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@#Nosiheptide is a typical thiopeptide antibiotic displaying potent activity toward various drug-resistant strains of Gram-positive pathogens.Although nosiheptide lacks in vivo activity, and good water-solubility with a series of uncontrollable analogues, which may limit its clinical application, glycosylated analogues may overcome problem of low activity and may improve its druggability.In search of novel glycosylated nosiheptide producers, we applied a genome mining strategy that identified Actinoalloteichus sp.AHMU CJ021 that contains all genes required.However, despite the presence of a predicted glycosyltransferase, glycosylated derivatives of nosiheptide were not detected, after following one strain many compounds (OSMAC) strategy and heterologous expression of a regulatory protein NocP.Nevertheless, nosiheptide produced by this strain was remarkably pure, and further experiments were conducted to improve its production by optimization of the culture medium.Under optimal conditions, 58.73 mg/L nosiheptide was produced, representing an almost 6-fold improvement compared to the original fermentation medium.Therefore, we consider Actinoalloteichus sp.AHMU CJ021 a suitable potential candidate for industrial production of nosiheptide, which provides the basis for solving the problem of nosiheptide structural analogues.
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Objective To provide data reference for improving the selection criteria of the dosage forms and specifications of the electrolytes and antipyretic analgesics in the Essential Medicines List, and to improve the applicability of these medicines to children and the availability of essential medicines. Methods The market and prices of electrolytes and antipyretic analgesics were retrieved by the system. The data were processed by Excel software, and the different dosage forms were compared and analyzed. Results 8 medication classes were included for adjusting water, electrolytes and acid-base balance, and another 16 classes were analgesic, antipyretic, anti-inflammatory, anti-rheumatic and anti-gout drugs. Those medications were characterized with many registered approval numbers, manufacturers and some considerations for pediatric uses. The proper prices were given for different dosage forms and specifications. There is a room for improvement regarding the specifications of potassium, glucose injections, and acetaminophen preparations. Conclusion The selection of pharmaceutical dosage forms and specifications in the Essential Medicines List should be comprehensively evaluated from the registered approval numbers of base medicines, the manufacturers and related prices in pharmaceutical procurement platforms from various provinces, and the clinical needs for special populations. It is recommended that 10 ml: 1 g potassium chloride injection, 50 ml glucose injection，acetaminophen suppositories and drops were included in the Essential Medicines List.
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OBJECTIVE：To compare the similarities and differences of antiepileptic drugs between 2019 edition of WHO Model List of Essential Medicines for Children （called“WHO-EMLc”for short ）and 2018 edition of the National Essential Medicines List （called“NEML”for short ），and to provide reference for the improvement of national essential medicines list and formulation of essential medicines list for children. METHODS ：By means of descriptive analysis ，the differences in the varieties ， dosage forms ，specifications and marker symbols of antiepileptic drugs were compared between WHO-EMLc and NEML. The marketing status of antiepileptic drugs included in WHO-EMLc and NEML were analyzed statistically. RESULTS & CONCLUSIONS：There were 9 kinds of antiepileptic drugs included in WHO-EMLc ，all of which were under the category of anticonvulsant/antiepileptic drugs. There were 6 kinds of antiepileptic drugs in NEML of China ，and the other three kinds of drugs included in WHO-EMLc were included in the category of psychotherapy drugs in NEML. Eight kinds of antiepileptic 126 drugs were shared by NEML and WHO-EMLc ， namely 109614043@qq.com carbamazepine， valproic acid ， phenytoin sodium ， pheno- barbital，lamotrigine，diazepam，lorazepam and midazolam. The special antiepileptic drug in NEML was ocazepine ，and edu.cn the special antiepileptic drug in WHO-EMLC was ethylsu c- cinate. Oral dosage forms involved in WHO-EMLc included oral solution ，ordinary tablet，enteric-coated tablet ，dispersed tablet ， etc.，while oral dosage forms involved in NEML included ordinary tablet ，dispersed tablet and oral solution. In terms of dosage form of a single drug ，the drug specifications in WHO-EMLc were more comprehensive than those in NEML. In WHO-EMLc ， lorazepam was labeled with “□”，indicating that it was more effective and safe in similar drugs . Lamotrigine ，midazolam injection and phenytoin （25 mg∶5 mL and 30 mg∶5 mL）were labeled with “*”，indicating that there were special precautions for the drug or dosage form and specification. In NEML ，diazepam was marked with “*”，and diazepam injection was marked with “△”， indicating that diazepam appeared repeatedly under different classifications ；diazepam injection should be used under the guidance of doctors with corresponding prescription qualifications or under the guidance of specialists ，and the use monitoring and efficacy evaluation should be strengthened. In addition ，most of the antiepileptic drugs included in WHO-EMLc had been marketed in China，but the dosage forms on the market were relatively simple ，which could not meet the drug demand of children. Our country could learn from WHO-EMLc selection method to further improve the national essential medicine list ，formulate essential medicine list for children which was suitable for Chinese national conditionsas soon as possible on the basis of disease spectrum and drug clinical comprehensive evaluation. At the same time ，the government should also encourage the development and production of children’s medicines to ensure that children fairly access to drugs.
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Objective@#To investigate the clinicopathologic features and possible causes of granulomatous lobular mastitis(GLM).@*Methods@#Three hundred cases of GLM were collected from surgical specimens diagnosed at Longhua Hospital, Shanghai University of Traditional Chinese Medicine from January 2015 to November 2017. Morphologic features were reviewed using HE staining. A total of 116 cases were investigated by Gram staining. The expression of CD3, CD20, CD68, IgG, IgG4, CD38 and CD138 was detected by immunohistochemical staining.@*Results@#The age of the patients was 23 to 47 years and the median age was 32 years. All patients were female, 96.7% (290/300) had a history of lactation.There were 143 cases of left breasts, 138 cases of right breast and 19 cases of bilateral breasts. Serum prolactin increased in 39.7%(119/300) patients. Within 15.7%(47/300) of patients were associated with nodular erythema or joint swelling and pain of the lower extremities. Pathological observation showed that lobular-centric suppurative granulomatous inflammation, accompanied by dilatation of intralobular and interlobular ducts. There were 16 cases accompanied with duct ectasia. Immunohistochemistry showed CD3-positive lymphocytes were more than CD20-positive lymphocytes in the peripheral aggregation zone of neutrophils within granulomatous lesions. Gram positive bacteria were found in the lipid vacuoles of the 51.7%(60/116) patients.@*Conclusions@#GLM has distinctive histologic features. It may be related to corynebacterium infection, or accompanied by the increase of serum prolactin and erythrocyte sedimentation rate. The age, location and history of the disease are importance in the diagnosis and differential diagnosis.
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Objective@#To estimate future excess mortality attributable to cold spells in Guangzhou, China.@*Methods@#We collected the mortality data and metrological data from 2009-2013 of Guangzhou to calculated the association between cold spell days and non-accidental mortality with GLM model. Then we projected future daily average temperatures (2020-2039 (2020s) , 2050-2069 (2050s) , 2080-2099 (2080s) ) with 5 GCMs models and 2 RCPs (RCP4.5 and RCP8.5) to identify cold spell days. The baseline period was the 1980s (1980-1999). Finally, calculated the yearly cold spells related excess death of 1980s, 2020s, 2050s, and 2080s with average daily death count of non-cold spell days, exposure-response relationship, and yearly number of cold spell days.@*Results@#The average of daily non-accidental mortality in Guangzhou from 2009 to 2013 was 96, and the average of daily average was 22.0 ℃. Cold spell days were associated with 3.3% (95%CI: 0.4%-6.2%) increase in non-accidental mortality. In 1980s, yearly cold spells related deaths were 34 (95%CI: 4-64). In 2020s, the number will increase by 0-10; in 2050s, the number will increase by 1-9; and in 2080s, will increase by 1-9 under the RCP4.5 scenario. In 2020s, the number will increase by 0-9; in 2050s, the number will increase by 1-6; and in 2080s, will increase by 0-11 under the RCP8.5 scenario.@*Conclusion@#The cold spells related non-accidental deaths in Guangzhou will increase in future under climate change.
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Objective@#To understand the correlation between ambient ozone (O3) and premature birth in Taiyuan.@*Methods@#The data of O3 daily average concentrations and maximum concentration of 8 hours, PM2.5 daily average concentrations, meteorological factors (including the average temperature and relative humidity) and daily premature birth numbers during 2013-2015 were collected in Taiyuan from China National Environmental Monitoring Center and China Meteorological Administration. The models were developed by using generalized linear model. The gender of the premature birth was analyzed by subgroup analysis. Sensitive analysis were used to estimate the model stability.@*Results@#Ambient O3 daily average concentrations and maximum concentration of 8 hours in Taiyuan of 2013 to 2015 were 45.35 μg/m3 and 71.33 μg/m3 respectively. In single pollutant model, the effects of different window exposures on premature birth were different. The RR of preterm birth about an increase of 10 μg/m3 of O3 (lag 3 weeks, lag 4 weeks) were 1.090 (95%CI: 1.042-1.139), 1.095 (95%CI: 1.032-1.163) respectively. According to the infant gender subgroup analysis, male infants were more likely to be affected by ambient O3. The average daily of O3 concentration increased by 10 μg/m3, and the RR for male infants and female infant were 1.013 (95%CI: 0.997-1.029), 0.996 (95%CI: 0.983-1.010) respectively. By comparing the daily average concentration of O3 with the maximum daily concentration of O3 for 8 hours as an indicator of exposure, it was found that the daily average concentration of O3 was more sensitive. The RR of preterm birth about an increase of 10 μg/m3 of average daily of O3 concentration and the maximum daily concentration of O3 for 8 hours. were 1.006 (95%CI: 0.994-1.017) and 0.997 (95%CI: 0.988-1.005) respectively. As for sensitive analysis, when O3 introduced PM2.5 or change the degree of model variables, the association of premature birth was still constant.@*Conclusion@#Prenatal exposure to O3 may increase the risk of premature birth, with different window exposures premature births have different risks and this risk is more pronounced in male infants.
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Objective To investigate the correlation between Framingham stroke risk profile(FSRP) and vascular cognitive impairment in stroke-free patients with cerebrovascular risk factors.Methods One hundred and eighty-four stroke-free subjects,selected from Zhejiang hospital,were divided into low risk group (56 subjects),moderate risk group (70 subjects) and high risk group (58 subjects) according to their FSRP score,and their cognitive function including memory ability,attention,executive function and language ability were assessed by Montreal cognitive assessment (MoCA),auditory verbal learning test (AVLT),digit symbol test,trail making test(TMT),digit span and verbal fluency test.Results The total MoCA scores which were (7.2±4.6),(13.8±3.9),(29.6± 12.7) respectively,AVLT-delay recall scores which were(8.2± 1.6),(6.7± 1.4),(5.9± 1.5) respectively,and digit symbol test score which were(34.7±9.3),(32.6± 16.4),(29.7± 13.6) respectively in low,intermediate and high risk groups,decreased with the increasing risk of stroke(P＜0.05).The elapsed time in TMT-B which were (115.2 ±36.9) s,(147.6±44.8) s,(173.9±58.5) s respectively in low,intermediate and high risk groups,prolonged with the increasing risk of stroke (P＜0.05).FSRP was associated with cognitive function,but inversely related to MoCA,AVLT-delay recall,digit symbol test,TMT-B and digit span fall back (P＜0.05),but positively related to consuming time in TMT-B (P＜ 0.05).Multivariate regression analysis showed that advanced age,hypertension,diabetes and smoking were the risk factors for vascular cognitive impairment(P＜0.05).Conclusion Advanced age,smoking,hypertension and diabetes are the most important in vascular risk factors for cognitive impairment.Vascular risk factors can damage cognitive function with the increased risk of stroke,among which delayed recall and executive function are the main affected cognitive area.
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To investigate the anti-inflammatory, anti-oxidative stress, and adipokine-ameliorating effects of Liuwei Dihuang (LWDH), a traditional Chinese herbal formula, in obese rats.
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<p><b>OBJECTIVE</b>To investigate the anti-inflammatory, anti-oxidative stress, and adipokine-ameliorating effects of Liuwei Dihuang (LWDH), a traditional Chinese herbal formula, in obese rats.</p><p><b>METHODS</b>After 2 weeks of acclimation with free access to regular rodent chow and water, obese-prone-caesarean-derived (OP-CD) rats were fed a modified AIN-93G diet containing 60% energy from fat. Treatment was performed twice daily by gavage feeding with 500, 1 500, or 3 500 mg/kg body weight LWDH suspended in water (n=12 rats per group). Twelve obese-resistant-CD (OR-CD) rats were fed the atherogenic diet and gavaged with water, and served as the normal control. Blood biomarkers of inflammation, oxidative stress and adiponectin were measured post-sacrifice and used to determine the treatment effect of LWDH and assess the suitability of OR/OP-CD rats for studying these parameters.</p><p><b>RESULTS</b>After 9 weeks of treatment, LWDH lowered serum C-reactive protein (CRP) and tumour necrosis factor-α (TNF-α) levels. Serum interleukin-6 (IL-6) levels showed a tendency towards reduction, but were not significantly different from the OP-CD control. Liver superoxide dismutase (SOD) activity was increased in response to all three doses of LWDH, while the levels of reduced (GSH) and oxidized glutathione (GSSG) and thiobarbituric acid reactive substances (TBARS) were unchanged. Serum adiponectin levels were increased in response to oral administration of LWDH at the dose of either 500 or 1 500 mg/kg body weight. In addition, comparisons between OR-CD and OP-CD rats revealed differential, and for some biomarkers, conflicting characteristics of high-fat diet-fed OP-CD rats in reference to obese human subjects in terms of inflammatory and oxidative stress biomarkers and circulating adiponectin levels.</p><p><b>CONCLUSION</b>The results show, for the first time, the anti-inflammatory, anti-oxidative stress and adiponectin-ameliorating effects of LWDH in obese rats. The suitability of the OR/OP-CD rat model as a research tool to study inflammation, oxidative stress, and adipokine production requires further investigation.</p>
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Animaux , Mâle , Rats , Adiponectine , Sang , Protéine C-réactive , Maladie chronique , Médicaments issus de plantes chinoises , Pharmacologie , Glutathion , Métabolisme , Inflammation , Traitement médicamenteux , Interleukine-6 , Sang , Obésité , Stress oxydatifRésumé
The present study was conducted to develop new inhibitors of pancreatic lipase and alpha-glucosidase from Chinese dietary herbs. Sixty-three dietary herbs from 39 taxonomic families were selected and extracted with aqueous ethanol or water. The extracts were then tested with in vitro enzyme assays for their ability to inhibit pancreatic lipase and alpha-glucosidase activities. Orlistat and acarbose were used as two positive controls. The extracts of Nelumbo nucifera, Curcuma longa, Piper longum and Morus alba showed strong pancreatic lipase inhibitory effects with IC50 at (28.00 +/- 5.51), (5.24 +/- 0.51), (14.76 +/- 2.58), (4.78 +/- 0.58), (3.41 +/- 0.67) mg x L(-1), respectively. These extracts also showed potent alpha-glucosidase inhibitory activities with IC50 at (1.98 +/- 0.13), (0. 18 + 0.007), (0.71 +/- 0.08), (0.077 +/- 0.005), (0.089 +/- 0.006) g x L(-1), respectively. The results provide useful information for developing new drugs or natural health products for hyperlipidemia and hypoglycemia from Chinese dietary herbs.
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Curcuma , Chimie , Médicaments issus de plantes chinoises , Chimie , Pharmacologie , Antienzymes , Chimie , Pharmacologie , Triacylglycerol lipase , Morus , Chimie , Nelumbo , Chimie , Pancréas , Piper , Chimie , Extraits de plantes , Chimie , Pharmacologie , alpha-Glucosidase , MétabolismeRésumé
Objective To evaluate the efficacy of pressure bladder indicator in guiding epidural puncture.Methods Test Ⅰ Thirty-two patients scheduled for epidural puncture were studied. After successful epidural puncture, the end of the epidural needle was connected to a pressure sensor to measure the epidural space pressure. Test Ⅱ Seventy patients scheduled for epidural puncture were studied. The epidural puncture was performed using the pressure bladder indicator. The successful condition of the pressure bladder indicator in guiding epidural puncture was recorded. Results The epidural space pressure was ( 10 ± 4) cm H2O. Seventy patients completed epidural pucture under the guidance of the pressure bladder indicator. The success rate was 100%.Conclusion The pressure bladder indicator can serve as an assistance for epidural puncture and has clinical application value.
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<p><b>BACKGROUND AND OBJECTIVE</b>The aim of this study is to determine the short-term efficacy, toxicity and the rate of life-quality improvement of BSD2000 deep hyperthermia combined with chemotherapy of PT regimen in patients with non-small cell lung cancer (NSCLC) by comparation with PT regimen alone.</p><p><b>METHODS</b>Sixty patients with NSCLC were randomly divided into the treatment group and control group, with 30 each. The treatment group was treated with chemotherapy (paclitaxel: 135 mg/m2 ivdirp 3 h qd d1+cisplatin: 20 mg/m2 ivdirp qd d1-5) in combination with BSD2000 deep hyperthermia, and hyperthermia was positioned precisely and maintained for 60 min (2 times a cycle: d1, 4 after the end of chemotherapy within two hours). The control group was treated with chemotherapy alone. Treatment response in both groups were evaluated as well as side-effects after 3 cycles. By observing the results, comparing response rate, toxic side effects and quality of life improvement rate in two groups.</p><p><b>RESULTS</b>The efficiency and the rate of life-quality improvement in the treatment group were 63.33%, 76.67% respectively, and 36.67%, 40.00% in the control group respectively. There were significant differences between two groups (P < 0.05). The main side-effects were myelosuppression and gastrointestinal reactions, no significant difference between two groups (P > 0.05).</p><p><b>CONCLUSION</b>BSD2000 deep hyperthermia combined with chemotherapy in patients with NSCLC can significantly increase the efficacy, response rate and quality of life improvement and without increasing side-effects compared to chemotherapy alone.</p>