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OBJECTIVE：To struc turally modify shikimic acid ，and to investigate the reversal effects of its derivatives on paclitaxel-resistant human breast cancer cells MCF- 7/PTX. METHODS ：Using shikimic acid as the lead structure ，1-position carboxyl group was structurally modified to synthesize a series of shikimic acid derivatives through esterification ，amidation， hydrogenation and reduction ，etc. Using non-drug resistant cells MCF- 7 as reference ，MTT assay was used to screen derivatives with inhibitory activity as well as half-inhibitory concentration （IC50）and reversal index （RI）of derivatives to MCF- 7/PTX. With the drug resistance-related transgelin 2 as the target ，the molecular docking of the active derivatives with the drug resistance-related protein was carried out by using Glide 1.0 computer-aided design software. RESULTS ：Totally 15 derivatives were obtained （T1-T15）， of which T 4-T15 were obtained for the first time. MTT assay showed that （3R， 4S， 5R） -N-benzyl-3， 4， 5-trihydroxy-1-cyclohexene-1-formamide（T7），（3R，4S，5R）-N-（3，4，5-trihydroxy-1-cyclohexenylmethyl）-benzylamine（T14）， （3R，4S，5R）-3，4-O-isopropyl-5-O-acetyl-1-cyclohexene-1-methyl formate （T15）inhibited MCF- 7 and MCF- 7/PTX cells to a certain extent ；IC50 values of T 7，T14 and T 15 combined with pacliaxel to MCF- 7/PTX cells were significantly lower than that in negative control （Paclitaxel alone ）group（P＜0.05）. RIs of T 14 and T 15 were higher ，and RIs of the highest dose were 8.8 and 9.3， which were equivalent to positive control verapamil （10.8）. Th e results of molecular docking showed that the hydroxyl groups at positions 3，4 of T 7 could form multiple hydrogen bonds with ； Arg625 and Asp 627 in the catalytic region of transgelin 2. In addition to the hydrogen bond mentioned above at T 7，the mail：batistuta28@126.com secondary amine side chain at position 1 of T 14 could also form hydrogen bond with Glu 657 of transgelin 2. When the hydroxyl group on the T 15 mother nucleus was derived from the donor group ，the binding of the hydroxyl group to transgelin 2 was closer and the inhibition was enhanced. CONCLUSIONS ： The derivatives T 7，T14 and T 15 have certain reverse activity to paclitaxel-resistant human breast cancer cells. The polyhydroxy structure of the mother nucleus is the main structural region of the hydrogen bond between shikimic acid and its derivatives and transgelin 2. The derivation of its power supply group or the introduction of secondary amines and hydrophobic groups into the 1-carboxyl group of shikimic acid is benifit for enhancing the drug resistance reversal effect of derivative .
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OBJECTIVE: To investigate the risk factors and clinical outcome for carbapenems-resistant Pseudomonas aeruginosa (CRPA) infection, and to provide reference for the prevention and treatment of CRPA infection.METHODS: In retrospective investigation, medical records of CRPA and carbapenems-sensitive Pseudomonas aeruginosa (CSPA) infection were collected from our hospital during 2013-2016. CRPA infection risk factors were judged by single factor analysis. The relationship of CRPA risk factors and death was judged by multivariate Logistic regression analysis. RESULTS: A total of 556 cases of P. aeruginosa infection were collected, including 96 cases of CRPA injection, accounting for 17. 3％. Multivariate Logistic regression analysis of related factors of CRPA infection showed that independent risk factors of CRPA infection included admission to ICU for more than 3 days before the isolation of P. aeruginosa [OR= 2. 691, 95％ CI (1. 348, 5. 373), P=0. 005], the use of third-generation or fourth-generation cephalosporin [OR= 0. 386, 95％ CI (0. 200, 0. 742), P=0. 004], complicated with other pathogenic bacteria infection [OR= 1. 892, 95％ CI (1. 132, 3. 164), P=0. 015], combined with 2 kinds of antibiotics or above [OR=5. 631, 95％ CI (2. 556, 12. 407), P=0. 000]. Clinical outcome analysis, mortality rate of CRPA infection were 12. 5％, significantly higher than CSPA infection (2. 8％), Logistic regression analysis, there is a correlation between death rate [OR=5. 003, 95％CI (1. 975, 12. 675), P=0. 001] and CRPA infection. CONCLUSIONS: For the prevention of CRPA nosocomial infection, it is necessary to reduce the time of ICU stay and rationally select antibiotics according to pathogenic bacteria so as to reduce the occurrence of CRPA infection.
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OBJECTIVE:To study risk factors for carbapenem-resistant Acinetobacter baumannii(CRAB)infection,and to provide reference for its clinical prevention. METHODS:In retrospective study,302 A. baumannii(AB)infection patients were collected from our hospital during Dec. 2012 to Jun. 2017. According to the results of drug sensitivity test,those patients were divided into CRAB group(116 cases)and non-CRAB group(186 cases). Risk factors for CRAB infection were analyzed by using univariate analysis. Multivariate Logistic regression analysis was performed for variables with significant difference between 2 groups. RESULTS:Univariate analysis showed that the factors of significant difference in 2 groups including patients suffering from septic shock(P=0.003),sepsis(P=0.000),combined with other infection(P=0.006),diabetes(P=0.029),malignant tumors(P=0.036),patients suffering from infection of other site except for pulmonary infection,intraabdominal infection and skin infection(P=0.009)before AB isolation,patients given carbapenems(P=0.002)and antifungal drugs 28 d before AB isolation(P=0.002). Multivariate Logistic regression analysis showed that the factors of significant difference in 2 groups including patients suffering from sepsis(P=0.033)or diabetes(P=0.011)before AB isolation. CONCLUSIONS:Independent risk factors for CRAB infection include patients suffer from sepsis or diabetes before AB isolation.
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OBJECTIVE:To explore the risk factors for nosocomial infection of multidrug-resistant organism (MDRO) in ICU,and to provide reference for preventing and controlling MDRO in ICU. METHODS:In retrospective study,246 patients with nosocomial infection from ICU of Xi'an Aerospace General Hospital (hereinafter referred to asour hospital) during Jan. 2011-Dec. 2015 were selected and divided into non-MDRO infection group (140 cases) and MDRO infection group (106 cases). The detection and drug resistance of MDRO were analyzed in MDRO group. Univariate analysis and binary Logistic regression anal-ysis were used to explore risk factors for nosocomial infection of MDRO. RESULTS:During 2011-2015,435 strains of MDRO were isolated from 106 MDRO infection patients,in which Gram-negative bacteria accounted for 89.43%,showing severe drug re-sistance. Univariate analysis showed that the following 13 factors were related to nosocomial infection of MDRO,such as ICU ad-mission time,hypoproteinemia,acute cerebrovascular diseases,renal abnormalities,mechanical ventilation time,arterivenous cath-eterization time,urethral catheterization time,indwelling gastric tube time,type and time of using antibiotics,combined use of an-tibiotics,application of carbapenems and the third generation caphalosporins(P<0.05). Binary Logistic regression analysis showed that acute cerebrovascular diseases,type and time of using antibiotics were the independent risk factors for nosocomial infection of MDRO in ICU [odds ratios were 2.816,1.582,1.265,95%CI were (1.540,5.151),(1.085,2.306),(1.131,1.415)]. CONCLU-SIONS:Some prevention and control measures should be taken actively for high-risk MDRO infection patients in ICU to reduce the incidence of nosocomial infection of MDRO and improve the quality of health care.
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Objective According to analyse SCI papers published by hospital faculties during the period of 2010-2015,this paper discussed influential factors and strategies for paper publishing from the perspective of hospital scientific research management,proposed suggestions to administrative department and leaderships for decision making.Methods Taking SCI database developed by Institute for Scientific Information (ISI) as data resource.Literature analysis method was used to analyze the SCI papers during 2010 2015 in terms of publishing amount,subject development,periodical distribution,foundation support,citation analysis,etc.Results The amount of the SCI papers increased sharply each year with a wide spread of extensive subjects which reveals the development of the medical research.However,the average Impact Factor of the paper is still struggling behind that of the top medical institutes.Most papers published in the hospital is supported by National Science Foundation of China (NSFC).Conclusions This paper proposed that the hospital needs to establish a series of policies to strengthen the project management and talent training in the long run,encourage publishing high quality papers to promote the development of disciplines,increasing the investment for constructing research platforms and also making good use of administration for better research.
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Objective:To discuss the risk factors in lung cancer patients with chemotherapy-induced severe neutropenia to provide reference for clinical drug use. Methods:A retrospective analysis was performed for the patients with lung cancer,and the risk factors of severe neutropenia were statistically analyzed and found out. Results:The results of single factor experiments showed that the incidence of severe neutropenia was related with radiotherapy history,cycles of chemotherapy and the use time of granulocyte colony factor. Based on a binary logistic regression analysis,the history of radiotherapy and the use of granulocyte colony factor were the significant risk factors of severe neutropenia in the lung cancer patients. Conclusion:For the patients with radiotherapy history,it is better to choose chemotherapy drugs with lower toxicity,decrease drug dosage or preventively use granulocyte colony factor. The rational use of rhG-CSF can alleviate chemotherapy-induced severe neutropenia.
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OBJECTIVE:To provide reference for the formulation of correct antifungal treatment strategy,and to promote stan-dard use of antifungal agent. METHODS:A retrospective survey was conducted for 138 haematologic patients from May 2013 to May 2014 in a third grade class A hospital,of whom all had used antifungal drugs during hospitalization. We collected all patients' information and analyzed it statistically. RESULTS:Of 138 haematologic patients,3 were proven IFD (all were Candida infec-tion),6 were probable IFD,12 were possible IFD,and 117 were undefined IFD. The positive rates of fungi pathogenic detection, fungal smear,G-test,and GM-test were 15.3%,9.4%,6.4% and 23.4% respectively. 6 kinds of antifungal were used,and vori-conazole had the highest frequency,followed by fluconazole,itraconazole,amphotericin B,caspofungin and micafungin. 62.3%patients used only one kind of antifungal,but 15.9% patients used 2 or more kinds of antifungal. The average medication course was 20.5 days(1 day to 125 days). Irrational drug use showed improper drug selection,unreasonable dose,and replacing antifun-gal with insufficient basis. CONCLUSIONS:The antifungal use in haematologic patients in the hospital is consistent with the re-quirements of guidelines,but there are still some issues as insufficient antifurgal drug treatment course to be further standardized.
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OBJECTIVE:To discuss the risk factors for lung infection of CRAb in ICU,and to provide reference for clinical di-agnosis and treatment. METHODS:The univariate analysis and multivariate Logistic regression analysis were conducted with the method of case-control study,in which the clinical data of 105 cases of lung infection of CRAb in ICU were collected from our hospital during Jun. 2012 to Jun. 2014,with the 81 cases of CRAb and 24 cases of CSAb. RESULTS:The univariate analysis showed that those factors were significantly correlated with lung infection of CRAb in ICU,such as ICU hospitalization days be-fore isolation of Ab,total stay in ICU,respiratory failure,hypoproteinemia,mechanical ventilation,mechanical ventilation days, the application of carbapenem antimicrobial agents and combined use of antimicrobial agents within 15 days before isolation of Ab, abnormal C-reactive protein detection,abnormal procalcitonin detection. The multivariate analysis showed that ICU hospitalization days before isolation of Ab,the application of carbapenem antimicrobial agents within 15 days before isolation of Ab,mechanical ventilation,hypoproteinemia were the independent risk factors of CRAb. CONCLUSIONS:Based on risk factors,the measures should be taken for high-risk patients as soon as possible in ICU to prevent and treat lung infection of CRAb.
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Objective:To establish the determination method for ATP, ADP and AMP in the myocardial tissue of rats and research the changes of ATP, ADP and AMP in heart fallure rats. Methods: A Thermo Hypersil C18 (250 mm × 4. 6 mm,5 μm) column was used. The solution of 0. 68% potassium dihydrogen phosphate and 0. 116% soduim hydroxide was applied as the mobilie phase; The detection wavelength was at 254 nm. The SD rats randomly divided into 2 groups received saline and adriamycin by intraperitoneal in-jection for 6 weeks, respectively. The heart tissue was withdrawn for homogenate. The contents of ATP, ADP and AMP in rat heart tis-sue were determined by HPLC. Results:The calibration curves were linear from 0. 625μg·ml-1 to 40μg·ml-1 for ATP, ADP and AMP. The limit of detection and limit of quantification were 0. 625μg·ml-1(r>0. 99). The precision of RSD was less than 9. 50%. The accuracy was 93. 2%-108. 0%. The method stability (RSD) was from 3. 0% to 14. 0%. The content of ATP in heart fallure mod-el group induced by adriamycin was significantly lower than that in saline group,while that of ADP were much higher than that in saline group(P<0. 01) and AMP. Conclusion:The HPLC method for the content determination of ATP, ADP and AMP in myocardial tissue meets the requirements of the determination of biological samples, which can be used to study the effects of anthracycline-based antitu-mor drugs in heart fallure rats.
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Objective:To analyze the drug use of a patient with intestinal obstruction induced by high dose of morphine to explore the role of clinical pharmacists during the therapeutic process. Methods:The dose titration of morphine, choice of analgesic drugs and dose conversion were adjusted by doctors and pharmacists using NRS scores of dynamic assessment for the patient. The pharmaceutical care was implemented for the patient induced by high dose of morphine. Results:The pharmaceutical supervision by clinical pharma-cists improved medication compliance of the patient. After fentanyl patches were used to replace morphine, the intestinal obstruction was relieved in the patient and the quality of life was improved. Conclusion:Clinical pharmacist can promote the rational use of opi-oids for patients with intestinal obstruction. The successful treatment of the patient with intestinal obstruction provides the reference for patients with intractable pain treated by opioids.
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Objective:To analyze the drug use in a patient with Crohn’ s disease and provide relevant pharmaceutical service by clinical pharmacists. Methods:Clinical pharmacists participated in the treatment of the patient. The medication was analyzed according to the check results and diagnosis and treatment process, and relevant pharmaceutical service was provided for the patient and nurses. Results: Through the participation in the patient treatment and health education for the patient and nurses performed by clinical pharmacists, the patient was recovered and discharged. Conclusion: Clinical pharmacist participating in pharmaceutical service can promote rational drug use in clinics.
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Objective:To improve the logistics management automation in hospital drugstore using internet drug supply chain coor-dination platform. Methods: According to the correspondent relationship between drug information and drug bar code, drug accept-ance, accurate location and batch input were achieved using bar code technique. Results: The platform could not only enhance the efficiency but also ensure the accuracy of drug information input. Conclusion:The platform provides a practical solution for developing modern pharmaceutical logistics and improving the efficiency of pharmaceutical distribution.
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Objective To determine the effects of curcumin microemulsion on proliferation and apoptosis of the human leukemia cell line K562 cells.Methods The curcumin microemulsion was prepared with the routine procedure.MTT assay was used to determine cell proliferation in cultured K562 cells,flow cytometry analysis was applied to examine cell apoptosis,and WT1 mRNA was determined with RT-PCR.The results about curcumin microemulsion were compared with these on curcumin.Results The prepared curcumin microemulsion was a stable clear solution with diameter of 10-100 nm.Curcumin microemulsion inhibited K562 cell proliferation by 24％,46％,68％with a 24 h incubation at dose of 2.5 μg/ml,5.0 μg/ml,and 10.0 μg/ml respectively,whereas curcumin reduced the proliferation by 6％,14％,25％at equal concentrations.WT1 mRNA level of curcumin microemulsion group(0.190±0.036)was reduced stronger than that of curcusin group(0.456±0.047).Conclusions Microemulsion is a great carrier for curcumin.Curcumin microemulsion is more effective in inhibiting proliferation,pro-apoptosis,and reducing WT1 gene expression than curcumin.A strong basis of medical value for the use of curcumin microemulsion to treat tumors is provided.
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Objective: To investigate the absorption and transepithelial transport characteristics of scutellarin and scutellarein in the human colonic adenocarcinoma cell (Caco-2) monolayer model. The influence factors on these two compounds' absorption were investigated, such as buffer solution, duration of culture, and inhibitors of multidrug resistance-associated protein 2 (MRP(2)), breast cancer drug resistance protein (BCRP) and P-glycoprotein (P-gp). Methods: By using Caco-2 monolayer as an intestinal epithelial cell model, the transport process was studied from apical (AP) side to basolateral (BL) side or from BL to AP. The two compounds were determined by high-performance liquid chromatography coupled with diode-array-detector detection. Transport parameters and apparent permeability coeffients (P(app)) were calculated. Results: The P(app) values of scutellarin and scutellarein were different in two buffer solutions, respectively. In phosphate buffered saline, scutellarin had no absorption from AP to BL, while its P(app) value was 0.74×10(-6) to 1.58×10(-6) cm/s from BL to AP. The P(app) values of scutellarein were 4.33×10(-6) to 6.79×10(-6) cm/s and 1.32×10(-6) to 2.56×10(-6) cm/s from AP to BL and from BL to AP, respectively. The P(app) value gradually decreased with time. The absorption of scutellarein was better than that of scutellarin. The scutellarin absorption was improved by verapamil, MK-571 and reserpine. The scutellarein absorption was improved by verapamil whereas its excretion was improved by MK-571. Conclusion: Absorption of scutellarin is difficult in Caco-2 monolayer cells, which contributes to its low bioavailability. Scutellarein absorption is better than scutellarin absorption. Scutellarein transepithelial transport is passive diffusion. The inhibitor of P-gp can improve scutellarin and scutellarein transportation. The inhibitors of MRP(2) and BCRP can promote transportation of scutellarin. The inhibitor of MRP(2) can promote efflux of scutellarein. The multidrug resistance-associated protein may be the second reason for low bioavailability of scutellarin.
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OBJECTIVE:To investigate the characteristics of pharmaceutical care for critical patients with multi-drug resistant Acinetobacter baumanni infection.METHODS:Retrospective analysis was applied to analyze the distribution of pathogenic bacteria,drug resistance,therapeutic results and pharmaceutical care in 36 critical patients with multi-drug resistant Acinetobacter baumanni infection.RESULTS:Multi-drug resistant Acinetobacter baumannii had severe drug resistance to antibiotics.It is difficult for critical patients to treat Acinetobacter baumannii infection after infection.CONCLUSION:Clinical pharmacist should be engage in clinical practice,give full play to their clinical expertise and enhance pharmaceutical care.It is very important for prevention of multi-drug resistant strains and appropriate use of drugs that clinical pharmacist be involved in formulating therapeutic regimes for multi-drug resistant Acinetobacter baumannii infection and strengthen pharmaceutical care.
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OBJECTIVE: To study the effect of taspine hydrochloride (TA/HCl) on skin wound healing in rats and its mechanism. METHODS: Bilateral round wounds were made on the backs of SD rats. The effect of TA/HCl on the skin wound was evaluated through determining closure time and contracting ability of the skin wound, observing histopathological characteristics and measuring contents of hydroxyproline (Hyp) and protein in the wound tissue. RESULTS: The closure time of the skin wounds was significantly shorter in the TA/HCl-treated groups than that in the model group. The percentages of wound contraction were higher in the TA/HCl-treated groups than that in the dimethyl sulfoxide (DMSO) control group of the same group (P<0.05 or P<0.01) on the 3rd to 14th days after wounding. The content of the protein in the wound tissue in the TA/HCl-treated group (2 mg/ml) was higher than that in the model group (P<0.05) on the 3rd to 7th days after wounding, and it arrived at the peak on the 7th day and gradually decreased to the normal level in skin tissue on the 14th to 21st days after wounding. The contents of Hyp in the wound tissues in the TA/HCl-treated groups were higher than that in the model group (P<0.05 or P<0.015) on the 3rd to 21st days after wounding, and they arrived at the peak on the 14th day and at the normal level in skin tissue on the 21st day. Histopathological test results showed that TA/HCl could promote the formation of newly born capillaries in the early period of the wound healing. CONCLUSION: TA/HCl has the ability of promoting skin wound healing in rats, and it can also accelerate the growth of newly born capillaries and raise the production of protein and collagen in wound tissue.
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Objective To study the effect and mechanism of taspine on wound healing and fibroblast proliferation. Methods The effect of taspine on skin wound was observed in vivo. The different concentration of taspine hydrochloride was added to L929 fibroblast cultivated in vitro, and lactate dehydrogenase was detected and MTT method was applied to observe effect of taspine on fibroblast proliferation. Results The local application of taspine 3 mg/Ml and 1.5 mg/mL accelerated the healing of skin wounded. In vitro, 0.01～0.5 μg/mL of taspine hydrochloride showed no effect on the change of lactate dehydrogenase activity and fibroblast proliferation. Conclusion Taspine is a kind of active alkaloid from leontice robustum which can enhance wound healing, its mechanism on wound healing is not by means of accelerating the proliferation of fibroblast, other mechanisms are necessary for being further studied.
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Objective To establish a high-performance liquid chromatography method for determination of mycophenolic acid in human plasma.Methods The method was performed with C18 column(3.9mm?300mm).The mobile phase consisted of 40mmoL/L TBA solution-acetonitrile adjusted to pH 4 with orthophosphoric acid(55∶45,V∶V),with a flow rate 0.8mL/min.The UV detection wavelength was 254nm.Plasma samples were extracted with methanol.Results The linear concentration of the calibration curve ranged from 0.8 to 51.45mg/L(r=0.9998).The relative recoveries were between 95.5% and 109.2%,and the extraction recoveries were more than 90%.Relative standard deviation(RSD) of intraday and interday assays were both less than 10%.Conclusion The method is proved to be reliable and simple for monitoring mycophenolic acid in human plasma and bioequivalence research.
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OBJECTIVE:To compare the pharmacoeconomic effectiveness of three antiviral agents for herpes zoster ME_THODS:101 patients with herpes zoster were divided into three groups who received acyclovir injection,valaciclovir tablet and ribavirin injection,respectively Evaluation was carried out with cost-effectiveness analysis RESULTS:The cost-effectiveness ratios of three groups were $1 288 2,$863 0 and $949 8 CONCLUSION:Valaciclovir was the best antiviral agents for herpes zoster
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OBJECTIVE:To optimize the formulation and preparation technic of azathioprine liposomes and evaluation the quality.METHODS:The liposomes were prepared by a film-vibration technique.The optimal formulation and preparation technic were selected by means of an orthogonal design test.The entrapment ratio of liposomes was studied by titrimetric method.The size distribution and appearance of liposomes were observed under microscope.RESULTS:The entrapment ratio of azathioprine liposomes was49.19%.The liposomes consisted of spherical or similar to spherical multilamellar vesicles with78.17%of particles in the liposomes smaller than2.4?m.CONCLUSION:The selected formulation and preparation technic of azathioprine liposomes are rational and stable.