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1.
Article in Chinese | WPRIM | ID: wpr-928161

ABSTRACT

Dachaihu Decoction is a classical Chinese herbal prescription that is effective in harmonizing lesser yang and purging internal accumulated heat. At present, it has been widely used in clinical practice, and the resulting outcomes are satisfactory. However, its quality indicators and action mechanism are still not clear. Therefore, this paper explored the efficacy markers of Dachaihu Decoction and its action mechanism based on literature mining, molecular biology, and network pharmacology, so as to better control its quality and ensure its clinical efficacy. The efficacy markers of Dachaihu Decoction were predicted and analyzed according to the "five principles" for Q-markers of Chinese herbs. Then the anti-inflammatory activity of the efficacy markers of Dachaihu Decoction was evaluated with Griess reagent after the establishment of RAW264.7 cell inflammation model in vitro with lipopolysaccharide(LPS). The potential targets of efficacy markers were predicted by Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP), ChEMBL, and SwissTargetPrediction, followed by the construction of the protein-protein interaction(PPI) network of the efficacy markers of Dachaihu Decoction. Topological, GO, and KEGG enrichment analysis was carried out to construct the "key target-signaling pathway-biological process" network, thus elucidating the action mechanism of the efficacy markers of Dachaihu Decoction. Saikosaponin B_2, baicalin, baicalein, wogonoside, neohesperidin, naringin, hesperidin, and paeoniflorin were considered as the potential efficacy markers of Dachaihu Decoction. The anti-inflammatory activity evaluation showed that the potential efficacy markers effectively inhibited the release of NO, exhibiting good anti-inflammatory activities. As demonstrated by network pharmacology, the efficacy markers of Dachaihu Decoction regulated the inflammatory response by acting on MAPK and NF-κB signaling pathways, the carbohydrate metabolism by HIF-1 and PI3 K-AKT signaling pathways, and the lipid metabolism by AMPK and PI3 K-AKT signaling pathways. This study discovered the efficacy markers of Dachaihu Decoction based on literature mining combined with molecular biological experiments and explored its action mechanism at the molecular level based on network pharmacology, which would provide reference for the quality control of Dachaihu Decoction and scientific basis for its clinical application.


Subject(s)
Biomarkers , Drugs, Chinese Herbal/pharmacology , Medicine, Chinese Traditional , Molecular Docking Simulation , Proto-Oncogene Proteins c-akt , Signal Transduction
2.
Acta Pharmaceutica Sinica ; (12): 1477-1485, 2022.
Article in Chinese | WPRIM | ID: wpr-924760

ABSTRACT

Da Chaihu decoction is a classic prescription for the treatment of cholecystitis that is widely used in clinical practice, and has a definite curative effect. However, due to its diverse components and complex functions, the traditional indexes fail to capture its overall efficacy. Therefore, this study analyzed and predicted the quality markers (Q-markers) of Da Chaihu decoction based on specific chromatogram and network pharmacology to provide a reference for the comprehensive control of the quality. The study obtained 35 potential practical components of Da Chaihu decoction through virtual screening. The specific chromatogram of 15 batches of Da Chaihu decoction was established by HPLC-DAD with neohesperidin as a reference. Compared with the chromatographic peaks and the reference substance, the chemical components were assigned to predict the nine components of albiflorin, paeoniflorin, naringin, hesperidin, neohesperidin, baicalin, wogonoside, saikosaponin b2, saikosaponin b1 as Q-markers of Da Chaihu decoction. Finally, the network of the "components-key targets-signal pathways-biological processes" was constructed by network pharmacology to explore the mechanism of Da Chaihu decoction in treating cholecystitis to clarify the accuracy of Q-markers. The results indicated that potential Q-markers could act on multiple targets to regulate inflammatory and metabolism, and then combine to treat cholecystitis. Q-markers could combine with the pharmacologic action of Da Chaihu decoction, which could elucidate the overall efficacy of Da Chaihu decoction. This study explored the Q-markers of Da Chaihu decoction combined with the specific chromatogram and network pharmacology, which provided a basis for the quality control and evaluation of Da Chaihu decoction.

3.
Article in Chinese | WPRIM | ID: wpr-921782

ABSTRACT

As a classic prescription for promoting blood circulation to remove blood stasis, Xuefu Zhuyu Decoction(XFZYD) is widely used in clinical practice and has notable curative effect. Based on the key targets of activating blood circulation, this study identified the active components of XFZYD to reveal the material basis. The components of XFZYD were collected from Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP). The molecular docking models were built for the blood-activating targets obtained from the previous study with the components of XFZYD. The top five active components with measurability for each target were selected as the potential blood-activating components in the prescription. The efficacy of the prescription can embody key pharmacological and high-content components. In this study, anti-platelet aggregation activity was used to characterize the effect of activating blood, and the in vivo experiments were conducted to verify the accuracy of the active components. A total of 210 chemical components of XFZYD were screened out from TCMSP and docked with the key targets with the function of activating blood. Ligustrazine, acteoside, naringin, etc. were selected as the potential active components for activating blood in XFZYD. The anti-platelet aggregation activity of the combination of Chuanxiong Rhizoma, Rehmanniae Radix, Aurantii Fructus, Glycyrrhizae Radix et Rhizoma, and Carthami Flos was 9.82%±5.11%. Compared with that in the control group, the platelet aggregation induced by adenosine diphosphate(ADP) was significantly inhibited in the test group(P<0.01), which verified the accuracy of the active components. This study can guide the research on the material basis of XFZYD and provide insights into the development and utilization of the classical prescription.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Medicine, Chinese Traditional , Molecular Docking Simulation , Network Pharmacology , Rhizome
4.
Article in Chinese | WPRIM | ID: wpr-906417

ABSTRACT

Objective:To explore the progression of diabetic macrovascular disease and the effects of Didangtang at different doses on it. Method:Four-week-old male apolipoprotein-E knockout (ApoE<sup>-/-</sup>) mice with diabetic macrovascular disease induced by exposure to high-fat diet combined with streptozotocin (STZ) were randomly divided into the model, simvastatin, as well as high-, medium-, and low-dose Didangtang groups. The age-matched ApoE<sup>-/-</sup> mice of the same batch only fed with a high-fat diet were classified into the ApoE<sup>-/-</sup> (model control) group, and C57BL/6 mice with the same genetic background receiving a regular diet into the normal group. The sampling was conducted at the 8th and 20th weeks of the experiment for observing the pathological characteristics of the aorta and the proportion of plaque area in mice of each group at different time points, followed by the comparison of blood glucose, blood lipid, and oxidized low-density lipoprotein (ox-LDL) levels. The aortic NOD-like receptor protein 3 (NLRP3) and cysteinyl aspartate-specific proteinase-1 (Caspase-1) protein expression was detected by Western blot assay, and the serum interleukin-1<italic>β</italic> (IL-1<italic>β</italic>), interleukin-18 (IL-18), interleukin-1<italic>α</italic> (IL-1<italic>α</italic>), and tumor necrosis factor-<italic>α</italic> (TNF-<italic>α</italic>) levels by enzyme-linked immunosorbent assay (ELISA). Result:The comparison with the normal group revealed that the proportions of plaque area in the ApoE<sup>-/-</sup> group and the model group were increased (<italic>P</italic><0.01), while the proportion of plaque area in each administration group was significantly reduced in contrast to that of the model group (<italic>P</italic><0.05). The aortic NLRP3 and Caspase-1 protein expression levels as well as the serum IL-1<italic>β</italic>, IL-18, IL-1<italic>α</italic>, and TNF-<italic>α </italic>levels in the ApoE<sup>-/-</sup> group and the model group were significantly higher than those in the normal group (<italic>P</italic><0.01). Compared with the model group, each administration group exhibited a significant reduction in aortic NLRP3 and Caspase-1 protein expression and serum IL-1<italic>β</italic>, IL-18, IL-1<italic>α</italic>, and TNF-<italic>α</italic> levels (<italic>P</italic><0.05), with the strongest inhibitory effect detected in the medium-dose Didangtang group (<italic>P</italic><0.05). Conclusion:Didangtang directly alleviates diabetic macrovascular disease possibly by down-regulating NLRP3 and Caspase-1 protein expression and easing the inflammatory cascade.

5.
Article in Chinese | WPRIM | ID: wpr-888190

ABSTRACT

As one of the most commonly diagnosed cancers in the world, female breast cancer is induced by the high level of estrogen. Saussureae Involucratae Herba(SIH), a gynecological medicinal, regulates estrogen-induced diseases. However, the therapeutic effect of SIH on breast cancer has not been reported. Therefore, this study aims to explore the potential efficacy of SIH on breast cancer based on in vitro experiment and network pharmacology. The inhibitory effect of SIH water extract on proliferation and migration of breast cancer MDA-MB-231 cells was examined. The result demonstrated SIH water extract significantly suppressed the proliferation of breast cancer cells(IC_(50)=6.47 mg·mL~(-1)) and also restricted the migration. A total of 39 components of SIH were retrieved from traditional Chinese medicine database(TCMD) and 160 targets of SIH were screened by target fishing with the PharmaDB database. The Online Mendelian Inheritance in Man(OMIM) was used to establish a 1 001-targets data set of breast cancer. Based on the overlaps(45) of targets between SIH and breast cancer, a protein-protein interaction(PPI) network was built to analyze the interactions among these targets with STRING platform and Cytoscape. Finally, through topology and GO and KEGG analysis, 8 targets, 101 pathways and 85 biological processes were found to involve the treatment of breast cancer by SIH. SIH may exert the anti-breast cancer effect by regulating cell cycle, inhibiting proliferation, migration and adhesion of cancer cells, and modulating estrogen receptor. This study clarified the mechanism of SIH in treating breast cancer, which lays a foundation for the further development of SIH.


Subject(s)
Breast Neoplasms/genetics , Databases, Genetic , Drugs, Chinese Herbal , Female , Humans , Medicine, Chinese Traditional
6.
Article in Chinese | WPRIM | ID: wpr-888123

ABSTRACT

The traditional Chinese medicines(TCM) for activating blood circulation and the TCM for regulating Qi are often used in combination in clinical practice. However, their mechanisms are still unclear. The activity spectrum of targets can fuse the active components, targets and intensity of action, which provides support for the discussion of efficacy targets. The chemical components of common TCM sets for activating blood circulation and regulating Qi, as well as the negative sets not for activating blood circulation and re-gulating Qi were obtained from the database of TCM. By the similarity analysis of chemical components in TCM for activating blood circulation and DrugBank database, the predicted targets of chemical components in TCM for activating blood circulation were obtained, and the similarity value of the two was taken as the activity value of the active components and predicted targets. Then, the component-target activity value was weighted. The activity values of herb acting on the same target were fused to construct activity spectra of targets of the herbs for activating blood circulation, herbs for regulating Qi and negative herbs. The targets whose activity values of activating blood circulation and regulating Qi were higher than those of negative herbs were selected as potential targets of efficacy. Protein-protein interaction networks were constructed for topological, GO and KEGG enrichment analysis to determine the key targets of efficacy of activating blood circulation and regulating Qi. The component-target activity information collected from DrugBank database contained 4 499 compounds, 627 targets and 11 295 action relationships. The activating blood function protein-protein interaction network contained 206 nodes and 1 728 edges, while the regulating Qi function protein-protein interaction network contained 230 nodes and 986 edges. The enrichment analysis of topology, GO and KEGG showed that TCM for activating blood circulation mainly exerted its anti-inflammatory, neuroprotective and angiogenic effects on signaling cascade pathway mediated by VEGF/VEGFR2, ERK signaling pathway, calcium signaling pathway and PI3 K-AKT signaling pathway, and the key targets included mitogen activated protein kinases 3(MAPK3), proto-oncogene tyrosine-protein kinase Src(SRC), mitogen activated protein kinases 1(MAPK1), epidermal growth factor receptor(EGFR), phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(PIK3 CA), peroxisome proliferators-activated receptor gamma(PPARG), nitric oxide synthase 3(NOS3), prostaglandin G/H synthetase 2(PTGS2), matrix metalloproteinase-9(MMP9), and vascular endothelial growth factor A(VEGFA). TCM for regulating Qi mainly exerted anti-inflammatory and neuroprotective effects by acting on MAPK signaling pathway and PI3 K-AKT signaling pathway, and the key targets included mitogen activated protein kinases 8(MAPK8), SRC, mitogen activated protein kinases 14(MAPK14), and RAC-alpha serine/threonine-protein kinase(AKT1), mitogen activated protein kinases 3(MAPK3). Based on the activity spectrum of targets, the targets of the TCM for activating blood and the targets of the TCM for regulating Qi were analyzed to provide reference for the study of efficacy targets of TCM, and also provide some scientific basis for clinical application.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Medicine, Chinese Traditional , Protein Interaction Maps , Qi , Vascular Endothelial Growth Factor A
7.
Article in Chinese | WPRIM | ID: wpr-888086

ABSTRACT

Wuwei Ganlu, a formula for medicated bath, consists of medicinal materials of Ephedra sinica, Platycladus orientalis, Myricaria squamosa, Artemisia carvifolia, and Rhododendron anthopogonoides, which is effective in inducing perspiration, resisting inflammation, relieving pain, regulating yellow water disease, and activating blood circulation. On this basis, a variety of formulas for Tibetan medicated bath have been derived for the treatment of diseases in internal organs, joints, nerves, etc. Modern studies have confirmed that Wuwei Ganlu has a good therapeutic efficacy on knee osteoarthritis(KOA). The present study explored the mechanism of Wuwei Ganlu in treating KOA based on network pharmacology and molecular docking. Firstly, the chemical components of Wuwei Ganlu were obtained through literature mining and database retrieval, and corresponding potential targets were predicted according to the BATMAN-TCM database. The protein-protein interaction(PPI) network was obtained after the potential targets were input into the STRING database. The network function modules were analyzed by the Molecular Complex Detection(MCODE) algorithm, and the functions of the modules were annotated to analyze the action mode of Wuwei Ganlu. Secondly, the related targets of KOA were collected through the DisGeNET database, and the overlapping targets were confirmed to analyze the mechanism of Wuwei Ganlu in treating KOA. Finally, the key targets were selected for molecular docking with the main components of Wuwei Ganlu to verify the component-target interaction. A total of 550 chemical components and 1 365 potential targets of Wuwei Ganlu were obtained. PPI analysis indicated that this formula could exert the effects of oxidation-reduction, inflammation resistance, bone absorption, bone mineralization, etc. Nineteen common targets were obtained from the intersection of potential targets of Wuwei Ganlu and KOA disease targets. It was found that the Wuwei Ganlu mainly acts on nuclear factor-κB(NF-κB), interleukin-1 beta(IL1β), tumor necrosis factor(TNF), IL6, IL1 receptor antagonist(IL1 RN), and prostaglandin-endoperoxide synthase-2(PTGS2) to treat KOA. Among the 550 chemical components of Wuwei Ganlu, 252 potential active components were docked with TNF and 163 with PTGS2, indicating good binding of the components with potential key targets. The study preliminarily explored the mechanism of Wuwei Ganlu in treating KOA to provide a reference for the further development and utilization of Tibetan medicated bath that has been included in the UN Intangible Cultural Heritage.


Subject(s)
Databases, Factual , Drugs, Chinese Herbal , Humans , Inflammation , Molecular Docking Simulation , Osteoarthritis, Knee
8.
Acta Pharmaceutica Sinica ; (12): 1015-1021, 2020.
Article in Chinese | WPRIM | ID: wpr-821680

ABSTRACT

Bexarotene is a synthetic analogue of retinoic acid and exerts protective effects on the nervous system. However, low bioavailability and poor solubility of the crystal type I form severely limits the application of bexarotene in the clinic. A co-amorphous sample of bexarotene-PVP-K30 was prepared and the structure was characterized by X-ray diffraction and infrared spectroscopy. To determine the pharmacokinetics and tissue distribution of bexarotene, an LC-MS method was established to profile and quantify bexarotene in plasma and tissues of SD rats. In vitro dissolution indicated that the co-amorphous form improved the dissolution of bexarotene in pure water 4.17-fold. After rats were orally administered bexarotene or bexarotene-PVP-K30 co-amorphous (equivalent to 30 mg·kg-1 bexarotene) the AUC of bexarotene was 7 034.89 and 10 174.03 μg·L-1·h respectively, the peak time was advanced from 7.33 h to 0.9 h with the amorphous form, and Cmax was enhanced from 627.76 to 3 011.88 μg·L-1. The co-amorphous form yielded higher concentrations of bexarotene in various tissues, especially brain, liver and kidney. Animal welfare and experimental procedures complied with the rules of the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences. The results indicate that bexarotene-PVP-K30 co-amorphous improves the pharmacokinetic characteristics of bexarotene and provides preclinical data in support of bexarotene-PVP-K30 for the treatment of brain diseases.

9.
Acta Pharmaceutica Sinica ; (12): 2642-2650, 2020.
Article in Chinese | WPRIM | ID: wpr-837508

ABSTRACT

Possible mechanisms by which Polygonati rhizoma opposes atherosclerosis (AS) were identified by network pharmacology and molecular docking analyses. The Traditional Chinese Medicine Database (TCMD) and the Traditional Chinese Medicine Systems Pharmacology Database (TCMSP) were utilized to identify the likely active components of Polygonati rhizoma. The potential targets set of Polygonati rhizoma were predicted with the PharmaDB database and the Swiss TargetPrediction database. The targets set for AS was retrieved by OMIM, DisGeNET and NCBI Gene database. We used the STRING platform to construct a protein-protein interaction network of the intersectional targets and performed visual analysis in Cytoscape. The key targets of Polygonati rhizoma in AS were searched by network topology and the resulting GO and KEGG enrichment was analyzed by Clue GO. In addition, the key targets were verified by molecular docking in Discovery Studio 4.0. A total of 45 active ingredients and 51 potential targets were obtained in the treatment of AS. The results of the topology analysis included five key targets: serum albumin, mitogen-activated protein kinase 3, mitogen-activated protein kinase 1, proto-oncogene tyrosine-protein kinase Src and matrix metalloproteinase-9. The 131 GO items showed that the biological process mainly involved the steroid receptor, cell response to steroid stimulation, the phosphatidylinositol-3 kinase signal pathway, and others. The KEGG pathway analysis included 37 pathways, which were closely related to peroxisome proliferation activated receptor signaling pathway, platelet activation pathway, vascular endothelial growth factor pathway, hypoxia inducible factor pathway and adhesion connection pathway. The results of molecular docking proved that the combined activity of the components with potential key targets is excellent. This study proposes mechanisms by which Polygonati rhizoma might act to reverse or minimize AS and provides a scientific basis for clinical research on Polygonati rhizoma.

10.
Article in Chinese | WPRIM | ID: wpr-878773

ABSTRACT

Hypertension is a kind of chronic cardiovascular system disease caused by a series of factors and carriers dysfunction, which belongs to the category of Tibetan medicine "Chalong disease", and has a high rate of disability and mortality. Zuomua Decoction is a classical Tibetan medicine for Chalong disease, but its mechanism is not clear. Therefore, in this paper we explored the multi-components, multi-targets and multi-channels mechanism of Zuomua Decoction in the treatment of hypertension based on network pharmacology and molecular docking technology. First of all, the chemical components of Zuomua Decoction were obtained in the retrieval of traditional Chinese medicine systems pharmacology database(TCMSP), China National Knowledge Infrastructure(CNKI) and Wanfang database. The potential targets of Zuomua Decoction were predicted by BATMAN-TCM database, and the targets of hypertension were obtained by using DisGeNET database. The intersection of these two targets set was taken to obtain the potential targets of Zuomua Decoction in the treatment of hypertension, and then the chemical compositions-targets network was constructed. Secondly, the intersection targets were imported into STRING database to obtain the interaction relationship of intersection targets, and the protein interaction network of Zuomua Decoction in the treatment of hypertension was constructed in Cytoscape. Topological, GO, and KEGG enrichment analysis were used to construct the key targets-signal pathways-biological processes network diagram and explore the mechanism of Zuomua Decoction in the treatment of hypertension. Finally, the key targets were selected to construct the pharmacodynamic identification models to verify the effect mode of Zomua Decoction in treating hypertension. The results showed that there were 61 chemical components and 90 potential targets in the compounds-targets network. We obtained 21 key targets, 154 signal pathways, and 382 biological processes in topological, GO, and KEGG enrichment analysis of the protein interaction network, and in the comprehensive analysis, it was found that Zuomua Decoction could reduce blood pressure by regulating renin angiotension aldosterone system, balancing the concentration of intracellular calcium and sodium ions and regulating vasoconstriction and relaxation. ACE, AGTR1, and ADRB2 were used as the carriers for molecular docking study on the components of Zuoma Decoction, and the results showed that the chemical components of Zuomua Decoction had a good binding activity with key targets. The purpose of this study is to provide ideas for the in-depth study of Zuoma Decoction in the treatment of hypertension, and provide scientific basis for its clinical rational application.


Subject(s)
Antihypertensive Agents , China , Drugs, Chinese Herbal , Humans , Hypertension/drug therapy , Medicine, Tibetan Traditional , Molecular Docking Simulation , Technology
11.
Article in Chinese | WPRIM | ID: wpr-828451

ABSTRACT

The quality marker(Q-marker) of traditional Chinese medicine(TCM) is a new concept of TCM quality control proposed in recent years. It is a hot issue in the research of modern Chinese medicine. The TCM efficacy is a high-level summary of the TCM therapeutic effect under the guidance of TCM theory. On this basis, it is of considerable significance to explore the TCM efficacy marker for the TCM modernization. However, the traditional research strategy based on the single herb and decoction piece in macro TCM level, or the drug research strategy based on the biological effect of the targets, is quite different from the characteristics of multiple components of TCM, as well as the weak and low-selective effect of Chinese medicine ingredients on targets. Therefore, how to select representative ingredients to characterize the TCM overall efficacy is a problematic point in establishing TCM efficacy markers. In this paper, the concept and method of Q-marker were introduced into the study of Chinese medicine efficacy. The research method for systematic TCM was used to systematically discuss the connotation of TCM efficacy markers, the principles of discovery and determination, common research ideas and techniques by taking the representative research results as an example. This study provides new ideas for the research and discovery of TCM efficacy markers.


Subject(s)
Biomarkers , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Quality Control , Research Design
12.
Article in Chinese | WPRIM | ID: wpr-828450

ABSTRACT

This paper aimed to establish efficacy systems of tanshinones and salvianolic acids, two representative substances in Salviae Miltiorrhizae Radix et Rhizoma by using literature mining and biological network construction, based on systematic traditional Chinese medicine theory. The systematic study on the efficacy of traditional Chinese medicine was carried out from the basic unit, the structure and relationship between the basic units, the boundary of the research object and the function of the system, so as to explain the overall efficacy of the two kinds of components at the molecular level. Firstly, we collected the elements of the efficacy systems of these two kinds of components by literature mining, and defined their boundaries based on biological processes. After that, the structure of the efficacy systems was clarified according to the relationship in the KEGG database. Finally, the function of the efficacy systems was analyzed from the level of pharmacology, pharmacodynamics, and efficacy, revealing the scientific connotation of traditional Chinese medicine efficacy system. The results showed that there were 201 targets(elements), 12 target sets(boundary), and 12 pathway networks(structure) in salvianolic acids' efficacy system. Meanwhile, there were 189 targets(elements), 11 target sets(boundary), and 11 pathway networks(structure) in tanshinones' efficacy system. The results suggested that the functions of salvia-nolic acids' and tanshinones' efficacy systems were different in pharmacology and pharmacodynamics from aspects of elements, boundary, relationship and structure, but they were same in functional level as both of them could promote blood circulation, remove blood stasis, clear away heart-fire, relieve restlessness, and soothe the nerves. Based on systematic traditional Chinese medicine, we constructed the efficacy system of two representative components in Salviae Miltiorrhizae Radix et Rhizoma in this paper, elucidated the overall efficacy and builded the bridge between reductionism and holism in traditional Chinese medicine.


Subject(s)
Acids , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Plant Roots , Rhizome , Salvia miltiorrhiza
13.
Article in English | WPRIM | ID: wpr-827207

ABSTRACT

Macroangiopathy is a complication of Type II Diabetes Mellitus (T2DM), which is mainly caused by fibrosis of blood vessels. Using T2DM rat models, we investigated whether the traditional Chinese medicine, Di-Dang Decoction (DDD), exhibited anti-fibrotic actions on great vessels. T2DM rats were randomly divided into non-intervention group, early-, middle-, late-stage DDD intervention groups and control groups, including pioglitazone group and aminoguanidine group. After administration of DDD to T2DM rats at different times, we detected the amount of extracellular matrix (ECM) deposition in the thoracic aorta. The results showed that early-stage intervention with DDD could effectively protect great vessels from ECM deposition. Considering that TGF-β1 is the master regulator of fibrosis, we further validated at the molecular level that, compared to middle- and late-stage intervention with DDD, early-stage intervention with DDD could significantly decrease the expression levels of factors related to the activated TGF-β1/Smad signalling pathway, as well as the expression levels of downstream effectors including CTGF, MMP and TIMP family proteins, which were directly involved in ECM remodelling. Therefore, early-stage intervention with DDD can reduce macrovascular fibrosis and prevent diabetic macroangiopathy.

14.
China Pharmacy ; (12): 991-990, 2019.
Article in Chinese | WPRIM | ID: wpr-817028

ABSTRACT

OBJECTIVE: To investigate the distribution, drug supply and quantity of licensed pharmacists in retail pharmacies around Third Grade Class A Hospitals, and to provide reference for decision-making of related management departments. METHODS: Field investigation and questionnaire survey were used to investigate the distribution, type, operating area, annual turnover, drug type, ranking of consumption sum, daily prescription amount and pharmacist allocation of 5 Third Grade Class A Hospitals in Beijing and general information of 100 surveyed pharmacists in 2017. RESULTS: There were 43 retail pharmacies in total within 1 km of 5 Third Grade Class A Hospitals, with an average of 8.60 retail pharmacies for each hospital. The number of retail pharmacies with distance between 200-400 m and 800-1 000 m was the largest (11), of which 21 (48.84%) were chain drugstores. The operating area of 38 pharmacies (88.37%) was in the range of 100-175 m2, mainly ranging 100-125 m2 (16 pharmacies, 37.21%). The annual turnover of 40 pharmacies were counted and ranged 50-10 000 ten thousand yuan, among which the pharmacies 0-200 m away from the hospital had the highest annual turnover. The average variety of drugs (prescription drugs and over-the-counter drugs) was 2 511 kinds. 34 pharmacies (79.07%) had more varieties of over-the-counter drugs than prescription drugs, and the consumption sum of over-the-counter drugs was higher than that of prescription drugs in 26 pharmacies (60.47%). Top 3 drugs in the list of consumption sum were antineoplastic drugs, cardiovascular drugs and anti-infective drugs. Average daily prescriptions of 28 drugstores (65.11%) were less than 10 pieces; average daily prescription were more than 20 pieces in only 7 pharmacies (16.28%). On average, each pharmacy had 7.4 staff members and 1.37 licensed pharmacists. 58 staff members’ first degree was junior college (58%), 38 staff members’ first degree was technical secondary school or high school (38%), and only 3 (3%) staff members’ first degree was undergraduates or above. CONCLUSIONS: With the gradual promotion of “health care policy” and the outflow of more hospital prescriptions, the retail pharmacies around hospitals should increase their numbers, expand the operating area, accelerate the construction of licensed pharmacists and improve the education level of pharmacists so as to improve the pharmaceutical care ability.

15.
Article in Chinese | WPRIM | ID: wpr-734310

ABSTRACT

Objective To explore the distribution characteristics on z-axis of scattered radiation from a wide-detector CT with different scan modes and detector widths.Methods The CT standard-dose phantom was scanned using a 16 cm wide detector Revolution CT.Thermoluminescent dosimeters (TLDs)were placed on the central axis (z-axis) of the scan hole at given intervals.As scan modes,both axial scan mode (using detector with width in 4,8 or 16 cm) and the helical scan mode (using detector with width in 4 and 8 cm) are used.The scan parameters were as follows:tube voltage 120 kV;effective tube current 200 mAs;scan length 16 cm;pitch (for helical scan):0.984 ∶ 1 and 0.516 ∶ 1,and all scans were repeated for 4 times.All TLDs were measured,after exposure,and divided by four for further analysis.Results The scattered radiation on z-axis was higher at the direction of human head than at the direction of human foot (Z=-2.366,-2.197,-2.366,-2.371,-2.028,-2.236,-2.028,P<0.05).Under the axial scan,the difference in distribution of scattered radiation with different detector widths was statistically significant.The maximum increase for detector width of 4 cm and 16 cm was 67.5 μ Gy(x2=28.000,P<0.05).Under the helical scan,the difference in distribution of scattered radiation with different detector widths was statistically significant (Z =-3.233,-2.982,P<0.05).The largest distribution of scattered radiation was found when the detector width was 8 cm and the smallest at the detector width is 4 cm.The maximum increase for detector width of 8 and 4 cm was 97.67 μGy at a pitch of 0.516 ∶ 1.Furthermore,when the detector width and effective mAs were the same,the scattered radiation at a pitch of 0.516∶1 was greater than that at a pitch of 0.984 ∶ 1,with the statistically significant difference(Z =-3.296,-3.296,P<0.05).The maximum increase was 49.95 μGy when the detector width was 8 cm.Conclusions In a 16 cm wide-detector CT,the selection of different detector widths can significantly influence the distribution of radiation field and related radiation values.Suitable detector width and relevant parameters shall be chosen according to the specific clinical requirements so as to reduce the radiation doses to workers,patients and carers.

16.
Article in Chinese | WPRIM | ID: wpr-692274

ABSTRACT

A sensing system based on AuNP-AuNP-UCNP triple structure for efficient detection of dual targets was constructed. In the preparation of triple structure, the gold nanoparticles (AuNPs) and upconversion nanoparticles (NaYF4: Yb, Er, Gd, UCNPs) were synthesized and surface modified. Then the two nanoparticles and their aptamers were connected to form two kinds of optical fluorescent probes. A nucleic acid sequence that matches with two aptamers was designed, rendering the probes to get close based on the principle of complementary base pairing. On the basis of this, a sensing system with a triple structure was prepared,and its connecting effect was characterized by TEM. With this system, dual targets of bisphenol A and estradiol were efficiently and conveniently detected through quantitative determination by fluorescence and UV spectrophotometer. At reaction temperature of 30℃ and pH=7.8,this method exhibited good linear range for determination of bisphenol A and estradiol from 2 ng/mL to 200 ng/mL and from 10 ng/mL to 150 ng/mL, with limits of detection of 0.2 ng/mL and 0.5 ng/mL, respectively. This sensing system with the triple structure owned better specificity to structural and functional analogues, and showed good repeatability and stability. What's more,this sensing system was applied in actual water detection,with the recoveries between 86.1% and 107. 4%, and the relative standard deviation below 6. 8%. This method showed promising applications in other environmental estrogens in water samples.

17.
Chinese Journal of Cardiology ; (12): 765-769, 2017.
Article in Chinese | WPRIM | ID: wpr-809249

ABSTRACT

Objective@#To explore the impact of hydrogen sulfide (H2S) on the heme oxygenase-1/carbon monoxide pathway in Coxsackie virus B3 (CVB3)-induced murine myocarditis (VMC) model.@*Method@#A total of 70 inbred male Balb/c mouse (4-6 weeks old) were randomized into the following four groups: Normal, VMC, PAG and NaHS (n=10 for Normal, n=20 for VMC, PAG and NaHS groups). Mice in Normal group were non-infected mice treated with intraperitoneal injection of sterile phosphate-buffered saline daily for 10 days.Mice in VMC group received intraperitoneal CVB3 injection (0.1 ml 10-5.69TCID50m·ml-1·d-1 and PBS for 10 days), and mice in PAG group received additional intraperitoneal DL-proparglygylcine injection (40 mg·kg-1·d-1 for 10 days), mice in NaHS group received additional intraperitoneal NaHS injection (50 μmol·kg-1·d-1 for 10 days). All mice were sacrificed on day 10th, and body weight and heart weight, the ratio of heart weight to body weight were compared among groups.Pathological changes of heart tissues were observed microscopically by HE and the histopathologic scores were valued.The content of COHb was tested after the gathering of blood specimens while reverse transcription-polymerase chain reaction was used to detect myocardial HO-1 mRNA expression.@*Results@#(1) Pathological findings in myocardium: hearts sections in Normal group were normal and no inflammatory cells and necrosis were found.A notable cellular infiltration, interstitial edema, vascular hyperemia and necrosis were observed in heart section of VMC, PAG and NaHS group.Extensive inflammations and larger area of myocardial cells necrosis were evidenced in PAG group and above changes were significantly reduced in NaHS group.(2) Comparison of the ratio of heart weight to body weight and histological scores of myocardium: the ratio was significantly higher in the VMC, PAG, NaHS groups than in Normal group (P<0.05), which was higher in PAG group and lower in NaHS group as compared with VMC group (both P<0.05). The histopathologic scores of all CVB3 innoculation groups were higher than in the Normal group, which was higher in PAG group and lower in NaHS group as compared to VMC group (both P<0.05). (3) The content of blood COHb in VMC, PAG or NaHS group was significantly higher than that in Normal group (P<0.05), which was significantly lower in PAG group, and higher in NaHS group as compared to VMC group (both P<0.05). (4) The mRNA expression of myocardial HO-1 detected by RT-PCR: weak expression was observed in Normal group, which was significantly upregulated in VMC, PAG and NaHS groups (P<0.05), which was downregulated in PAG group and upregulated in NaHS group as compared to VMC group (both P<0.05). (5) Correlation analysis: blood COHb concentration was positively correlated with myocardial HO-1 mRNA expression(r=0.927, P=0.000), negatively correlated with histopathologic scores(r=-0.753, P=0.000)and the histopathologic scores were negatively correlated with the myocardial HO-1 mRNA expression (r=-0.754, P=0.000).@*Conclusions@#H2S could play a protective role in murine CVB3 myocarditis model through inducing HO-1 expression and upregulating HO-1/CO pathway.

18.
Article in English | WPRIM | ID: wpr-327197

ABSTRACT

<p><b>OBJECTIVE</b>To assess the antinociceptive and anti-inflammatory properties of the aqueous extract of Armadillidium vulgare (AV).</p><p><b>METHODS</b>The antinociceptive effect of AV (400, 600 and 800 mg/kg) was investigated in mice using the acetic acid-induced writhing, formalin-induced nociceptive, and hot plate tests. Phlogogen-induced paw edema using carrageenan, dextran, or compound 48/80 as phlogogen was used as inflammatory models to evaluate AV's anti-inflammatory effect. Additionally, the bioactive substances glucosamine (GLcN) and taurine in AV were determined using high-performance liquid chromatography.</p><p><b>RESULTS</b>Oral treatment of the mice with AV (600 and 800 mg/kg) significantly reduced the number of writhes in the acetic acid-induced writhing test (P<0.01) but not the hot plate test (P>0.05). All doses tested significantly inhibited paw-withdrawal during the second phase of the formalin-induced nociceptive model (P<0.01). AV demonstrated a strong anti-inflammatory effect in all those inflammatory models (P<0.05).</p><p><b>CONCLUSIONS</b>AV has antinociceptive and anti-inflammatory effects, providing scientific evidence of the efficacy of its traditional use in pain treatment. Furthermore, GLcN and taurine contribute, at least in part, to the anti-inflammatory activity of AV.</p>


Subject(s)
Analgesics , Pharmacology , Animals , Anti-Inflammatory Agents , Pharmacology , Edema , Drug Therapy , Female , Inflammation , Drug Therapy , Isopoda , Chemistry , Male , Mice , Pain , Drug Therapy , Pain Measurement , Phytotherapy , Plant Extracts , Chemistry , Pharmacology , Water , Chemistry
19.
China Occupational Medicine ; (6): 341-344, 2017.
Article in Chinese | WPRIM | ID: wpr-881620

ABSTRACT

OBJECTIVE: To compare the effects of ~(56)Fe~(17+),~(12)C~(6+)ion beams and~(60)Co γ rays on chromosome aberration in human lymphoblastoid cells. METHODS: The human lymphoblastoid cells were divided into 0. 1,0. 3,0. 5,0. 7,1. 0,2. 0 Gy irradiated groups and 0. 0 Gy control group. They were separately exposed to ~(56)Fe~(17+)ion beams( linear energy transfer was 400. 0 ke V/μm),~(12)C~(6+)ion beams( linear energy transfer was 26. 0 ke V/μm) and~(60)C γ rays. Chromosome specimens were harvested 48 hours after irradiation. The effects of different radiation on dicentric plus centric ring( “d + r”) aberration rate and chromosome aberration in human lymphoblastoid cells were detected by light microscope with artificial counting. RESULTS: The “d + r”aberration rates induced by 0. 3-2. 0 Gy ~(12)C~(6+)ion beams were significantly higher than those of ~(56)Fe~(17+)ion beams and~(60)Co γ rays at the same dose( P < 0. 017). Chromosome aberration cell rates of 0. 1-2. 0 Gy ~(12)C~(6+)ion beams were significantly higher than those of ~(56)Fe~(17+)ion beams and~(60)C γ rays at the same dose( P < 0. 017). At the dose range of 0. 0-2. 0 Gy,chromosome aberration effects of three kinds of radiations were gradually increased( P < 0. 01). The relative biological effectiveness of ~(56)Fe~(17+)ion beams was lower than that of ~(12)C~(6+)ion beams.CONCLUSION: The chromosome aberration induced by ~(12)C~(6+)ion beams was more serious than that of~(60)Co γ rays and ~(56)Fe~(17+)ion beams.

20.
Chinese Mental Health Journal ; (12): 734-738, 2017.
Article in Chinese | WPRIM | ID: wpr-668265

ABSTRACT

Objective:To investigate the mediating roles of perceived social support and relative deprivation in the relationships between life events and Internet addiction among Chinese college students.Methods:Totally 413 college students (200 males and 213 females,aged 16-21 years),completed the Relative Deprivation Questionnaire,Adolescent Self-Rating Life Events Check List,Perceived Social Support Scale and Chinese Internet Addiction Scale Revised to measure the level of relative deprivation,life events,perceived social support and Internet addiction.The Bollen-Stine of structural equation modeling and Bootstrap were used to test the mediating effect of perceived social support and relative deprivation on the relationship between life events and Internet addiction.Results:The scores of PSSS were negatively correlated with the scores of ASLEC,RDQ,and CIAS-R (r=0.11-0.36,Ps <0.05).The scores of ASLEC,RDQ,and CIAS-R were positively correlated with each other (r=0.14-0.23,Ps < 0.01).Path analyses showed that the ASLEC scores were not associated with the CIAS-R scores directly (β =0.11,P >0.05),but indirectly through the mediating roles of the scores of PSSS and RDQ and the chain mediating effect of them among Chinese college students.The structural equation model could be accepted by Bollen-Stine Bootstrap (P <0.01).The confidence interval from Bootstrap output of the mediating effects of the scores of PSSS and RDQ and the chain mediating effect of them were (0.010,0.103),(0.002,0.032) and (0.005,0.061) respectively.Conclusion:It suggests that life events could not directly affect Internet addiction,but indirectly lead to Internet addiction through reducing perceived social support and increasing relative deprivation.

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