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1.
Plants (Basel) ; 12(18)2023 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-37765365

RESUMO

E. rutaecarpa var. officinalis is a traditional Chinese medicinal plant known for its therapeutic effects, which encompass the promotion of digestion, the dispelling of cold, the alleviation of pain, and the exhibition of anti-inflammatory and antibacterial properties. The principal active component of this plant, limonin, is a potent triterpene compound with notable pharmacological activities. Despite its significance, the complete biosynthesis pathway of limonin in E. rutaecarpa var. officinalis remains incompletely understood, and the underlying molecular mechanisms remain unexplored. The main purpose of this study was to screen the reference genes suitable for expression analysis in E. rutaecarpa var. officinalis, calculate the expression patterns of the genes in the limonin biosynthesis pathway, and identify the relevant enzyme genes related to limonin biosynthesis. The reference genes play a pivotal role in establishing reliable reference standards for normalizing the gene expression data, thereby ensuring precision and credibility in the biological research outcomes. In order to identify the optimal reference genes and gene expression patterns across the diverse tissues (e.g., roots, stems, leaves, and flower buds) and developmental stages (i.e., 17 July, 24 August, 1 September, and 24 October) of E. rutaecarpa var. officinalis, LC-MS was used to analyze the limonin contents in distinct tissue samples and developmental stages, and qRT-PCR technology was employed to investigate the expression patterns of the ten reference genes and eighteen genes involved in limonin biosynthesis. Utilizing a comprehensive analysis that integrated three software tools (GeNorm ver. 3.5, NormFinder ver. 0.953 and BestKeeper ver. 1.0) and Delta Ct method alongside the RefFinder website, the best reference genes were selected. Through the research, we determined that Act1 and UBQ served as the preferred reference genes for normalizing gene expression during various fruit developmental stages, while Act1 and His3 were optimal for different tissues. Using Act1 and UBQ as the reference genes, and based on the different fruit developmental stages, qRT-PCR analysis was performed on the pathway genes selected from the "full-length transcriptome + expression profile + metabolome" data in the limonin biosynthesis pathway of E. rutaecarpa var. officinalis. The findings indicated that there were consistent expression patterns of HMGCR, SQE, and CYP450 with fluctuations in the limonin contents, suggesting their potential involvement in the limonin biosynthesis of E. rutaecarpa var. officinalis. This study lays the foundation for further research on the metabolic pathway of limonin in E. rutaecarpa var. officinalis and provides reliable reference genes for other researchers to use for conducting expression analyses.

2.
ACS Appl Mater Interfaces ; 15(21): 25898-25908, 2023 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-37191997

RESUMO

The heat tolerance of tumor cells induced by heat shock proteins (HSPs) is the major factor that seriously hinders further application of PTT, as it can lead to tumor inflammation, invasion, and even recurrence. Therefore, new strategies to inhibit HSPs expression are essential to improve the antitumor efficacy of PTT. Here, we prepared a novel nanoparticle inhibitor by synthesizing molecularly imprinted polymers with a high imprinting factor (3.1) on the Prussian Blue surface (PB@MIP) for combined tumor starvation and photothermal therapy. Owing to using hexokinase (HK) epitopes as the template, the imprinted polymers could inhibit the catalytic activity of HK to interfere with glucose metabolism by specifically recognizing its active sites and then achieve starvation therapy by restricting ATP supply. Meanwhile, MIP-mediated starvation downregulated the ATP-dependent expression of HSPs and then sensitized tumors to hyperthermia, ultimately improving the therapeutic effect of PTT. As the inhibitory effect of PB@MIP on HK activity, more than 99% of the mice tumors were eliminated by starvation therapy and enhanced PTT.


Assuntos
Hipertermia Induzida , Impressão Molecular , Nanopartículas , Neoplasias , Animais , Camundongos , Polímeros Molecularmente Impressos , Terapia Fototérmica , Hexoquinase , Neoplasias/tratamento farmacológico , Nanopartículas/química , Trifosfato de Adenosina
3.
Zhongguo Zhong Yao Za Zhi ; 48(6): 1673-1681, 2023 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-37005855

RESUMO

This study employed bibliometrics tools to review the studies of traditional Chinese medicine(TCM) treatment of Alzheimer's disease(AD) in recent ten years, aiming to explore the research status, hotspots, and future trends in this field at home and abroad. The relevant literature published from January 1, 2012 to August 15, 2022 was retrieved from Web of Science and CNKI. CiteSpace 6.1R2 and VOSviewer 1.6.15 were used for the visual analysis of authors, countries, institutions, keywords, journals, etc. A total of 2 254 Chinese articles and 545 English articles were included. The annual number of articles published showed a rising trend with fluctuations. The country with the largest number of relevant articles published and the largest centrality was China. SUN Guo-jie and WANG Qi were the authors publishing the most Chinese articles and English articles, respectively. Hubei University of Chinese Medicine and Beijing University of Chinese Medicine published the most articles in Chinese and English, respectively. Journal of Ethnopharmacology and Neuroscience Letters published the articles with the highest cited frequency and the highest centrality. According to the keywords, the research on TCM treatment of AD mainly focused on the mechanism of action and treatment methods. Metabolomics, intestinal flora, oxidative stress, tau hyperphosphorylation, ß-amyloid(Aß), inflammatory cytokines, and autophagy were the focuses of the research on mechanism of action. Acupuncture, clinical effect, kidney deficiency and phlegm stasis, and dredging governor vessel to revitalize mind were the hotspots of clinical research. This research field is still in the stage of exploration and development. Exchanges and cooperation among institutions should be encouraged to carry out more high-quality basic research on TCM treatment of AD, obtain high-level evidence, and clarify the pathogenesis and prescription mechanism.


Assuntos
Terapia por Acupuntura , Doença de Alzheimer , Medicina , Humanos , Doença de Alzheimer/tratamento farmacológico , Peptídeos beta-Amiloides , Medicina Tradicional Chinesa
4.
World J Clin Cases ; 10(31): 11299-11312, 2022 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-36387821

RESUMO

BACKGROUND: Ribonucleotide reductase (RR) is a key enzyme in tumor proliferation, especially its subunit-RRM2. Although there are multiple therapeutics for tumors, they all have certain limitations. Given their advantages, traditional Chinese medicine (TCM) monomers have become an important source of anti-tumor drugs. Therefore, screening and analysis of TCM monomers with RRM2 inhibition can provide a reference for further anti-tumor drug development. AIM: To screen and analyze potential anti-tumor TCM monomers with a good binding capacity to RRM2. METHODS: The Gene Expression Profiling Interactive Analysis database was used to analyze the level of RRM2 gene expression in normal and tumor tissues as well as RRM2's effect on the overall survival rate of tumor patients. TCM monomers that potentially act on RRM2 were screened via literature mining. Using AutoDock software, the screened monomers were docked with the RRM2 protein. RESULTS: The expression of RRM2 mRNA in multiple tumor tissues was significantly higher than that in normal tissues, and it was negatively correlated with the overall survival rate of patients with the majority of tumor types. Through literature mining, we discovered that berberine, ursolic acid, gambogic acid, cinobufagin, quercetin, daphnetin, and osalmide have inhibitory effects on RRM2. The results of molecular docking identified that the above TCM monomers have a strong binding capacity with RRM2 protein, which mainly interacted through hydrogen bonds and hydrophobic force. The main binding sites were Arg330, Tyr323, Ser263, and Met350. CONCLUSION: RRM2 is an important tumor therapeutic target. The TCM monomers screened have a good binding capacity with the RRM2 protein.

5.
Fitoterapia ; 146: 104727, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32950600

RESUMO

Two new atranones T and U (1 and 2), and three known analogues atranone B (3), atranone Q (4), and stachatranone C (5) were isolated from the toxigenic fungus Stachybotrys chartarum. Their structures and absolute configurations were elucidated by spectroscopic data and calculated ECD analyses. The cytotoxicities of all the atranones (1-5) were evaluated against MG-63 human osteosarcoma cell lines. Compound 4 exhibited significant cytotoxic effect against MG-63 with IC50 value of 8.6 µM, being more active than the positive control, 5-FU (IC50 10.4 µM). Morphological features of apoptosis activities were evaluated in 4-treated MG-63 cells. Compound 4 effectively induced apoptosis of MG-63, which was associated with G0/G1-phase cell cycle arrest. Flow cytometric analysis showed that the treatment by 4 significantly induced MG-63 cell apoptosis in a dose-dependent manner.


Assuntos
Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Neoplasias Ósseas/patologia , Osteossarcoma/patologia , Stachybotrys/química , Antineoplásicos/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Estrutura Molecular
6.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao ; 42(4): 521-530, 2020 Aug 30.
Artigo em Chinês | MEDLINE | ID: mdl-32895105

RESUMO

Objective To explore the optimal therapy time for the treatment of severe coronavirus disease 2019(COVID-19)by traditional Chinese medicine(TCM)and its influence on the therapeutic effect and prognosis. Methods The clinical data,laboratory findings,and outcomes of 64 patients with severe COVID-19 treated with TCM and western medicine in Chongqing from January 20,2020, to March 11,2020 were retrospectively analyzed.Patients were divided into early intervention group[TCM was initiated within 3 days (including day 3) after the first diagnosis of severe type/critical type COVID-19]and late intervention group[TCM was initiated after 7 days (including day 7) after the first diagnosis of severe type /critical type COVID-19].The changes in clinical parameters during the course of disease were compared between the two groups. Results On day 14,the oxygenation index was 292.5(252.0,351.0)mmHg in the early intervention group,which was significantly higher than that in the late intervention group [246.0(170.0,292.5)mmHg](P=0.005).The length of hospital stay [(18.56±1.11)d vs.(24.87±1.64)d,P=0.001],duration of ICU stay [(14.12±0.91)d vs.(20.00±1.53)d,P=0.000] and time to negativity [(16.77±1.04)d vs.(22.48±1.66)d,P=0.001] in the early intervention group were significantly shorter than those in the late intervention group.The intubation rate(7.3%)in the early intervention group was significantly lower than that in the late intervention group(30.4%)(P=0.028). Conclusion Early TCM therapy within three days after a diagnosis of severe COVID-19 can shorten the length of hospital stay,duration of ICU stay,and time to negativity and decrease intubation rate.


Assuntos
Betacoronavirus , Infecções por Coronavirus , Medicina Tradicional Chinesa , Pandemias , Pneumonia Viral , COVID-19 , Infecções por Coronavirus/tratamento farmacológico , Humanos , Pneumonia Viral/tratamento farmacológico , Prognóstico , Estudos Retrospectivos , SARS-CoV-2 , Tratamento Farmacológico da COVID-19
7.
Medicine (Baltimore) ; 99(7): e19102, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32049817

RESUMO

BACKGROUND: Traditional Chinese medicine (TCM) has been used to treat diabetic complications including diabetic retinopathy for many years. OBJECTIVES: This review was performed to systematically assess the efficacy and safety of TCM for treating non- proliferative diabetic retinopathy (NPDR). METHODS: Retrieval from 7 electronic databases was conducted to determine eligible trials published until March 1, 2018. Randomized controlled trials of NPDR that comparing compound Chinese medicine containing the therapeutic method of activating blood and remove stasis versus controls were included for analysis. Primary outcomes were progression of retinopathy. Secondary outcomes included visual acuity, mean defect of visual field, micro-aneurysms, hemorrhage areas, exudates, capillary nonperfusion areas, hemorheological indicators, oscillatory potentials (Ops), glycated haemoglobin (HbA1c), and adverse events. Data extraction and quality assessment were performed. Results expressing as risk ratios (RRs) or mean differences (MD) were analyzed with a fixed- or random- effect model. I statistics were used to assess heterogeneity. RESULTS: A total of 33 trials and 3373 participants were included. Findings revealed that no included studies reported the progression of retinopathy. Compared with conventional medicine, TCM was significantly better at improving visual acuity (MD, -0.10; 95% confidence interval [CI] -0.16 to -0.05) and Ops (MD, -4.68, 95% CI -8.51 to -0.85), and reducing the mean defect of visual field (MD, -1.43; 95%CI, -2.17 to -0.68), micro-aneurysms (MD, -4.51; 95% CI, -6.23 to -2.79), hemorrhage areas (MD, -0.62; 95% CI, -1.06 to -0.19), plasma viscosity (MD, -0.10; 95% CI, -0.20 to 0.00), and HbA1c (MD, -0.22; 95% CI, -0.42 to -0.03). Compared with placebo, TCM was also associated with a decline in the number of microaneurysms (MD, -4.35; 95% CI, -6.25 to -2.45), exudates (MD, -0.17; 95% CI -0.31 to -0.03), capillary nonperfusion areas (MD, -0.18; 95% CI, -0.31 to -0.04), and HbA1c (MD, -0.88; 95% CI, -1.44 to -0.32). Compared with blank groups, TCM was superior at decreasing the mean defect of visual field (MD, -0.87; 95% CI -0.95 to -0.79) and the numbers of micro-aneurysms (MD, -3.35; 95% CI, -4.73 to -1.97). Adverse events were also assessed. CONCLUSION: Activating blood compound Chinese herbal medicine could help to improve visual acuity, micro-aneurysms and HbA1c. Further trials are needed to provide more reliable evidence.


Assuntos
Retinopatia Diabética/tratamento farmacológico , Medicina Tradicional Chinesa/métodos , Adulto , Idoso , Retinopatia Diabética/sangue , Progressão da Doença , Feminino , Humanos , Masculino , Medicina Tradicional Chinesa/efeitos adversos , Pessoa de Meia-Idade , Ensaios Clínicos Controlados Aleatórios como Assunto , Resultado do Tratamento , Acuidade Visual/efeitos dos fármacos
8.
Curr Med Sci ; 40(6): 1099-1106, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33428138

RESUMO

The effects of low ratio of n-6/n-3 polyunsaturated fatty acids (PUFA) have been clarified against atherosclerosis. Increasing evidence indicated that plant sterols (PS) have a significant cholesterol-lowering effect. This study explored the effects of PS combined with n-6/n-3 (2:1) PUFA on atherosclerosis and investigated the possible mechanism. In ApoE-/- mice, the milk fat in high fat diets was replaced with n-6/n-3 (2:1) PUFA alone or supplemented with 6% PS for 16 weeks. Results demonstrated that PS combined with PUFA exerted commentary and synergistic effects on ameliorating atherosclerosis, improving lipid metabolism and lipid deposition in liver, and alleviating inflammatory response. These changes were accompanied with decreased serum TC, TG, LDL-C and increased fecal cholesterol efflux, as well as the lower inflammatory cytokine CRP, IL-6, TNF-α. It is suggested that the underlying mechanism of PS combined with n-6/n-3 (2:1) PUFA promoting the fecal cholesterol efflux may be mediated by liver X receptor α/ATP-binding cassette transporter A1 pathway.


Assuntos
Anti-Inflamatórios/administração & dosagem , Apolipoproteínas E/genética , Aterosclerose/tratamento farmacológico , Ácidos Graxos Insaturados/administração & dosagem , Fitosteróis/administração & dosagem , Animais , Anti-Inflamatórios/farmacologia , Aterosclerose/genética , Aterosclerose/metabolismo , Colesterol/metabolismo , Citocinas/genética , Citocinas/metabolismo , Modelos Animais de Doenças , Sinergismo Farmacológico , Ácidos Graxos Insaturados/farmacologia , Técnicas de Silenciamento de Genes , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/metabolismo , Receptores X do Fígado/metabolismo , Masculino , Camundongos , Fitosteróis/farmacologia
9.
Food Res Int ; 126: 108604, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31732021

RESUMO

This work aimed to develop a novel colorimetric indicator film for monitoring of food freshness based on gelatin/polyvinyl alcohol matrix incorporated with anthocyanin extracts from mulberry. The color of anthocyanin extracts solutions obviously changed from bright red to dark green in the pH range of 2.0-11.0. FTIR spectra and isothermal titration calorimetry showed that the anthocyanin extracts were successfully combined with gelatin/polyvinyl alcohol matrix by hydrogen binding and electrostatic interaction, which enhanced the stability of anthocyanin. The scanning electric microscopy showed that the compatibility between polyvinyl alcohol and gelatin were improved owing to the addition of anthocyanin extracts. With the anthocyanin extracts addition from 0 to 45 mg/100 mL mixed solution, the tensile strength decreased from 30.80 to 21.01 MPa and the elongation at break increased from 589.22% to 905.86%. The color response of film in buffer solution of different pH were in accordance with anthocyanin extracts solutions, and its color changes were clearly visible with naked eye. Finally, the film was evaluated by a test on monitoring fish spoilage, which presented visible color changes due to volatile nitrogenous compounds formed over time. These results showed that this developed film could be used as an effective method for the monitoring of food freshness.


Assuntos
Antocianinas/química , Embalagem de Alimentos/instrumentação , Indicadores e Reagentes/química , Morus/química , Álcool de Polivinil/química , Alimentos Marinhos , Animais , Colorimetria , Peixes , Armazenamento de Alimentos/instrumentação , Gelatina/química , Ligação de Hidrogênio , Concentração de Íons de Hidrogênio , Microscopia Eletrônica de Varredura , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática
10.
Artigo em Chinês | WPRIM | ID: wpr-657294

RESUMO

Objective:To study the effect of electroacupuncture (EA) at the Pericardium Meridian on the heart function of volunteers with acute hypoxia, and to provide scientific evidence for the acupoints selection along the affected meridian in acupuncture-moxibustion therapy. Methods:Based on a self-control design, eighteen healthy volunteers were recruited in the study. Points from the Pericardium Meridian [Neiguan (PC 6), Ximen (PC 4), Quze (PC 3) and Tianquan (PC 2)], non-Pericardium Meridian point [Shousanli (LI 10)], non-meridian and non-acupoint points [1.0-1.5 cm lateral to Neiguan (PC 6) and Ximen (PC 4), respectively on both sides], and a blank control (only inhaling low-oxygen gas without EA stimulation) were selected to observe, once every week, 10 sessions in total, and only 1 acupoint was observed once. The volunteers inhaled low-oxygen gas mixture (10.8% O2 and 89.2% N2) for 30 min to imitate acute hypoxia. EA was conducted when the gas mixture was inhaled for 10 min and then lasted for 20 min; meanwhile, hemodynamic indexes such as cardiac output (CO), cardiac index (CI), systemic vascular resistance (SVR), systemic vascular resistance index (SVRI), left cardiac work (LCW), left cardiac work index (LCWI) and heart rate (HR) were recorded on a hemodynamic monitor. Results:EA at the acupoints of Pericardium Meridian significantly down-regulated the increased CO/CI, LCW/LCWI, and HR (P<0.05), and significantly up-regulated the decreased SVR/SVRI in hypoxia (P<0.05); EA at other meridian acupoints or at non-meridian and non-acupoint points didn't produce such effects. Conclusion: EA at the Pericardium Meridian can obviously improve the cardiac hyper-activation caused by acute hypoxia in healthy volunteers.

11.
Artigo em Chinês | WPRIM | ID: wpr-659200

RESUMO

Objective:To study the effect of electroacupuncture (EA) at the Pericardium Meridian on the heart function of volunteers with acute hypoxia, and to provide scientific evidence for the acupoints selection along the affected meridian in acupuncture-moxibustion therapy. Methods:Based on a self-control design, eighteen healthy volunteers were recruited in the study. Points from the Pericardium Meridian [Neiguan (PC 6), Ximen (PC 4), Quze (PC 3) and Tianquan (PC 2)], non-Pericardium Meridian point [Shousanli (LI 10)], non-meridian and non-acupoint points [1.0-1.5 cm lateral to Neiguan (PC 6) and Ximen (PC 4), respectively on both sides], and a blank control (only inhaling low-oxygen gas without EA stimulation) were selected to observe, once every week, 10 sessions in total, and only 1 acupoint was observed once. The volunteers inhaled low-oxygen gas mixture (10.8% O2 and 89.2% N2) for 30 min to imitate acute hypoxia. EA was conducted when the gas mixture was inhaled for 10 min and then lasted for 20 min; meanwhile, hemodynamic indexes such as cardiac output (CO), cardiac index (CI), systemic vascular resistance (SVR), systemic vascular resistance index (SVRI), left cardiac work (LCW), left cardiac work index (LCWI) and heart rate (HR) were recorded on a hemodynamic monitor. Results:EA at the acupoints of Pericardium Meridian significantly down-regulated the increased CO/CI, LCW/LCWI, and HR (P<0.05), and significantly up-regulated the decreased SVR/SVRI in hypoxia (P<0.05); EA at other meridian acupoints or at non-meridian and non-acupoint points didn't produce such effects. Conclusion: EA at the Pericardium Meridian can obviously improve the cardiac hyper-activation caused by acute hypoxia in healthy volunteers.

12.
Chem Biol Drug Des ; 86(4): 731-45, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25711282

RESUMO

Interference with dynamic equilibrium of microtubule-tubulin has proven to be a useful tactics in the clinic. Based on investigation into the structure-activity relationship (SAR) studies of tubulin polymerization inhibitors obtained from several worldwide groups, we attempted to design 691 compounds covering several main heterocyclic scaffolds as novel colchicine-site inhibitors (CSIs). Evaluated by a series of combination of commonly used computer methods such as molecular docking, 3D-QSAR, and pharmacophore model, we can obtain the ultimate 16 target compounds derived from five important basic scaffolds in the field of medicinal chemistry. Among these compounds, compound A-132 with in silico moderate activity was synthesized, and subsequently validated for preliminary inhibition of tubulin polymerization by immunofluorescence assay. In additional, the work of synthesis and validation of biological activity for other 15 various structure compounds will be completed in our laboratory. This study not only developed a hierarchical strategy to screen novel tubulin inhibitors effectively, but also widened the spectrum of chemical structures of canonical CSIs.


Assuntos
Colchicina/metabolismo , Relação Quantitativa Estrutura-Atividade , Moduladores de Tubulina/química , Moduladores de Tubulina/farmacologia , Sítios de Ligação , Proliferação de Células/efeitos dos fármacos , Técnicas de Química Sintética , Avaliação Pré-Clínica de Medicamentos/métodos , Células Hep G2/efeitos dos fármacos , Humanos , Simulação de Acoplamento Molecular , Reprodutibilidade dos Testes , Moduladores de Tubulina/síntese química
13.
Mol Cancer Ther ; 14(2): 407-18, 2015 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25519702

RESUMO

The clinical prognosis of pancreatic cancer remains rather disappointing despite tremendous efforts in exploring medical treatments in the past two decades. Development of more effective treatment strategies is still desperately needed to improve outcomes in patients with pancreatic cancer. SKLB261 is a multikinase inhibitor obtained recently through a lead optimization. In this investigation, we shall evaluate its anti-pancreatic cancer effects both in vitro and in vivo. SKLB261 is a multikinase inhibitor potently inhibiting EGFR, Src, and VEGFR2 kinases. It could significantly inhibit cell proliferation, migration, and invasion, and induce apoptosis in cellular assays of human pancreatic cancer cells that are sensitive or resistant to dasatinib and/or gemcitabine. Western blot analysis showed that SKLB261 inhibited the activation of EGFR and Src kinases as well as their downstream signaling proteins, including FAK, ERK, and STAT3. SKLB261 also showed potent antiangiogenic effects in transgenic zebrafish models. In vivo, SKLB261 displayed more potent antitumor activities than dasatinib, gemcitabine, or erlotinib in pancreatic cancer xenografts, including BxPC-3, PANC-1, AsPC-1, and HPAC. Furthermore, mice receiving SKLB261 therapy showed significant survival advantage compared with vehicle-treated and gemcitabine-treated groups in an experimental metastasis model of pancreatic cancer. These data, together with the good pharmacokinetic properties and low toxicity of this compound, provide a rationale for the ongoing clinical evaluation of SKLB261 in the treatment of pancreatic cancer.


Assuntos
2-Aminopurina/análogos & derivados , Avaliação Pré-Clínica de Medicamentos , Receptores ErbB/antagonistas & inibidores , Neoplasias Pancreáticas/tratamento farmacológico , Piperazinas/uso terapêutico , Inibidores de Proteínas Quinases/uso terapêutico , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/antagonistas & inibidores , Quinases da Família src/antagonistas & inibidores , 2-Aminopurina/química , 2-Aminopurina/farmacocinética , 2-Aminopurina/farmacologia , 2-Aminopurina/uso terapêutico , Inibidores da Angiogênese/farmacologia , Inibidores da Angiogênese/uso terapêutico , Animais , Antineoplásicos/química , Antineoplásicos/farmacocinética , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Modelos Animais de Doenças , Receptores ErbB/metabolismo , Feminino , Fase G1/efeitos dos fármacos , Humanos , Camundongos Nus , Metástase Neoplásica/patologia , Neoplasias Pancreáticas/patologia , Piperazinas/química , Piperazinas/farmacocinética , Piperazinas/farmacologia , Inibidores de Proteínas Quinases/química , Inibidores de Proteínas Quinases/farmacocinética , Inibidores de Proteínas Quinases/farmacologia , Ratos Sprague-Dawley , Proteínas Recombinantes/metabolismo , Fase de Repouso do Ciclo Celular/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/metabolismo , Peixe-Zebra , Quinases da Família src/metabolismo
14.
Zhong Yao Cai ; 37(2): 210-4, 2014 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-25095337

RESUMO

OBJECTIVE: To assay five lignans in Schisandrae Fructus collected from different habitats. METHODS: HPLC method was developed to assay Schizandrol A, Schizandrol B, Schisantherain A, deoxyschizandrin and gamma-schizandrin in Schisandrae Fructus. Hierarchical clustering analysis (HCA) and principal components analysis (PCA) were performed to evaluate and classify 30 batches of samples based on the contents of the five lignans using SOLO and SPSS 19.0 software. RESULTS: 30 batches of samples were divided into three groups, which reflecting their quality characteristics. CONCLUSION: PCA and HCA provide the basis for the classification and quality evaluation of Schisandrae Fructus. The content analysis provides reference for resources saving and rational using of Schisandrae Fructus.


Assuntos
Frutas/química , Lignanas/análise , Plantas Medicinais/química , Schisandra/química , Cromatografia Líquida de Alta Pressão , Análise por Conglomerados , Ecossistema , Lignanas/normas , Plantas Medicinais/crescimento & desenvolvimento , Análise de Componente Principal , Controle de Qualidade , Schisandra/classificação , Schisandra/crescimento & desenvolvimento
15.
Zhong Xi Yi Jie He Xue Bao ; 6(9): 952-5, 2008 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-18782541

RESUMO

OBJECTIVE: To explore the effects of Rhodiola rosea on the body weight and the intake of sucrose and water in depressive rats induced by chronic mild stress.dz METHODS: A total of 70 male SD rats were divided into seven groups, including normal control group (treated with 0.5% sodium carboxymethycellulose), untreated group, negative control group (treated with 0.5% sodium carboxymethycellulose), positive control group (treated with fluoxetine), low-, medium- and high-dose Rhodiola rosea group (treated with 1.5, 3, 6 g/kg Rhodiola rosea respectively). Except for rats in normal control group, the other sixty rats endured chronic stress for 4 weeks to establish the depression model. After that, rats were administered Rhodiola rosea for 3 weeks. During the whole experiment, the body weight, and sucrose intake, tap water intake of all rats were examined once a week. RESULTS: After the termination of the stress regime, compared with the normal control group, the body weight and 1% sucrose intake in depressive rats were decreased. After 3-week Rhodiola rosea treatment, the body weight and 1% sucrose intake increased in rats of the low-dose Rhodiola rosea group and recovered to the level of the normal control group. CONCLUSION: Low-dose Rhodiola rosea can increase the body weight and sucrose intake of depressive rats, making them recover to normal status.


Assuntos
Peso Corporal/efeitos dos fármacos , Depressão/tratamento farmacológico , Ingestão de Líquidos/efeitos dos fármacos , Fitoterapia , Rhodiola/química , Animais , Depressão/etiologia , Depressão/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Masculino , Ratos , Ratos Sprague-Dawley , Estresse Psicológico/tratamento farmacológico , Sacarose/administração & dosagem
16.
Zhong Xi Yi Jie He Xue Bao ; 6(3): 283-8, 2008 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-18334150

RESUMO

OBJECTIVE: To explore the effects of Valerian on the level of 5-hydroxytryptamine (5-HT), cell proliferation and neuron number in cerebral hippocampus of rats with depression induced by chronic mild stress. METHODS: Seventy rats were divided into 7 groups: normal control, untreated, negative control, positive control, and low-, medium- and high-dose Valerian-treated groups. There were 10 rats in each group. Except for the normal control group, depression was induced in rats by chronic mild stress. The depressive rats in the other six groups were intragastrically administered with sodium carboxymethycellulose, fluoxetine, and low, medium and high-dose Valerian, respectively for 3 weeks. After the treatment, the proliferating cells in the hippocampus were labeled by injecting bromodeoxyuridine (BrdU) in 7 groups. The content of 5-hydroxytryptamine (5-HT) in the hippocampus was detected by high-performance liquid chromatography (HPLC), and the number of hippocampal neurons was counted by morphometry. RESULTS: Compared with the normal control group, the levels of 5-HT in the hippocampus in the low- and medium-dose Valerian-treated groups were increased and recovered to normal level. After the administration of low-dose Valerian for 3 weeks, the number of BrdU positive cells and neurons in the hippocampus of the depressive rats were recovered to the normal status. CONCLUSION: Minidose Valerian may promote the level of 5-HT and cell proliferation in the hippocampus of the depressive rats, and may play a role in saving injured neurons of the hippocampus.


Assuntos
Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Hipocampo/metabolismo , Fitoterapia , Serotonina/metabolismo , Valeriana/química , Animais , Proliferação de Células/efeitos dos fármacos , Depressão/etiologia , Depressão/metabolismo , Hipocampo/patologia , Masculino , Neurônios/patologia , Ratos , Ratos Sprague-Dawley , Estresse Psicológico/complicações
17.
Biol Trace Elem Res ; 123(1-3): 218-28, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-18265951

RESUMO

As a new attempt to control iodine deficiency disorder (IDD), we explored a method of iodine supplementation by raising the iodine content in vegetables. When grown in the soil supplemented with iodized fertilizer, the three experimental plant species (cucumber, aubergine, and radish) show increasing iodine levels in both leaf and fruit/rhizome tissues as the iodine content added in soil increases. Excessive iodine added to soil can be toxic to plants, whereas the tolerance limit to excessive iodine varies in the three plant species tested. The migration and volatilization of iodine in soil is correlated with the properties of the soil used. The residual iodine in soil increases as the iodine added to soil increases. The diatomite in the iodized fertilizer helps to increase the durability of the iodized fertilizer. This study potentially provides a safe and organic iodine supplementation method to control IDD.


Assuntos
Fertilizantes , Iodo/metabolismo , Solo/análise , Verduras/química , Espectrofotometria Infravermelho , Volatilização
18.
Zhongguo Zhong Yao Za Zhi ; 33(23): 2842-6, 2008 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-19260327

RESUMO

OBJECTIVE: To explore the effects of Rhodiola rosea on the level of 5-hydroxytryptamine (5-HT), cell proliferation and differentiation, and number of neuron in cerebral hippocampus of rats with depression induced by chronic mild stress. METHOD: Fifty rats were divided into 5 groups: normal control, untreated, negative control, positive control and Rhodiola rosea-treated groups. There were 10 rats in each group. Except for normal control group, depression was induced in rats by chronic mild stress. The depressive rats in the other four groups were intragastrically administered with 0.5% sodium carboxymethycellulose, fluoxetine and Rhodiola rosea for 3 weeks. After the treatment, the content of 5-HT in the hippocampus was detected by high-performance liquid chromatography. The proliferating cells and differentiated cells in the hippocampus were labeled by bromodeoxyuridine (BrdU) or/and beta-tubulin III immunohistochemistry, and the number of hippocampal neurons was counted by morphometry. RESULT: Compared with the normal control group, the content of 5-HT, number of BrdU positive cells, percentage of BrdU and beta-tubulin III double labeled cells and number of neurons in cerebral hippocampus in the Rhodiola rosea-treated group were increased and recovered to normal level. CONCLUSION: Rhodiola rosea may enhance the level of 5-HT and promote the proliferation and differentiation of neural stem cells in the hippocampus of the depressive rats, and may play a role in saving injured neurons of the hippocampus.


Assuntos
Diferenciação Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Depressão/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Hipocampo/citologia , Neurônios/efeitos dos fármacos , Rhodiola/química , Serotonina/metabolismo , Animais , Depressão/metabolismo , Depressão/fisiopatologia , Medicamentos de Ervas Chinesas/química , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Humanos , Masculino , Neurônios/citologia , Neurônios/metabolismo , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Estresse Psicológico/tratamento farmacológico , Estresse Psicológico/metabolismo , Estresse Psicológico/fisiopatologia
19.
Artigo em Inglês | MEDLINE | ID: mdl-16931180

RESUMO

An automated online gel permeation chromatography-gas chromatograph mass spectrometer (GPC-GC/MS) was developed for the rapid determination of residual pesticides in agricultural products. Pesticides were extracted from homogenized food samples with acetonitrile and decontaminated via the matrix solid-phase dispersion (MSPD) technique, using a primary secondary amine as sorbent prior to GPC-GC/MS analysis. A slightly modified preparation method and automated GPC step proved useful in minimizing matrix interference. To evaluate the performance of the system, 97 target pesticides were spiked at a concentration of 0.1mg/kg into a range of food types, including potato, cabbage, carrot, apple, orange, cucumber, and rice. A low flow rate of 0.1 mL/min in GPC resulted in a 40-fold reduction in solvent consumption compared with conventional GPC column applications. The combination of MSPD technique and GPC-GC/MS for the analysis of the 97 pesticides can be accomplished within 90 min. Most pesticides were recovered in the range of 70-120%, with relative standard deviation generally less than 10%. The results demonstrate that the method can be successfully applied with acceptable recoveries to a broad range of target pesticides within a diverse range of food types.


Assuntos
Cromatografia em Gel/métodos , Produtos Agrícolas/química , Contaminação de Alimentos/análise , Cromatografia Gasosa-Espectrometria de Massas/métodos , Resíduos de Praguicidas/análise , Praguicidas/análise , Automação , Brassica/química , Citrus sinensis/química , Cucumis sativus/química , Daucus carota/química , Malus/química , Sistemas On-Line , Oryza/química , Reprodutibilidade dos Testes , Solanum tuberosum/química
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