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1.
Article in Chinese | WPRIM | ID: wpr-906464

ABSTRACT

Objective:Ultra-high performance liquid chromatography coupled with quadrupole/electrostatic field orbital trap high resolution mass spectrometry (UHPLC-Q Exactive Focus MS/MS) was developed to rapidly analyze and identify the chemical components in the rhizomes of <italic>Bergenia scopulosa</italic>. Method:The 75% methanol extract of <italic>B</italic>.<italic> scopulosa</italic> rhizomes was analyzed on a Thermo Accucore aQ RP18 column (2.1 mm×150 mm, 2.6 μm) with the mobile phase of methanol (A) and 0.1% formic acid aqueous solution (B) for gradient elution (0-40 min 5%-95%A, 40-45 min 95%A), the flow rate was 0.3 mL·min<sup>-1</sup> and the column temperature was at 30 ℃. The information of the chemical constituents was acquired in positive and negative ion modes by heated electrospray ion source (HESI), and the scanning range was <italic>m</italic>/<italic>z</italic> 80-1 200. Result:A total of 66 chemical constituents were identified, including 2 free amino acids, 7 bergenin derivatives, 15 flavonoids, 15 organic acids, 25 glycosides, and 2 others. Conclusion:The chemical constituents in the rhizomes of <italic>B</italic>.<italic> scopulosa</italic> can be identified systematically, accurately and rapidly by this method. Among them, 8 compounds were unambiguously identified by comparing with reference substances (succinic acid, arbutin, gallic acid, protocatechuic acid, bengenin, catechin, chlorogenic acid and caffeic acid), 51 compounds were found from <italic>B</italic>.<italic> scopulosa</italic> for the first time and 28 compounds were found from the genus <italic>Bergenia</italic> for the first time. This paper can provide an important basis for the further material basis clarification and quality assessment of <italic>B</italic>.<italic> scopulosa</italic>.

2.
Article in Chinese | WPRIM | ID: wpr-906230

ABSTRACT

Objective:To explore the molecular mechanism of modified Guizhi Fulingwan in rats with uterine fibroids. Method:Seventy-two female adult SD rats of SPF grade were randomly divided into a model group, a normal group, and a preventive administration group. The model group and preventive administration group were established by estrogen and progestin loading method. After successful modeling, the rats in the model group were randomly divided into a western medicine group (mifepristone), the high-dose traditional Chinese medicine(TCM) group, and a low-dose TCM group. All the rats were dosing as required once a day for 28 consecutive days. Hematoxylin-eosin(HE)staining was used to observe the morphological changes of the uterus. The micRNA gene chip was used to detect the expression profile of uterine micRNA gene. Differential expressions of micRNA were screened by bioinformatics methods. Gene function enrichment was used to predict the possible signaling pathways in rats with uterine fibroids by modified Guizhi Fulingwan. Result:Compared with the normal group, microRNA of the model group was 1 up-regulated and 9 down-regulated. Compared with the model group, microRNA of the high-dose group of TCM group was 2 up-regulated and 1 down-regulated, in the preventive administration group, 9 was up-regulated and 2 was down-regulated. Gene function enrichment analysis indicated that four signaling pathways were closely related to uterine fibroids. They were mitogen-activated protein kinase (MAPK) signaling pathway, Wnt signaling pathway, mammalian rapamycin target protein (mTOR) signaling pathway and vascular endothelial cell growth factor (VEGF) signaling pathway. Conclusion:Modified Guizhi Fulingwan affected the expression profile of micRNA in rat model of uterine fibroids induced by estrogen and progesterone, suggesting that modified Guizhi Fulingwan may involve in a variety of biological processes such as signal transduction and gene regulation in the treatment of uterine fibroids.

3.
Article in Chinese | WPRIM | ID: wpr-906136

ABSTRACT

Objective:To explore the mechanism of Sishenwan, Baitouweng Tang, and Lianlitang in the treatment of ulcerative colitis (UC), and compare their efficacies on UC in rats. Method:Ninety SD rats of SPF grade were randomly divided into blank group (distilled water, 2 mL·d<sup>-1</sup>) and experimental group. The rats in the experimental groups were administered with 2,4,6-trinitrobenzene sulfonic acid (TNBS) by clysis to induce the UC model. Subsequently, the model rats were divided into a model group (distilled water, 2 mL·d<sup>-1</sup>), positive group [sulfasalazine (SASP), 0.4 g·kg<sup>-1</sup>·d<sup>-1</sup>], Sishenwan group (1.76 g·kg<sup>-1</sup>·d<sup>-1</sup>), a Baitouweng Tang group (1.40 g·kg<sup>-1</sup>·d<sup>-1</sup>), and Lianlitang group (2.13 g·kg<sup>-1</sup>·d<sup>-1</sup>) according to the random number table. The rats in each group were dosed at 2 mL·d<sup>-1</sup> for 14 days. The pathological score for colonic mucosa was detected. Cytokines were detected by the cytokine chip. The enzyme-linked immunosorbent assay (ELISA) was used to detect the free triiodothyronine (FT<sub>3</sub>), glucagon-like peptide-1 (GLP-1), and corticosterone (CORT) in plasma, and neurotensin (NT), substance P (SP), vasoactive intestinal peptide (VIP), and somatostatin (SST) in colon tissues. Result:Compared with the normal group, the model group showed increased colon mass-length ratio and pathological score for colonic mucosa (<italic>P</italic><0.01), infiltration of massive lymphocytes, disordered or absent intestinal villi, elevated levels of cytokine-induced neutrophil chemoattractant-1/2<italic>α</italic>/<italic>β</italic>/3 (CINC-1/2<italic>α</italic>/<italic>β</italic>/3), interleukin-1<italic>α</italic> (IL-1<italic>α</italic>), interferon-inducible protein-10 (IP-10) and other factors in colon tissues (<italic>P</italic><0.05), dwindled CORT and GLP-1 levels in plasma (<italic>P</italic><0.05), and increased SP content in colon tissues (<italic>P</italic><0.05). Compared with the results in the model group, the mucosal injury in the colon of rats in each drug group was relieved. The levels of IL-1<italic>α</italic>, IP-10, lipopolysaccharide-inducible CXC chemokine (LIX), and L-selectin of rats in the Lianlitang group and Sishenwan group were reduced (<italic>P</italic><0.05), and the CINC-3 and IL-17 levels were diminished in the Baitouweng Tang group (<italic>P</italic><0.05). The levels of CINC-1/3, IL-1<italic>α</italic>, and IP-10 were reduced in the SASP group (<italic>P</italic><0.05). The plasma FT<sub>3</sub> was up-regulated in the Lianlitang group, and the plasma GLP-1 levels were elevated in the three Chinese medicine groups (<italic>P</italic><0.05). The VIP content in colon tissues of the Sishenwan group and Baitouweng Tang group was down-regulated (<italic>P</italic><0.05), and the SST content in colon tissues of the SASP group was significantly up-regulated (<italic>P</italic><0.01). Conclusion:The intervention of Lianlitang and Sishenwan on UC was significant, and the underlying mechanism of action might be related to inflammation inhibition and immune balance by regulating the cytokine network. The efficacy of Lianlitang was predominant, followed by Sishenwan and Baitouweng Tang.

4.
Article in Chinese | WPRIM | ID: wpr-921796

ABSTRACT

Breast cancer is a major chronic disease threatening women's health. It has topped the global cancers as the diagnosed cases outnumbered lung cancer patients in 2020. Internal damage due to the seven emotions is an important cause of breast cancer and the disorders of hypothalamic-pituitary-adrenal(HPA) axis and endocrine system and the abnormal immune defense mechanism in response to psychological stress all affect the occurrence and development of breast cancer. It is noteworthy that the theory of seven emotions in traditional Chinese medicine and the psychological stress theory of modern medicine have something in common in some aspects. Therefore, this study explored the correlation between internal damage due to the seven emotions and psychological stress and analyzed the molecular biological mechanisms of psychological stress influencing breast cancer from the perspective of modern medicine, which is helpful to reasonably prevent breast cancer and other related tumors and improve the prognosis of breast cancer patients through emotion regulation.


Subject(s)
Breast Neoplasms/genetics , Emotions , Female , Humans , Hypothalamo-Hypophyseal System , Medicine, Chinese Traditional , Pituitary-Adrenal System , Stress, Psychological
5.
Article in Chinese | WPRIM | ID: wpr-921769

ABSTRACT

Clinical comprehensive evaluation was conducted in "6+1" dimensions(safety, effectiveness, economy, innovation, suitability, accessibility, and characteristics of traditional Chinese medicine) to reflect the advantages and characteristics of Diemai-ling~® Kudiezi Injection in the treatment of cerebral infarction. This study adopted a combination of qualitative and quantitative evaluation methods. Based on the methodologies of evidence-based medicine, epidemiology, clinical medicine, evidence-based pharmacy, pharmacoeconomics, mathematical statistics, and health technology assessment(HTA), experts gave weight to the criterion layer and index layer, and multi-criteria decision analysis(MCDA) model and CSC v2.0 were used for calculations to evaluate the clinical value of Diemailing~® Kudiezi Injection. The existing evidence showed that active monitoring and a number of randomized controlled trials(RCTs) have been carried out after the listing of Diemailing~® Kudiezi Injection. Since the total incidence of adverse reactions is 0.099% and the incidence of adverse drug reactions(ADR) is rare, the safety evaluation is grade A. The evidence value of effectiveness demonstrated that Diemailing~® Kudiezi Injection combined with conventional western medicine improves the total effective rate of neurological deficit score and quality of daily life in the acute stage of cerebral infarction, which is superior to that in the conventional western medicine treatment group, and the level of evidence is high. Therefore, its efficacy is assessed as grade A. According to the results of economic research, when Diemailing~® Kudiezi Injection combined with conventional western medicine treatment is compared with conventional western medicine treatment, the Diemailing~® Kudiezi Injection group has a greater incremental effect, but the cost is affordable. Given the overall quality evaluation results of economic report is clear, it is evaluated as grade B. The innovation is grade A. The drug is favorable for clinical operation by medical staff and can be accepted by patients due to easy usage without special technical and management requirements. Since the drug exhibits good suitability for clinicians, nurses, pharmacists, and patients, it is evaluated as grade B. Considering its moderate price among similar drugs and good affordability and availability, it is evaluated as grade B. Diemailing~® Kudiezi Injection can evidently improve the clinical symptoms and neurological deficits of fire toxin syndrome of acute cerebral infarction, and this medicine belongs to ethnic medicine. Large-sample active monitoring research has been conducted with rich experience in human use. Therefore, the characteristics of traditional Chinese medicine are evaluated as grade A. The comprehensive clinical evaluation of Diemailing~® Kudiezi Injection is class A. We suggest that it can be directly transformed into relevant policy results of basic clinical medication management by procedure.


Subject(s)
Cerebral Infarction/drug therapy , Drugs, Chinese Herbal/therapeutic use , Humans , Injections , Medicine, Chinese Traditional
6.
Article in Chinese | WPRIM | ID: wpr-921766

ABSTRACT

This study explored the clinical comprehensive evaluation of Mudan Granules, aiming to promote the safe, effective and rational use of Mudan Granules, reflect its clinical value and provide a basis for medical decision-making. The safety, effectiveness, economy, innovation, suitability, accessibility, and characteristics of traditional Chinese medicine of Mudan Granules were combed, and the multi-criteria decision analysis(MCDA) model was used to carry out comprehensive evaluation on each dimension. In terms of safety, multiple sources of evidence showed that the adverse reactions of Mudan Granules mainly involved gastrointestinal system, with controllable safety risk rated as grade B. In terms of effectiveness, Mudan Granules can significantly alleviate the diabetic peripheral neuropathy(Qi-deficiency and collateral stagnation syndrome), limb and trunk numbness, pain and sensory abnormalities and other clinical symptoms, exhibiting positive curative effect rated as grade A. In terms of economy, Mudan Granules combined with Mecobalamin and other conventional western medicines is economical compared with the western medicine alone group, which is supported by sufficient evidence and clear results, rated as grade B. In terms of innovation, Mudan Granules is the only Chinese patent medicine with the indication of benefiting Qi for activating blood circulation and dredging collaterals in the Medicine Catalogue for National Basic Medical Insurance, Industrial Injury Insurance, and Maternity Insurance. It has important clinical innovation and is evaluated as grade A. In the aspect of suitability, Mudan Granules has good suitability in ADR treatment, drug characteristics and usage, and is rated as grade B. In terms of accessibility, Mudan Granules has the price level comparable to that of similar drugs, with good affordability. The resources of medicinal materials for the preparation of Mudan Granules are abundant and available, which is rated grade B. Moreover, Mudan Granules, as a hospital preparation with both functions of tonification and purgation, reflects the combination between syndrome differentiation and disease differentiation as well as the combination between overall and local characteristics, and has prominent Chinese medicine features. According to the above dimensions, we suggest to classify Mudan Granules as a class A preparation which can be directly included the policy results of basic clinical drug administration.


Subject(s)
Diabetes Mellitus , Diabetic Neuropathies , Drugs, Chinese Herbal/therapeutic use , Female , Humans , Medicine, Chinese Traditional , Pregnancy , Qi , Syndrome
7.
Article in Chinese | WPRIM | ID: wpr-921764

ABSTRACT

The clinical comprehensive evaluation of drugs is an important basis for the return of clinical value, decision-making of medical and health authorities, and allocation of medical resources. In July 2021, the National Health Commission issued the Guidelines for the Management of Clinical Comprehensive Evaluation of Drugs(trial version 2021), which required the evaluation to be implemented from the six dimensions(safety, effectiveness, economy, innovation, suitability, and accessibility), and made detailed arrangements for the clinical comprehensive evaluation of drugs. As Chinese patent medicine differs from chemical medicines in terms of effective components and action modes, the clinical comprehensive evaluation of Chinese patent medicine should highlight the characteristics and advantages of traditional Chinese medicine(TCM) on the basis of general requirements of comprehensive clinical evaluation of drugs. At present, in the clinical comprehensive evaluation of Chinese patent medicine, unified report standards have not yet been generated, resulting in the uneven quality of existing reports. To standardize the clinical comprehensive evaluation report of Chinese patent medicine and improve its quality, the editorial team, based on the relevant policy documents of clinical comprehensive evaluation of drugs, formulated the clinical comprehensive evaluation report standards for Chinese patent medicine in combination with the previous practice and expert opinions. The report standards, containing seven sections with 15 items determined, focus on data source, evaluation content, evidence synthesis, quality control, and evaluation results supported with detailed interpretations to help researchers better understand and apply the report standards for clinical comprehensive evaluation of Chinese patent medicine, improve the report quality, and provide references for the decision-making by the national medical management authorities.


Subject(s)
China , Drugs, Chinese Herbal , Information Storage and Retrieval , Medicine, Chinese Traditional , Nonprescription Drugs , Quality Control
8.
Article in Chinese | WPRIM | ID: wpr-921727

ABSTRACT

The safety of modern Chinese medicine has attracted increasing attention from society. Experts and scholars have carried out extensive in-depth research on the safety of commonly used Chinese medicines from various aspects such as safety monitoring, clinical research, and experimental analysis. The findings in the safety performance of Chinese medicines can inspire the mining and analysis of relevant signals in the drug safety alerts. A variety of methods are employed for the mining of risk signals or analysis and screening of relevant signals to accurately determine the correlation between medication and adverse reactions. The safety signal acquisition and mining techniques are the technical basis for the safety risk management of medicine products after Chinese medicines are marketed, which is critical in drug safety alerts. To accurately collect the safety signals of Chinese medicines and effectively and rapidly track, determine, and assess the sources of signals are important technical links in drug risk management. The ultimate purpose of safety signal discovery is to achieve normalized risk management through downgrading drugs from a high-risk level to a low-risk level.The five main steps in the standard drug risk management are listed below: to extensively collect predicted risk signals; to accurately identify drug risks by the techniques such as data mining; to evaluate the risks with process-based quality risk control; to employ management measures minimizing the impact of drug risks for risk management; to update and apply risk assessment to clinical evaluation after medication.


Subject(s)
Data Mining , Drug-Related Side Effects and Adverse Reactions/prevention & control , Drugs, Chinese Herbal/adverse effects , Humans , Medicine, Chinese Traditional , Quality Control
9.
Article in Chinese | WPRIM | ID: wpr-911393

ABSTRACT

Objective:To explore the mechanism of potassium iodide-induced pyrolysis of thyroid follicular cells.Methods:Thyroid gland tissue was obtained from patients with thyroid cancer (TC) coexisting with Hashimoto′s thyroiditis, and the tumor-adjacent Hashimoto′s thyroiditis tissue was used as the control. ELISA was used to detect the concentration of the pyroptosis inflammatory cytokines interleukin (IL)-1β and IL-18 in the tissues, and Western blotting was used to detect the activation of gasdermin (GSDM) proteins, a biomarker for pyroptosis. Thyroid follicular cells treated with different concentrations of potassium iodide, and IL-1β, IL-18, lactate dehydrogenase (LDH), GSDMD were measured. Transcriptome chip analysis was used to explore the differentially expressed genes involved in pyroptosis of thyroid follicular cells induced by potassium iodide treatment.Results:The levels of IL-1β and IL-18 cytokines in the tissues of patients with Hashimoto′s thyroiditis and thyroid cancer were higher than control tissues ( P<0.01), and the activation of the pyroptosis executive protein GSDMD was significant increased, while GSDME was not activated. IL-1β, IL-18, and LDH secretion were significantly increased in response to potassium iodide stimulation in thyroid follicular cells ( P<0.01) and GSDMD was cleaved, which indicated that potassium iodide induced the pyroptosis of thyroid follicular cells. Moreover, potassium iodide could activate NLRP3 inflammasomes to promotethe pyroptosis of thyroid follicular cells. Transcriptome chip analysis further found that PARP1 protein was highly upregulated by the stimulation of potassium iodide, and then enhanced the activity of nuclear factor-κB (NF-κB) transcription factor to induce pyroptosis. Conclusions:The findings in this study reveal that potassium iodide promotesthe pyroptosis of thyroid follicular cells through activating NF-κB-NLRP3 inflammasome, which may be a novel mechanism that promots the development of Hashimoto′s thyroiditis under the condition of excessive iodine intake. PARP1 is a pivotal protein that mediates the pyroptosis induced by potassium iodide and may be a potential therapeutic target to control Hashimoto′s thyroiditis progression.

10.
Chinese Medical Journal ; (24): 1933-1940, 2021.
Article in English | WPRIM | ID: wpr-887616

ABSTRACT

BACKGROUND@#Colorectal cancer (CRC) is the fourth cause of cancer death in China. We aimed to provide national and subnational estimates and changes of CRC premature mortality burden during 2005-2020.@*METHODS@#Data from multi-source on the basis of the national surveillance mortality system were used to estimate mortality and years of life lost (YLL) of CRC in the Chinese population during 2005-2020. Estimates were generated and compared for 31 provincial-level administrative divisions in China.@*RESULTS@#Estimated CRC deaths increased from 111.41 thousand in 2005 to 178.02 thousand in 2020; age-standardized mortality rate decreased from 10.01 per 100,000 in 2005 to 9.68 per 100,000 in 2020. Substantial reduction in CRC premature mortality burden, as measured by age-standardized YLL rate, was observed with a reduction of 10.20% nationwide. Marked differences were observed in the geographical patterns of provincial units, and they appeared to be obvious in areas with higher economic development. Population aging was the dominant driver which contributed to the increase in CRC deaths, followed by population growth and age-specific mortality change.@*CONCLUSIONS@#Substantial discrepancies were observed in the premature mortality burden of CRC across China. Targeted considerations were needed to promote a healthy lifestyle, expand cost-effective CRC early screening and diagnosis, and improve medical treatment to reduce CRC mortality among high-risk populations and regions with inadequate healthcare resources.


Subject(s)
China/epidemiology , Colorectal Neoplasms , Humans
11.
Article in Chinese | WPRIM | ID: wpr-882729

ABSTRACT

Objective:To investigate the prognostic factors and pathological characteristics of mixed subtype thyroid cancer (MSTC) .Methods:Data of 41 cases of MSTC, which were confirmed by postoperative pathology, among from 24, 912 cases of thyroid cancer admitted in Mar. 2005 to Aug. 2020 in the First Medical Center of Chinese People’s Liberation Army General Hospital, were retrospectively analyzed. 37 cases underwent surgical treatment, while 4 cases only underwent puncture to confirm the pathology due to physical conditions, and no surgical treatment was performed. The tumor size, number of lesions, capsule invasion, AJCC 8th TNM staging, surgical methods, radiotherapy and chemotherapy were collected. The MSTC patients in the group were followed up to obtain the postoperative situation. SPSS 25.0 and R studio statistical software was used for data processing, and Cox single factor and multivariate regression were used to analyze independent risk factors.Results:In the 41 cases, there were 9 cases of papillary carcinoma (PTC) mixed with follicular carcinoma (FTC) , and 8 cases of mixed medullary and follicular carcinoma (MMFTC) . There were 15 cases of poorly differentiated thyroid cancer (PDTC) , 4 cases of squamous cell carcinoma of thyroid (SCCT) , and 5 cases of undifferentiated thyroid carcinoma (ATC) . The median follow-up time was 18 months, and 11 patients died during the follow-up, with a mortality rate of 26.8%. Average onset age was (51.41+15.69) years. 4 cases had postoperative recurrence during the follow-up, including 2 cases of local recurrence, and 2 cases of distant metastasis. Single factor results showed that age, degree of tumor differentiation, surgical method, radiotherapy and chemotherapy were the risk factors affecting the prognosis of patients with MSTC ( P<0.05) . Multivariate analysis showed that age at diagnosis ( P=0.007) and surgical procedure ( P=0.017) were independent risk factors for prognosis in patients with MSTC. Conclusion:Middle-aged and elderly women are at high risk for MSTC, and the degree of tumor differentiation is proportional to survival. Due to the multi-type and pleomorphic pathological findings, a reasonable treatment plan has good effects on prognosis of MSTC.

12.
Acta Pharmaceutica Sinica ; (12): 1727-1738, 2021.
Article in Chinese | WPRIM | ID: wpr-881568

ABSTRACT

In the research and development of new drugs, it is very important to investigate the in vitro metabolism of candidate drugs. Traditional models such as liver microsomes have many limitations, while the in vitro model of recombinant human drug metabolizing enzymes is considered as an important and useful approach because of its convenient access, stable activity and low cost. In this study, six major human UDP-glucuronosyltransferases (UGTs) genes (UGT1A1, 1A3, 1A4, 1A6, 1A9 and 2B7) were cloned from human liver cDNA and heterologously expressed in Saccharomyces cerevisiae and baculovirus-infected insect cell. UGT1A1, 1A3, 1A6 and 1A9 were successfully expressed in yeast and showed glucuronidation activity against a variety of different structural types of substrates, but their activities were low. All six UGTs were successfully expressed and exhibited significantly improved glucuronidation activity when Trichopolusia ni cells BTI-TN5B1-4 (High Five) were used as the host. The recombinant human UGTs expressed in insect cells can catalyze the glucuronidation of their specific substrates, and the glucuronidation products were synthesized at milligram-scale with yields of 13%-66% for the first time, of which the structures were identified via MS, 1H NMR, and 13C NMR spectroscopic analysis. Above all, the recombinant human UGTs yeast and insect cell expression systems constructed in this study can be used for in vitro metabolism evaluation in the early stage of new drugs research and development, and also provide a new tool for the synthesis of glucuronide metabolites.

13.
Article in Chinese | WPRIM | ID: wpr-879279

ABSTRACT

This study aims to explore the intraventricular pressure difference (IVPD) within left ventricle in patients with paroxysmal atrial fibrillation (PAF) by using the relative pressure imaging (RPI) of vector flow mapping (VFM). Twenty patients with paroxysmal atrial fibrillation (PAF) and thirty control subjects were enrolled in the study. Systolic and diastolic IVPD derived from VFM within left ventricle and conventional echocardiographic parameters were analyzed. It was found that the B-A IVPD of left ventricle in PAF patients showed the same pattern as controls-single peak and single valley during systole and double peaks and double valleys during diastole. Basal IVPD was the main component of base to apex IVPD (B-A IVPD). The isovolumetric systolic IVPD was associated with early systolic IVPD, early systolic IVPD was associated with late systolic IVPD, and late systolic IVPD was associated with isovolumic diastolic IVPD (all


Subject(s)
Atrial Fibrillation/diagnostic imaging , Diastole , Heart Ventricles , Humans , Ventricular Function, Left , Ventricular Pressure
14.
Article in Chinese | WPRIM | ID: wpr-878963

ABSTRACT

This study aims to establish a method for the determination of the concentration of five main components of phthalide target areas of Chaxiong(CPTA) and its inclusion of β-CD in the plasma of rats, and determine the pharmacokinetic parameters, absolute bioavailability and relative bioavailability of CPTA/β-CD inclusion compound in vivo. The plasma concentrations of senkyunolide A, N-butylphthalide, new osthol lactone, Z-ligustilide and butenyl phthalide were determined with UPLC-MS/MS. The content determination was conducted at the chromatographic conditions as follows: Shim-pack GIST C_(18)-AQ HP column(2.1 mm×100 mm, 3 μm), mobile phase of 0.1% formic acid solution(A)-acetonitrile(B), gradient elution, flow rate of 0.3 mL·min~(-1), column temperature of 35 ℃ and injection volume of 2 μL. The mass spectra were obtained with electrospray ion source(ESI), positive ion mode and multi reaction monitoring. CPTA/β-CD inclusion compound was prepared by grinding method, DAS 2.0 software was used to model the data, and the absolute bioavailability of CPTA and relative bioavailability of inclusion compound were calculated. Finally, the methods for the determination of five components of senkyunolide A, N-butylphthalide, new osthol lactone, Z-ligustilide and butenyl phthalide in CPTA, were successfully established. The linear relationship among the five components was good within their respective ranges, r>0.99. The absolute bioavailability of the five components in rats was 22.30%, 16.32%, 21.90%, 10.16% and 12.43%, respectively. After CPTA/β-CD inclusion was prepared, the relative bioavailability of the five components was 138.69%, 198.39%, 218.01%, 224.54% and 363.55%, respectively, significantly improved. This method is rapid, accurate and sensitive, so it is suitable for the pharmacokinetic study of extracts in traditional Chinese medicine and their preparations.


Subject(s)
Animals , Benzofurans , Chromatography, High Pressure Liquid , Chromatography, Liquid , Rats , Rats, Sprague-Dawley , Reproducibility of Results , Tandem Mass Spectrometry
15.
Acta Pharmaceutica Sinica ; (12): 679-688, 2021.
Article in Chinese | WPRIM | ID: wpr-876508

ABSTRACT

Neuropathic pain (NP) is a medical problem that has been bothering human beings and seriously affects people's quality of life. Although great progress has been made in the study of NP in recent years, there are still many patients who are ineffective to the existing treatments. At present, drug therapy is still the main method to relieve pain, however, adverse drug reactions has hindered the curative effects of drugs. It is extremely urgent to find new drug targets and reduce the adverse effects of existing drugs. This review will mainly describe the current situation and pathogenesis of neuropathic pain, effectiveness and limitations of existing drugs for treating neuropathic pain, and the current status of drug discovery.

16.
Article in English | WPRIM | ID: wpr-829011

ABSTRACT

Objective@#High PM concentration is the main feature of increasing haze in developing states, but information on its microbial composition remains very limited. This study aimed to determine the composition of microbiota in PM in Guangzhou, a city located in the tropics in China.@*Methods@#In Guangzhou, from March 5 to 10 , 2016, PM was collected in middle volume air samplers for 23 h daily. The 16S rDNA V4 region of the PM sample extracted DNA was investigated using high-throughput sequence.@*Results@#Among the Guangzhou samples, , , , , and were the dominant microbiota accounting for more than 90% of the total microbiota, and was the dominant gram-negative bacteria, accounting for 21.30%-23.57%. We examined the difference in bacterial distribution of PM between Beijing and Guangzhou at the genus level; was found in both studies, but was only detected in Guangzhou.@*Conclusion@#In conclusion, the diversity and specificity of microbial components in Guangzhou PM were studied, which may provide a basis for future pathogenicity research in the tropics.


Subject(s)
Air Microbiology , Air Pollutants , Bacteria , Classification , China , Cities , Environmental Monitoring , Microbiota , Particle Size , Particulate Matter , RNA, Bacterial , RNA, Ribosomal, 16S
17.
Article in English | WPRIM | ID: wpr-828990

ABSTRACT

Objective@#Owing to antibiotic abuse and the subsequent development of antibiotic resistance, bacterial infection has become one of the most persistent unresolved problems. New antibacterial agents, especially those that are environmental-friendly, are urgently needed.@*Methods@#Melanin extracted by filtration centrifugation and acid and proteolytic hydrolysis was characterized using UV, FTIR, TEM, and XPS. Photothermal conversion was calculated, and the bacteriostatic effects, and , were assessed by plate counting and ratios (%) of wound areas.@*Results@#Natural melanin hydrolyzed by trypsin had good photothermal conversion effects, which resulted in superior bacteriostatic activities. The extracted melanin along with laser NIR irradiation at 808 nm promoted the healing of wounds infected by drug-resistant bacteria and was biocompatible according to toxicity tests and .@*Conclusion@#The present findings indicated a safe and efficient method of developing natural antibacterial agents.


Subject(s)
Animal Shells , Chemistry , Animals , Anti-Bacterial Agents , Pharmacology , Escherichia coli , Radiation Effects , Escherichia coli Infections , Drug Therapy , Melanins , Pharmacology , Mytilus edulis , Chemistry , Photochemical Processes , Rats , Rats, Sprague-Dawley , Staphylococcal Infections , Drug Therapy , Staphylococcus aureus , Radiation Effects , Wound Healing
18.
Article in English | WPRIM | ID: wpr-828463

ABSTRACT

Objective Graves' disease is the most common autoimmune thyroid disease and its prevalence and clinical manifestations are disparate between females and males. Costimulatory molecules play an essential role in regulating autoimmune responses. The objective of this study was to determine if expression of inhibitory molecules was correlated with treatment by dihydrotestosterone (DHT) in an BALB/c mouse model of experimental autoimmune Graves' disease.Methods Female BALB/c mice were immunized three times with thyroid stimulating hormone receptor A-subunit encoded by adenovirus to establish a Graves' disease model. Three different doses of DHT or a matching placebo were administered by implantation of slow-release pellets a week before the first immunization. Four weeks after the third immunization, the mice were euthanatized, and then the spleen and thymus were removed. Total thyroxine and free thyroxine levels in serum of mice were detected using a radioimmunoassay kit. Real-time polymerase chain reaction was performed to estimate the expression of costimulatory molecules in lymphocytes from the spleen and thymus. Flow cytometry was used to analyze the percentage of CD4 T cells in splenic lymphocytes. Quantitative data were compared with unpaired -tests. Correlation between two variables was analyzed using Analysis of Variance.Results Treatment with DHT can dramatically reduce total thyroxine and free thyroxine levels. Higher expression of programmed death-1 was found in the spleen of Graves' disease mice receiving 5 mg of DHT treatment (0.635±0.296 . 0.327±0.212; =2.714, =0.014), similarly, T-cell immunoglobulin domain and mucin domain 3 (TIM-3) in both the spleen (1.004±0.338 . 0.646±0.314; =2.205, =0.022) and the thymus (0.263±0.127 . 0.120±0.076; =3.221, =0.004) also increased after 5 mg of DHT treatment compared with the parallel placebo model mice. Moreover, the percentage of CD4 T cells declined in the splenic lymphocytes of Graves' disease mice treated with 5 mg of DHT (19.90%±3.985% . 24.05%±2.587%; =2.804, =0.012). A significant negative association was observed between expression of TIM-3 in the spleen and serum levels of total thyroxine (=-0.7106, =0.014) as well as free thyroxine (=-0.6542, =0.029).Conclusion This study demonstrates that DHT can ameliorate experimental autoimmune Graves' disease, which may occur by up-regulating expression of programmed death-1 and TIM-3 and inhibiting development of CD4 T cells.

19.
Article in Chinese | WPRIM | ID: wpr-843255

ABSTRACT

Objective:To study the structure of the human THOC1-THOC2-THOC3 subcomplex by negative-staining electron microscopy. Methods:The recombinant protein components were co-expressed in cultured insect cells, and the protein complex was isolated via sequential Ni-NTA and Strep-Tactin affinity purification followed by Superose gel filtration chromatography. The purified protein sample was then subjected to negative-staining electron microscopy and single particle image analysis. Results:The recombinant human THOC1-THOC2-THOC3 complex with high purity and good homogeneity was obtained by using a tandem affinity purification scheme with Ni-NTA and streptavidin-based chromatography. Preliminary study on the structure of human THOC1-THOC2-THOC3 subcomplex was achieved by electron microscopy using negative staining with uranium formate. Conclusion:A low resolution model of human THOC1-THOC2-THOC3 subcomplex was achieved by single particle reconstruction.

20.
Experimental Neurobiology ; : 138-149, 2020.
Article | WPRIM | ID: wpr-832439

ABSTRACT

Neuropsychiatric disorders are the leading cause of mental and intellectual disabilities worldwide. Current therapies against neuropsychiatric disorders are very limited, and very little is known about the onset and development of these diseases, and their most effective treatments. MIR137 has been previously identified as a risk gene for the etiology of schizophrenia, bipolar disorder, and autism spectrum disorder. Here we generated a forebrain-specific MIR137 knockout mouse model, and provided evidence that loss of miR-137 resulted in impaired homeostasis of potassium in mouse hippocampal neurons. KCC2, a potassium-chloride co-transporter, was a direct downstream target of miR-137. The KCC2 specific antagonist VU0240551 could balance the current of potassium in miR-137 knockout neurons, and knockdown of KCC2 could ameliorate anxiety-like behavior in MIR137 cKO mice. These data suggest that KCC2 antagonists or knockdown might be beneficial to neuropsychiatric disorders due to the deficiency of miR-137.

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