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1.
ACS Omega ; 9(22): 23822-23831, 2024 Jun 04.
Article En | MEDLINE | ID: mdl-38854564

Increasing the rate of penetration (ROP) is an effective means to improve the drilling efficiency. At present, the efficiency and accuracy of intelligent prediction methods for the rate of penetration still need to be improved. To improve the efficiency and accuracy of rate of penetration prediction, this paper proposes a ROP prediction model based on Informer optimized by principal component analysis (PCA). We take the Taipei Basin block oilfield as an example. First, we use principal component analysis to extract data features, transforming the original data into low-dimensional feature data. Second, we use the PCA-optimized data to build an Informer model for predicting ROP. Finally, combined with actual data and using the recurrent neural network (RNN) and long short-term memory (LSTM) as baselines, we perform algorithm performance comparative analysis using root-mean-square error (RMSE), mean absolute error (MAE), and coefficient of determination (R 2). The results show that the average MAE, RMSE, and R 2 of the PCA-Informer model are 9.402, 0.172, and 0.858, respectively. Compared with other methods, it has a larger R 2 and smaller RMSE and MAPE, indicating that this method significantly outperforms existing methods and provides a new solution to improve the rate of penetration in actual drilling operations.

2.
J Adv Res ; 56: 167-179, 2024 Feb.
Article En | MEDLINE | ID: mdl-37059221

INTRODUCTION: Metastasis is an important cause of high mortality and lethality of oral cancer. Fusobacterium nucleatum (Fn) can promote tumour metastasis. Outer membrane vesicles (OMVs) are secreted by Fn. However, the effects of Fn-derived extracellular vesicles on oral cancer metastasis and the underlying mechanisms are unclear. OBJECTIVES: We aimed to determine whether and how Fn OMVs mediate oral cancer metastasis. METHODS: OMVs were isolated from brain heart infusion (BHI) broth supernatant of Fn by ultracentrifugation. Tumour-bearing mice were treated with Fn OMVs to evaluate the effect of OMVs on cancer metastasis. Transwell assays were performed to determine how Fn OMVs affect cancer cell migration and invasion. The differentially expressed genes in Fn OMV-treated/untreated cancer cells were identified by RNA-seq. Transmission electron microscopy, laser confocal microscopy, and lentiviral transduction were used to detect changes in autophagic flux in cancer cells stimulated with Fn OMVs. Western blotting assay was performed to determine changes in EMT-related marker protein levels in cancer cells. Fn OMVs' effects on migration after blocking autophagic flux by autophagy inhibitors were determined by in vitro and in vivo experiments. RESULTS: Fn OMVs were structurally similar to vesicles. In the in vivo experiment, Fn OMVs promoted lung metastasis in tumour-bearing mice, while chloroquine (CHQ, an autophagy inhibitor) treatment reduced the number of pulmonary metastases resulting from the intratumoral Fn OMV injection. Fn OMVs promoted the migration and invasion of cancer cells in vivo, leading to altered expression levels of EMT-related proteins (E-cadherin downregulation; Vimentin/N-cadherin upregulation). RNA-seq showed that Fn OMVs activate intracellular autophagy pathways. Blocking autophagic flux with CHQ reduced in vitro and in vivo migration of cancer cells induced by Fn OMVs as well as reversed changes in EMT-related protein expression. CONCLUSION: Fn OMVs not only induced cancer metastasis but also activated autophagic flux. Blocking autophagic flux weakened Fn OMV-stimulated cancer metastasis.


Fusobacterium nucleatum , Mouth Neoplasms , Animals , Mice , Autophagy
3.
Int Dent J ; 73(2): 186-194, 2023 Apr.
Article En | MEDLINE | ID: mdl-35810010

OBJECTIVES: Periodontitis is a chronic inflammatory illness that may lead to tooth loosening and even loss, and its pathogenesis is not fully understood. Ferroptosis is an iron-dependent, regulated cell death. The present study aims to find the key ferroptosis-related genes (FRGs) in periodontitis and develop an mRNA-miRNA-lncRNA network to deeply explore the pathogenesis of periodontitis. METHODS: Data from the Gene Expression Omnibus (GEO) database and FerrDb database were downloaded to discover the differentially expressed mRNA, miRNA, and FRGs. Functional enrichment analysis was conducted for the differentially expressed FRGs (DE-FRGs), including gene ontology, Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway, and protein-protein interaction (PPI) network analysis. Targetscan and miRtarbase were used to estimate the miRNAs that DE-FRGs may interact with, whilst StarBase v3.0 was used for lncRNA-miRNA interaction. RESULTS: Seven DE-FRGs were identified through differential expression analysis. Interleukin 1 beta (IL1B) interacted with XBP1 and MMP13 in the PPI network. After taking the intersection between DE-miRNAs and predicted miRNAs, a ceRNA network containing IL1B, has-miR-185, has-miR-204, has-miR-211, has-miR-4306, and 28 lncRNAs was established. CONCLUSIONS: Seven FRGs in periodontitis were identified, which might promote deeper understanding of ferroptosis in periodontitis.


Ferroptosis , MicroRNAs , Periodontitis , RNA, Long Noncoding , Humans , RNA, Long Noncoding/genetics , RNA, Long Noncoding/metabolism , Gene Regulatory Networks , MicroRNAs/genetics , RNA, Messenger/genetics
4.
Int Dent J ; 73(2): 178-185, 2023 Apr.
Article En | MEDLINE | ID: mdl-35820930

OBJECTIVES: Oral cancer is the ninth most common cancer worldwide and a leading cause of cancer-related death. Oral squamous cell carcinoma (OSCC) accounts for 90% of all oral cancers. Autophagy is a conserved essential catabolic process related to OSCC. The aim of this study was to elucidate diagnostic and prognostic autophagy-related biomarkers in OSCC. METHODS: The OSCC gene expression data set was obtained from the Gene Expression Omnibus (GEO) database. Differentially expressed genes (DEGs) between the OSCC samples and adjacent healthy tissues were identified by R software. The Human Autophagy Database was screened, which revealed 222 autophagy-related genes. The autophagy-related DEGs were identified. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were applied. Protein-protein interaction network analysis was performed in the STRING database. cytoHubba in the Cytoscape software was applied to determine the top 10 hub genes. The data set of patients with OSCC from The Cancer Genome Atlas (TCGA) was used to evaluate the prognostic value of the 10 hub genes. The association between prognosis-related hub genes and immune infiltrates was explored. RESULTS: Twenty-seven autophagy-related DEGs were identified. The top 10 hub genes were CCL2, CDKN2A, CTSB, CTSD, CXCR4, ITGA6, MAP1LC3A, MAPK3, PARP1, and RAB11A. ITGA6 was identified as the most efficient biomarker. Receiver operating characteristic curve analysis indicated that ITGA6 had the highest diagnostic accuracy for OSCC (area under the curve = 0.925). ITGA6 expression was significantly related to immune infiltrates. CONCLUSIONS: The autophagy-related gene ITGA6 might be an efficient diagnostic and prognostic biomarker in OSCC.


Carcinoma, Squamous Cell , Head and Neck Neoplasms , Mouth Neoplasms , Humans , Squamous Cell Carcinoma of Head and Neck , Carcinoma, Squamous Cell/pathology , Mouth Neoplasms/pathology , Gene Expression Profiling , Biomarkers, Tumor/genetics , Prognosis , Integrin alpha6/genetics
5.
Contrast Media Mol Imaging ; 2022: 1470389, 2022.
Article En | MEDLINE | ID: mdl-36101801

Pulpitis is one of the common diseases indicated by the department of stomatology that is located in the tooth and contains abundant nerve vessels. In order to evaluate the pain degree and functional recovery of patients after treatment by visual analogue pain scale (VAS) and temporomandibular joint function score, a retrospective analysis was performed on 128 patients diagnosed with pulpitis who received root canal treatment in the department of stomatology from January 2020 to March 2021. The results show that 3%NaClO combined with 0.9% sodium chloride injection can effectively relieve the pain degree of patients after treatment, and the antibacterial effect is significantly better than 3%H2O2 combined with 0.9% normal saline. Meanwhile, it can effectively improve the temporomandibular joint function and reduce the recurrence rate, which has good clinical application value.


Pulpitis , Dental Pulp Cavity , Humans , Hydrogen Peroxide/therapeutic use , Pain , Pain Measurement , Pulpitis/drug therapy , Retrospective Studies , Temporomandibular Joint
6.
Mol Omics ; 18(5): 439-448, 2022 06 13.
Article En | MEDLINE | ID: mdl-35416237

PURPOSES: To identify the circular RNA (circRNA) expression profile in the synovium of patients with osteoarthritis (OA) and explore their potential regulatory mechanism. METHODS: Transcriptome high-throughput sequencing was used to detect the expression profiles of circRNA and mRNA. We performed real-time PCR for the validation of circRNAs and used bioinformatics analysis to predict their possible biological functions. The conservation of circRNAs was evaluated, a circRNA-miRNA-mRNA interaction network was constructed and the receiver operating characteristic (ROC) curves of target genes were also drawn. RESULTS: We found 136 differentially expressed circRNAs, 64 upregulated and 72 downregulated. We also found 2035 differentially expressed mRNAs, 1216 upregulated and 819 downregulated. It was verified by qRT-PCR that hsa_circ_0072697 was significantly upregulated. The GO analysis results showed that the parental genes were mainly enriched in organelle organization, cytosol and anion binding. The most enriched pathways for these circRNAs participated in cellular senescence. And hsa_circ_0072697 might act as a sponge of hsa-miR-6736-5p, which could therefore lead to increased LEP and ULK1 mRNA expression. CONCLUSIONS: CircRNAs are significantly expressed in the knee synovium of OA patients and may play an important role in the occurrence and development of OA. The potential mechanism could be sponging miRNAs to increase mRNA expression.


MicroRNAs , Osteoarthritis , RNA, Circular , Computational Biology , Humans , MicroRNAs/genetics , Osteoarthritis/genetics , RNA, Circular/genetics , RNA, Messenger/genetics , Synovial Membrane/metabolism
7.
Front Microbiol ; 13: 815638, 2022.
Article En | MEDLINE | ID: mdl-35391731

Periodontitis is a chronic inflammatory oral disease that affects nearly 50% of all adults. Fusobacterium nucleatum (F. nucleatum) is known to be involved in the formation and development of periodontitis. Outer membrane vesicles (OMVs) harboring toxic bacterial components are continuously released during F. nucleatum growth and regulate the extent of the inflammatory response by controlling the functions of immune and non-immune cells in tissues. Macrophages are important immune cells in periodontal tissue that resist pathogen invasion and play an important role in the pathophysiological process of periodontitis. However, the role of the interaction between F. nucleatum OMVs and macrophages in the occurrence and development of periodontitis has not been studied. The purpose of this study was to clarify the effect of F. nucleatum OMVs on the polarization of macrophages and the roles of this specific polarization and F. nucleatum OMVs in the pathophysiology of periodontitis. The periodontitis model was established by inducing ligation in C57BL/6 mice as previously described. Micro-CT, RT-qPCR, hematoxylin-eosin (H&E) and tartrate acid phosphatase (TRAP) staining assays were performed to analyze the periodontal tissue, alveolar bone loss, number of osteoclasts and expression of inflammatory factors in gingival tissue. The changes in the state and cytokine secretion of bone marrow-derived macrophages (BMDMs) stimulated by F. nucleatum OMVs were observed in vivo by confocal microscopy, flow cytometry, Western blot and ELISA. Mouse gingival fibroblasts (MGFs) were isolated and then cocultured with macrophages. The effects of F. nucleatum OMVs on the proliferation and apoptosis of MGFs were analyzed by flow cytometry and lactate dehydrogenase (LDH) assays. The periodontitis symptoms of mice in the F. nucleatum OMVs + ligation group were more serious than those of mice in the simple ligation group, with more osteoclasts and more inflammatory factors (IL-1ß, IL-6, and TNF-α) being observed in their gingival tissues. M0 macrophages transformed into M1 macrophages after the stimulation of BMDMs with F. nucleatum OMVs, and the M1 macrophages then released more inflammatory cytokines. Analysis of the coculture model showed that the MGF apoptosis and LDH release in the inflammatory environment were increased by F. nucleatum OMV treatment. In conclusion, F. nucleatum OMVs were shown to aggravate periodontitis, alveolar bone loss and the number of osteoclasts in an animal model of periodontitis. F. nucleatum OMVs promoted the polarization of macrophages toward the proinflammatory M1 phenotype, and the inflammatory environment further aggravated the toxicity of F. nucleatum OMVs on MGFs. These results suggest that M1 macrophages and F. nucleatum OMVs play roles in the occurrence and development of periodontitis.

8.
PLoS One ; 17(2): e0263383, 2022.
Article En | MEDLINE | ID: mdl-35113928

Using microdata from the Chinese General Social Survey (CGSS 2010), this paper investigates whether there are green returns to education in China, where educational attainment promotes pro-environmental attitudes and behaviors. We establish causality by exploiting the exogenous variation induced by the implementation of the Compulsory Schooling Law (CSL) in China. We find evidence that educational attainment is associated with higher levels of pro-environmental attitudes and behaviors, and these estimates are robust to various robustness checks. Further analysis reveals that the acquisition of environmental knowledge is the channel that drives the effect of education on pro-environmental attitudes and behaviors. Finally, the effects of education are heterogeneous across individuals.


Education , Environment , Attitude , China , Climate Change , Educational Status , Health Behavior , Health Knowledge, Attitudes, Practice , Health Status , Humans , Knowledge , Regression Analysis , Reproducibility of Results , Socioeconomic Factors , Surveys and Questionnaires
9.
J Periodontol ; 92(7): 1036-1048, 2021 07.
Article En | MEDLINE | ID: mdl-33094479

BACKGROUND: Occlusal trauma can aggravate periodontitis, but the mechanism remains unclear. Yes-associated protein (YAP), a mechanical stressor protein, may play an important role in this process. METHODS: Western blot and quantitative real-time polymerase chain reaction (qRT-PCR) were applied to detect the expression of YAP and inflammatory factors in patients with periodontitis accompanied with or without occlusal trauma. Through local administration of Porphyromonas gingivalis and composite resin bonding on maxillary molars in mice, we established periodontitis and occlusal trauma models. Treatment with or without XAV939, to inhibit YAP activation, was performed in these models. Micro-computed tomography, immunofluorescence (IF), and qRT-PCR were used to explore the YAP pathway in periodontitis with occlusal trauma. Cyclic stress and lipopolysaccharide (LPS) stimuli were applied to the L929 mouse fibroblast cell line with or without XAV939. Western blot, IF, and qRT-PCR were used to verify the in vivo results. RESULTS: Activated dephosphorylated YAP and increased expression of inflammatory factors were observed in patients with periodontitis accompanied with occlusal trauma. In the mouse model of periodontitis with occlusal trauma, YAP transferred into the nucleus, resulting in Jun N-terminal kinases (JNK) related pro-inflammatory pathway up-regulation. L929 cell cyclic stress and LPS stimulation results confirmed the in vivo results. Application of XAV939 inhibited YAP protein dephosphorylation and reduced JNK pro-inflammatory pathway factor expression in vivo and in vitro. CONCLUSIONS: Occlusal trauma can activate YAP nuclear transfer, resulting in the up-regulation of the JNK pro-inflammatory pathway. This can be inhibited by the XAV939 YAP inhibitor.


Dental Occlusion, Traumatic , Periodontitis , Animals , Dental Occlusion, Traumatic/complications , Humans , Lipopolysaccharides , Mice , Porphyromonas gingivalis , X-Ray Microtomography
10.
Zhonghua Kou Qiang Yi Xue Za Zhi ; 50(1): 18-22, 2015 Jan.
Article Zh | MEDLINE | ID: mdl-25779070

OBJECTIVE: To investigate the Raman spectral characteristics of oral squamous cell carcinoma, high-grade epithelial dysplasia and normal mucosa. METHODS: Fifty- six fresh samples of oral carcinoma, 50 of high-grade epithelial dysplasia and 32 of normal mucosa were collected. The i-Raman spectrometer with an optical fiber tube was applied to acquire Raman spectrum. The diagnostic model established by principle component analysis (PCA) and discriminant function analysis (DFA) was used to analyze and classify the spectra of different samples. RESULTS: There were significant differences among the Raman spectra of these samples. Compared with the spectra of normal mucosa, the spectra of oral carcinoma and dysplasia showed strong peaks which were contributed to nucleic acids, proteins and lipids. The diagnostic models established by PCA-DFA could successfully classify these Raman spectra of different samples with a high accuracy of 96.4% (133/138). The model was evaluated by 'Leave one out' cross-validation and reached a high accuracy of 92.8% (128/138). CONCLUSIONS: The proliferation and metabolism of oral squamous cell carcinoma and epithelial high-grade dysplasia are more active than normal mucosa. The diagnostic models established by PCA-DFA can classify these Raman spectra of different samples with a high accuracy.


Carcinoma, Squamous Cell/chemistry , Epidermis/chemistry , Mouth Mucosa/chemistry , Mouth Neoplasms/chemistry , Spectrum Analysis, Raman , Carcinoma, Squamous Cell/pathology , Discriminant Analysis , Epidermis/pathology , Humans , Mouth Neoplasms/pathology , Mucous Membrane/chemistry , Principal Component Analysis
11.
Teach Learn Med ; 26(4): 412-9, 2014.
Article En | MEDLINE | ID: mdl-25318039

BACKGROUND: A comprehensive search of the literature published between 2001 and 2010 was performed to gain a greater understanding of curricular reform practices at Chinese medical schools. SUMMARY: There were 10,948 studies published between 2001 and 2010 that were retrieved from the database. Following preliminary screening, 76 publications from 49 different medical schools were selected. Thirty-one publications regarding clinical medicine curricular reforms were analyzed further. Of the 76 studies, 53 described curricular reforms that were instituted in theoretical courses, 22 described curricular reforms that were instituted in experimental courses, and 1 described curricular reforms that were instituted in a clinical skills training course. Of the 31 clinical medicine publications, 2 described reforms that were implemented for 3-year program medical students, 12 described reforms that were implemented for 5-year program medical students, 6 described reforms that were implemented for 7-year program medical students, and 2 described reforms that were implemented for 8-year program medical students. Currently, the majority of medical schools in China use the discipline-based curriculum model. Thirteen studies described transition to an organ-system-based curriculum model, 1 study described transition to a problem-based curriculum model, and 3 studies described transition to a clinical presentation-based curriculum model. In 7 studies educators decided to retain the discipline-based curriculum model while integrating 1 or several new courses to remedy the weaker aspects of the traditional curriculum, in 7 studies educators decided to integrate the preclinical courses with the clinical courses by using the systemic-integrating curricular system that dilutes classical disciplines and integrates material based on organ systems, and in 2 studies educators limited reforms to clinical courses only. Eight studies discussed the implementation of a formative evaluation system, 4 studies discussed faculty training, and 15 studies discussed the application of various instructional methods. Other issues that were also addressed include enhancing research, improving patient-doctor communication, developing interpersonal and teamwork skills, cultivating independent lifelong learning habits, and improving problem-solving capabilities. CONCLUSIONS: The medical schools in our study have adopted various comprehensive curricular changes, moving from a knowledge-based to a competency-based model, and from traditional standards to international standards. Many institutions face challenges when implementing curricular reforms, such as what to integrate and how to do so, the unintended omission of important material, ensuring coordination between different organizations and departments, and the training of faculty.


Curriculum/trends , Education, Medical/trends , Schools, Medical/organization & administration , China , Humans , Organizational Innovation
12.
Med Teach ; 36(12): 1043-50, 2014 Dec.
Article En | MEDLINE | ID: mdl-24896639

INTRODUCTION: Curriculum reform at Chinese medical schools has attracted a lot of attention recently. Several leading medical schools in China have undergone exploratory reforms and in so doing, have accumulated significant experience and have made considerable progress. METHODS: An analysis of the reforms conducted by 38 Chinese medical colleges that were targeted by the government for upgrade was performed. Drawing from both domestic and international literature, we designed a questionnaire to determine what types of curricular reforms have occurred at these institutions and how they were implemented. Major questions touched upon the purpose of the reforms, curricular patterns, improvements in teaching methods post-reform, changes made to evaluation systems post-reform, intra-university reform assessment, and what difficulties the schools faced when instituting the reforms. Besides the questionnaire, relevant administrators from each medical school were also interviewed to obtain more qualitative data. RESULTS: Out of the 38 included universities, twenty-five have undergone major curricular reforms. Among them, 60.0% adopted an organ system-based curriculum model, 32.0% adopted a problem-based curriculum model, and 8.0% adopted a hybrid curriculum model. About 60.0% of the schools' reforms involved both the "pre-clinical" and the "clinical" curricula, 32.0% of the schools' reforms were limited to the "pre-clinical" curricula, and 8.0% of the schools' reforms only involved the "clinical" curricula. Following curricular reform, 60.0% of medical schools experienced an overall reduction in teaching hours, 76.0% reported an increase in their students' clinical skills, and 60.0% reported an increase in their students' research skills. DISCUSSION: Medical curricular reform is still in its infancy in China. The republic's leading medical schools have engaged in various approaches to bring innovative teaching methods to their respective institutions. However, due to limited resources and the shackle of traditional pedagogical beliefs among many faculty and administrators, progress has been significantly hindered. Despite these and other challenges, many medical schools report positive initial results from the reforms that they have enacted. Although the long term effects of such reforms remain unclear, curricular reform appears to be the inevitable solution to China's growing need for high-quality medical doctors.


Curriculum/standards , Quality Improvement/organization & administration , Schools, Medical , Education, Medical, Undergraduate , Organizational Innovation , Schools, Medical/organization & administration , Surveys and Questionnaires , Taiwan
13.
Med Teach ; 36(7): 615-20, 2014 Jul.
Article En | MEDLINE | ID: mdl-24787523

INTRODUCTION: In North America, where it was born, problem-based learning (PBL) has seen dips and rises in its popularity, but its inherent strengths have led to its spread to medical schools all over the world. Although its use at medical schools in some Western countries has already been examined, no one has looked at its status in many other countries, including China. The aim of this study is to determine the number of schools currently using PBL in China, the degree to which they use it, and the reasoning behind such usage. METHODS: We used survey and internet search to examine PBL usage at Chinese medical schools. We were able to collect data from 43 first-class Chinese medical schools that are geographically diverse and thus representative of medical schools all across China. RESULTS: 34 (79.1%) of the 43 medical schools use PBL in the preclinical curriculum. Of the 34, data were collected from 24 (70.6%) medical schools regarding the extent of their PBL usage. Nine (37.5%) schools use PBL for less than 10% of preclinical hours, 14 (58.3%) schools use PBL for 10-50% of preclinical hours, and one (4.2%) school uses PBL for more than 50% of preclinical hours. CONCLUSION: In our sample of Chinese medical institutions, a large majority of schools use PBL, however, most schools use it for less than 50% of total preclinical curricular hours. Our results suggest that schools are interested in increasing the number of curricular hours devoted to PBL but are constrained by resources.


Education, Medical, Undergraduate/methods , Problem-Based Learning/statistics & numerical data , Schools, Medical/statistics & numerical data , China , Data Collection , Education, Medical, Undergraduate/economics , Education, Medical, Undergraduate/statistics & numerical data , Faculty, Medical/statistics & numerical data , Humans , Internet , Problem-Based Learning/economics , Problem-Based Learning/methods , Resource Allocation , Schools, Medical/economics
14.
Zhongguo Zhong Yao Za Zhi ; 37(14): 2164-7, 2012 Jul.
Article Zh | MEDLINE | ID: mdl-23126207

To study the effect of Banxiaxiexin Tang and different conbinations on CYP450 in rat liver microsomes, from the point of liver metabolism, evaluate significance of Banxiaxiexin Tang compatibility. The rats were randomly divided into five groups: Banxiaxiexin Tang group, pungent-swelling group, bitter-descending group, sweet-invigorating group and control group, which were all given decoction by gavage. Using liver microsomes in vitro incubation method, probe substrate were incubated and their metabolites was detected by ultra-high performance liquid chromatography, then was calculated metabolic rate to reflect the drug-treated liver microsomes CYP2C6, CYP2E1, CYP3A1/2 activity. The results showed that comparing with the control group, both Banxiaxiexin Tang group and bitter-descending group showed inhibition on all enzyme subtype (P < 0.01), pungent-swelling group showed significant inhibition on CYP2C6, but no inhibition on CYP2E1 and CYP3A1/2; sweet-invigorating group showed inhibition on CYP2C6 and CYP2E1, but no inhibition on CYP3A1/2. Compared the inhibition on CYP with the three conbinations, bitter-descending group was significant higher than other groups. Banxiaxiexin Tang group showed inhibition on rat liver microsomes CYP450, and the activity maybe come from bitter-descending group.


Cytochrome P-450 Enzyme System/metabolism , Liver/drug effects , Plant Extracts/pharmacology , Animals , Drug Compounding , Liver/enzymology , Male , Rats , Rats, Sprague-Dawley
15.
Zhong Yao Cai ; 35(8): 1286-90, 2012 Aug.
Article Zh | MEDLINE | ID: mdl-23320363

OBJECTIVE: To study the metabolism kinetics of baicalin and baicalein from Scutellaria baicalensis in rat liver microsomes and compare the effect of Banxiaxiexin-Decoction with different combinations on the metabolic activities of the flavonoids (baicalin and baicalein). METHODS: An UPLC method was developed for determination of baicalin and baicalein in rat liver microsomes incubation system. The effect of Banxiaxiexin-Decoction and different combinations (pungent-swelling group, bitter-descending group, sweet-invigorating group) on the metabolic activities of the flavonoids was investigated by vivo-induction and vitro-incubation method. RESULTS: The elimination of the flavonoids was linear, and the metabolism of baicalin had significant eliminated linear within 60 min, baicalein within 10 min. The peak area showed good linear relation when baicalin and baicalein was the concentration of 0.5 - 25 microg/mL. Microsomal protein concentration had significant effect on the flavonoids metabolism with the gradient from 0.2 g/L to 1.0 g/L in their corresponding time, and showed linear elimination with the growth of the concentration. The metabolic rate of baicalein in the blank liver microsomes was bigger than that of baicalin. The effect on metabolic of baicalin and baicalein, comparing the blank group, all parts showed inhibition strongest among the combinations, bitter-descending group second of that, pungent-swelling group had no significant for both, and sweet-invigorating group was without inhibition for baicalin, no significant inhibition for baicalein. CONCLUSION: Banxiaxiexin-Decoction shows inhibition on the metabolic for baicalin and baicalein, and is stronger than other combinations. This provides important pharmacological basis for compound prescription reasonable and clinical compatibility which plays the effect of mutual promotion.


Flavanones/metabolism , Flavonoids/metabolism , Microsomes, Liver/metabolism , Plant Extracts/pharmacology , Animals , Biotransformation/drug effects , Chromatography, High Pressure Liquid/methods , Drug Compounding , Kinetics , Male , Microsomes, Liver/drug effects , Plant Extracts/chemistry , Rats , Rats, Sprague-Dawley , Scutellaria baicalensis/chemistry
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