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1.
Entropy (Basel) ; 25(1)2022 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-36673221

RESUMO

We propose a multidimensional reconciliation encoding algorithm based on a field-programmable gate array (FPGA) with variable data throughput that enables quantum key distribution (QKD) systems to be adapted to different throughput requirements. Using the circulatory structure, data flow in the most complex pipeline operation in the same time interval, which enables the structural multiplexing of the algorithm. We handle the calculation and storage of eight-dimensional matrices cleverly to conserve resources and increase data processing speed. In order to obtain the syndrome more efficiently, we designed a simplified algorithm according to the characteristics of the FPGA and parity-check matrix, which omits the unnecessary operation of matrix multiplication. The simplified algorithm could adapt to different rates. We validated the feasibility and high speed of the algorithm by implementing the multidimensional reconciliation encoding algorithm on a Xilinx Virtex-7 FPGA. Our simulation results show that the maximum throughput could reach 4.88 M symbols/s.

2.
FASEB J ; 34(9): 12255-12268, 2020 09.
Artigo em Inglês | MEDLINE | ID: mdl-33411355

RESUMO

Akt, a crucial protein involved in a variety of signaling pathways in cancer, acts as an important regulator of survival in hepatocellular carcinoma (HCC), and provides curative option for the related drugs development. We have found an active phenanthroindolizidine alkaloid, (13aR,14R)-9,11,12,13,13a,14-hexahydro-3,6,7-trimethoxydibenzo[f,h]pyrrolo[1,2-b]isoquinolin-14-ol (HTBPI), is a promising Akt inhibitor effective in the suppression of HCC cells proliferation through stimulating apoptotic and autophagic capability in vivo and in vitro. Treatment of HTBPI combined with a classical autophagy-lysosomal inhibitor (bafilomycin A1), could enhance stimulation effects of apoptosis on HCC cell lines. In addition, we confirmed HTBPI targeting Akt, occupied the kinase binding domain (Thr 308) of Akt to inactivate its function by CETSA and DARTS assay. In contrast, ectopic Akt-induced overexpression significantly abrogated inhibitory effects of HTBPI on cell viability and proliferation. Furthermore, high p-Akt (Thr 308) expression is collated with liver tumor formation and poor survival in HCC patients. In conclusions, HTBPI impeded HCC progress through regulation of apoptosis and autophagy machinery via interaction with p-Akt (Thr 308). This may provide potential molecular candidate by targeting Akt for the therapy of HCC patients.


Assuntos
Alcaloides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Indolizinas/farmacologia , Neoplasias Hepáticas/tratamento farmacológico , Fenantrolinas/farmacologia , Proteínas Proto-Oncogênicas c-akt/antagonistas & inibidores , Animais , Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Carcinoma Hepatocelular/mortalidade , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Feminino , Humanos , Neoplasias Hepáticas/mortalidade , Neoplasias Hepáticas/patologia , Masculino , Camundongos
3.
Biogerontology ; 22(6): 589-602, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34542790

RESUMO

Aging often leads to an increase risk of age-related diseases, and the development of anti-aging drugs have become the trend and focus of the current scientific research. In this experiment, serum samples from healthy people of different ages were analyzed based on clinical lipidomics, and a total of 10 potential biomarkers in middle-aged and youth group, 20 biomarkers in the youth and the elderly group were obtained. Furthermore, dhSph and dhCer involved above may affect the aging process through sphingolipid metabolic pathway. As the first and rate-limiting step of catalyzing de novo sphingolipid pathway, SPT may play a key role in human anti-aging, which is revealed by lipidomics liposome tracer analysis. The potential active components in ginseng on SPT was further verified by molecular docking virtual screening and atomic force microscope. Four ingredients of ginseng may reduce the levels of metabolites dhSph and dhCer by inhibiting the activity of SPT, and play an anti-aging effect by affecting the sphingolipid metabolism pathway.A clinical trials registration number: ChiCTR1900026836.


Assuntos
Lipidômica , Panax , Adolescente , Idoso , Envelhecimento , Biomarcadores , Humanos , Pessoa de Meia-Idade , Simulação de Acoplamento Molecular
4.
Support Care Cancer ; 29(9): 5435-5445, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33704565

RESUMO

PURPOSE: Breast cancer-related lymphedema (BCRL) is a major long-term complication for post-surgery breast cancer survivors. Although several risk factors have been identified, lifestyle characteristics have been neglected in previous studies. The aim of this study was to develop and validate a nomogram for estimating this population's risk of developing lymphedema, taking into consideration their demographic, clinical, and personal lifestyle behaviors. METHODS: In a cross-sectional study, we collected data from 775 post-operative breast cancer survivors who had attended a follow-up session in the recent 10 years (primary cohort). Lymphedema was assessed using the Norman telephone questionnaire, self-reported by patients. Multiple logistic regression was used to identify risk factors for lymphedema, including demographic, clinical, and lifestyle-related factors. A nomogram was constructed based on those factors and was validated using a separate group of 314 breast cancer patients (validation cohort). RESULTS: The factors independently associated with lymphedema were higher body mass index (BMI), modified radical mastectomy (MRM), postsurgical infection, chemotherapy, radiotherapy, exercise of the affected arm, and the active participation in physical activity (P<0.05). The area under the curve (AUC) values of the primary and the validation cohorts were 0.721 (95% confidence interval: 0.685-0.756) and 0.702 (95% confidence interval: 0.646-0.759), respectively. CONCLUSIONS: BCRL risk factors include MRM, radiotherapy, chemotherapy, and higher BMI, while the active physical activity behavior of patients appears to be a factor against lymphedema. The nomogram incorporating the patients' clinical and lifestyle factors might be useful for predicting lymphedema in breast cancer survivors.


Assuntos
Linfedema Relacionado a Câncer de Mama , Neoplasias da Mama , Sobreviventes de Câncer , Linfedema , Linfedema Relacionado a Câncer de Mama/epidemiologia , Linfedema Relacionado a Câncer de Mama/etiologia , Neoplasias da Mama/cirurgia , China , Estudos Transversais , Feminino , Humanos , Linfedema/epidemiologia , Linfedema/etiologia , Mastectomia , Nomogramas
5.
Phytochem Anal ; 32(5): 836-849, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-33503685

RESUMO

INTRODUCTION: Radix Paeoniae Alba (RPA) presents several pharmacological effects, including analgesia, liver protection, and toxicity reduction. RPA consists mostly of monoterpenes and their glycosides, tannins, flavonoids, and organic acids, with monoterpenes being the main active pharmaceutical ingredients. OBJECTIVE: To establish an effective method for rapid classification and identification of the main monoterpenes, flavonoids, and organic acids in RPA. METHODS: We used ultrahigh-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS) and data post-processing technology to rapidly classify and identify the monoterpenoids, flavonoids, and organic acids in RPA. We also summarised the diagnostic product ions and neutral losses of monoterpenoids, flavonoids, and organic acids in RPA reported in the literature. RESULTS: We identified 24 components, namely 18 monoterpenoids, one flavonoid, and five organic acids. CONCLUSION: In this study, we analysed the chemically active pharmaceutical ingredients and assessed the quality of RPA. In addition, we demonstrated that UHPLC-Q-TOF-MS can be used to qualitatively classify and identify the variety of chemical components of traditional Chinese medicines (TCMs) to a certain extent. Moreover, we confirmed that mass spectrometry can be used to identify the components of TCMs.


Assuntos
Medicamentos de Ervas Chinesas , Paeonia , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Espectrometria de Massas
6.
Mol Ther ; 27(1): 244-260, 2019 01 02.
Artigo em Inglês | MEDLINE | ID: mdl-30527756

RESUMO

Immunotherapy based on the immune checkpoint blockade has emerged as the most promising approach for cancer therapy. However, the proportion of colorectal cancer patients who benefit from immunotherapy is small due to the immunosuppressive tumor microenvironment. Hence, combination immunotherapy is an ideal strategy to overcome this limitation. In this study, we developed a novel combination of CSF-1R (colony-stimulating factor 1 receptor) inhibitor (PLX3397), oncolytic viruses, and anti-PD-1 antibody. Our results demonstrated that the triple treatment synergistically conferred significant tumor control and prolonged the survival of mouse models of colon cancer. Approximately 43% and 82% of mice bearing the CT26 and MC38 tumor, respectively, survived long term following the triple treatment. This combination therapy reprogrammed the immunosuppressive tumor microenvironment toward a CD8+ T cell-biased anti-tumor immunity by increasing T cell infiltration in the tumor and augmenting anti-tumor CD8+ T cell function. Our results provide a robust strategy for clinical combination therapy.


Assuntos
Vírus Oncolíticos/fisiologia , Receptor de Morte Celular Programada 1/imunologia , Receptor de Fator Estimulador de Colônias de Macrófagos/antagonistas & inibidores , Aminopiridinas/farmacologia , Animais , Antígeno B7-H1/metabolismo , Linfócitos T CD8-Positivos/metabolismo , Neoplasias do Colo/metabolismo , Feminino , Citometria de Fluxo , Humanos , Imunoterapia/métodos , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos C57BL , Vírus Oncolíticos/genética , Pirróis/farmacologia , Receptor de Fator Estimulador de Colônias de Macrófagos/metabolismo , Microambiente Tumoral/efeitos dos fármacos , Microambiente Tumoral/imunologia
7.
Eur J Cancer Care (Engl) ; 29(5): e13259, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32424878

RESUMO

OBJECTIVE: We investigated the effects of mindfulness-based cognitive therapy on insomnia (MBCT-I) in breast cancer survivors. METHODS: In total, 136 participants were allocated randomly to a MBCT-I group or a waitlist control (WLC) group. Indicators of insomnia and mindfulness were evaluated using the Insomnia Severity Index, actigraphy and the Five Facet Mindfulness Questionnaire. Data were collected at baseline (T1), post-intervention (T2), 3-month follow-up (T3) and 6-month follow-up (T4) time points. RESULTS: Insomnia severity decreased significantly in the MBCT-I group, compared with the WLC group, at T2, T3 and T4 (all p < .001). We found that 59.6% of the MBCT-I group with moderate and severe insomnia improved to no insomnia and subclinical insomnia at T4 relative to T1, accounting for 7.9% and 55.3%, respectively. Compared with the WLC group, the MBCT-I group improved on actigraphy measures of sleep; they exhibited a pattern of decreased sleep onset latency and waking after sleep onset, as well as increased total sleep time and sleep efficiency. Mindfulness also increased more in the MBCT-I group than in the WLC group at T2, T3 and T4 (all p < .001). CONCLUSIONS: MBCT-I may be an efficacious non-pharmacologic intervention to improve sleep quality in breast cancer survivors.


Assuntos
Neoplasias da Mama , Sobreviventes de Câncer , Terapia Cognitivo-Comportamental , Atenção Plena , Distúrbios do Início e da Manutenção do Sono , Neoplasias da Mama/terapia , Feminino , Humanos , Distúrbios do Início e da Manutenção do Sono/terapia , Resultado do Tratamento
8.
Phytochem Anal ; 31(3): 384-394, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31880044

RESUMO

INTRODUCTION: Alismatis Rhizoma (AR) has been widely used to treat various diseases. Its complex chemical composition has caused certain difficulties in the analysis of this traditional Chinese medicine. Therefore, it is necessary to establish a method for the rapid classification and identification of the chemical constituents of AR. OBJECTIVE: This article describes a method for the rapid classification and identification of major triterpenoids in AR. METHODOLOGY: The samples were analysed by ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). The assay was performed on a Waters ACQUITY UPLC BEH C18 column (100 mm × 2.1 mm, 1.7 µm) with 0.1% formic acid in water (A), and acetonitrile (B) as mobile phase by gradient elution at a flow rate of 0.3 mL/min. In the positive ion mode, the fragment information was obtained and compared with the characteristic fragments and neutral losses described in the literature. Then, the rapid classification and identification of the chemical components from AR were achieved. RESULTS: Finally, 25 triterpene compounds of AR were identified. CONCLUSIONS: The method established in this study achieved the rapid classification and identification of chemical components in AR, which promotes the development of research methods to study the constituents of traditional Chinese medicine.


Assuntos
Alisma , Medicamentos de Ervas Chinesas , Triterpenos , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas em Tandem
9.
J Sep Sci ; 41(19): 3791-3805, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30074686

RESUMO

Bupleuri radix and liquorice are commonly used as a hepatoprotectants. Their main effective ingredients are triterpenoid saponins. It is known that the saponins in liquorice and Bupleuri radix not only promote the metabolism of sugar and lipids but also have anti-inflammatory functions and hepatoprotective effect. However, the complexity of these compounds results in difficulty in studying their pharmacodynamics and mechanism. In this study, glycosides were the main components that were identified and selected as the main research object. First, the mass spectrometry information of the main chemical components in liquorice and Bupleuri radix were collected from the literature. The characteristic fragments and neutral losses were summarized according to typical cleavage methods. Second, the samples were analysed using ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry, and characteristic fragment filters and neutral loss filters were successfully applied to screen 18 saponins from Bupleuri radix and 23 saponins and nine flavonoid glycosides from liquorice. Rapid classification and identification of the main components in Bupleuri radix and liquorice were finally achieved. This method promoted the development of chemical components in Bupleuri radix and liquorice, and provided a new way for screening, classifying, and identifying target components in complex samples of metabolomics and pharmacokinetics.


Assuntos
Bupleurum/química , Medicamentos de Ervas Chinesas/análise , Glicosídeos/análise , Glycyrrhiza/química , Extratos Vegetais/análise , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas , Fatores de Tempo
10.
Zhongguo Zhong Yao Za Zhi ; 43(4): 676-683, 2018 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-29600640

RESUMO

ABC efflux proteins are a kind of transporters mediating diversified endogenous and exogenous efflux protein substrates across the plasma membrane by depending on the chemical energy released by ATP hydrolysis. As a vitally important functional membrane, it is widely found in various tissues and organs. The drug changes the expressions and/or functions of the transport proteins, which will affect the disposal process of substrate drugs corresponding to transporters in vivo, and finally lead to the pharmacokinetic interactions. The efflux proteins take part in the absorption, distribution, metabolism and excretion of drugs, and mainly consist of P-glycoprotein(P-gp), multidrug resistance associated protein(MRP) and breast cancer resistance protein(BCRP). The induction effect or inhibition effect of drugs on efflux protein plays a greatly significant role in the drug interaction produced by the compatibility of traditional Chinese medicine, which may be one of the important mechanisms of the theory of seven features of compatibility. In this article, the effects of seven features of compatibility on the ABC efflux transporters were reviewed, in order to reveal the roles of efflux protein in the herb-pairs compatibility, and provide new ideas for the mechanism and rationality of herb compatibility.


Assuntos
Transportadores de Cassetes de Ligação de ATP/metabolismo , Medicina Tradicional Chinesa , Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo , Preparações de Plantas/farmacologia , Interações Medicamentosas , Humanos
11.
Molecules ; 22(10)2017 Oct 20.
Artigo em Inglês | MEDLINE | ID: mdl-29053630

RESUMO

Schisandra chinensis (known in Chinese as WuWeiZi, WWZ) has observable effects such as astringing the lung to stop coughs, arresting sweating, preserving semen and preventing diarrhea. The major components of WWZ include lignans, triterpenoids, organic acids and fatty acids. In this paper, a reliable method for the rapid identification of multiple components in WWZ by their characteristic fragments and neutral losses using UPLC-Q-TOF/MS technology was developed. After review of the literature and some reference experiments, the fragmentation pattern of several compounds were studied and summarized. Then, according to the corresponding characteristic fragments coupled with neutral losses in the positive or negative ion mode produced by different types of substances a rapid identification of target compounds was achieved. Finally, a total of 30 constituents of WWZ were successfully identified, including 15 lignans, nine triterpenoids, three organic acids and three fatty acids. The method established in this study not only provides a comprehensive analysis of the chemical ingredients of WWZ, providing a basis for further phytochemical studies on WWZ but also provides a more efficient way to solve the problem of identification of complex chemical constituents in traditional Chinese medicines.


Assuntos
Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/química , Schisandra/química , Cromatografia Líquida de Alta Pressão/métodos , Frutas/química , Estrutura Molecular , Extratos Vegetais/análise , Extratos Vegetais/química , Espectrometria de Massas em Tandem/métodos
12.
ACS Omega ; 9(8): 9792-9802, 2024 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-38434849

RESUMO

Molybdenum disulfide shows promise as an anode material for lithium-ion batteries. However, its commercial potential has been constrained due to the poor conductivity and significant volume expansion during the charge/discharge cycles. To address these issues, in this study, N-doped MoS2/C composites (NMC) were prepared via an enhanced hydrothermal method, using ammonium molybdate and thiourea as molybdenum and sulfur sources, respectively. Polyethylene glycol 400 (PEG400) and polyvinylpyrrolidone (PVP) were added in the hydrothermal procedure as soft template surfactants and nitrogen/carbon sources. The crystal structure, morphology, elemental composition, and surface valence state of the N-doped MoS2/C composites were characterized by X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), high-resolution transmission electron microscopy (HRTEM), and X-ray photoelectron spectroscopy (XPS), respectively. The results indicate that the NMC prepared by this method are spherical particles with a nanoflower-like structure composed of MoS2 flakes, having an average particle size of about 500 nm. XPS analysis shows the existence of C and N elements in the samples as C-N, C-C, and pyrrolic N. As anodes for LIBs, the NMC without annealing deliver an initial discharge capacity of 548.2 mAh·g-1 at a current density of 500 mA·g-1. However, this capacity decays in the following cycles with a discharge capacity of 66.4 mAh·g-1 and a capacity retention rate of only 12% after 50 cycles. In contrast, the electrochemical properties of the counterparts are enhanced after annealing, which exhibits an initial discharge capacity of 575.9 mAh·g-1 and an ultimate discharge capacity of 669.2 mAh·g-1 after 70 cycles. The capacity retention rate decreases initially but later increases and elevated afterward to reach 116% at the 70th cycle, indicating an improvement in charge-discharge performance. The specimens after annealing have a smaller impedance, which indicates better charge transport and lithium-ion diffusion performance.

13.
Cell Signal ; 121: 111262, 2024 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-38901722

RESUMO

Many solid tumors frequently overexpress Non-SMC Condensin I Complex Subunit H (NCAPH), and new studies suggest that NCAPH may be a target gene for clinical cancer therapy. Numerous investigations have shown that a variety of transcription factors, including as MYBL2, FOXP3, GATA3, and OTC1, can stimulate the transcription of NCAPH. Additionally, NCAPH stimulates many oncogenic signaling pathways, such as ß-Catenin/PD-L1, PI3K/AKT/SGK3, MEK/ERK, AURKB/AKT/mTOR, PI3K/PDK1/AKT, and Chk1/Chk2. Tumor immune microenvironment modification and tumor growth, apoptosis, metastasis, stemness, and treatment resistance all depend on these signals. NCAPH has the ability to form complexes with other proteins that are involved in glycolysis, DNA damage repair, and chromatin remodeling. This review indicates that NCAPH expression in most malignant tumors is associated with poor prognosis and low recurrence-free survival.

14.
Toxicology ; 505: 153841, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38796053

RESUMO

Paclobutrazol (PBZ) is a plant growth regulator that can delay plant growth and improve plant resistance and yield. Although it has been widely used in the growth of medicinal plants, human beings may take it by taking traditional Chinese medicine. There are no published studies on PBZ exposure in humans or standardized limits for PBZ in medicinal plants. We measured the solubility, oil-water partition coefficient (logP), and pharmacokinetics of PBZ in rats and established a physiologically based pharmacokinetic (PBPK) model of PBZ in rats. This was followed by extrapolation to healthy Chinese adult males as a theoretical foundation for future risk assessment of PBZ. The results showed that PBZ had low solubility and high fat solubility. Pharmacokinetic experiments showed that PBZ was absorbed rapidly but eliminated slowly in rats. On this basis, the rat PBPK model was successfully constructed and extrapolated to healthy Chinese adult males to predict the plasma concentration-time curve and exposure of PBZ in humans. The construction of the PBPK model of PBZ in this study facilitates the determination of the standard formulation limits and risk assessment of PBZ residues in medicinal plants.


Assuntos
Modelos Biológicos , Ratos Sprague-Dawley , Triazóis , Masculino , Animais , Triazóis/farmacocinética , Triazóis/sangue , Humanos , Ratos , Reguladores de Crescimento de Plantas/farmacocinética , Adulto , Solubilidade , Medição de Risco
15.
Diabetes Metab Syndr ; 18(6): 103068, 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38959546

RESUMO

BACKGROUND AND AIM: Clinical evidence for early identification and diagnosis of liver cirrhosis (LC) caused by different types of liver disease is limited. We investigated this topic through a meta-analysis of quantitative metabolomics. METHODS: Four databases were searched until October 31, 2022 for studies comparing metabolite levels between patients with different types of liver disease and control individuals. A random-effects model was applied for the meta-analysis. RESULTS: This study included 55 studies with 8266 clinical participants, covering 348 metabolites. In LC related to drug-induced liver injury (DILI), hepatitis B virus (HBV) infection, and non-alcoholic fatty liver disease (NAFLD), the primary bile acid biosynthesis (taurocholic acid: SMD, 1.08[0.81, 1.35]; P < 0.00001; glycocholic acid: SMD, 1.35[1.07, 1.62]; P < 0.00001; taurochenodeoxycholic acid: SMD, 1.36[0.94, 1.78]; P < 0.00001; glycochenodeoxycholic acid: SMD, 1.49[0.93, 2.06]; P < 0.00001), proline and arginine (l-proline: SMD, 1.06[0.53, 1.58]; P < 0.0001; hydroxyproline: SMD, 0.81[0.30, 1.33]; P = 0.002), and fatty acid biosynthesis (palmitic acid: SMD, 0.44[0.21, 0.67]; P = 0.0002; oleic acid: SMD, 0.46[0.19, 0.73]; P = 0.0008; stearic acid: SMD, 0.37[0.07, 0.68]; P = 0.02) metabolic pathways were significantly altered. CONCLUSION: We identified key biomarkers and metabolic characteristics for distinguishing and identifying LC related to different types of liver disease, providing a new perspective for early diagnosis, disease monitoring, and precise treatment.

16.
Nat Prod Res ; : 1-8, 2023 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-37950736

RESUMO

As a compound preparation of traditional Chinese medicine, Jianwei Xiaoshi Tablets (JXT) is made from five Chinese herbs: Taizishen (Pseudostellariae Radix), Chenpi (Citri Reticulatae Pericarpium), Shanyao (Dioscoreae Rhizoma), Maiya (Hordei Fructus Germinatus) and Shanzha (Crataegi Fructus). It is mainly used to treat dyspepsia. However, the chemical composition of JXT is complex and unclear. In this study, ultra performance liquid chromatography-quadrupole-orbitrap-mass spectrometry and data post-processing technologies were used to analyse the samples of JXT. Firstly, the mass spectrometric information of the main components of five traditional Chinese herbs in JXT was summarised and a compound database was established. Then, the mass spectrometric data detected by the prepared samples was compared with the database. Finally, 93 chemical components were successfully identified, including 6 amino acids, 34 flavonoids, 18 alkaloids, 15 organic acids, 9 cyclic peptides and 11 other components, and the rapid classification and identification of chemical components of JXT were realised.

17.
J Mater Sci Mater Med ; 23(2): 443-55, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22170300

RESUMO

The purpose of this study was to develop an in situ forming SAIB (sucrose acetate isobutyrate)-PLGA (poly (d, lactide-co-glycolide)) mixture matrix depot for sustained release of risperidone. The factors affecting the risperidone release kinetics were investigated to obtain further insight into the drug release mechanisms. The burst release in vitro was significantly reduced (4.95%) by using DMSO as solvent. And, increasing the PLGA content from 2 to 10% w/w decreased the initial release from 6.95 to 1.05%. The initial release in vivo decreased with increasing PLGA content (2.0% w/w PLGA, C(max) = 1161.7 ± 550.2 ng ml(-1); 10% w/w PLGA, C(max) = 280.3 ± 98.5 ng ml(-1)). The persistence (AUC(4-20 days)) over 20 days increased from 76.8 ± 20.7 to 362.8 ± 75.0 ng d ml(-1) by inclusion of 10% PLGA compared with the PLGA-free depot. These results demonstrate that the SAIB-PLGA mixture matrix depot could be useful as a sustained delivery system for risperidone.


Assuntos
Antagonistas de Dopamina/administração & dosagem , Ácido Láctico/química , Ácido Poliglicólico/química , Risperidona/administração & dosagem , Animais , Área Sob a Curva , Cromatografia/métodos , Difusão , Antagonistas de Dopamina/química , Sistemas de Liberação de Medicamentos , Feminino , Concentração de Íons de Hidrogênio , Cinética , Masculino , Microscopia/métodos , Óptica e Fotônica , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Porosidade , Ratos , Reologia , Risperidona/química , Solubilidade , Solventes/química , Fatores de Tempo
18.
Drug Dev Ind Pharm ; 38(1): 104-10, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-21774632

RESUMO

Berberine chloride (BBR) is a plant alkaloid that has been used for centuries for treatment of inflammation, dysentery, and liver diseases. It is poorly absorbed from the gastrointestinal (GI) tract and its various clinical uses are limited because of its poor bioavailability. The object of the present study was to investigate the absorption enhancing effect of chitosan on BBR. Mixtures of BBR and chitosan were prepared and the absorption enhancement was investigated in rats. The results showed a dose-dependent absorption enhancement produced by chitosan. Formulations containing 0.5%, 1.5%, and 3.0% chitosan resulted in improvement of AUC(0-36 h) values by 1.9, 2.2, 2.5 times. The absorption enhancing ability of chitosan may be due to its ability to improve the BBR paracellular pathway in the intestinal tract. Chitosan hydrochloride, a salt of chitosan, was also investigated in this study. However, the addition of 2.0% and 3.3% chitosan hydrochloride to BBR solution did not produce any increase in either C(max) or AUC(0-36 h) of BBR. Subsequent solubility studies suggested that the reduced berberine chloride solubility in chitosan hydrochloride may limit the enhancement ability. This study showed that the optimum formulation producing the highest BBR absorption is the BBR solution containing 3.0% chitosan.


Assuntos
Berberina/química , Berberina/farmacocinética , Quitosana/química , Absorção Intestinal , Animais , Área Sob a Curva , Disponibilidade Biológica , Química Farmacêutica/métodos , Trato Gastrointestinal/metabolismo , Masculino , Ratos , Ratos Wistar , Solubilidade , Soluções/química
19.
J Clin Endocrinol Metab ; 107(7): 1956-1964, 2022 06 16.
Artigo em Inglês | MEDLINE | ID: mdl-35349673

RESUMO

CONTEXT: Ischemic stroke (IS) is a serious public health problem worldwide, threatening human life and health. Atherosclerosis is the cause of stroke. At present, there are few selective indexes that can be used to evaluate atherosclerosis in the clinic; providers rely mainly on the atherosclerotic index (AI). Disturbance of lipid metabolism is considered to be a key event leading to IS. OBJECTIVE: The purpose of this study was to discover potential biomarkers in the serum of atherosclerosis-induced IS, combined with the AI to provide early warning for the diagnosis of IS. METHODS: In this study, we used nontargeted metabolomics based on ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS) to measure the changes in serum metabolites in a group of patients with IS. To verify the reproducibility of candidate biomarkers in the population, we expanded the sample size. RESULTS: Five metabolites were identified, including sphingomyelin (18:0/14:0), 1-Methylpyrrolinium, PC (18:0/18:0), LysoPC (18:0/0:0), and PC (18: 2/18:2). The combination of these 5 metabolic markers has good diagnostic and predictive ability, and the change level of these metabolites is significantly related to IS. Our results also indicate that changes in glycerophospholipid metabolism may indicate an early risk of IS development. CONCLUSION: These findings may contribute to the development of new diagnostic methods of potential biomarkers in serum combined with the AI, thereby providing early warning for the diagnosis of atherosclerosis-induced IS, and may provide a new insights for pathogenesis in IS.


Assuntos
Aterosclerose , AVC Isquêmico , Aterosclerose/diagnóstico , Biomarcadores , Cromatografia Líquida de Alta Pressão , Humanos , Metabolômica/métodos , Reprodutibilidade dos Testes
20.
AAPS PharmSciTech ; 12(2): 705-11, 2011 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-21637946

RESUMO

Berberine chloride (BBR) is a natural isoquinoline alkaloid extracted from medicinal herbs. It has been reported that the intestinal absorption of BBR is very low. In this study, the absolute bioavailability of BBR was studied, and the enhancing effects of D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on intestinal absorption were investigated in rats. BBR injection was administrated via the femoral vein at a dose of 1.0 mg kg(-1) in intravenous group, and BBR oral formulations were administrated by oral gavage at a dose of 100 mg kg(-1) in BBR control (control) group and BBR-TPGS (test) group, respectively. The result showed that BBR had a very low absolute bioavailability of 0.68%, and TPGS could enhance intestinal absorption of BBR significantly. TPGS at a concentration of 2.5% could improve peak concentration (C(max)) and area under the curve (AUC(0-36)) of BBR by 2.9 and 1.9 times, respectively. The absorption enhancing ability of TPGS may be due to its ability to affect the biological activity of P-glycoprotein and thereby reduce the excretion of absorbed BBR into the intestinal lumen. This study indicated that absolute bioavailability of BBR was 0.68% in rats, and TPGS was a good absorption enhancer capable of enhancing intestinal absorption of BBR significantly.


Assuntos
Berberina/farmacocinética , Portadores de Fármacos/farmacocinética , Absorção Intestinal/fisiologia , Vitamina E/análogos & derivados , Administração Oral , Animais , Berberina/administração & dosagem , Berberina/normas , Disponibilidade Biológica , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/normas , Sinergismo Farmacológico , Absorção Intestinal/efeitos dos fármacos , Masculino , Polietilenoglicóis/administração & dosagem , Polietilenoglicóis/farmacocinética , Polietilenoglicóis/normas , Distribuição Aleatória , Ratos , Ratos Wistar , Vitamina E/administração & dosagem , Vitamina E/farmacocinética , Vitamina E/normas
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