13(1): 21459, 2023 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-38052914

RESUMO

The signal in the receiver is mainly a combination of different modulation types due to the complex electromagnetic environment, which makes the modulation recognition of the mixed signal a hot topic in recent years. In response to the poor adaptability of existing mixed signals recognition methods, this paper proposes a new recognition method for mixed signals based on cyclic spectrum projection and deep neural network. Firstly, through theoretical derivation, we prove the feasibility of using cyclic spectrum for mixed communication signal identification. Then, we adopt grayscale projections on the two-dimensional cyclic spectrum as identifying representation. And a new nonlinear piecewise mapping and directed pseudo-clustering method are used to enhance the above-mentioned grayscale images, which reduces the impact of energy ratios and symbol rates on signal identification. Finally, we use deep neural networks to extract deep abstract modulation information to achieve effective recognition of mixed signals. Simulation results show that the proposed method is robust against noise. When signal-to-noise ratio is not less than 0 dB, the average recognition rate is greater than 95%. Furthermore, this method exhibits good robustness towards the changes in signal symbol rates and energy ratios between mixed signals.

3.
Spectrochim Acta A Mol Biomol Spectrosc ; 294: 122488, 2023 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-36822121

RESUMO

Exploring novel dithienylethenes (DTEs) with efficient photochromism has drawn increasing attention in virtue of the potential applications for photoelectric functional materials. In this contribution, we presented two novel acceptor-acceptor (A-A) type DTE derivatives (4a and 4b) by incorporating the diestervinyl moieties with strong electron-withdrawing capacity into two sides of DTE skeleton. The corresponding structures were well confirmed by the NMR (1H and 13C) and HRMS. When irradiated alternately with ultraviolet and visible light, 4a and 4b showed efficient photochromism in toluene, chloroform and DMSO, clearly implying a solvent-dependence feature. Moreover, excellent photoswitching behaviors were also observed in the poly(methyl methacrylate) (PMMA) film. The density functional theory (DFT) calculations suggested that strong Acceptor-Acceptor effect plays a dominative role in the efficient photochromic performance. Hence, this study will provide a useful guidance for developing high-performance DTE derivatives in multi-media.

4.
J Cancer ; 11(20): 6133-6139, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32922553

RESUMO

Background: We aimed to determine whether splenic features change during tumor progression by evaluating the clinicopathological characteristics relevant to splenic density in patients with gastric cancer (GC) and identify a new predictive indicator of prognosis and chemotherapy benefits. Methods: In the present analysis, 408 patients who underwent gastrectomy were included. Density was expressed in mean spleen Hounsfield units on computed tomography. Other clinical characteristics and detailed follow-up data were collected. The cutoff splenic density was 47.8 by the Xtile software. The R software was used for characteristic differential analysis in patients with different splenic densities. The Cox proportional hazards model and forest plot were used for prognosis and chemotherapy benefit analyses. Results: Patients with low splenic density had significantly worse 3-year disease-free survival (DFS) and overall survival (OS) rates (high vs low splenic density: DFS, 63.4% vs 44.6%, p<0.001; OS, 69.8% vs 52.4%, p<0.001). Splenic density showed strong negative correlations with age, number of metastasized lymph nodes, tumor size, and depth of tumor invasion. The benefits of adjuvant chemotherapy were better in the low splenic density group (hazard ratio of OS, 0.546; p=0.001) than in the low-density group (hazard ratio of OS, 0.701; p=0.106). Conclusions: Patients with low splenic density tended to have more advanced tumors and poor prognosis, but better chemotherapy benefits. Splenic density can be regarded as a new indicator of chemotherapy benefits and increase the accuracy of preoperative staging evaluation. Moreover, preoperative evaluation of splenic density may help establish individualized treatment strategies.

5.
Front Oncol ; 10: 1050, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32714867

RESUMO

Objectives: The present study aimed to explore the association between spleen density and post-operative outcomes of patients after curative gastrectomy. Methods: From June 2014 to December 2015, we conducted a retrospective study to analyze pertinent clinical data from gastric cancer patients who underwent gastrectomy at the First and the Second Affiliated Hospital of Wenzhou Medical University. Spleen density was determined via computed tomography scans. Univariate and multivariate analyses were performed to determine the risk factors associated with post-operative outcomes after gastric cancer surgery. Results: Three hundred and ninety five patients were included, of whom 98 (24.8%) were defined as having a diffuse reduction of spleen density based on diagnostic cutoff values (spleen density ≤43.89 HU). Multivariate analysis revealed diffuse reduction of spleen density as an independent risk factor for post-operative complications and long-term overall survival. Conclusions: Spleen density can predict severe postoperative complications and long-term overall survival in gastric cancer patients. As an imaging evaluation method, spleen density is a novel tool can be used in clinical as a prognostic predictor for patients with gastric cancer.

6.
J Biomed Mater Res A ; 108(9): 1816-1823, 2020 09.
Artigo em Inglês | MEDLINE | ID: mdl-32276284

RESUMO

IR808, an IR780 derivative, is capable of fluorescently imaging and photodynamic therapy in vitro and in vivo. However, its application is greatly hampered by hydrophobicity, toxicity and nonspecific delivery to the targeting tissue and that causes accumulation in the liver and kidney. In order to overcome these limitations, we prepared IR808-PEG-FA from IR808, amino-terminated poly(ethylene glycol) (NH2 -PEG-NH2 , denoted as PEG) and folate (FA). PEG, an accepted hydrophilic medicinal agent, was introduced to improve hydrophobicity, and FA was used to increase targeting ability of the conjugate. The obtained product provides a good water solubility and stronger light intensity in near infrared (NIR)-imaging, and CCK-8 test demonstrated which had no appreciable toxicity. In addition, the cell uptake results indicated that IR808-PEG-FA was specifically targeted to positive tumors cells with folate receptor (FR) compared with IR808, and thus it may be used as a novel diagnostic agent or imaging-guided agent for cancer treatment. So this article provides a way to improve hydrophobicity, optical stability and targeting ability in the field of nano-probe for fluorochromes.


Assuntos
Corantes Fluorescentes/análise , Ácido Fólico/análogos & derivados , Polietilenoglicóis/análise , Células A549 , Sobrevivência Celular/efeitos dos fármacos , Corantes Fluorescentes/síntese química , Corantes Fluorescentes/toxicidade , Ácido Fólico/análise , Ácido Fólico/síntese química , Ácido Fólico/toxicidade , Humanos , Células MCF-7 , Neoplasias/diagnóstico por imagem , Imagem Óptica , Fotoquimioterapia , Polietilenoglicóis/síntese química , Polietilenoglicóis/toxicidade
7.
Food Chem ; 289: 313-319, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-30955618

RESUMO

A method was developed to simultaneously determine eight bioactive compounds in edible oil based on ultrasound-assisted saponification, liquid-liquid extraction and liquid chromatography coupled with tandem mass spectrometry. Central composite design was employed to optimize ultrasonic temperature and time of saponification. Sample treatment was conducted by ultrasound-assisted saponification at temperature of 75 °C for 40 min. Limits of detection and limits of quantification ranged from 2.0 to 3.2 and from 6.1 to 10.0 ng/mL, respectively. Linear correlations were obtained (R2 > 0.99) and the recoveries at three spiked levels were between 81.7% and 112.0%. This method was employed to determine eight compounds in camellia oils and olive oils. As results, the contents of stigmasterol, δ-tocopherol, γ-tocopherol, ß-carotene and lutein in camellia oils were significantly higher than those in olive oils (p < 0.05). The proposed method can be successfully used to determination of these eight active compounds in camellia oil and other edible oils.


Assuntos
Carotenoides/análise , Fitosteróis/análise , Óleos de Plantas/química , Espectrometria de Massas em Tandem/métodos , Tocoferóis/análise , Camellia/química , Camellia/metabolismo , Carotenoides/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Limite de Detecção , Extração Líquido-Líquido , Fitosteróis/isolamento & purificação , Sonicação , Estigmasterol/análise , Estigmasterol/isolamento & purificação , Tocoferóis/isolamento & purificação
8.
Food Funct ; 10(3): 1302-1316, 2019 Mar 20.
Artigo em Inglês | MEDLINE | ID: mdl-30793717

RESUMO

Increasing evidence indicates that high-fat diet (HFD) is a predisposing factor for metabolic syndrome-associated systemic inflammation and nonalcoholic fatty liver disease (NAFLD). Tumor necrosis factor-α/receptor-interacting protein kinase 3 (TNF-α/RIPK3) axis has recently become regarded as an important regulator and contributor in many inflammation-related diseases. Fisetin (Fn) is a bioactive flavonoid polyphenol with anti-inflammatory and anti-tumor activity. Lately it has gained increasing attention due to its potential advantages in prevention of tumors, metabolic disorders, neuroinflammation and chronic liver injury. However, its role in NAFLD is still not fully understood. Thus, we studied whether prolonged HFD causes TNF-α/RIPK3 activation-associated hepatic steatosis, further evaluating the protective effects of Fn in HFD-fed mice. As expected, HFD promotes metabolic syndrome and pro-inflammatory cytokine generation in serum, enhances liver inflammatory infiltration-related lipid accumulation by increase of TNF-α/RIPK3 activation, ultimately resulting in development of nonalcoholic steatohepatitis. In contrast to this, dietary Fn intervention could suppress metabolic disorder and HFD-triggered hepatic function loss, downregulate TNF-α/RIPK3 signaling-associated hepatic inflammation, balance lipid metabolism-related gene expression, and finally inhibit lipid accumulation and steatohepatitis. Hence, Fn restrains HFD-induced hepatic inflammation and lipid deposition by downregulating metabolic disorder and excessive liver inflammation-associated TNF-α/RIPK3 axis activation.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Dieta Hiperlipídica/efeitos adversos , Flavonoides/uso terapêutico , Proteína Serina-Treonina Quinases de Interação com Receptores/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Animais , Linhagem Celular , Regulação para Baixo/efeitos dos fármacos , Flavonóis , Regulação da Expressão Gênica/efeitos dos fármacos , Hepatócitos/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Distribuição Aleatória
9.
Food Sci Nutr ; 6(8): 2355-2362, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30510736

RESUMO

The radical scavenging capabilities of the extracts from eleven edible vegetable oils were investigated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis-3- ethylbenzothiazoline-6-sulfonic acid (ABTS), and ferric reducing ability of plasma (FRAP) assays. The results indicated that rapeseed oil and sesame oil showed higher radical scavenging abilities than other vegetable oils. When the radical scavenging capabilities of the extracts from virgin camellia oils and commercially available refined camellia oils were evaluated by FRAP assay, the results showed that the antioxidant capabilities of the former were higher than the latter. Therefore, it is recommended that moderate refining processes should be taken to minimize the loss of antioxidant components and people consume virgin oils or less processed edible vegetable oils for higher antioxidant activities.

10.
Mater Sci Eng C Mater Biol Appl ; 91: 297-302, 2018 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-30033258

RESUMO

In this paper, the micro-structure of amphiphilic copolymer Polylactic acid-Polyethylene glycol-Folate (PLA-PEG-FA) was studied firstly by a differential scanning calorimetry (DSC). During the process of nanoparticles (NPs) preparation, we found good inter-structure consistency of polymer was the precondition for forming into stable NPs, and those with micro-phase separation structure were prepared of NPs within limits. Hemolytic test and CCK-8 assay results demonstrated the biotoxicity of both NPs and whose leaching liquor was far below related toxicity standards. Two kinds of cell, human breast cancer cell line (MCF-7) and human umbilical vein endothelial cells (EC), showed different manners in test of NPs size-cell proliferation relationship, respectively. Monitored by a nuclear magnetic resonance (NMR) and a gel permeation chromatography (GPC), the degradation behavior of NPs in aqueous solution indicated amide bond break more difficultly than ester bond, and FA classic proton peak disappeared in the third week, meanwhile lactic acid (LA) unit number became 25% of the initial. Finally the NPs was completely degraded in the eighth week. In the whole process, NPs underwent a change from compact to loose state. We hope these results will benefit to improve design of drug delivery system in nanomedicine, which could offer the selection rule for amphiphilic polymer NPs on material and size.


Assuntos
Portadores de Fármacos , Ácido Fólico , Teste de Materiais , Nanopartículas/química , Poliésteres , Polietilenoglicóis , Portadores de Fármacos/química , Portadores de Fármacos/farmacologia , Avaliação de Medicamentos , Ácido Fólico/química , Ácido Fólico/farmacologia , Células Endoteliais da Veia Umbilical Humana , Humanos , Células MCF-7 , Poliésteres/química , Poliésteres/farmacologia , Polietilenoglicóis/química , Polietilenoglicóis/farmacologia
11.
J Chromatogr Sci ; 55(10): 1037-1042, 2017 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-28977404

RESUMO

A simple, optimized and sensitive high-performance liquid chromatograph method with ultraviolet (UV) detection (HPLC/UV) was developed and validated for determination of isochlorogenic acid A in rat plasma. The analytes were successfully separated on a Shodex C18 column (5 µm particle size, 250 mm × 4.6 mm, i.d.), the mobile phase contained 0.1% phosphoric acid aqueous solution (solvent A) and methanol (solvent B) (50:50, v/v) at a flow rate of 1.0 mL/min. The wavelength for UV detection was set at 300 nm and the column temperature was maintained in 30°C. Calibration curve for isochlorogenic acid A was found to be good linear over the range of 0.04-40 µg/mL (r = 0.9998). The intra- and inter-day precisions (relative standard deviation) were within 7.63% and the assay accuracy (RE) ranged from -1.41 to 3.25%. The limit of detection and the lower limit of quantification were 0.012 and 0.04 µg/mL, respectively. The validated method was successfully applied to pharmacokinetic study of isochlorogenic acid A in rats for the first time. The pharmacokinetic parameters were evaluated after the rats were administered intravenously and intragastrically isochlorogenic acid A at the single dose of 18 mg/kg, respectively. The absolute bioavailability was calculated to be 22.6%.


Assuntos
Ácido Clorogênico/análogos & derivados , Cromatografia Líquida de Alta Pressão/métodos , Animais , Ácido Clorogênico/sangue , Ácido Clorogênico/química , Ácido Clorogênico/farmacocinética , Limite de Detecção , Modelos Lineares , Masculino , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes
12.
Artigo em Inglês | MEDLINE | ID: mdl-28572828

RESUMO

Apigenin is a nonmutagenic flavonoid that has antitumor properties. Polyamines are ubiquitous cellular polycations, which play an important role in the proliferation and differentiation of cancer cells. Highly regulated pathways control the biosynthesis and degradation of polyamines. Ornithine decarboxylase (ODC) is the rate-limiting enzyme in the metabolism, and spermidine/spermine-N1-Acetyl transferase (SSAT) is the rate-limiting enzyme in the catabolism of polyamines. In the current study, the effect of increasing concentrations of apigenin on polyamine levels, ODC and SSAT protein expression, mRNA expression, cell proliferation and apoptosis, and the production of reactive oxygen species (ROS) was investigated in SW620 colon cancer cells. The results showed that apigenin significantly reduced cell proliferation, decreased the levels of spermidine and spermine, and increased previously downregulated putrescine contents. Apigenin also enhanced SSAT protein and mRNA levels and the production of reactive oxygen species in SW620 cells, though it had no significant effect on the levels of ODC protein or mRNA. Apigenin appears to decrease the proliferation rate of human SW620 cells by facilitating SSAT expression to induce polyamine catabolism and increasing ROS levels to induce cell apoptosis.

13.
Pharm Biol ; 55(1): 554-559, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-27937684

RESUMO

CONTEXT: Yinzhihuang oral liquid, a well-known Chinese herbal formula, is a clinical drug for the treatment of neonatal jaundice, and a number of clinical trials have been published addressing this issue, but there is no comprehensive analysis that evaluates its efficacy for the treatment of newborn with hyperbilirubinaemia. OBJECTIVE: A meta-analysis was conducted to evaluate the efficacy of Yinzhihuang oral liquid on neonatal jaundice. METHODS: Search was performed throughout PubMed, Cochrane Library, EMBASE, Ovid, Wanfang, VIP Medicine Information System (VMIS) and China National Knowledge Infrastructure (CNKI) databases up to December 2015. The search terms were (Yinzhihuang oral liquid or Yinzhihuang oral solution), (neonatal jaundice or neonatal hyperbilirubinaemia), and (efficacy). Review Manager 5.2 software was used for analyzing the data. Data were pooled by using the random-effects models and expressed as relative ratio (RR), standardized mean difference (SMD) or mean difference (MD) with a 95% confidence interval (CI). The Cochrane tool was applied to assess the risk of bias of the trials. RESULTS: Yinzhihuang oral liquid in conjunction with other therapy increased effective rate of neonatal jaundice therapy (RR =1.14, 95%CI: 1.08-1.20). Yinzhihuang oral liquid significantly eliminated overproduced bilirubin which was measured by TSB or TCB at the third day and fifth day during the treatment {[third day, SMD = -1.63, 95%CI: -2.20 to (-1.06)], [fifth day, SMD = -5.00, 95%CI: -7.88 to (-2.12)]}; Yinzhihuang oral liquid significantly shortened jaundice subsiding time [MD = -3.20, 95%CI: -6.01to (-0.39)]. CONCLUSION: Yinzhihuang oral liquid can be considered as an effective treatment option for neonatal jaundice.


Assuntos
Bilirrubina/sangue , Medicamentos de Ervas Chinesas/uso terapêutico , Hiperbilirrubinemia Neonatal/tratamento farmacológico , Biomarcadores/sangue , Distribuição de Qui-Quadrado , Medicamentos de Ervas Chinesas/efeitos adversos , Humanos , Hiperbilirrubinemia Neonatal/sangue , Hiperbilirrubinemia Neonatal/diagnóstico , Recém-Nascido , Razão de Chances , Fitoterapia , Plantas Medicinais , Resultado do Tratamento
14.
Pharm Biol ; 54(10): 2168-75, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26983455

RESUMO

Context Oxymatrine (OMT) is beneficial to human health by exerting various biological effects. Objective To investigate the absorption mechanism of OMT and discover absorption enhancers using Madin-Darby canine kidney (MDCK) cell monolayers. Materials and methods Concentration effects on the transport of OMT were measured in the range of 1.0 × 10(-5)-1.0 × 10(-3) M in 2 h. Then, the effect of time, direction, temperature and pH on the transport of OMT at 10(-4) M was studied. Moreover, Papp of OMT was determined in the absence/presence of cyclosporine and surfactants at 100 µM to further confirm the relative transport mechanism. Results The Papp AP→BL ranged from (3.040 ± 0.23) × 10(-6) to (3.697 ± 0.19) × 10(-6 )cm/s as the concentration varied from 10(-5) to 10(-3) M. OMT showed similar Papp at 4 and 37 °C (p > 0.05). Increasing the apical pH 7.4 and 8.0 resulted in Papp versus pH 5.0 (p < 0.01). Furthermore, in the presence of cyclosporine and surfactants including sodium citrate, sodium dodecyl sulphate (SDS) and deoxysodium cholate, Papp was (0.318 ± 0.033) × 10(-5), (0.464 ± 0.048) × 10(-5), (0.897 ± 0.115) × 10(-5) and (1.341 ± 0.122) × 10(-5 )cm/s, respectively. In the presence of surfactants, Papp significantly increased up to 1.5-4.3-fold (p < 0.05). Discussion and conclusion OMT transport across MDCK cell monolayers was by passive diffusion. Sodium citrate, SDS and deoxysodium cholate serve as excellent absorption enhancers which are useful for the related research improving the oral bioavailability of OMT.


Assuntos
Alcaloides/metabolismo , Células Epiteliais/metabolismo , Rim/metabolismo , Quinolizinas/metabolismo , Reabsorção Renal , Animais , Citratos/farmacologia , Ciclosporina/farmacologia , Ácido Desoxicólico/farmacologia , Difusão , Cães , Relação Dose-Resposta a Droga , Células Epiteliais/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Rim/efeitos dos fármacos , Cinética , Modelos Lineares , Células Madin Darby de Rim Canino , Permeabilidade , Reabsorção Renal/efeitos dos fármacos , Citrato de Sódio , Dodecilsulfato de Sódio/farmacologia , Tensoativos/farmacologia , Temperatura
15.
J Pharm Biomed Anal ; 115: 214-24, 2015 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-26232587

RESUMO

A simple and reliable high performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MS) analysis method was established to simultaneously determine thirteen flavonoids of Xiaobuxing-Tang in intestine perfusate, namely onpordin, 3'-O-methylorobol, glycitein, patuletin, genistein, luteolin, quercetin, nepitrin, quercimeritrin, daidzin, patulitrin, quercetagitrin and 3-glucosylisorhamnetin. Detection was performed on a quadrupole mass spectrometer equipped with an electrospray ionization (ESI) source operating in negative ionization mode. Negative ion ESI was used to form deprotonated molecules at m/z 315 for onpordin, m/z 299 for 3'-O-methylorobol, m/z 283 for glycitein, m/z 331 for patuletin, m/z 269 for genistein, m/z 285 for luteolin, m/z 301 for quercetin, m/z 477 for nepitrin, m/z 463 for quercimeritrin, m/z 461 for daidzin, m/z 493 for patulitrin, m/z 479 for quercetagitrin, m/z 477 for 3-glucosylisorhamnetin and m/z 609.2 for rutin. The linearity, sensitivity, selectivity, repeatability, accuracy, precision, recovery and matrix effect of the assay were evaluated. The proposed method was successfully applied to simultaneous determination of these thirteen flavonoids, and using this method, the intestinal absorption profiles of thirteen flavonoids were preliminarily predicted.


Assuntos
Antidepressivos/análise , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/análise , Flavonoides/análise , Espectrometria de Massas por Ionização por Electrospray/métodos , Animais , Antidepressivos/farmacocinética , Calibragem , Estabilidade de Medicamentos , Medicamentos de Ervas Chinesas/farmacocinética , Flavonoides/farmacocinética , Absorção Intestinal , Mucosa Intestinal/metabolismo , Intestinos/irrigação sanguínea , Masculino , Perfusão , Ratos Sprague-Dawley , Padrões de Referência , Reprodutibilidade dos Testes , Sensibilidade e Especificidade
16.
Asian Pac J Cancer Prev ; 16(6): 2307-12, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25824755

RESUMO

Curcumol is a sesquiterpene originally isolated from curcuma rhizomes, a component of herbal remedies commonly used in oriental medicine. Its beneficial pharmacological activities have attract significant interest recently. In this study, anti-cancer activity of curcumol was examined with both in vitro and in vivo models. It was found that curcumol exhibited time- and concentration-dependent anti-proliferative effects in SPC-A-1 human lung adenocarcinoma cells with cell cycle arrest in the G0/G1 phase while apoptosis-induction was also confirmed with flow cytometry and morphological analyses. Interestingly, curcumol did not display growth inhibition in MRC-5 human embryonic lung fibroblasts, suggesting the anti-proliferative effects of curcumol were specific to cancer cells. Anti-neoplastic effects of curcumol were also confirmed in tumor bearing mice. Curcumol (60 mg/kg daily) significantly reduced tumor size without causing notable toxicity. In conclusion, curcumol appears a favorable anti-cancer candidate for further development.


Assuntos
Adenocarcinoma/patologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Neoplasias Pulmonares/patologia , Pulmão/patologia , Sesquiterpenos/farmacologia , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma/metabolismo , Animais , Western Blotting , Ciclo Celular/efeitos dos fármacos , Células Cultivadas , Medicamentos de Ervas Chinesas , Citometria de Fluxo , Humanos , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Ensaios Antitumorais Modelo de Xenoenxerto
17.
Pharm Biol ; 52(9): 1150-7, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24635458

RESUMO

CONTEXT: Caffeic acid (CA) is widely distributed in edible plants, and it is beneficial to human health by exerting various biological effects. The potential pharmacological activities of CA are dependent on its absorption in the gastrointestinal tract. OBJECTIVE: To investigate the bioavailability of CA in rats and its absorption properties in the Caco-2 cell model. MATERIALS AND METHODS: A sensitive LC-MS/MS method was successfully applied to determine CA in rat plasma, perfusate, and Hank's balanced salt solution (HBSS). The absolute bioavailability (Fabs) of CA was obtained after i.v. (2 mg/kg) or i.g. administration (10 mg/kg) to rats. Blood samples (approximately 250 µL) were collected from the jugular vein catheter. Pharmacokinetic parameters were calculated using the 3P97 software (version 2.0 PK software; Chinese Society of Mathematical Pharmacology, Anhui, China). The intestinal absorption of CA was explored by the in situ vascularly perfused rat intestinal preparation. CA (5 mg/kg) was administered into the duodenum. Samples (250 µL) were collected from reservoir at specific times, and the same volume fresh perfusate was replaced. The Caco-2 cell model was applied to measure the permeability of CA from the apical to basolateral side (A → B) and from the basolateral to apical side (B → A). RESULTS: The absolute bioavailability (Fabs) of CA was 14.7%, and its intestinal absorption was 12.4%. The Papp A→B values of CA were ranging from (4.87 ± 1.72) × 10(-7) cm/s to (5.05 ± 0.66) × 10(-7) cm/s as the concentration varied from 5 to 15 µg/mL. CONCLUSION: CA was shown to have low oral bioavailability in rats, low intestinal absorption, and poor permeability across Caco-2 cells.


Assuntos
Ácidos Cafeicos/farmacocinética , Absorção Intestinal , Administração Oral , Animais , Disponibilidade Biológica , Células CACO-2 , Cromatografia Líquida/métodos , Feminino , Humanos , Masculino , Permeabilidade , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em Tandem/métodos
18.
Colloids Surf B Biointerfaces ; 102: 130-5, 2013 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-23000678

RESUMO

Folate-conjugated Dol-poly(D,L-lactic acid)-b-poly (ethylene glycol)-folate (Dol-PLA-PEG-FA), was synthesized from dodecanol-poly(D,L-lactic acid), amino-terminated poly(ethylene glycol) and folate. (1)H NMR proved the successful synthesis of Dol-PLA-PEG-FA. Nanoparticles (NPs) were further fabricated from Dol-PLA-PEG-FA by using solvent evaporation-induced interfacial self-assembly method. The size, critical micelle concentration (CMC), cytotoxicity and selecting capability to cancer cells in vitro were examined for Dol-PLA-PEG-FA NPs. The size of NPs showed polymer concentration-dependent phenomenon in the fabrication process, and its polydispersity index (PDI) was very narrow. The CMC was determined as 1.995×10(-4) g/L in aqueous solution, which is much lower than the reported CMC of block copolymer self-assemble micelles. The cytotoxicity evaluation revealed that the obtained NPs2 are non-toxic to either breast cancer cell or normal endothelial cells, and the cell uptake of NPs indicated that the NPs demonstrated much higher selecting capability to breast cancer cells compared to normal fibroblast cells. The possible receptor-mediated endocytosis pathway mechanism was proposed. Based on the above results, it could be concluded that Dol-PLA-PEG-FA polymer and its nanoparticles can be potentially used as a safe drug carrier with strong tumor cells targeting capability for tumor chemotherapy.


Assuntos
Ácido Fólico/análogos & derivados , Nanopartículas/química , Polietilenoglicóis/química , Sobrevivência Celular/efeitos dos fármacos , Ácido Fólico/química , Humanos , Células MCF-7 , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Nanopartículas/efeitos adversos
19.
Zhongguo Zhong Yao Za Zhi ; 38(23): 4152-6, 2013 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-24791508

RESUMO

OBJECTIVE: To investigate the absolute bioavailability of caffeic acid in rats and its intestinal absorption properties. METHOD: The absolute bioavailability (Fabs) of caffeic acid was obtained after iv (2 mg x kg(-1)) or ig (10 mg x kg(-1)) administration to rats. The intestinal absorption of caffeic acid was explored by the recirculating vascularly perfused rat intestinal preparation. Caco-2 cell model was applied to measure the permeability of caffeic acid from apical to basolateral said (A-B) and from basolateral to apical said (B-A). RESULT: A two-compartment pharmacokinetic model was best to describe the pharmacokinetics of caffeic acid following iv or ig administration. The Fabs of caffeic acid was 14. 7% , and its intestinal absorption was 12.4%. The values of Papp A-->B and Papp B-->A of caffeic acid were retained stable while its concentration was changed. The efflux ratio values in this study surveyed were above 2.0, and suggesting caffeic acid was active transport. CONCLUSION: Caffeic acid was shown to have poor permeability across the Caco-2 cells, low intestinal absorption and low oral bioavailability in rats.


Assuntos
Ácidos Cafeicos/farmacocinética , Absorção Intestinal , Animais , Disponibilidade Biológica , Células CACO-2 , Ácidos Cafeicos/metabolismo , Humanos , Masculino , Ratos , Ratos Sprague-Dawley
20.
Sensors (Basel) ; 12(10): 13471-9, 2012 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-23202005

RESUMO

CD105 is a well-known tumor metastasis marker and useful for early monitoring of metastasis and cancer relapse. It is important to generate rapid, reliable and precise analytical information regarding CD105 levels. To establish a simple, selective and sensitive detection method, we prepared an immunosensor with novel bioconjugates based on Pt nanoparticles, thionin acetate and antibodies. The proposed immunosensor displayed a broader linear response to CD105, with a working range of 1.3 to 200.0 ng/mL and a detection limit of 0.9 ng/mL under optimal conditions. Moreover, the studied immunosensor exhibited high sensitivity, fast analysis and adequate stability. The proposed methodology could readily be extended to other clinical- or environment-related biospecies.


Assuntos
Antígenos CD/análise , Técnicas Biossensoriais/métodos , Metástase Neoplásica/diagnóstico , Recidiva Local de Neoplasia/diagnóstico , Platina , Receptores de Superfície Celular/análise , Antígenos CD/imunologia , Técnicas Biossensoriais/instrumentação , Detecção Precoce de Câncer/instrumentação , Detecção Precoce de Câncer/métodos , Técnicas Eletroquímicas , Endoglina , Humanos , Imunoensaio/instrumentação , Imunoensaio/métodos , Nanopartículas Metálicas/química , Platina/química , Receptores de Superfície Celular/imunologia
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