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1.
Article in Chinese | WPRIM | ID: wpr-928741

ABSTRACT

OBJECTIVE@#To investigate the expression of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9) in multiple myeloma (MM) patients, and analyze the effect of doxycycline (DOX) on the expression of MMP-2 and MMP-9 in MM cells.@*METHODS@#The peripheral blood and bone marrow samples of MM patients were collected, and the patients were divided into three groups: newly diagnosed group, remission group and relapsed/refractory group, while the peripheral blood samples of 34 health people and the bone marrow samples of 17 IDA patients were selected as normal control and control group. The levels of MMP-2 and MMP-9 were detected by ELISA. The protein levels of MMP-2 and MMP-9 in H929 cells treated by different concentrations of DOX were analyzed by Western blot. After H929 cells was treated by Akt inhibitor MK-2206 2HCl in combination with DOX, Western blot was used to detect the levels of MMP-2 and MMP-9.@*RESULTS@#The levels of MMP-2 and MMP-9 in newly diagnosed MM patients were higher than those in control (P<0.05), while for the patients in the remission group were decreased, but still higher than those in control. The levels of MMP-2 and MMP-9 were increased again for the patients in relapsed/refractory group, and showed no significant difference as compared with those in newly diagnosed group. The levels of MMP-2 and MMP-9 could be inhibited by 10 mg/L and 15 mg/L DOX treated by H929 cell. The protein levels of MMP-2 and MMP-9 showed no altered in H929 cells treated by 5 nmol/L MK-2206 2HCl alone. DOX exerted more profound inhibitory effect to MMP-2 and MMP-9 expression in H929 cells when Akt inhibitor MK-2206 2HCl was combined with DOX.@*CONCLUSION@#The levels of MMP-2 and MMP-9 are increased in MM patients and related to the disease status of MM. DOX can inhibit the expression of MMP-2 and MMP-9 in MM cells, and antagonizing its activation of Akt signaling pathway can further enhance the inhibitory effect.


Subject(s)
Doxycycline/pharmacology , Humans , Matrix Metalloproteinase 2/metabolism , Matrix Metalloproteinase 9/metabolism , Multiple Myeloma/metabolism , Proto-Oncogene Proteins c-akt
2.
Article in Chinese | WPRIM | ID: wpr-880067

ABSTRACT

OBJECTIVE@#To investigate the clinical value of expression level of interleukin-2 receptor (IL-2R) and interleukin-8 (IL-8) in the fever patients with hematological malignancies.@*METHODS@#A total of 121 inpatients in the First Affiliated Hospital of Anhui Medical University from April 2018 to October 2019 were enrolled in this study. The patients were separated into infection group (61 cases) and non-infection group (60 cases). In the meantime, 40 healthy people without fever or infection in the hospital for physical examination were set as matched group. C-reactive protein (CRP), procalcitonin (PCT), and cytokines were detected in all the patients with fever after admission and infection control. While, blood samples were taken from healthy people during physical examination.@*RESULTS@#The expression levels of IL-2R in infection group were higher than those in the control group (P<0.001), and the level of serum IL-2R in infection group was also higher than that in the non-infection group (P<0.05). Based on Spearman analysis, in patients with malignant hematologic disease, serum IL-2R level was positively correlated with CRP (r=0.557, P<0.001) and IL-8 (r=0.479, P<0.001), and IL-8 level was positively correlated with CRP (r=0.318, P<0.001). Compared with the non-infection group, the area under the curve (AUC) for the level of CRP, PCT, and IL-2R of the infection group was 0.714 (95%CI: 0.623-0.806), 0.765 (95%CI: 0.680-0.851), and 0.761 (95%CI: 0.686-0.836), the sensitivity was 0.705, 0.852, and 0.705, and the specificity was 0.717, 0.70, and 0.60, respectively. While, AUC of CRP+PCT, CRP+IL-2R, PCT+IL-2R, and CRP+PCT+IL-2R was 0.789 (95%CI: 0.712-0.866), 0.702 (95%CI: 0.623-0.782), 0.757 (95%CI: 0.677-0.838), and 0.789 (95%CI: 0.712-0.866), the sensitivity was 0.738, 0.934, 0.705, and 0.738, and the specificity was 0.840, 0.470, 0.810, and 0.840, respectively.@*CONCLUSION@#CRP, PCT, IL-2R, and IL-8 are useful parameters for diagnosis of the infectious fever in patients with hematological malignancies, which provides the basis of initial diagnosis and rational use of antibioties for clinician.


Subject(s)
Biomarkers , C-Reactive Protein , Calcitonin , Calcitonin Gene-Related Peptide , Hematologic Neoplasms , Humans , Interleukin-8 , Protein Precursors , Receptors, Interleukin-2 , Sepsis
3.
China Pharmacy ; (12): 480-484, 2021.
Article in Chinese | WPRIM | ID: wpr-873490

ABSTRACT

OBJECTIVE:To establish the method for simultaneous determination of 5-fluorouracil(5-FU)and its metabolites 5-fluoro-5,6-dihydrouracil (5-FUH2) in human plasma ,and apply it in the clinic. METHODS :After plasma samples were processed twice by ethyl acetate ,UPLC-MS/MS method was adopted using 5-bromouracil (5-Bru) as internal standard. The determination was performed on Acquity UPLC HSS T 3 column with mobile phase consisted of methanol-water (30 ∶ 70,V/V)at the flow rate of 0.3 mL/min. The column temperature was 20 ℃,and sample size was 5 μL. An electrospray ion source was used to carry out negative ion scanning with multiple reaction monitoring. The capillary voltage was 1.5 kV;the taper hole voltage was 20 V;the desolvent temperature was 450 ℃;the desolvent air flow was 850 L/h;the cone hole gas velocity was 50 L/h. The ion transitions for quantitative analysis were m/z 129.00→41.90(5-FU),m/z 130.87→82.92(5-FUH2),m/z 189.00→42.10(5-Bru), respectively. From Aug. to Oct. 2020,10 patients with advanced colorectal cancer were treated with continuous intravenous drip of 5-FU for 46 hours were collected from Harbin Medicinal University Cancer Hospital. Steady-state plasma concentration of 5-FU and plasma concentration of 5-FUH2 were determined at 18-30 h of continuous intravenous drip. The area under the curve (AUC)for 5-FU and concentration ratio of 5-FUH2/5-FU were calculated. RESULTS :The linear range of 5-FU and 5-FUH2 were 20 to 1 000 μg/mL(R 2>0.990). The quantification limits were 20 ng/mL. RSDs of precision test were all lower than 20%,and relative error ranged ±10%. The extraction recovery and matrix effects didn ’t affect the determination of substance to be measured. Among 10 patients with advanced colorectal cancer ,the steady-state concentration of 5-FU were 180.04-622.83 ng/mL,and AUC of 5-FU ranged from 8.28 to 28.65 mg·h/L. The concentration of 5-FUH2 ranged 336.48-948.43 ng/mL,and concentration ratio of 5-FUH2/ 5-FU ranged 0.93-4.21. AUC of 5-FU in 10 patients had about 3-4 fold individual differences. CONCLUSIONS :The established method has good precision and accuracy ,high sensitivity ,and simple operation. It can be used for plasma monitoring of 5-FU in patients with advanced colorectal cancer.

4.
Journal of Leukemia & Lymphoma ; (12): 588-592, 2021.
Article in Chinese | WPRIM | ID: wpr-907219

ABSTRACT

Objective:To investigate the effect of prognostic nutrition index (PNI) and clinical characteristics on the prognosis of patients with diffuse large B-cell lymphoma (DLBCL).Methods:The clinical data of 236 patients with DLBCL treated in the Affiliated Hospital of Xuzhou Medical University from November 2014 to December 2018 were retrospectively analyzed. X-Tile software and restricted cubic spline (RCS) were used to determine the best cut-off values of PNI, age and hemoglobin; Cox proportional hazard regression model was used for univariate and multivariate analyses; Kaplan-Meier method was used to analyze the overall survival (OS) of patients, and log-rank test was also performed.Results:One-hundred and fifteen of the 236 patients (48.7%) died, with a median OS time of 32 months. The 3-year OS rate was 46%, and the 5-year OS rate was 36%. The best cut-off value of PNI was 49. There was a significant non-linear relationship between PNI and the risk of poor prognosis of DLBCL ( χ2=34.64, P < 0.01); the analysis of the dose-response relationship showed that with the change of PNI, the correlation strength of the risk of poor prognosis declined non-linearly. The best cut-off value of age was 63 years old, and the correlation strength between age and the risk of poor prognosis of DLBCL showed a non-linear upward trend ( χ2=14.86, P=0.022). The best cut-off values of hemoglobin calculated by X-Tile software were 93 g/L and 129 g/L. Multivariate analysis showed that PNI, central nervous system involvement, liver involvement, age, hemoglobin, international prognostic index (IPI) score, and bulky disease were independent influencing factors of OS in DLBCL patients (all P < 0.05). In patients with germinal center B-cell-like (GCB) subtype, bcl-2-positive and bcl-6-positive, there were statistical differences in the 3-year OS rate of patients with PNI < 49 and PNI ≥ 49 (all P < 0.05). Conclusion:PNI has a certain value in the prognosis assessment of DLBCL patients, and PNI ≥ 49 indicates that the patient has a good prognosis.

5.
Article in Chinese | WPRIM | ID: wpr-905943

ABSTRACT

Objective:To analyze the compatibility rules of prescriptions containing Forsythiae Fructus based on data mining and explore the anti-inflammatory mechanism of Forsythiae Fructus based on network pharmacology,so as to provide reference for the rational clinical application of Forsythiae Fructus and the development of health foods and new Chinese medicines. Method:The prescriptions containing Forsythiae Fructus in the<italic> Dictionary of Traditional Chinese Medicine Prescriptions</italic> were collected,based on which a clinical prescription database was constructed. The Chinese herbs combined with Forsythiae Fructus and the corresponding indications were subjected to frequency statistics,association rule analysis,and complex network analysis using SPSS Statistics 26,IBM SPSS Modeler 18.0,and Gephi 9.2. The active components and targets of Forsythiae Fructus for anti-inflammation were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP),BATMAN-TCM,and SEA,and the targets related to anti-inflammation from GeneCards,Online Mendelian Inheritance in Man (OMIM),CTD,and GenCLiP3. Following the analysis of protein-protein interactions (PPI) with STRING,a PPI network was constructed. The enrichment analysis was performed using Metascape,and the active component-anti-inflammation target-signaling pathway network of Forsythiae Fructus was constructed by Cytoscape 3.8.2. Result:According to the inclusion and exclusion criteria,2 245 prescriptions containing Forsythiae Fructus were harvested,involving 512 Chinese herbs,with a total usage frequency of 27 314. The Chinese herbs that were most frequently combined with Forsythiae Fructus (>800 times) were Glycyrrhizae Radix et Rhizoma (1 483 times),Scutellariae Radix (964 times),and Angelicae Sinensis Radix (842 times). Hence,the herbal pairs "Forsythiae Fructus-Scutellariae Radix" and "Forsythiae Fructus-Angelicae Sinensis Radix" were further explored. The prescriptions containing Forsythiae Fructus could be utilized for the treatment of 29 kinds of diseases,and three representative disease categories including "carbuncle,gangrene,sores and ulcers","ophthalmic diseases and syndromes" and "epidemic diseases" are selected for data mining. There were 19 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Lonicerae Japonicae Flos-Angelicae Sinensis Radix" as the core herb combination for "carbuncle,gangrene,sores and ulcers". The clustering analysis revealed one multi-herb clustering group,four herbal pairs,and single herb Lonicerae Japonicae Flos,the complex network analysis four herbal modules,and the factor analysis six common factors. There were 23 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Scutellariae Radix-Angelicae Sinensis Radix" as the core herb combination for "ophthalmic diseases and syndromes". The clustering analysis revealed two multi-herb clustering groups and four herbal pairs,the complex network analysis four herbal modules,and the factor analysis five common factors. There were 28 association rules obtained with "Forsythiae Fructus-Glycyrrhizae Radix et Rhizoma-Menthae Haplocalycis Herba-Lonicerae Japonicae Flos" as the core herb combination for "epidemic diseases". The clustering analysis revealed three multi-herb clustering groups,one herbal pair,and two single herbs Forsythiae Fructus and Glycyrrhizae Radix et Rhizoma,the complex network analysis four herbal modules,and the factor analysis five common factors. As demonstrated by network pharmacology-based analysis,the core anti-inflammation components of Forsythiae Fructus were quercetin,luteolin,and kaempferol,and the core targets were phosphoinositide-3-kinase regulatory subunit 1 (PIK3R1),protein kinase B 1 (Akt1),and epidermal growth factor receptor(EGFR). The biological pathways were mainly concentrated in proteoglycans in cancer,pathways in cancer,and PI3K/Akt signaling pathway,with such functions as inhibition of transcription factors,regulation of enzyme activity,and inflammation-related gene expression involved. Conclusion:This study employed a variety of data mining techniques to objectively,intuitively,and scientifically uncover the compatibility rules of Forsythiae Fructus in the treatment of high-frequency diseases. It has been found that Forsythiae Fructus is often combined with heat-clearing herbs,tonifying herbs,exterior-releasing herbs,and blood-activating and stasis-resolving herbs for diverse diseases and syndromes. Under the premise of clearing heat and removing toxin,reinforcing healthy Qi and dredging stagnation are also emphasized. According to the degree of internal heat exuberance,the heat-clearing herbs with different merits are combined. This study has revealed the unique advantages of Forsythiae Fructus in the treatment of specific diseases and syndromes as well as its multi-component,multi-target,and multi-pathway mechanisms in anti-inflammation,breaking through the limitations in modern clinical and experimental research of Forsythiae Fructus. These findings are of great significance for guiding the rational clinical application of Forsythiae Fructus and the development of health foods and new Chinese medicines,thus better accelerating the development of Chinese medicine health industry.

6.
Article in Chinese | WPRIM | ID: wpr-905937

ABSTRACT

Objective:To investigate the effects of polyethylene glycol 400 (PEG400) on the pharmacokinetics and anti-inflammatory effect of baicalin, and to preliminarily explore the anti-inflammatory effects of baicalin and its main metabolite baicalein 6-<italic>O</italic>-<italic>β</italic>-<italic>D</italic>-glucuronide (B6G) by molecular docking. Method:Rats were randomly divided into two groups with water and PEG400 as the dissolving matrix, and rats were administrated the equal dose of baicalin aqueous solution (baicalin+water group) and baicalin PEG400 solution (baicalin+PEG400 group). After the plasma samples were processed at different time periods, the concentrations of baicalin and B6G in rat plasma were determined by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS), and pharmacokinetic parameters were processed by DAS 3.2.2 software. Mice were randomly divided into a blank group (normal saline, 20 mL·kg<sup>-1</sup>), aspirin group (dose of 0.2 g·kg<sup>-1</sup>), baicalin/baicalin+PEG400 high and low dose (3.0, 1.5 g·kg<sup>-1</sup>) groups, after continuous administration for 7 days, the mouse ear swelling and foot swelling models were established, and the swelling degree and swelling inhibition rate were calculated. Result:The pharmacokinetic study showed that compared with baicalin+water group, the plasma concentrations of baicalin and B6G increased after administration of baicalin PEG400 solution, and the area under the curve (AUC<sub>0-</sub><italic><sub>t</sub></italic>) increased by 2.36, 1.97 times, and the peak concentration (<italic>C</italic><sub>max</sub>) increased by 2.12, 1.65 times, respectively. The results of mouse ear and foot swelling inflammation models showed that the anti-inflammatory effect was enhanced after intragastric administration of baicalin PEG400 solution. In addition, molecular docking results showed that baicalin and B6G could site bind to multiple target proteins [tumor necrosis factor (TNF)-<italic>α</italic>, interleukin (IL)-6, IL-1<italic>β</italic>, prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) and nuclear transcription factor-<italic>κ</italic>B (NF-<italic>κ</italic>B)] with higher affinity, which was superior to the positive drug aspirin. Conclusion:PEG400 can increase the plasma concentration of baicalin and its main metabolite B6G, and enhance the anti-inflammatory effect. Baicalin and B6G can form strong hydrogen bonds with various inflammatory factors and of nuclear transcription factors, it is speculated that baicalin and B6G jointly play an anti-inflammatory role.

7.
Article in English | WPRIM | ID: wpr-888702

ABSTRACT

Oral immunosuppression caused by smoking creates a microenvironment to promote the occurrence and development of oral mucosa precancerous lesions. This study aimed to investigate the role of metabolism and macrophage polarization in cigarette-promoting oral leukoplakia. The effects of cigarette smoke extract (CSE) on macrophage polarization and metabolism were studied in vivo and in vitro. The polarity of macrophages was detected by flow cytometric analysis and qPCR. Liquid chromatography-mass spectrometry (LC-MS) was used to perform a metabolomic analysis of Raw cells stimulated with CSE. Immunofluorescence and flow cytometry were used to detect the polarity of macrophages in the condition of glutamine abundance and deficiency. Cell Counting Kit-8 (CCK-8), wound-healing assay, and Annexin V-FITC (fluorescein isothiocyanate)/PI (propidium iodide) double-staining flow cytometry were applied to detect the growth and transferability and apoptosis of Leuk-1 cells in the supernatant of Raw cells which were stimulated with CSE, glutamine abundance and deficiency. Hyperkeratosis and dysplasia of the epithelium were evident in smoking mice. M2 macrophages increased under CSE stimulation in vivo and in vitro. In total, 162 types of metabolites were detected in the CSE group. The metabolites of nicotine, glutamate, arachidic acid, and arginine changed significantly. The significant enrichment pathways were also selected, including nicotine addiction, glutamine and glutamate metabolism, and arginine biosynthesis. The results also showed that the supernatant of Raw cells stimulated by CSE could induce excessive proliferation of Leuk-1 and inhibit apoptosis. Glutamine abundance can facilitate this process. Cigarette smoke promotes oral leukoplakia via regulating glutamine metabolism and macrophage M2 polarization.


Subject(s)
Animals , Glutamine , Leukoplakia, Oral , Macrophages , Mice , Smoking , Tumor Microenvironment
8.
Article in Chinese | WPRIM | ID: wpr-888145

ABSTRACT

Twenty batches of Aurantii Fructus Immaturus(AFI) were collected, with their peel and pulp taken as research objects. Ultra-high performance liquid chromatography(UPLC) fingerprints of peel and pulp of AFI were established with 17 common peaks in peel and 10 in pulp. Six kinds of flavonoids were identified, i.e., narirutin, naringin, rhoifolin, hesperidin, neohesperidin and nobiletin. The Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine was employed for similarity analysis, which showed that the chromatographic peaks of peel and pulp were basically similar to their respective reference fingerprints, with all similarities greater than 0.90. The similarity between peel and pulp of the same batch of AFI ranged from 0.850 to 0.983. Cluster analysis(CA), principal component analysis(PCA), and orthogonal partial least squares discriminant analysis(OPLS-DA) were conducted on the common peaks of peel and pulp of AFI with SPSS 17.0 and SIMCA 14.1. Combined with the reference fingerprints, these analyses revealed 12 differential components regarding peel and pulp. Further, the content of the 6 flavonoids and synephrine was determined. The proposed method integrating UPLC fingerprint and multicomponent quantitative analysis is applicable to the quality evaluation of AFI. The results provide a certain basis for the scientific connotation about the appearance characteristic of AFI.


Subject(s)
Chromatography, High Pressure Liquid , Citrus , Drugs, Chinese Herbal , Synephrine
9.
Acta Pharmaceutica Sinica ; (12): 1416-1423, 2021.
Article in Chinese | WPRIM | ID: wpr-887064

ABSTRACT

The aim of this study was to investigate the effects of polyethylene glycol (PEGs) with different molecular weights (MW: 400, 1 000, 4 000) on the pharmacokinetics of baicalin, and preliminarily analyze its mechanism. Rats were gavaged with baicalin (168 mg·kg-1) + aqueous solution or baicalin + PEGs solution and plasma samples were collected from 0 to 24 h after administration. The concentration of baicalin and its main metabolite baicalein 6-O-β-D-glucuronide (B6G) were determined at different time points by UPLC-MS/MS, and the pharmacokinetic parameters were calculated with DAS 3.0 software. The results showed that PEGs with different molecular weights could effectively increase the AUC0-t of baicalin and B6G, increase the Cmax, and prolong the t1/2, effectively increasing the concentration of baicalin and B6G in vivo. The mechanism may be by promoting the activity of uridine diphosphate glucuronosyl-transferases 1A8 (UGT1A8) and 1A9 (UGT1A9), thereby increasing the transformation rate of baicalin and B6G. The rate of metabolism of B6G was faster than that of baicalin, suggesting that PEGs had a higher affinity for UGT1A8, and PEG400 had the most significant effect. The purpose of this study was to provide a basis for the clinical safe use of baicalin and other flavonoids and the design of new dosage forms with the participation of PEGs. The animal experiment protocol in this study was approved by the Experimental Animal Ethics Committee of Guizhou Medical University.

10.
Clinical Medicine of China ; (12): 161-166, 2021.
Article in Chinese | WPRIM | ID: wpr-884151

ABSTRACT

Objective:To investigate the relationship between blood lipid level and low birth weight infants in late pregnancy.Methods:Data of 303 low birth weight newborns delivered in ShengJing Hospital affiliated to China Medical University were collected from January 2018 to February 2020, and 303 cases of full-term normal birth weight infants delivered in our hospital during the same period (birth weight 2500 ~ 3999 g) for retrospective study.The general situation of puerpera was analyzed, including age, gestational age, times of pregnancy, times of labor, weight growth during pregnancy, pre pregnancy body mass index, and blood lipid indexes of puerpera within one week before termination of pregnancy, including triglyceride, total cholesterol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, apolipoprotein A, apolipoprotein B.Results:The normal birth weight group was (31.60±3.90) years old, the weight gain during pregnancy was (16.29±5.31) kg, and the triglyceride levels was(3.21±1.33) mmol/L.The low birth weight group was (30.30±4.65) years old, the weight gain during pregnancy was (14.45±8.08) kg, and the triglyceride level was(2.88±1.37) mmol/L, and there were differences between groups( P<0.01). In the low term birth weight group, birth weight was negatively correlated with maternal age ( r=-0.24, P=0.01), positively correlated with gestational age ( r=0.24, P=0.02), and negatively correlated with pregnancy weight gain ( r=-0.26, P<0.01), and was positively correlated with triglyceride ( r=0.15, P=0.01) and total cholesterol ( r=0.20, P<0.01). Conclusion:The incidence of full-term low birth weight infants is closely related to the blood lipid level, age, gestational age at delivery and the growth of body weight during pregnancy.

11.
China Pharmacy ; (12): 800-805, 2020.
Article in Chinese | WPRIM | ID: wpr-819090

ABSTRACT

OBJECTIVE:To isolate and purify baicalin metabolites from rat bile ,and to study its effect on the proliferation of liver cancer HepG 2 cells. METHODS :Totally of 6 SD rats were collected ,anesthetized and then intubated with bile ducts. They were given baicalin (168 mg/kg)intragastrically after the rats were awake as well as the bile sample 1 was collected during 24 h after intragastric administration. After processed ,bile sample 1 was preliminarily analyzed by HPLC. Another 5 SD rats were anesthetized and intubated in the same way as above ,and then given baicalin intragastrically (400 mg/kg). The bile sample 2 was collected during 48 h after intragastric administration. After processed ,the bile sample 2 was isolated and purified by semi-preparative HPLC. The isolated metabolites were identified by using UV ,IR,MS and NMR ,as well as based on physical and chemical properties. MTT method combined with high content cell imaging analysis system was used to study the effect of the metabolites on the proliferation of HepG 2 cells. RESULTS :Baicalin was mainly metabolized into metabolite 1 and metabolite 2 through bile. After isolation and purification , they were identified as oroxylin A- 7-O-β-D-glucuronide and 2726719792@qq.com baicalein 6-O-β-D-glucuronide. The results of MTT assay showed that the metabolite 2 had a significant inhibitory effect 分析。E-mail:gaoxl@gmc.edu.cn on the proliferation of HepG 2 cells,and its IC 50 was 90 µg/mL;the results of high content cell imaging analysis showed that at a certain concentration metabolite 2 may inhibit proliferation by changing the mitochondrial distribution and membrane permeability of HepG 2 cells(studies on the pharmacological activities of metabolism 1 had been reported ,it was skipped in this study ). CONCLUSIONS :In this study ,two baicalin bile metabolites were successfully isolated and identified ,of which baicalein 6-O-β-D-glucuronide has a significant inhibitory effect on the proliferation of HepG 2 cells.

12.
Article in Chinese | WPRIM | ID: wpr-878777

ABSTRACT

Autophagy is a highly conservative and multi-component activated energy metabolism and self-renewal mechanism, which plays a crucial regulatory role in maintaining the normal physiological state of cells and is involved in various pathological processes. In recent years, the mechanism study has made great progress in regulating autophagy with effective components of Chinese materia medica(CMM),which are reported to prevent and treat cancers, neurodegenerative diseases, cardiovascular diseases and metabolic and immune-related diseases. This review outlines the molecular regulation mechanisms of cell autophagy with CMM components in controlling the above-mentioned diseases. There are many relevant reports on the regulatory mechanisms of autophagy in tumor and cardiovascular cells with CMM monomers. The main chemical structural types are alkaloids, saponins, polyphenols, flavonoids and terpenes. And m-TOR pathway is the main mechanism relating to the regulatory mechanisms of autophagy with CMM. Therefore, the regulatory mec-hanisms of cell autophagy become a new research targeting strategy of therapies with CMM. This review provides evidences for the effectiveness and scientificity of CMM in regulating autophagy, in the expectation of providing references for the in-depth studies of CMM in the field of autophagy and the development of natural autophagy regulators.


Subject(s)
Asians , Autophagy , Drugs, Chinese Herbal/pharmacology , Humans , Materia Medica , Medicine, Chinese Traditional , Saponins
13.
Article in Chinese | WPRIM | ID: wpr-873254

ABSTRACT

Objective::To investigate the effect of polyethylene glycol 400 (PEG400) on rat bile excretion of baicalin and its main metabolite [baicalein 6-O-β-D-glucuronide (B6G)], and to analyze its mechanism of action. Method::Rats were randomly divided into baicalin+ water group and baicalin+ PEG400 group, the anesthesia was induced by intraperitoneal injection of 10% chloral hydrate (dose of 4 mL·kg-1) to prepare a rat bile duct intubation model. After the rats were fully awake, rats were given baicalin aqueous solution and baicalin PEG400 solution with dose of 168 mg·kg-1 for baicalin, respectively. And bile was collected from 0 h to 12 h after administration. UPLC-MS/MS was used to determine the concentration of drug excreted through bile at different time periods. Thermo Hypersil GOLD C18 column was used with acetonitrile (A)-0.1% formic acid solution (B) as the mobile phase for gradient elution (0-9 min, 90%-27%B; 9-10 min, 27%-90%B; 10-12 min, 90%B), the flow rate was 0.3 mL·min-1, the column temperature was 30 ℃, the injection volume was 5 μL. The mass spectra were obtained in positive ion mode with electrospray ionization (ESI). The effects of PEG400 on the activities and expressions in rat liver of uridine diphosphate glucuronyltransferase (UGT) 1A8 and UGT1A9 were studied in vitro incubation assay and enzyme linked immunosorbent assay (ELISA). Result::Compared with the baicalin+ water group, in the baicalin+ PEG400 group, the bile cumulative excretions of baicalin and B6G increased by 1.8 times and 2.1 times within 12 h, respectively. PEG400 increased the enzyme activities of UGT1A8 and UGT1A9 by 2.0 times and 1.5 times, and their concentrations in liver were increased by 2.2 times and 1.3 times, respectively. Conclusion::PEG400 can significantly increase the bile excretion of baicalin and its main metabolite B6G by enhancing the activities and expressions of UGT1A8 and UGT1A9, and its promoting effect on bile excretion of B6G is greater than that of baicalin, which provides a basis for the rational clinical application of PEG400 and the design of new dosage forms of flavonoids such as baicalin.

14.
Article in Chinese | WPRIM | ID: wpr-868914

ABSTRACT

With the popularity and development of minimally invasive surgery such as laparoscopic cholecystectomy, the incidence of iatrogenic biliary tract injury and biliary duct stenosis after injury has been increased significantly. The biliary duct injury of laparoscopic cholecystectomy is mainly heat damage, and the biliary duct tissue is prone to biliary duct stenosis after heat injury. Currently the treatment of complex iatrogenic biliary stricture has still been a difficult and unfinished problem. It’s necessary to explore the therapy options of iatrogenic biliary stricture based on animal models of biliary stricture. According to the literature at home and abroad, this article reviewed the methods and advantages and disadvantages of several models of benign biliary stricture.

15.
Article in Chinese | WPRIM | ID: wpr-865877

ABSTRACT

In the battle of COVID-19 epidemic prevention and control in China, the "countermarching people" faced up to all difficulties and went forward one after another to the forefront of anti-epidemic. Many vivid figures and examples have aroused our feelings and thoughts on life. Under the background of this special period, medical colleges should take the COVID-19 prevention and control as an opportunity to enrich the contents of bioethics education, blend in patriotism education, social responsibility education, medical moral education, and life and death culture education. By strengthening the construction of teaching staff, attaching importance to the integration of teaching contents, optimizing teaching carriers, expanding practical activities and recommending online teaching resources, the teaching reform of bioethics education is explored in order to enhance the effectiveness and sustainability of bioethics education and moral education.

16.
Article in Chinese | WPRIM | ID: wpr-886773

ABSTRACT

Neutrophil extracellular trap (NET) is a type of bead-like, fibrous and reticular substances that is actively released by activated inflammatory neutrophils during the stage of infections or inflammatory responses. NET, which is composed of chromatin DNA and multiple intracellular protein components, may wrap pathogens to limit their diffusions. Meanwhile, NET may kill pathogens via a wide range of antibacterial proteins, which is considered as the third antibacterial mechanism of neutrophils, in addition to phagocytosis and degranulation. Recent studies have shown the involvement of NET in the immune response against parasitic infections. This review summarizes the advances of NETs in the immune responses against parasitic infections, so as to provide insights into the elucidation of the pathogenesis and development of therapeutics of parasitic diseases.

17.
Article in Chinese | WPRIM | ID: wpr-827954

ABSTRACT

In December 2019, an outbreak of viral pneumonia began in Wuhan, Hubei Province, which caused the spread of infectious pneumonia to a certain extent in China and neighboring countries and regions, and triggered the epidemic crisis. The coronavirus disease 2019(COVID-19) is an acute respiratory infectious disease listed as a B infectious disease, which is managed according to standards for A infectious disease. Traditional Chinese medicine and integrated traditional Chinese and Western medicine have played an active role in the prevention and control of this epidemic. China's ethnomedicine has recognized infectious diseases since ancient times, and formed a medical system including theory, therapies, formula and herbal medicines for such diseases. Since the outbreak of the COVID-19 epidemic, Tibet Autonomous Region, Qinghai Province, Inner Mongolia Autonomous Region, Xinjiang Uygur Autonomous Region and Chuxiong Autonomous Prefecture of Yunnan, Qiandongnan Autonomous Prefecture of Guizhou have issued the prevention and control programs for COVID-19 using Tibetan, Mongolian, Uygur, Yi and Miao medicines. These programs reflect the wisdom of ethnomedicine in preventing and treating diseases, which have successfully extracted prescriptions and preventive measures for the outbreak of the epidemic from their own medical theories and traditional experiences. In this paper, we summarized and explained the prescriptions and medicinal materials of ethnomedicine in these programs, and the origin of Tibetan medicine prescriptions and Mongolian medicine prescriptions in ancient books were studied. These become the common characteristics of medical prevention and treatment programs for ethnomedicine to formulate therapeutic programs under the guidance of traditional medicine theories, recommend prescriptions and prevention and treatment methods with characteristics of ethnomedicine, and focus on the conve-nience and standardization. However, strengthening the support of science and technology and the popularization to the public, and improving the participation of ethnomedicine in national public health services and the capacity-building to deal with sudden and critical diseases are key contents in the development of ethnomedicine in the future.


Subject(s)
Betacoronavirus , China , Coronavirus Infections , Drug Therapy , Humans , Medicine, Traditional , Pandemics , Pneumonia, Viral , Drug Therapy , Tibet
18.
Acta Pharmaceutica Sinica ; (12): 694-702, 2020.
Article in Chinese | WPRIM | ID: wpr-820865

ABSTRACT

Ebola virus is extremely virulent and highly contagious. Ebola virus causes outbreaks of severe hemorrhagic fever, with human mortality rates of up to 90%. There is currently no preventive or therapeutic treatment in the form of vaccines, biological or small molecular agents. Currently, a lot of anti-Ebola virus agents have been reported. Here, we review the latest advances in this field.

19.
China Pharmacy ; (12): 1236-1240, 2019.
Article in Chinese | WPRIM | ID: wpr-816970

ABSTRACT

OBJECTIVE: Compare the contents of free ellagic acid and total ellagic acid in fruits, roots and levels of Rosa roxburghii, and to evaluate the in vitro anti-oxidant activity of ethanol extract of three medicinal parts of R. roxburghii. METHODS: Free ellagic acid and total ellagic acid were obtained from different medicinal parts of R. roxburghii by ultrasonic extraction and acid hydrolysis, respectively. The contents of them were determined by UPLC. Using half-clearance value (IC50) as anti-oxidant evaluation index, free radical scavenging test of 1,1-diphenyl-2-trinitrophenylhydrazine (DPPH) and 2,2′ -binitro-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) were conducted for ethanol extract of different medicinal part, using vitamin C (VC) as positive control. RESULTS: There were significant differences in the content of free ellagic acid and total ellagic acid in different medicinal parts of R. roxburghii. The content level of free ellagic acid was in descending order: R. roxburghii leaves (38.49 mg/g)>R. roxburghii fruits (20.59 mg/g)>R. roxburghii roots (11.35 mg/g); the content level of total ellagic acid was in descending order: R. roxburghii leaves (197.08 mg/g) > R. roxburghii fruits (49.36 mg/g) > R. roxburghii roots (21.86 mg/g). The contents of total ellagic acid in the fruits and roots of R. roxburghii were twice as much as that of free ellagic acid in corresponding parts; the contnets of total ellagic acid in the leaves of R. roxburghii were five times higher than that of free ellagic acid in corresponding parts. In the DPPH free radical scavenging test and ABTS free radical scavenging test, the order of antioxidant activity was VC > R. roxburghii leaves>R. roxburghii fruits>R. roxburghii roots. There was no statistical significance in the effects of R. roxburghii leaves [IC50 to DPPH free radical and ABTS free radical were (4.57±0.70)、(115.99±2.21) μg/mL] and R. roxburghii fruits [IC50 to DPPH free radical and ABTS free radical were (5.12±0.24)、(127.61±3.31)    μg/mL], compared with the effects of VC [IC50 to DPPH free radical and ABTS free radical were (4.47±0.38)、(121.42±2.65)      μg/mL] (P>0.05). CONCLUSIONS: Among fruits, roots and leaves of R. roxburghii, the content of free (total) ellagic acid is the highest in the R. roxburghii leaves and in vitro anti-oxidant activity of its ethanol extract is the strongest.

20.
Chinese Journal of Neurology ; (12): 371-378, 2019.
Article in Chinese | WPRIM | ID: wpr-745941

ABSTRACT

Objective To explore the diagnostic value of tremor analysis in patients with coexisting essential tremor (ET) and Parkinson's disease (PD).Methods A cross-sectional survey was conducted to collect 30 patients with PD,30 patients with ET and 20 patients with ET + PD in Peking University Third Hospital from January 2015 to December 2017.Tremor analysis was performed in all the patients.Results There were statistically significant differences in age (63.0(54.8,68.0),49.0(26.5,58.5),57.0(50.0,66.0) years,H=21.336,P<0.05),disease course (12.0(8.0,13.3),36.0(12.0,87.0),22.0(11.5,33.0) years,H=18.233,P<0.05) and Unified Parkinson's Disease Rating Scale score (21.13± 8.85,8.00± 3.68,24.35±9.14,F=36.443,P<0.05) among the PD,ET and ET+PD groups.The average tremor frequencies in PD,ET and ET+PD groups at rest were (5.46±0.77),(7.11 ± 1.80) and (6.18± 1.55) Hz,respectively,with statistically significant differences among the three groups (F=5.77,P=0.006).The average tremor frequencies in the three groups at posture were (6.19±2.21),(8.23± 1.96) and (6.49± 1.23) Hz,respectively,with statistically significant differences (F=9.673,P<0.01).There was no statistically significant difference in tremor amplitude among the three groups at rest and posture position.In the PD,ET and ET+PD groups,the proportion of electromyography alternating contractions of the active and antagonistic muscles was 76.9%(20/26),0/6 and 5/15 at rest (x2=17.192,P<0.01),and 53.8% (14/26),20.0% (6/30) and 4/15 at posture (x2=7.564,P=0.023),both with statistically significant differences.Conclusions The clinical manifestations of patients with ET+PD have both characteristics of PD and ET,but they have their own characteristics.Tremor analysis can objectively identify the bilaterally synchronous or alternate discharges of electromyography at rest,which are different from those of typical PD and ET.Tremor analysis is helpful for the identification of this disease.

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