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1.
Acta Pharmaceutica Sinica B ; (6): 1351-1362, 2022.
Article in English | WPRIM | ID: wpr-929342

ABSTRACT

Scaffold hopping refers to computer-aided screening for active compounds with different structures against the same receptor to enrich privileged scaffolds, which is a topic of high interest in organic and medicinal chemistry. However, most approaches cannot efficiently predict the potency level of candidates after scaffold hopping. Herein, we identified potent PDE5 inhibitors with a novel scaffold via a free energy perturbation (FEP)-guided scaffold-hopping strategy, and FEP shows great advantages to precisely predict the theoretical binding potencies ΔG FEP between ligands and their target, which were more consistent with the experimental binding potencies ΔG EXP (the mean absolute deviations | Δ G FEP - Δ G EXP |  < 2 kcal/mol) than those ΔG MM-PBSA or ΔG MM-GBSA predicted by the MM-PBSA or MM-GBSA method. Lead L12 had an IC50 of 8.7 nmol/L and exhibited a different binding pattern in its crystal structure with PDE5 from the famous starting drug tadalafil. Our work provides the first report via the FEP-guided scaffold hopping strategy for potent inhibitor discovery with a novel scaffold, implying that it will have a variety of future applications in rational molecular design and drug discovery.

2.
Article in Chinese | WPRIM | ID: wpr-928074

ABSTRACT

Lonicera Japonica Flos is the dried bud or nascent flower of Lonicera japonica(Caprifoliaceae). The plant suffers from various diseases and pests in the growth period and thus pesticides are often used. As a result, the resultant pesticide residues in Lonicera Japonica Flos have aroused great concern. This review summarized the investigation, detection methods, content analysis, and risk assessment of pesticide residues in Lonicera Japonica Flos since 1996, and compared the maximum residue limits among different countries and regions. The results showed that the pesticide residues were detected in Lonicera Japonica Flos from different production areas, and only some exceeded the limits. The residual pesticides have changed from organochlorines to new types such as tebuconazole and nitenpyram. The detection method has upgraded from chromatography to chromatography-mass spectrometry. Most pesticide residues will not cause health risks, except carbofuran. Pesticide residues limit the development of Lonicera Japonica Flos industry in China. In practice, we should improve the drug registration of Lonicera Japonica Flos, promote ecological prevention and control technology, and formulate and promote pesticide residue limit standard of Lonicera Japonica Flos.


Subject(s)
Flowers/chemistry , Lonicera/chemistry , Mass Spectrometry , Pesticide Residues/analysis , Pesticides/analysis
3.
Article in Chinese | WPRIM | ID: wpr-928071

ABSTRACT

Panacis Quinquefolii Radix is the dry root of Panax quinquefolium, which is a perennial plant of Araliaceae. The plant has a long growth cycle and serious growth barrier problem, which leads to the use of pesticides. As a result, the pesticide residues in Panacis Quinquefolii Radix are arousing great concern. This paper reviews the research findings on the investigation, detection methods, content analysis and risk assessment of pesticide residues in Panacis Quinquefolii Radix since 1993, and compares the pesticide residue limit standards of different countries and regions. The pesticide residues in Panacis Quinquefolii Radix have been changing from organochlorines with high toxicity to triazines and triazoles with low toxicity. The pesticide residues are generally low, while the pollution of pentachloronitrobenzene and other pesticides still exist. The detection method has evolved from chromatography to chromatography-mass spectrometry. There are no reports of health risks caused by pesticide residues of Panacis Quinquefolii Radix. Pesticide residue is a major factor restricting the sound development of Panacis Quinquefolii Radix industry in China. Therefore, we suggest to improve the registration of pesticides applied to the plant, popularize mature ecological planting mode and supporting technology, and strengthen the research on the risk assessment and limit standard of pesticide residue in Panacis Quinquefolii Radix.


Subject(s)
Drugs, Chinese Herbal/chemistry , Ginsenosides/analysis , Mass Spectrometry , Panax/chemistry , Pesticide Residues/analysis
4.
Article in Chinese | WPRIM | ID: wpr-924042

ABSTRACT

Objective To observe the correlation and clinical significance between serum homocysteine (HCY) level and the severity of coronary heart disease (CHD). Methods A total of 497 hospital-based patients with newly diagnosed coronary heart disease from June 2018 to June 2021 in our hospital were selected as the study subjects. The patients' sociodemographic information, coronary heart disease condition information and HCY level information at diagnosis were collected. The correlation between serum HCY level and the severity of coronary heart disease was analyzed from multiple perspectives. Data were collected and analyzed using SPSS 19.0 statistical software package. Results The average level of HCY in all patients was (20.23±2.18) μmol/L, among which 330 cases exceeded the standard level of HCY and 167 cases did not exceed the standard level. There were statistically significant differences in serum HCY levels among patients with different genders, different ages, different altitudes, and different types of coronary heart disease (P<0.05). The correlation coefficients between HCY level and the severity of CHD in different genders were r1=0.356, and r2 =0.198, P<0.05. The correlation coefficients between HCY level and the severity of CHD in patients of different ages were r1=0.304, r2=0.50, r3=0.217, and r4=0.185, P<0.05. The correlation coefficients between HCY level and the severity of CHD in patients living at different altitudes were r1=0.129, r2=0.369, and r3 =0.473, P<0.05. The correlation coefficients between HCY level and the severity of CHD in patients with different types of CHD was r1=0.137, r2=0.200, and r3=0.205, P<0.05. Logistic multivariate regression analysis showed that serum HCY, altitude, gender and age were independent risk factors for coronary heart disease (P<0.05). Conclusion The correlation between serum HCY level and the severity of CHD is stronger in male patients than in female patients. The correlation between HCY level and the severity of CHD was strongest in patients aged 40-50. Serum HCY level is more strongly correlated with the severity of CHD in patients with high altitude. Serum HCY test can be used to diagnose CHD and evaluate the severity of coronary artery disease.

5.
Article in Chinese | WPRIM | ID: wpr-910815

ABSTRACT

Objective:To explore the classification of the therapeutic effect of patients with high-risk differentiated thyroid carcinoma (DTC) after surgery and 131I treatment, and to analyze the relevant factors that affect the therapeutic effect. Methods:From January 2015 to January 2018, 256 high-risk DTC patients (70 males, 186 females; age (47.6±12.9) years) in the First Affiliated Hospital of Zhengzhou University were retrospectively analyzed. According to the 2015 American Thyroid Association(ATA)guidelines for therapeutic effect classification standards and the data measured during 6 months postoperative stimulation state, patients were divided into excellent response (ER) group, inderterminate response (IDR) group, biochemical incomplete response (BIR) group and structurally incomplete response (SIR) group, and the latter two groups were further combined into incomplete response (IR) group. χ2 test, Fisher exact test and Kruskal-Wallis rank sum test were used to compare the clinical characteristics among the four groups. The receiver operating characteristic (ROC) curve of the relationship with ER and IR was established. Multivariate logistic regression was used to analyze the independent influencing factors of ER and IR. The subgroups with B-Raf proto-oncogene, serine/threonine kinase (BRAF) V006E results were individually tested with χ2 test of therapeutic efficacy. Results:There were 48.05%(123/256), 20.31%(52/256), 19.53%(50/256) and 12.11%(31/256) of DTC patients in ER, IDR, BIR and SIR groups respectively. The differences in gender ( χ2=11.495, P=0.008), tumor size ( H=21.368, P<0.001), N stage ( χ2=42.012, P<0.001), distant metastasis ( P<0.001) and pre-ablation stimulated thyroglobulin (psTg) level ( H=142.829, P<0.001) were statistically significant among the 4 groups. The cut-off values of psTg for predicting ER and IR were 5.38 μg/L and 15.85 μg/L with the sensitivities of 79.7%(98/123) and 88.9%(72/81), with the specificities of 84.2%(112/133) and 91.4%(160/175) respectively. The cut-off values of tumor size for predicting ER and IR were 1.45 cm and 1.95 cm with the sensitivities of 63.4%(78/123) and 53.1%(43/81), with the specificities of 66.2%(88/133) and 74.3%(130/175) respectively. Multivariate regression analysis showed that female (odds ratio ( OR)=2.305, 95% CI: 1.041-5.104), N0 stage ( OR=2.365, 95% CI: 1.104-5.066), psTg<5.38 μg/L ( OR=17.271, 95% CI: 8.561-34.841) and tumor size <1.5 cm ( OR=2.194, 95% CI: 1.092-4.409) were independent predictors of ER; psTg≥15.85 μg/L ( OR=81.544, 95% CI: 30.561-217.577), N1b stage ( OR=3.617, 95% CI: 1.276-10.253) and tumor size >4.0 cm( OR=47.060, 95% CI: 2.449-904.360) were independent predictors of IR. The BRAF V006E mutation rate of patients in the distant metastasis subgroup of the SIR group was significantly lower than that in ER, IDR, and BIR groups ( χ2 values: 20.852-40.905, all P<0.008). Conclusions:About 48.05% of high-risk patients can achieve ER half a year after the initial treatment and be classified as low-risk again. Female, patients with N0 stage, psTg<5.38 μg/L and tumor size <1.5 cm have better therapeutic effect after initial treatment; patients with N1b stage, psTg≥15.85 μg/L and tumor size >4.0 cm have poor therapeutic effect after initial treatment.

6.
Chinese Critical Care Medicine ; (12): 618-620, 2021.
Article in Chinese | WPRIM | ID: wpr-909371

ABSTRACT

Hypothermia can have adverse effects on various systems of trauma patients, and significantly increase the mortality. All of the current rewarming equipments are contact rewarming equipment, which have the shortcomings of single function and poor effect. The medical staff of the First People's Hospital of Chenzhou designed a multi-functional infrared heating medical rewarming equipment, and obtained the National Utility Model Patent of China (ZL 2018 2 1705172.9). By integrating the infrared heating lamp tube and the air heating device and controlling them independently, the equipment can not only treat the wound by infrared alone, but also keep the wound warm by using the air heating function at low room temperature. In addition, it can also warm the patients with hypothermia separately. The device's dual functions of promoting wound healing and rewarming by infrared therapy and wind-heating are accurate. It is easy to operate with good controllability, and contributes to individualized precision treatment, which is worthy of transformation and promotion.

7.
Article in Chinese | WPRIM | ID: wpr-908236

ABSTRACT

Objective:To explore the symptom experience of patients with acute coronary syndrome before diagnosis, in order to improve their early recognition ability, timely medical treatment rate and formulate relevant measures to provide reference.Methods:Semi-structured interview was performed in 18 patients with acute coronary syndrome from August 12 2020 to September 8 in Shanxi Provincial people′s Hospital using phenomenological research, and the data were analyzed under the guidance of symptom experience model.Results:A total of four themes were summarized: symptom perception: diseases being easily predicted, symptom experiences being diverse and diseases being easily overlooked; symptom evaluation: correct evaluation and evaluation bias; symptom response: self-response and family-society support; reflection on the process of symptom experience:medical behaviour and lack of awareness of disease.Conclusions:At present, the identification of acutecoronary syndrome is still a challenge. Patients should enrich relevant knowledge, pay attention to their own symptom experience, make the correct evaluation and deal with it effectively. Medical workers should carry out relevant education to improve the ability of patients to identify diseases.

8.
Article in Chinese | WPRIM | ID: wpr-906182

ABSTRACT

Objective:To identify the chemical constituents of Platycladi Cacumen<italic> </italic>before and after being carbonized. Method:Chemical constituents in 3 batches of Platycladi Cacumen and its carbonized products<italic> </italic>were identified and compared by ultra performance liquid chromatography-quadrupole-time of flight-mass spectrometry (UHPLC-QTOF-MS/MS). Chromatographic separation was performed on an ACQUITY UPLC BEH C<sub>18</sub> column (2.1 mm×100 mm, 1.7 μm) with 0.1% formic acid aqueous solution (A)- acetonitrile (B) as mobile phase for gradient elution (0-3.5 min, 5%-15%B; 3.5-6 min, 15%-30%B; 6-6.5 min, 30%B; 6.5-12 min, 30%-70%B; 12-12.5 min, 70%B; 12.5-18 min, 70%-100%B; 18-22 min, 100%B). The flow rate was 0.4 mL·min<sup>-1</sup> and the injection volume was 5 μL. Mass spectrometry was performed by an electrospray ionization, and the primary and secondary mass spectrometry data were collected with the full scan mode of positive and negative ions, the peaks containing MS/MS data were identified by self-established secondary mass spectrometry database and corresponding fragmentation law matching method. Result:A total of 77 and 76 substances with the same change trend were identified under positive and negative ion modes. After being<italic> </italic>carbonized, the disappeared components of Platycladi Cacumen were mainly amino acids, ketone aldehydes and other volatile components. Among newly produced components, there were 6 kinds of flavonoid aglycones (rhamnetin, 6,7,3'-trihydroxyflavone, 3,6,3'-trihydroxyflavone, 4'-hydroxy-2'-methyl-3,4,5-trimethoxychalcone, herbacetin and 3',5'-dimethoxy-3,5,7,4'-tetrahydroxyflavone), 3 kinds of coumarins (7-hydroxycoumarin, 7,8-dihydroxycoumarin and 8-acetyl-7-hydroxycoum-arin) and 3 kinds of benzoic acids (3-methylcatechol, pyrocatechol and chromone-3-carboxylic acid). There were a total of 40 flavonoids (quercitrin, quercetin, kaempferol, etc.) among these identified chemical constituents. Conclusion:There are significant quantitative and qualitative changes in the chemical compositions of Platycladi Cacumen after being carbonized. The flavonoids, the identified main active ingredients, can provide data reference for further study on the material basis of efficacy changes of Platycladi Cacumen<italic> </italic>before and after being carbonized.

9.
Acta Pharmaceutica Sinica ; (12): 1893-1901, 2021.
Article in Chinese | WPRIM | ID: wpr-887004

ABSTRACT

The threat of fungal diseases is increasingly rigorous. The clinically invasive fungal infections remain a main cause of morbidity and mortality in certain high-risk groups, especially in critical patients or immunocompromised patients. In drug therapy, the problems of off-target toxicity and antifungal drug resistance are still challenging. With the wide application of biomaterials and nanotechnology, more nanomedicine studies have been carried out on antifungal drugs, such as the amphotericin B liposome which greatly reduced the renal toxicity of drugs has been successfully marketed. For the unique physical and chemical properties, the nano-drug delivery system possessed great potential in improving the bioavailability, reducing the side effects of drugs, increasing the stability of drugs, and achieving cells or tissue-specificity through the modification. This review summarized the applications and limitations of antifungal drugs. Some nanomedicines were summarized in discussion oriented around the antifungal therapy, including liposomes, niosomes, lipid nanoparticles, polymer nanoparticles, microemulsion, dendrimers, inorganic nanocarriers. Nanotechnology and nano-drug delivery system provide promising strategies for the research and development of new formulations that can improve antifungal activity and possibly overcome antifungal drug resistance.

10.
Article in Chinese | WPRIM | ID: wpr-884802

ABSTRACT

Objective:To screen the factors that were conducive to prolonging the effective half-life of 131I, and to provide a basis for selecting more suitable patients for the treatment of hyperthyroidism with lithium carbonate assisted radioactive 131I. Methods:Between July 2017 and March 2019, a total of 61 patients (23 males, 38 females, age: 13-73 (37.7±1.9) years) who received lithium carbonate adjuvant therapy before 131I treatment in the First Affiliated Hospital of Zhengzhou University were collected into this prospective study. Clinical parameters (serum free triiodothyronine (FT 3), serum free thyroxine (FT 4), iodine uptake rate (2 h, 12 h, 24 h) and ratio of iodine uptake rate (2 h/24 h, 4 h/24 h) before and after taking lithium carbonate were compared by using paired t test. The factors which were conducive to prolonging the effective half-life of 131I were analyzed by linear and multiple regression analyses. Results:Compared with the pretreatment results, lithium carbonate treatment significantly improved the 24 h iodine uptake rate ((74.82±2.69)% vs (82.38±2.33)%; t=2.674, P=0.010), decreased the ratio of 4 h/24 h iodine uptake rate ((88.96±2.85)% vs (82.12±2.27)%; t=2.644, P=0.010), prolonged the effective half-life of 131I ((123.03±3.09) vs (130.38±2.49) h; t=2.656, P=0.010), and decreased serum FT 3 ((26.46±1.65) vs (21.31±1.42) pmol/L; t=3.421, P=0.001) and serum FT 4 ((56.59±2.12) vs (49.24±2.19) pmol/L; t=3.289, P=0.002). Linear regression analysis showed that 2 h and 4 h iodine uptake rate, the ratios of 2 h/24 h and 4 h/24 h iodine uptake rate, and effective half-life of 131I before lithium carbonate treatment were related to the effective half-life of 131I after lithium carbonate treatment ( b values: from -0.576 to 0.642, all P<0.05). Multiple linear regression analysis showed that the ratio of 4 h/24 h iodine uptake rate was the main factor affecting the effective half-life of 131I after taking lithium carbonate ( b=0.642, 95% CI: 0.453-0.832, P<0.001). Multiple linear regression equation was y=-49.785+ 0.642 x. Lithium carbonate treatment could prolong the effective half-life of 131I if the ratio of 4 h/24 h iodine uptake exceeded 77.55%. Conclusion:The ratio of 4 h/24 h iodine uptake rate is the main factor affecting the change of the effective half-life of 131I after lithium carbonate treatment, and patients with hyperthyroidism whose ratio of 4 h/24 h iodine uptake rate exceeds 77.55% can effectively prolong the effective half-life of 131I after taking lithium carbonate.

11.
National Journal of Andrology ; (12): 904-908, 2021.
Article in Chinese | WPRIM | ID: wpr-922174

ABSTRACT

Objective@#To analyze the correlation of the sperm DNA fragmentation index (DFI) level with semen parameters and pregnancy outcomes of artificial insemination of the husband (AIH) in the cycle of intrauterine insemination (IUI).@*METHODS@#We collected the clinical data on 777 cases of IUI, including female clinical indicators, male semen parameters, sperm DFI and pregnancy outcomes. According to the DFI level, we divided the patients into three groups: DFI < 15%, 15% ≤ DFI < 30% and DFI ≥ 30%.@*RESULTS@#The sperm DFI level was significantly elevated with the increased age of the males (P = 0.002) and closely related to the total number of motile sperm (P = 0.002) and total sperm motility (P = 0.000) before treatment, as well as to sperm concentration (P = 0.000), total sperm motility (P = 0.001) and total number of progressively motile sperm (P = 0.000) after density gradient centrifugation. The rate of clinical pregnancy was decreased in the DFI ≥ 30% group. There were no statistically significant differences between sperm DFI and the rates of clinical pregnancy and abortion.@*CONCLUSIONS@#Male age significantly affects the sperm DFI level. Sperm DFI is closely related to sperm motility and total number of progressively motile sperm, but not to the rates of clinical pregnancy and abortion in patients undergoing IUI. IUI can be used as an effective method of assisted reproduction for male infertility./.


Subject(s)
DNA Fragmentation , Female , Humans , Insemination, Artificial, Homologous , Male , Pregnancy , Pregnancy Outcome , Semen , Sperm Motility , Spermatozoa
12.
China Pharmacy ; (12): 176-181, 2021.
Article in Chinese | WPRIM | ID: wpr-862640

ABSTRACT

OBJECTIVE:To establish a method for online detection of antioxidant active components in Glycyrrhiza uroalensis decoction pieces ,and to identify it. METHODS :The free radical scavenging rate of 1,1-diphenyl-2-trinitrobenzene hydrazine (DPPH)was determined to evaluate the antioxidant activity of G. uralensis decoction pieces. HPLC-UV-DPPH method was used to screen the anti oxidant active components of G. uralensis decoction pieces. HPLC-TOF/MS was used to obtain mass spectrum data and Qualitive Analyst B 06.00 Build 6.0.633.0 software was used to analyze data. Through contrast analysis of UV absorption spectrum,online chromatogram ,mass spectrum information of G. uralensis and the retention time of each compound ,accurate molecular weight ,antioxidant active components were identified by referring to relevant literature. Validation test was also conducted. RESULTS :DPPH free radical scavenging rate in 8 batches of G. uralensis decoction pieces ranged 55.71%-60.17%. Seven antioxidative active compounds ,including avolomotor ,8-isopentenyl naringin ,yellow lupulin weitone ,isoflavone B ,3′, 4′-dimethoxy3-hydroxy-6-methyl flavone ,glycyrrhizin E and glycyrrhizin H ,could be screened from G. uralensis decoction pieces. After validation ,the peak area of inverted peak generated by online reaction was positively correlated with DPPH free radical scavenging rate. CONCLUSIONS :Established method is simple and accurate ,and can be used to quickly screen and identify the main antioxidant components of G. uralensis decoction pieces ;the peak area of inverted peak can be used to evaluate the antioxidant active components of G. uralensis decoction pieces.

13.
China Pharmacy ; (12): 850-859, 2021.
Article in Chinese | WPRIM | ID: wpr-875819

ABSTRACT

OBJECTIVE:To systematicall y review the pharmacoeconomics of anticoagulants for the prevention and therapy of venous thromboembolism (VTE)in cancer patients. METHODS :Retrieved from PubMed ,Embase,Cochrane library ,CNKI, Wanfang database ,VIP,SinoMed,The NHS Economic Evaluation Database ,The Healthy Technology Assessment Database and EconLit,supplemented by manual retrieval ,the economic evaluation studies on the prevention and therapy of VTE in cancer patients with different anticoagulants were collected. The retrieval time was from the inception to Nov. 12th,2020. After screening and extracting ,the Consolidated Health Economic Evaluation Reporting Standards (CHEERS)was used to evaluate the quality of the included literatures. The basic characteristics of the included literatures were summarized by descriptive methods ,and the economic results were summarized according to medication purpose and different intervention grouping. RESULTS :A total of 15 literatures were included. Three literatures were of excellent quality ;ten were of good quality ;and the other two were of moderate quality. Included studies were widely conducted in countries of different economic levels ,including China (1 piece),the United States(7 pieces),Canada(3 pieces),France(2 pieces),the Netherlands (1 piece),Brazil(1 piece)and Austria (1 piece). For preventing VTE in cancer patients ,the economic evaluation results of warfarin and low-molecular-weight heparin (LMWH)needed to be updated. Novel oral anticoagulants (NOACs)for the prevention of VTE were less cost-effective among cancer patients with medium- and high-risk venous thrombosis in China than in the United States ,but the economic advantage increased among the high-risk patients. Compared to enoxaparin ,aspirin was absolutely dominant to preventing VTE in patients with myeloma. For the treatment of VTE in cancer patients ,LMWH was not cost-effective ,compared to warfarin in the United States ;but it was cost-effective in Canada and some countries of Northern Europe. Compared with LMWH ,NOACs could save total cost ,but the incremental utility in the United States and Brazil were opposite. Sensitivity analysis showed that economic results were sensitive to drug prices ,the baseline rate of thrombosis risk ,and the risk of adverse events (thrombosis recurrence ,major bleeding and death ) of different interventions ,the first two of which could reverse the conclusions. CONCLUSIONS :For the prevention of VTE in cancer patients ,compared with no intervention or placebo ,the economic advantages of NOACs were different in different countries or for patients with different thrombosis risk ;the economics of warfarin and LMWH were not yet clear. Aspirin had obvious economic advantages compared with enoxaparin. For the treatment of VTE in cancer patients ,LMWH had different economic advantages compared with warfarin in different countries ;NOACs could save costs compared with LMWH. Economic strategies are greatly affected by the risk of diseases ,medical systems ,drug price ,patient preferences and values ,economic levels ,cost-utility threshold standards in different countries. Therefore ,the final economic strategies need to be based on the contexts of different countries.

14.
Yonsei Medical Journal ; : 210-217, 2020.
Article in English | WPRIM | ID: wpr-811475

ABSTRACT

PURPOSE: The goal of this study was to explore the effects of hsa-let-7g on cell proliferation and apoptosis, and elucidate its role in lung cancer development.MATERIALS AND METHODS: The expression levels of has-let-7g and HOXB1 in tissues and cells were measured by qRT-PCR. An inhibitor of hsa-let-7g or one targeting a control messenger RNA were transfected into A549 and H1944 lung cancer cells, and the effects of hsa-let-7g dysregulation on cell viability and apoptosis were analyzed using CCK-8 and apoptosis detection assays. HOXB1 was confirmed as the target gene of hsa-let-7g, based on luciferase reporter assay results. The relationship between hsa-let-7g and HOXB1 was confirmed by co-transfection of inhibitors of hsa-let-7g and HOXB1 followed by Western blot, CCK-8, and apoptosis detection assays.RESULTS: We observed high expression of hsa-let-7g in lung cancer tissues compared to the corresponding normal tissues, and generally higher expression of hsa-let-7g in patients with advanced tumor classification. The results of CCK-8 and apoptosis detection experiments showed that the inhibition of hsa-let-7g significantly inhibited proliferation of A549 and H1944 cells, but also promoted apoptosis. HOXB1 is a specific target of hsa-let-7g, and downregulation of HOXB1 in lung cancer cells reversed the suppressive effects caused by knocking down hsa-let-7g.CONCLUSION: These data collectively suggest that the expression of hsa-let-7g inhibits lung cancer cells apoptosis and promotes proliferation by down-regulating HOXB1. The results from this study demonstrate the potential of hsa-let-7g/HOXB1 axis as a therapeutic target for the treatment of lung cancer.


Subject(s)
Apoptosis , Blotting, Western , Cell Proliferation , Cell Survival , Classification , Down-Regulation , Humans , Luciferases , Lung Neoplasms , Lung , MicroRNAs , RNA, Messenger , Sincalide
15.
Article in Chinese | WPRIM | ID: wpr-864594

ABSTRACT

Objective:To systematically evaluate the qualitative study of the real experience of patients with enteral nutrition after gastro/jejunostomy and their caregivers and to deeply understand the real feelings and physical and mental experience of patients and caregivers.Methods:Databases were searched including PubMed, Embase, CINAHL, The Cochrane Library, Web of Science, PsycINFO, CNKI, Wanfang Database, VIP Database and CBM from inception to September 30th, 2019. To collect the qualitative studies on the real experience of patients with enteral nutrition after gastro/jejunostomy and their caregivers. According to the inclusion and exclusion criteria, the included literature was determined, the literature was evaluated according to the quality evaluation criteria of qualitative research of the JBI Evidence-based Health Care Center, and the results were integrated using a collective integration method.Results:A total of 11 studies were included and 37 results were extracted. Based on the quality of life theory, the topics extracted are as follows: patients with enteral nutrition after gastro/jejunostomy and their caregivers experienced dynamic cycle of change and challenge, coping and adaptation, demand and support in the domain of health and function, psychology/spiritual, socioeconomic and family.Conclusions:The four domains of quality of life of patients and caregivers were affected during enteral nutrition after gastro/jejunostomy. In particular, patients and caregivers showed strong inner and information needs in the psychological/spiritual and socioeconomic domain. It is suggested that medical staff should provide effective psychological, emotional and information support in disease treatment and nursing, in order to improve the quality of life of patients and caregivers.

16.
Acta Pharmaceutica Sinica B ; (6): 2339-2347, 2020.
Article in English | WPRIM | ID: wpr-881115

ABSTRACT

Optimization efforts were devoted to discover novel PDE10A inhibitors in order to improve solubility and pharmacokinetics properties for a long-term therapy against pulmonary arterial hypertension (PAH) starting from the previously synthesized inhibitor

17.
Article in Chinese | WPRIM | ID: wpr-828375

ABSTRACT

Licorice is one of the most commonly used traditional Chinese medicine. In clinic, raw licorice and honey-fried licorice are used in medicines, with the main effects in clearing away heat and detoxifying, moistening lungs and removing phlegm. Honey-fried licorice has effects in nourishing the spleen and stomach and replenishing Qi and pulse. Because traditional Chinese medicine exerts the effects through multiple components and multiple targets, the index components used in the quality evaluation of licorice are often difficult to reflect their real quality. In addition, most of studies for the quality standards have shown that honey-fried licorice are the same as licorice, with a lack of quality evaluation standards that can demonstrate their processing characteristics. The quality of medicine is directly related to its clinical efficacy, so it is necessary to establish a more effective quality control method. Licorice has a beany smell, which is one of the main quality identification characteristics. In this study, by taking advantage of the odor characteristics, a headspace-gas chromatography-ion migration mass spectrometry technology was used to establish a quality evaluation method. A total of 76 volatile components were identified. Through the dynamic principal component analysis, 7 kinds of volatile substances in raw licorice and 13 kinds of volatile substances in honey-fried licorice were statistically obtained, and could be taken as index components for the quality evaluation of raw and honey-fried licorice, respectively. This study could help realize the combination and unification of modern detection and traditional quality evaluation methods, and make a more realistic evaluation for the quality of licorice.


Subject(s)
Gas Chromatography-Mass Spectrometry , Glycyrrhiza , Honey , Ion Mobility Spectrometry , Volatile Organic Compounds
18.
Chinese Journal of Biotechnology ; (12): 1659-1671, 2020.
Article in Chinese | WPRIM | ID: wpr-826811

ABSTRACT

To construct TeI3c/4c-based and temperature-inducible gene inactivation system (Thermotargetron) and to apply it to gene inactivation of mesophilic bacteria. The subunit of flagellum (fliC) and C4 dicarboxylate orotate:H⁺ symporter (dctA) genes were chosen as targets in the genome of Escherichia coli HMS174 (DE3) strain. According to recognition roles of TeI3c/4c intron, the fliC489a, fliC828s, fliC1038s and dctA2a sites were chosen as target sites. Gene-targeting plasmids were constructed based on pHK-TT1A by using overlap PCR method and transformed into HMS174 cells. An aliquot mid-log phase cultures of the transformants were shocked at 48 °C and plated on LB plate (containing chloramphenicol). Afterwards, gene mutants were screened by using colony PCR and DNA sequencing. After the mutants were obtained, the phenotypes of ΔfliC and ΔdctA gene mutants were characterized by using agar puncture and carbon metabolism experiments. Colony PCR and sequencing results show that TeI3c/4c intron was inserted in the designed sites of fliC and dctA genes. The gene-targeting efficiency of Thermotargetron system was 100%. Phenotype verification experiments of the mutants demonstrated that the cell motility of all ΔfliC mutants was damaged and the malate assimilation ability of ΔdctA mutant was deprived comparing to wild-type HMS174 strain. In our study, a temperature-inducible and high-efficiency gene inactivation system was established for mesophilic bacteria. This system could achieve high efficiency and precise gene inactivation by modulation of the incubation duration of the transformants at 48 °C.

19.
Article in Chinese | WPRIM | ID: wpr-796600

ABSTRACT

Objective@#To analyze the serotype distribution and antibiotic resistance characteristics of food-borne Salmonella strains isolated from food and patients with gastroenteritis in Guizhou Province from 2016 to 2018.@*Methods@#Serotypes of the strains were characterised using slid agglutination method with Salmonella antisera. Minimal inhibitory concentrations (MIC) of antibiotics were determined by the broth microdilution method. Microsoft Excel 2007 and SPSS18.0 were used for statistical analysis.@*Results@#A total of 170 strains of food-borne Salmonella were detected in food and patients with gastroenteritis in Guizhou Province from 2016 to 2018. Thirty-five serotypes were identified and 6 were found in both food and patients. The main serotypes in food were Salmonella Typhimurium (16.67%) and Salmonella Stanley (8.33%), and the predominant serotypes in patients were Salmonella Typhimurium (41.79%), Salmonella Enteritidis (16.42%) and Salmonella London (8.96%). The rate of resistance to ampicillin, chloramphenicol, tetracycline, ciprofloxacin, nalidixic and trimeth-sulfame were 27.78%-33.33% among the isolates from food, and 22.22%-25.00% to gentamicin, cefocime and ampicillin/sulbatan. Among the isolates from patients, the highest resistance was to ampicillin (55.97%), followed by that to tetracycline (49.25%), ampicillin/sulbatan (44.03%), nalidixic acid (41.04%) and cefazolin (37.31%), and 20.90%-30.60% strains were resistant to chloramphenicol, ciprofloxacin, gentamicin, cefotaxime and ampicillin/sulbatan. There were 25.00% isolates from food and 25.37% isolates from patients resistant to at least 6 antibiotics, and the main multi-resistant pattern was ampicillin-tetracyline-nalidixic-cephalosporin antibiotics (partial).@*Conclusions@#There were many kinds of serotypes of food-borne Salmonella in Guizhou Province from 2016 to 2018 and the predominant types were Salmonella Typhimurium, Salmonella Enteritidis and Salmonella London. Drug resistance was common in the strars and some multidrug resistant strains were detected.

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Article in Chinese | WPRIM | ID: wpr-792031

ABSTRACT

Objective To analyze the serotype distribution and antibiotic resistance characteristics of food-borne Salmonella strains isolated from food and patients with gastroenteritis in Guizhou Province from 2016 to 2018. Methods Serotypes of the strains were characterised using slid agglutination method with Salmonella antisera. Minimal inhibitory concentrations (MIC) of antibiotics were determined by the broth microdilution method. Microsoft Excel 2007 and SPSS18. 0 were used for statistical analysis. Results A to-tal of 170 strains of food-borne Salmonella were detected in food and patients with gastroenteritis in Guizhou Province from 2016 to 2018. Thirty-five serotypes were identified and 6 were found in both food and pa-tients. The main serotypes in food were Salmonella Typhimurium ( 16. 67% ) and Salmonella Stanley (8. 33% ), and the predominant serotypes in patients were Salmonella Typhimurium (41. 79% ), Salmonel-la Enteritidis (16. 42% ) and Salmonella London (8. 96% ). The rate of resistance to ampicillin, chloram-phenicol, tetracycline, ciprofloxacin, nalidixic and trimeth-sulfame were 27. 78% -33. 33% among the iso-lates from food, and 22. 22% -25. 00% to gentamicin, cefocime and ampicillin/ sulbatan. Among the isolates from patients, the highest resistance was to ampicillin ( 55. 97% ), followed by that to tetracycline (49. 25% ), ampicillin/ sulbatan (44. 03% ), nalidixic acid (41. 04% ) and cefazolin (37. 31% ), and 20. 90% -30. 60% strains were resistant to chloramphenicol, ciprofloxacin, gentamicin, cefotaxime and am-picillin/ sulbatan. There were 25. 00% isolates from food and 25. 37% isolates from patients resistant to at least 6 antibiotics, and the main multi-resistant pattern was ampicillin-tetracyline-nalidixic-cephalosporin an-tibiotics (partial). Conclusions There were many kinds of serotypes of food-borne Salmonella in Guizhou Province from 2016 to 2018 and the predominant types were Salmonella Typhimurium, Salmonella Enteritidis and Salmonella London. Drug resistance was common in the strars and some multidrug resistant strains were detected.

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