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1.
J Agric Food Chem ; 72(12): 6613-6624, 2024 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-38501445

RESUMO

Propaquizafop is a highly efficient aryloxy phenoxy propionate chiral herbicide. However, the use of propaquizafop, including its safe use methods, residue patterns, dietary risk assessment, and maximum residue limits, for ginseng, a traditional Chinese medicinal plant, has not been studied. An analytical method was established for the simultaneous determination of propaquizafop and its four metabolites in ginseng soil, fresh ginseng, ginseng plant, and dried ginseng using HPLC-MS/MS. This approach showed good linearity (R2 ranging from 0.9827 to 0.9999) and limit of quantification ranging from 0.01 to 0.05 mg/kg. The intra- and interday recovery rates of this method ranged from 71.6 to 107.1% with relative standard deviation ranging from 1.3 to 23.2%. The method was applied to detect residual samples in the field, and it was found that the degradation of propaquizafop in ginseng plants and soil followed a first-order kinetic equation. R2 was between 0.8913 and 0.9666, and the half-life (t1/2) ranged from 5.04 to 8.05 days, indicating that it was an easily degradable pesticide (T1/2 < 30 days). The final propaquizafop residues in ginseng soil, plants, fresh ginseng, and dried ginseng ranged from 0.017 to 0.691 mg/kg. A dietary risk assessment was conducted on the final propaquizafop residue in fresh and dried ginseng. The results showed that the chronic exposure risk quotient values were less than 100% for fresh and dried ginseng (1.15% for fresh ginseng and 1.13% for dried ginseng). This illustrates that the dietary risk associated with the use of 10% propaquizafop emulsifiable concentrate in ginseng is very low. Thus, applying 750 mL/ha of propaquizafop on ginseng could not pose an unacceptable risk to public health. The results of the present study support the registration of propaquizafop in ginseng.


Assuntos
Panax , Resíduos de Praguicidas , Poluentes do Solo , Espectrometria de Massas em Tandem/métodos , Panax/química , Resíduos de Praguicidas/análise , Poluentes do Solo/química , Medição de Risco , Meia-Vida , Solo/química , China
2.
Ecotoxicol Environ Saf ; 274: 116199, 2024 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-38492485

RESUMO

This study established a residue detection method based on the QuEChERS pre-treatment method and combined it with high-performance liquid chromatography-tandem mass spectrometry to test six herbicides (metamitron, clopyralid, desmedipham, phenmedipham, ethofumesate, and haloxyfop-p-methyl) in sugar beet plants, soil, and roots. The degradation dynamics and terminal residues of each herbicide in sugar beets were analysed. Finally, the dietary risks of various herbicides in sugar beets were evaluated based on the dietary structure of Chinese people, and the risk quotient values were below 100%. Using this detection method, all reagents exhibited good linearity (0.9724 ≤ R2 ≤ 0.9998), The limit of quantification (LOQ) ranged from 0.01 to 0.05 mg/L, the matrix effect ranged from -1.2% to -50%, the addition recovery rate ranged from 77.00% to 103.48%, and the relative standard deviation ranged from 1.61% to 16.17%; therefore, all indicators of this method met the residue detection standards. Under field conditions, the half-lives (t1/2) ranged about 0.65 ∼ 2.96 d and 0.38 ∼ 27.59 d in sugar beet plants and soil, respectively. All herbicides were easily degraded in sugar beet plants and soil (t1/2 < 30 d). The terminal residue amounts in the beet plants, soil, and roots ranged from < LOQ to 0.243 mg/kg. The dietary risk assessment of each pesticide was conducted based on the residual median of the terminal residues and the highest residual values on the edible part of the beetroot. The chronic exposure risk quotient (RQc) and acute exposure risk quotient (RQa) values were < 100%, indicating that the residue of each pesticide in beetroot posed low risks to consumers in China at the recommended dosage.


Assuntos
Beta vulgaris , Compostos de Flúor , Herbicidas , Resíduos de Praguicidas , Praguicidas , Piridinas , China , Herbicidas/análise , Resíduos de Praguicidas/análise , Praguicidas/análise , Solo/química , Açúcares , Verduras
3.
Transl Psychiatry ; 14(1): 67, 2024 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-38296956

RESUMO

BACKGROUND: The causal effects of gut microbiome and the development of posttraumatic stress disorder (PTSD) are still unknown. This study aimed to clarify their potential causal association using mendelian randomization (MR). METHODS: The summary-level statistics for gut microbiome were retrieved from a genome-wide association study (GWAS) of the MiBioGen consortium. As to PTSD, the Freeze 2 datasets were originated from the Psychiatric Genomics Consortium Posttraumatic Stress Disorder Working Group (PGC-PTSD), and the replicated datasets were obtained from FinnGen consortium. Single nucleotide polymorphisms meeting MR assumptions were selected as instrumental variables. The inverse variance weighting (IVW) method was employed as the main approach, supplemented by sensitivity analyses to evaluate potential pleiotropy and heterogeneity and ensure the robustness of the MR results. We also performed reverse MR analyses to explore PTSD's causal effects on the relative abundances of specific features of the gut microbiome. RESULTS: In Freeze 2 datasets from PGC-PTSD, eight bacterial traits revealed a potential causal association between gut microbiome and PTSD (IVW, all P < 0.05). In addition, Genus.Dorea and genus.Sellimonas were replicated in FinnGen datasets, in which eight bacterial traits revealed a potential causal association between gut microbiome and the occurrence of PTSD. The heterogeneity and pleiotropy analyses further supported the robustness of the IVW findings, providing additional evidence for their reliability. CONCLUSION: Our study provides the potential causal impact of gut microbiomes on the development of PTSD, shedding new light on the understanding of the dysfunctional gut-brain axis in this disorder. Our findings present novel evidence and call for investigations to confirm the association between their links, as well as to illuminate the underlying mechanisms.


Assuntos
Microbioma Gastrointestinal , Transtornos de Estresse Pós-Traumáticos , Humanos , Transtornos de Estresse Pós-Traumáticos/genética , Estudo de Associação Genômica Ampla , Reprodutibilidade dos Testes , Suplementos Nutricionais
4.
PLoS One ; 18(12): e0296410, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38128017

RESUMO

[This corrects the article DOI: 10.1371/journal.pone.0168892.].

5.
Chin J Integr Med ; 2023 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-37930511

RESUMO

OBJECTIVE: To investigate the therapeutic effect of Sanhuang Xiexin Decoction (SXD) on triple-negative breast cancer (TNBC) in mice and its underlying mechanism. METHODS: The high-performance liquid chromatography (HPLC) was used to quantitate and qualify SXD. A total of 15 female BALB/c mice were inoculated subcutaneously on the right hypogastrium with 3×105 of 4T1-Luc cells to establish TNBC mouse model. All mice were divided randomly into 3 groups, including phosphate buffered solution (PBS), SXD and doxorubicin (DOX) groups (positive drug). Additionally, tumor growth, pathological changes, serum lipid profiles, expression of Janus kinase 2 (JAK2)-signal transducer and activator of transcription 3 (STAT3) signaling pathway and its key targets including inflammatory factors, cell cycle and epithelial-mesenchymal transition (EMT) markers were investigated. Besides, the biosafety of SXD was also evaluated in mice. RESULTS: Rhein, coptisine, berberine hydrochloride and baicalin were all found in SXD, and the concentrations of these 4 components were 0.57, 2.61, 2.93, and 46.04 mg/g, respectively. The mouse experiment showed that SXD could notably suppress the development of tumors and reduce the density of tumor cells (P<0.01). The serum lipid analysis and Oil-Red-O staining both showed the differences, SXD group exhibited higher serum adiponectin and HDL-C levels with lower TC and LDL-C levels compared to the PBS and DOX groups (P<0.05 or P<0.01), respectively. SXD also decreased the levels of phospho-JAK2 (p-JAK2), phospho-STAT3 (p-STAT3) expressions and its downstream factors, including mostly inflammatory cytokine, EMT markers, S phase of tumor cells and vascular endothelial growth factor (VEGF) expression (P<0.05 or P<0.01), respectively. The biosafety assessment of SXD revealed low levels of toxicity in mice. CONCLUSION: SXD could inhibit TNBC by suppressing JAK2-STAT3 phosphorylation which may be associated with modulation of lipid metabolism.

6.
ACS Omega ; 8(5): 4853-4861, 2023 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-36777569

RESUMO

In this study, we established a simple and rapid in vitro method for screening multidrug resistance (MDR) reversal agents in traditional Chinese medicines (TCMs), which could better correspond to the MDR reversing effect in vivo. Here, D-luciferin, a substrate for the enzyme firefly luciferase and also a substrate for ATP-binding cassette transporters (ABC transporters), was used as the probe to detect its efflux kinetics caused by ABC transporters. First, we established a stable doxorubicin (DOX)-resistant cell line (MCF-7/DOXFluc) that overexpressed luciferase. Then, some kinds of TCMs were chosen for the MDR reversal agents to measure its effect on inhibiting the D-luciferin outflow from MCF-7/DOXFluc, and the ideal reversal agent with the least D-luciferin efflux from MCF-7/DOXFluc was selected to further investigate its effect combined with DOX on MCF-7/DOXFluc tumor-bearing mice. The results indicated that quercetin (Qu) could remarkably increase the retention of D-luciferin in MCF-7/DOXFluc in vitro and in vivo. Also, the combination of Qu and DOX could exceedingly inhibit the tumor growth, which proved the feasibility of this in vitro screening method. The study proposed a feasible method for mass screening of MDR agents from TCMs in vitro.

7.
Artigo em Chinês | WPRIM | ID: wpr-988733

RESUMO

ObjectiveTo explore the practical value of environment-friendly sample release agent combined with ultrasound in the preparation of pathological tissue sections. MethodsFrom February 2013 to December 2022, 2 518 pathological specimens submitted by Foshan Municipal Hospital of Traditional Chinese Medicine were selected as the study objects. Two samples of the same specimen were randomly divided into two groups: the environment-friendly fast group, in which the pathological tissue sections were made by using the environment-friendly sample release agent combined with ultrasound; and the traditional group, in which formaldehyde, ethanol and xylene were used to make slices in the conventional way. The differences of hematoxylin (HE) staining effect, immunohistochemistry (IHC) staining effect and MDM2 gene detection result of atypical lipomatous tumor/highly differentiated liposarcoma (ALT/WDL) tissue sections between the two groups were compared. Results① The wax of the two groups' pathological tissues was dehydrated well and the tissue hardness was moderate. After HE staining, the sections of the two groups were intact, without cracks and tremor marks, and the contrast between nucleus and cytoplasm was appropriate, with good transparency, uniform staining, and no tissue loss. The excellent rate and score of HE staining in the environmental fast group were higher than those in the traditional group, but the difference was not statistically significant (χ2 = 3.125,P1 = 0.070;t = 0.965,P2 = 0.334). ②After IHC staining of the two groups of sections, the positive location of the cells was accurate, the staining was specific and uniform, the staining intensity was moderate, the staining sensitivity was good, and there was no tissue loss. The excellent rate of IHC staining and the positive rate of IHC staining in the environmental fast group were lower than those in the traditional group, but the difference was not statistically significant (χ12 = 2.769,P1 = 0.092;χ22 = 0.800,P2 = 0.375). ③The background and outline of the two groups of WDL tissue sections were clear, the staining was uniform, the cells were clear and visible, the nuclear boundary was clear, the hybridization signal was clear and bright under the background fluorescence, and there was no miscellaneous signal. The two groups of sections were hybridized successfully, and MDM2 showed positive amplification. The number of cells successfully hybridized in the environment-friendly fast group was lower than that in the traditional group, but the difference was not statistically significant (t = 1.414,P = 0.230). ConclusionsThe tissue treatment method of using environment-friendly sample release agent combined with ultrasound can ensure the detection effect of HE staining, IHC staining and MDM2 gene detection of pathological tissue sections, and is more efficient and environment-friendly, suitable for promotion and use in hospitals at all levels.

8.
Front Endocrinol (Lausanne) ; 12: 768529, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34858340

RESUMO

Background: The causal association between coffee consumption and the risk of OA is limited. This study was conducted to identify the potential causal effects of coffee consumption on total, knee, hip, and self-reported OA. Methods: Genome-wide association studies (GWAS) of OA were derived from the UK Biobank, comprising 50,508 participants of European ancestry (10,083 with cases and 40,425 controls), and genetic data for specific diagnosed knee OA (4462 cases and 17,885 controls), hip OA (12,625 cases and 50,898 controls), and self-reported OA (12,658 cases and 50,898 controls). Primary and secondary genetic instruments (11 SNPs and 8 SNPs) were selected as instrumental variants from GWAS among 375,833 and 91,462 participants. Two-sample Mendelian randomization (MR) analyses were performed to test the effects of the selected single nucleotide polymorphisms (SNPs) and the OA risk. The causal effects were primarily estimated using weighted median and inverse-variance weighted method with several sensitivity analyses. Results: The MR analyses suggested that genetically predicted 1% increase of coffee consumption was associated with an increased risk of overall OA (OR:1.009, 95% CI:1.003-1.016), knee OA (OR:1.023, 95% CI:1.009-1.038), self-reported OA (OR:1.007, 95% CI:1.003-1.011), but not hip OA (OR: 1.012, 95%CI:0.999-1.024) using primary genetic instruments. Similar results were found when using secondary genetic instruments that genetically predicted coffee consumption (cups/day). Additionally, the sensitivity analyses for leave-one-out methods supported a robust association between exposure traits and OA. Conclusion: Our findings indicate that genetically predicted coffee consumption exerts a causal effect on total, knee, and self-reported OA risk, but not at the hip. Further research is required to unravel the role of coffee consumption in OA prevention.


Assuntos
Café , Osteoartrite do Quadril/epidemiologia , Osteoartrite do Joelho/epidemiologia , Polimorfismo de Nucleotídeo Único , Bases de Dados Factuais , Feminino , Estudo de Associação Genômica Ampla , Humanos , Masculino , Análise da Randomização Mendeliana , Pessoa de Meia-Idade , Osteoartrite do Quadril/genética , Osteoartrite do Joelho/genética , Risco
9.
Artigo em Inglês | MEDLINE | ID: mdl-31988657

RESUMO

BACKGROUND: Smartphone use disorder (SUD) of college students has drawn increasing attention. Although future time perspective (FTP) may be an important protective factor for individual SUD, the moderating and mediating mechanisms underlying this relationship remain unknown. We tested the individual roles of depression and mindfulness as moderators of this relationship. METHODS: A cross-sectional study was conducted in two colleges in Shandong and Chongqing in China using a sample of 1304 college students recruited by stratified cluster sampling. Data were collected through a validated self-report instrument. A moderation-mediation model was constructed, and an SPSS PROCESS macro was used to analyse the data. RESULTS: The correlation analyses showed that FTP was negatively associated with SUD of college students. The mediation model revealed that depression partially mediated the link between FTP and SUD of college students. The moderation-mediation model suggested that mindfulness moderates two direct paths: FTP to depression and depression to SUD. In the first path (FTP to depression), a high level of mindfulness among college students had weakened the relationship between FTP and depression. Here, the relationship is strengthened by a low level of mindfulness. In the second path (depression to SUD), low levels of mindfulness strengthen the link between depression and FTP. In contrast, significant association was not found with high levels of mindfulness. CONCLUSIONS: Results suggest that interventions, such as improving the individual level of FTP and mindfulness, should be conducted. These interventions, in turn, help control the level of depression in college students and ultimately decrease their level of SUD.

10.
Int J Mol Sci ; 20(21)2019 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-31652737

RESUMO

A deep insight into the function and kinetics of ATP-binding cassette (ABC) transporters may aid in the development of pharmaceutics that can minimize the particular facet of chemo-resistance. We utilized bioluminescence imaging to monitor the ABC transporter mediated intracellular drug efflux function. We also investigated the potential association between the intracellular bioluminescent pharmacokinetic profiles and the anti-tumor efficacy of the coix seed extract and gemcitabine against pancreatic cancer cells in vitro and in vivo. The bioluminescent pharmacokinetic parameters and pharmacodynamic index (IC50 and TGI) were determined. The expression levels ABCB1 and ABCG2 were assessed. Results showed that coix seed extract could synergistically enhance the anti-cancer efficacy of gemcitabine (p < 0.05). Meanwhile coix seed extract alone or in combination with gemcitabine could significantly increase the AUCluc while decreasing the Kluc (p < 0.01). Western blot and immunohistochemistry assay demonstrated that coix seed extract could significantly mitigate gemcitabine-induced upregulation of ABCB1 and ABCG2 protein. The Pearson correlation analysis demonstrated that the bioluminescent pharmacokinetic parameters and pharmacodynamic index have strong association in vitro and in vivo. In conclusion coix seed extract could augment the efficacy of gemcitabine therapy in pancreatic cancer cells may at least partly due to the alteration of ABC transporter-mediated drug efflux function.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos/farmacocinética , Coix/química , Desoxicitidina/análogos & derivados , Neoplasias Pancreáticas/tratamento farmacológico , Extratos Vegetais/farmacocinética , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética , Membro 2 da Subfamília G de Transportadores de Cassetes de Ligação de ATP/genética , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/uso terapêutico , Linhagem Celular Tumoral , Desoxicitidina/administração & dosagem , Desoxicitidina/farmacocinética , Desoxicitidina/uso terapêutico , Sinergismo Farmacológico , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Gencitabina
11.
Biomed Res Int ; 2019: 9083068, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31915707

RESUMO

Antitumor therapy using a combination of drugs has shown increased clinical efficacy. Active constituents derived from plants can offer several advantages, such as high efficiacy, low toxicity, extensive effects, and multiple targets. At present, the combination of plants' active constituents and chemotherapeutic drugs has attracted increased attention. Nanodrug delivery systems (NDDSs) have been widely used in tumor-targeted therapy because of their efficacy of delivering antitumor drugs. The in vivo process of tumor-targeted NDDSs has several steps. They include blood circulation, tumor accumulation and penetration, target cell internalization and uptake, and drug release and drug response. In each step, NDDSs encounter multiple barriers that prevent their effective delivery to target sites. Studies have been performed to find alternative strategies to overcome these barriers. We reviewed the recent progress of codelivery of active constituents of plants and chemotherapeutics using NDDSs. Progress into transversing the physiological barriers for more effective in vivo antitumor delivery will be discussed in this review.


Assuntos
Sistemas de Liberação de Medicamentos , Tratamento Farmacológico , Nanomedicina , Neoplasias/tratamento farmacológico , Fitoterapia , Antineoplásicos/administração & dosagem , Antineoplásicos/uso terapêutico , Humanos , Preparações de Plantas/administração & dosagem , Preparações de Plantas/uso terapêutico
12.
Artigo em Inglês | MEDLINE | ID: mdl-30622616

RESUMO

BACKGROUND: Using the lateral wedge insole is a conservative management strategy for knee osteoarthritis. The theoretical basis for this intervention is to correct femorotibial angle, thereby reducing pain and optimising function. OBJECTIVE: This systematic review evaluates the evidence on the effectiveness of wedge insole compared with flat insole for the treatment of knee osteoarthritis. METHODS: A systematic review was performed, searching published (MEDLINE, EMBASE, CNKI, Cochrane Library, and Web of Science) and unpublished literature from their inception to April 2018. Randomized controlled trials (RCTs) that compared the use of wedge insole with a flat insole were included. Risk of bias and clinical relevance were assessed, and outcomes were analysed through meta-analysis. RESULT: From a total of 413 citations, 8 studies adhered to the a priori eligibility criteria. The WOMAC pain was shown to be statistically nonsignificant change with the use of wedge insole (SMD=0.07), and low heterogeneity (I2=22%) and a 95% CI that crossed zero (95% CI: -0.09 to 0.24). The 5 independent trials were not significant in improving pain score (SMD = -0.02, 95% CI: -0.19 to 0.16). This review also revealed no significance in improving Lequesne index (SMD = -0.27, 95% CI: -0.72 to 0.19). The meta-analysis from the 2 independent trials was significant in improving femorotibial angle (SMD = -0.41, 95% CI: -0.73 to -0.09). In conclusion, this meta-analysis suggested that lateral wedge insoles can improve femorotibial angle but are of no benefit with pain and functions in knee osteoarthritis.

13.
PLoS One ; 11(12): e0168892, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-28036353

RESUMO

The compound fuling granule (CFG) is a traditional Chinese drug which has been used to treat ovarian cancer in China for over twenty years. Nevertheless, the underlying molecular mechanism of its anti-cancer effect remains unclear. In this study, microarray data analysis was performed to search differentially expressed genes in CFG-treated ovarian cancer cells. Several cell cycle and epithelial-mesenchymal transition (EMT) related genes were identified. The microarray analyses also revealed that CFG potentially regulates EMT in ovarian cancer. We also found that, functionally, CFG significantly suppresses ovarian cancer cell proliferation by cell cycle arrest, apoptosis and senescence and the AKT/GSK-3ß pathway is possibly involved. Additionally, the invasion and migration ability of ovarian cancer induced by TGFß is significantly suppressed by CFG. In conclusion, our results demonstrated that CFG suppresses ovarian cancer cell proliferation as well as TGFß1-induced EMT in vitro. Finally, we discovered that CFG suppresses tumor growth and distant metastasis in vivo. Overall, these findings provide helpful clues to design novel clinical treatments against cancer.


Assuntos
Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Transição Epitelial-Mesenquimal/efeitos dos fármacos , Medicina Tradicional Chinesa/métodos , Neoplasias Ovarianas/tratamento farmacológico , Fator de Crescimento Transformador beta1/metabolismo , Wolfiporia/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , China , Feminino , Glicogênio Sintase Quinase 3 beta/metabolismo , Humanos , Neoplasias Ovarianas/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais/efeitos dos fármacos
14.
Oncol Rep ; 36(3): 1517-25, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-27459907

RESUMO

Clinical outcomes in patients with pancreatic cancer (PC) continue to be dismal, in part due to de novo and acquired chemoresistance. In the present study, we provide preclinical evidence that pre-treatment with coix seed emulsion, an injectable agent extracted from coix seeds, synergistically sensitized PC cell lines (BxPC-3, PANC-1 and AsPC-1) to gemcitabine, both in vitro and in vivo. Such pretreatment led to significant induction of pro-apoptosis proteins, including caspase-3, cleaved-PARP and Bax (P<0.05), after lower doses of gemcitabine compared to monotherapy. We also showed that coix seed emulsion suppressed the constitutive and gemcitabine-induced activation of nuclear factor-κB (NF-κB), as shown with the use of electrophoretic mobility shift, reporter and immunoblotting analyses. Coix seed emulsion pretreatment also downregulated the NF-κB-dependent anti­apoptotic molecules Bcl-2, survivin and cyclooxygenase-2. In vivo, coix seed emulsion combined with gemcitabine had a much greater antitumor effect than the effect of either agent alone, consistent with the downregulation of the proliferation index, and the results of immunostaining for Ki-67, or for the NF-κB subunit p65. Overall, our data demonstrated that coix seed emulsion abrogated gemcitabine-induced activation of NF-κB, and synergistically sensitized PC cells to gemcitabine therapy.


Assuntos
Coix/química , Desoxicitidina/análogos & derivados , Medicamentos de Ervas Chinesas/farmacologia , Emulsões/farmacologia , NF-kappa B/metabolismo , Neoplasias Pancreáticas/tratamento farmacológico , Sementes/química , Animais , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Desoxicitidina/farmacologia , Regulação para Baixo/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Neoplasias Pancreáticas/metabolismo , Transdução de Sinais/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto/métodos , Gencitabina
15.
Eur J Drug Metab Pharmacokinet ; 41(1): 27-32, 2016 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-25336326

RESUMO

The present study aims to investigate the influence of metabolic behavior by the introduction of bromo atom into the structure of noscapine. Oral gavage of 50 mg/kg bromo-noscapine for 6- to 8-week-old male mice with C57BL/6 background resulted in the detection of the metabolite undergoing cleavage of methylenedioxy group (II), demethylated bromo-noscapine (III, IV), meconine (V), bromo-cotarnine (VI), bisdemethylated bromo-noscapine (VII), and their corresponding glucuronides (G1-G4) in urine, feces, and serum (24 h). In vitro human liver microsomes or mice liver microsomes incubation system can also give the formation of phase I metabolites. Furthermore, the phase I drug-metabolizing enzymes involved in the metabolism of bromo-noscapine was screened. Many CYP isoforms were involved in the formation of metabolite II, and CYP3A4, CYP1A1, CYP2C19, and CYP2D6 were major CYP isoforms. All the determined CYP isoforms showed the catalytic activity towards the formation of metabolites III, V, and VI. The major CYP isoforms involved in the catalytic formation of metabolite IV were CYP2C19, CYP2D6, and CYP2E1. In conclusion, to date, many structural derivatives of noscapine have been synthesized based on the efficiency. However, the metabolic behavior remains to be elucidated, and the present study gave an example through the investigation of metabolic pathway of bromo-noscapine. The introduction of bromo atom into the structure of noscapine did not alter the metabolites profile, but changed the drug-metabolizing enzyme profiles.


Assuntos
Redes e Vias Metabólicas/fisiologia , Noscapina/química , Noscapina/metabolismo , Animais , Humanos , Masculino , Redes e Vias Metabólicas/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos C57BL , Microssomos Hepáticos/efeitos dos fármacos , Microssomos Hepáticos/metabolismo , Noscapina/administração & dosagem
16.
Artigo em Chinês | WPRIM | ID: wpr-304829

RESUMO

Ten isoflavonoids were isolated from the heartwoods of Caragana changduensis Lion f. by means of various column chromatographic techniques. Based on the detailed spectral data analysis (MS and NMR), as well as comparison with the literatures, their chemical structures were determined as 7,2'-dihydroxy-8,4'-dimethoxyisoflavone (1), 4'-hydroxy-7,3'-dimethoxyisoflavone (2), 5, 7, 4'-trihydroxy-2',5'-dimethoxyisoflavone (3), prunetin (4), afrormosin (5), odoratin (6), genistein (7), texasin (8), pratensein (9), and 6,7,3'-trihydroxy-4'-methoxyisoflavone (10). Among them, compounds 1-3 and 9-10 were isolated from the Caragana genus for the first time. All the compounds were obtained from this species for the first time. In the preliminary assays, compounds 1, 2, 6, and 7 possessed significant inhibitory effects on NO production, with IC50 values of 48.12, 25.32, 62.71, 43.59 μmol x L(-1), respectively.


Assuntos
Animais , Camundongos , Caragana , Química , Medicamentos de Ervas Chinesas , Química , Farmacologia , Isoflavonas , Química , Farmacologia , Macrófagos , Metabolismo , Estrutura Molecular , Óxido Nítrico , Metabolismo
17.
Artigo em Chinês | WPRIM | ID: wpr-318483

RESUMO

<p><b>OBJECTIVE</b>To compare the difference in the clinical efficacy on primary trigeminal neuralgia (PTN) between the comprehensive therapy of electroacupuncture (EA) at qi streets acupoints combined with spinal regulation method and medication with carbamazepine (CBZ).</p><p><b>METHODS</b>Sixty patients were randomized into a comprehensive therapy group (30 cases) and a medication group (30 cases). In the comprehensive therapy group, the acupoints at qi streets on the head such as Taiyang (EX-HN 5) and Sishencong (EX-HN 1) and those at qi streets on the chest and abdomen such as Shenshu (BL 23), Zhongwan (CV 12) and Guanyuan (CV 4), etc. were selected. After arrival of qi, EA was attached on 2 to 4 groups of acupoints. After acupuncture, the spinal regulation method was applied. This comprehensive therapy was given once a day. In the medication group, CBZ was used for oral administration, 100 mg at the first time, twice a day, and 400 to 600 mg each day as the maintenance dose. Separately, before and after treatment, in 2 and 6 months in follow-up, pain rating index (PRI), life satisfaction index B (LSI-B) and hamilton depression scale (HAMD) were adopted to evaluate comprehensively the clinical efficacy in the two groups and compare the adverse reaction during the treatment between the two groups.</p><p><b>RESULTS</b>After treatment, the curative and markedly effective rate in the comprehensive therapy group was 76.7% (23/30), which was better than 63.3% (19/30) in the medication group (P < 0.01). The difference in PRI was not significant after treatment between the two groups (all P > 0.05). In 2 and 6 months follow-up, PRI grade in the comprehensive therapy group was superior to that of the medication group (both P<0. 05). After treatment and in follow-up, HAMD score was all reduced in the two groups (P < 0.01, P < 0.05) and the result in follow-up in the comprehensive therapy group was significant as compared with that in the medication group (all P<0. 05). After treatment, LSI-B score was increased obviously in the two groups (all P < 0.05) and the result in the comprehensive therapy group was better than that in the medication group (P < 0.05). The incidence of adverse reaction in the comprehensive therapy group was 16.7% (5/30), which was lower than 30.0% (9/30, P < 0.01) in the medication group.</p><p><b>CONCLUSION</b>The comprehensive therapy of EA at qi streets acpoints combined with spinal regulation method achieves the long-term efficacy on PTN as compared with oral administration of CBZ in terms of the improvement of psychological condition, analgesia and life quality. It is the safe, effective and stable therapy.</p>


Assuntos
Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pontos de Acupuntura , Terapia Combinada , Eletroacupuntura , Manipulação da Coluna , Neuralgia do Trigêmeo , Terapêutica
18.
Artigo em Chinês | WPRIM | ID: wpr-318458

RESUMO

<p><b>OBJECTIVE</b>To compare the clinical efficacy difference between electroacupuncture (EA) at qijie area combined with spine balance-regulating massage and medication for posterior circulation ischemia (PCI).</p><p><b>METHODS</b>One hundred cases of PCI were randomly divided into a treatment group (50 cases) and a medication group (50 cases). The treatment group was treated with EA at Baihui (GV 20), Sishencong (EX-HN 1), Fengchi (GB 20), Shenshu (BL 23), Danzhong (CV 17), etc. in qijie area combined with spine muscle-relieving massage and comprehensive chiropractic. The medication group was treated with oral administration of nimodipine (30 mg per time, three treatments per day) and vinpocetine injection with 500 mL of glucose injection or intravenous drip of 500 mL 0.9% sodium chloride injection, once a day. Ten treatments were taken as one course in both groups, and two courses were given. The symptom score, mean resistance index (RI) of vertebral artery (VA) and basilar artery (BA), mean velocity of blood flow (Vm) and comprehensive clinical efficacy were compared before and after treatment in two groups.</p><p><b>RESULTS</b>The cured and markedly effective rate was 79.6% (39/49) in the treatment group, which was superior to 54.7% (23/42) in the medication group (P<0.05). The symptom score was both significantly improved after treatment in two groups (both P<0.05), which was more obvious in the treatment group (P<0.05). The RI of VA and BA, Vm of VA and BA were significantly improved after treatment in two groups (all P<0.05), which were more obvious in the treatment group (all P<0.05).</p><p><b>CONCLUSION</b>The electroacupuncture combined with spine balance-regulating massage has superior effect on improving mean velocity of blood flow and resistance index of vertebral artery and basilar artery as well as symptom score to medication, and is believed to be a safe and effective treatment for posterior circulation ischemia.</p>


Assuntos
Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pontos de Acupuntura , Circulação Sanguínea , Terapia Combinada , Eletroacupuntura , Isquemia , Terapêutica , Massagem , Resultado do Tratamento
19.
Zhongguo Zhong Yao Za Zhi ; 38(20): 3489-92, 2013 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-24490559

RESUMO

To establish an HPLC method for determining components in monocrotalinum liposomes. The results showed a good linear relationship in monocrotalinum liposomes within the concentration range between 1.6-102.4 mg x L(-1) (r = 0.999 8), with RSDs of intra-day precision, inter-day precision, stability and reproducibility of 0.61%, 0.92%, 1.7%, 1.6%, respectively. The recovery rate of monocrotaline was (99.96 +/- 0.50)%. These data indicated that the HPLC method could accurately determine components in monocrotalinum liposomes. Meanwhile, the microcolumn centrifugation method was established to determine the entrapment efficiency of components in monocrotalinum liposomes. As a result, the recovery rate and the blank liposome recovery of free components were (94.44 +/- 0.77)%, (95.86 +/- 0.68 )%, respectively. According to the parallel determination of the entrapment efficiency of three monocrotaline liposomes, their RSD was 4.0%. The data indicated that the microcolumn centrifugation method was an accurate and feasible method for determining the entrapment efficiency of monocrotaline liposomes.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Portadores de Fármacos/química , Lipossomos/química , Monocrotalina/química , Composição de Medicamentos
20.
Artigo em Chinês | WPRIM | ID: wpr-253948

RESUMO

<p><b>OBJECTIVE</b>To compare the difference in the efficacy of cervical spondylosis between the combined therapy of spinal balancing and the intervention of pathway of qi and the conventional acupuncture and massage therapy.</p><p><b>METHODS</b>Two hundred and seventy-four cases of cervical spondylosis were randomized into a spinal balancing group and a conventional acupuncture group, 137 cases in each one. In the spinal balancing group, the points on the pathway of qi on the head and on the abdomen were selected [the pathway of qi on the head: Baihui (GV 20), Tianzhu (BL 10), Wangu (GB 12) and the others; the pathway of qi on the abdomen: Shenshu (BL 23), Guanyuan (CV 4), Zhongji (CV 3) and the others]. The bimanual needling technique was applied in combination with spinal balancing therapy. In the conventional acupuncture group, the points were Jiaji (EX-B 2) (C3-C7), Fengchi (GB 20), Wangu (GB 12), Baihui (GV 20), etc. The conventional acupuncture technique and massage therapy were adopted. The neck pain questionnaire (NPQ) was adopted to assess the clinical efficacy of the two groups before and after treatment.</p><p><b>RESULTS</b>NPQ score was all improved significantly after treatment in the two groups (all P < 0.05). The result in the spinal balancing group was superior to the conventional acupuncture group (P < 0.05). The curative and effective rate was 83.2% (114/137) in the spinal balancing group, which was better than 69.3% (95/137) in the conventional acupuncture group (P < 0.05). In terms of the types of cervical spondylosis, from high to low, the efficacy sequence was cervical type, nerve root type, vertebral artery type, sympathetic nerve type and spinal cord type.</p><p><b>CONCLUSION</b>The combined therapy of spinal balancing and the intervention of pathway of qi achieves the superior efficacy on various types of cervical spondylosis as compared with the conventional acupuncture and massage therapy. It apparently relieves the symptoms and improves the life quality of the patients.</p>


Assuntos
Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pontos de Acupuntura , Terapia por Acupuntura , Terapia Combinada , Manipulações Musculoesqueléticas , Qi , Espondilose , Terapêutica
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