1.Effect of Pingfei Oral Liquid on the Distribution of Mast Cells and Expression of IL-6 in Radiation Pneumonia Rats
Xuan LIU ; Lin PAN ; Hong LI ; Bo XU ; Yaoying JIN ; Jing JIA ; Peiwen LI ; Zhiqiang CHENG
Traditional Chinese Drug Research & Clinical Pharmacology 2009;20(4):303-308
Objective To investigate the effect of Pingfei Oral Liquid (POL) on the distribution of mast cells (MCs) and the expression of interleukin 6 (IL-6) in the lung tissue of radiation pneumonia rats. MethodsForty-five SD rats were randomized into 3 groups : normal control,model group and POL group. The rat model of radiation lung fibro-sis was set up by a single X-ray dose of 20Gy irradiation over the whole chest of the rats. POL (20 g·kg-1·d-1,once a day, five times a week) was given orally one week before irradiation and the treatment lasted 5 weeks. MCs in the lung tissue were stained with toluidine blue firstly and then were counted 2, 4 and 8 weeks after irradiation. IL-6 protein expression of lung tissue was measured by immunohistochemical assay 8 weeks after irradiation, and mRNA ex-pression was determined with RT-PCR 4 weeks after irradiation. ResultsIt's showed the aggregation of large amount of pulmonary mast cells and increase of IL-6 protein expression 8 weeks after irradiation (P < 0.01).IL-6 mRNA expression in the irradiated lung of rats increased 4 weeks after irradiation (P < 0. 01). POL could reduce the aggrega- tion of MCs (P < 0. 01) and the expression of IL-6 protein (P < 0. 01) and mRNA (P < 0. 05) in the lung tissue. ConclusionPOL can prevent radiation pneumonia in rats by reducing the aggregation of mast cells and inhibiting IL-6 expression in the lung tissue.
2.The levels of angiopoietin-2 in patients with acute respiratory distress syndrome and its value on prognosis
Mingmei ZHONG ; Lin ZHANG ; Fan WANG ; Song PENG ; Jin ZHANG ; Guoping XUAN
Chinese Critical Care Medicine 2014;(11):804-809
Objective To approach the correlation between angiopoietin-2 (Ang-2) levels and degree of lung injury and prognosis and its clinical significance in patients with acute respiratory distress syndrome (ARDS). Methods A prospective observation was conducted. Fifty-three ARDS patients admitted to Department of Critical Care Medicine of Third Affiliated Hospital of Anhui Medical University from January 2012 to March 2014 were enrolled. According to the criteria of the Berlin Definition of ARDS,the patients were divided into mild group (n=15),moderate group(n=22)and severe group(n=16). Meanwhile,ARDS patients were further divided into survival group(n=29)and non-survival group(n=24)according to 28-day outcomes. Twenty cases of non-ARDS patients were served as control. The acute physiology and chronic health evaluationⅡ(APACHEⅡ)score,sequential organ failure assessment(SOFA)score,oxygenation index(PaO2/FiO2),lung injury score(LIS)were recorded within 24 hours after admission. And the plasma levels of Ang-2,interleukin-6(IL-6)and C-reaction protein (CRP)were measured. The independent risk factors of ARDS were analyzed by univariate and multivariable logistic regression. Receiver operating characteristic curve(ROC)was plotted to evaluate the value of Ang-2 in predicting ARDS. Results Compared with non-ARDS group,APACHEⅡ score,SOFA score,LIS score,mortality were significantly increased,PaO2/FiO2 was significantly decreased,and plasma Ang-2,IL-6,CRP were significantly elevated〔APACHEⅡscore:20.7±5.0 vs. 14.1±5.3,SOFA score:7.7±3.5 vs. 3.5±2.1,LIS score:1.69±0.71 vs. 0.28±0.27,PaO2/FiO2(mmHg,1 mmHg=0.133 kPa):159.5±61.3 vs. 394.0±63.2,mortality:45.3%(24/53) vs. 20.0%(4/20),Ang-2(μg/L):4.73(2.59,6.99)vs. 1.22(0.61,1.52),IL-6(ng/L):56.50(27.15,139.90)vs. 13.05(4.38,15.55),CRP(mg/L):95.75(41.74,189.72)vs. 10.56(3.92,21.36),P<0.05 or P<0.01〕. Each index increased or decreased more significantly with the aggravation of the disease. It was shown by correlation analysis that the plasma levels of Ang-2 was significantly positive correlated with IL-6(r=0.468,P=0.000),CRP(r=0.492,P=0.000),APACHEⅡscore(r=0.560,P=0.000),SOFA score(r=0.508,P=0.000)and LIS score (r=0.588,P=0.000),significantly negatively correlated with PaO2/FiO2(r=-0.685,P=0.000). Factors, APACHEⅡ score,LIS score,PaO2/FiO2,Ang-2 and IL-6 founded statistical significance in univariate analysis were analyzed using multivariable logistic regression. High APACHEⅡscore at admission〔odds ratio(OR)=1.316, 95% confidence interval(95%CI)=1.040-1.633,P=0.022〕and increased plasma Ang-2 levels(OR=1.287, 95%CI=1.041-1.760,P=0.038)were the independent prognostic factors for the 28-day mortality in ARDS. The area under the ROC curve of Ang-2 was 0.964,the optimal critical value of Ang-2 was 1.79μg/L,the specificity was 90.0%,and sensitivity was 92.5%. Plasma levels of Ang-2 was better in predicting ARDS than APACHEⅡscore, SOFA score and IL-6. Conclusions The plasma level of Ang-2 was significantly increased in patients with ARDS. The plasma level of Ang-2 was correlated with the severity of acute lung injury and had important prognosis evaluation.
3.Experiences of sentinel lymph node biopsy in breast cancer
Baoning ZHANG ; Lixue XUAN ; Tao ZHANG ; Zhongzhao WANG ; Guoji CHEN ; Jin YI ; Lin LIU ; Shengzu CHEN
Chinese Journal of General Surgery 2000;0(11):-
Objective To evaluate the feasibility of sentinel lymph node biopsy(SLNB)during surgery of breast cancer. MethodsRadioactive colloid and blue dye were injected intradermally around the tumor seperately before the operation and the SLN were detected first by lymph scintigraphy. SLN was detected and located using ?-finder and the blue dye. Axillary lymph node dissection(ALND)was performed routinely after the SLNB. Results Among 116 breast cancer patients,this procedure was successful in 98.3% of cases. The sensitivity, accuracy and false negative rate were 93.6%, 97.4% and 6.4%, respectively. Conclusions SLNB is a simple, safe and reliable technique.Routine ALND could be raplaced by SLNB in breast cancer patients undergoing surgery.
4.Direct inhibitory effects of 153Sm-DTPA-c(CGRRAGGSC) on human prostate cancer PC-3 cells
Qing-hua, WU ; Lu, LIU ; Ze-xuan, YANG ; Hai-lin, GAO ; Jin, SUN ; Qi, NIE
Chinese Journal of Nuclear Medicine 2011;31(4):241-244
Objective To investigate the direct inhibitory effects of 153Sm- DTPA-c (Cys-Gly-Arg-Arg-Ala-Gly-Gly-Ser-Cys) NH2 ( 153 Sm-DTPA-c (CGRRAGGSC)) on human prostate cancer PC-3 cells. Methods 153Sm-DTPA-c(CGRRAGGSC) was synthesized by the reaction of 153SmCl3 with DTPA-c(CGRRAGGSC) using indirect synthesis method. PC-3 cells in vitro culture were divided into four study groups, groug A ( the control, with PBS only), group B with 1.5 mg/L c ( CGRRAGGSC), group C with 370 kBq 153 SmCl3 and group D with 370 kBq 153Sm-DTPA-c(CGRRAGGSC). PC-3 cell growth was assayed by 3-(4, 5-dimethylthiazol-2-yl ) -2, 5-diphenyltetrazolium bromide (MTT) method. Cell cycle and apoptosis were analyzed by flow cytometry. The expression changes of interleukin 11 (IL11 ) and IL11 receptor (IL1 1 R) in PC-3 cells were examined by Western Blot. One way analysis of variance (ANOVA) and paired-t test were applied for statistic analysis. Results The labeling yield of 153Sm-DTPA-c (CGRRAGGSC) was 85% and the radiochemical purity was 95.8%. The specific activity of 153Sm-DTPA-c(CGRRAGGSC) was 1.32 × 105 MBq/μmol. Significant inhibitory effects on the growth of PC-3 cells were found in both group C and D, with a time-dependent manner. However, no obvious inhibition was found either in group A or in group B. After 48 h,significant differences of sub-G1 peak area were found among groups, (0. 98 ± 0. 18)%, (0. 35 ±0. 10)%, (4.05 ±0.28)% and (13.38 ±0. 89)% for group A, B, C and D, respectively. Furthermore,sexpression of ILl 1R in group D was significantly lower than that in group B and C with absorbance values 0. 339 ~ 0.014, 0.338 ~ 0.019, 0.226 ~ 0. 015 for group B, C and D, respectively. Absorbance values in groups B and C were not significantly different after treatment, compared with those before treatment; however, there was difference between absorbance values after and before treatment in group D ( t = 0. 405,1. 163,135.989,P>0.05 >0.05, <0.05). Conchluion 153Sm-DTPA-c(CGRRAGGSC) can directly in hibit the cell growth and expression of human prostate cancer cells PC-3.
5.Preparation and in vitro embolic efficiency evaluation of hydroxycamptothecine-loaded liquid embolic agent.
Ling-Zhen QIN ; Xuan ZHANG ; Lin-Na WU ; Jin ZHANG ; Xin PAN ; Ge LI ; Chuan-Bin WU
Acta Pharmaceutica Sinica 2014;49(7):1069-1075
The purpose of this study is to investigate the preparation of hydroxycamptothecine (HCPT)-loaded cubic crystal liquid embolic precursor solution, and evaluate its in vitro embolic efficiency. Phytantriol was used as cubic crystal liquid embolic material, and the optimal formulation was selected according to ternary phase diagram. Polarized light microscopy, differential scanning calorimetry, and small angle X-ray scattering (SAXS) were used to characterize the cubic crystal structure. High performance liquid chromatography and X-ray diffraction analysis were used to investigate the lactone ring of HCPT. In vitro dissolution was preliminary evaluated, and the simulation embolic model was constructed to evaluate the embolic efficiency of precursor solution. Meanwhile, the gelation time and adhesion force were investigated. The results showed that HCPT-loaded precursor solution for embolization had been successfully prepared with low viscosity which was injectable. The precursor solution could transform into Pn3m structure liquid crystal phase gel rapidly when contracting with excess water. The formed HPCT gel remained its lactone form as the same in precursor solution, and expressed the good ability to block the saline flow, and HCPT could keep sustained releasing drug over 30 days. The prepared drug-loaded embolic precursor solution showed a promising potential for vascular embolization and application in clinical treatment of tumor.
Antineoplastic Agents, Phytogenic
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chemistry
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Calorimetry, Differential Scanning
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Camptothecin
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analogs & derivatives
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chemistry
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Delayed-Action Preparations
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chemistry
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Fatty Alcohols
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chemistry
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Liquid Crystals
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Scattering, Small Angle
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Water
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X-Ray Diffraction
6.Effects and Safety of Hemoperfusion Therapy on Infants with Tetramine Poisoning
de-xuan, WANG ; rui-xia, LIN ; qing, YANG ; guo-quan, PAN ; chun-xue, YAN ; ling-wei, JIN
Journal of Applied Clinical Pediatrics 1992;0(06):-
Objective To explore the effects and safety of hemoperfusion(HP) therapy on tetramine poisoning in infants.Methods Thirty-five infants with tetramine poisoning were divided into two groups: HP group(n=18) and non HP group(n=17).The changes of blood tetramine concentration and clinical symptom improving of both groups after the treatment were observed together with the adverse effects of HP group.Results The average blood tetramine concentration of HP group was higher than that of non HP group(342.2?333.4 vs 117.9?50.8 ?g/L,P
7.Label-free target discovery technology of small molecule drug and its application in traditional Chinese medicines
Yuan-yuan LIN ; Jin-hao YU ; Hua-qiu LU ; Xuan CHEN ; Ning-bo CHEN ; Jian-liang ZHOU
Acta Pharmaceutica Sinica 2023;58(5):1117-1127
The discovery of drug targets plays a crucial role in drug research. Accurate information of small molecule drug-protein interaction can be provided by label-free target discovery technology without any structural modification at the small molecule. So, the label-free drug target discovery technology had become the powerful tool to discover the targets of drugs. Due to the “multi-component and multi-target” characteristics of traditional Chinese medicines (TCMs), the research on its targets and mechanism had been restricted. Based on potential of the label-free target discovery technology in the research of TCMs, this paper summarized the label-free target discovery technology and its application in TCMs research. It will provide a reference for the discovery of targets of TCMs and a new view for promoting the modernization of TCMs.
8.Synthesis and protective effect of ligustrazine intermediates against CoCl2-induced neurotoxicity in differentiated PC12 cell.
Guo-Liang LI ; Peng-Long WANG ; Xin XU ; Jin-Xuan LIN ; Fu-Hao CHU ; Ji-Xiang SONG ; Shen ZHOU ; Mi-Na WANG ; Yu-Zhong ZHANG ; Hai-Min LEI
China Journal of Chinese Materia Medica 2014;39(14):2679-2683
Ligustrazine, one of the major effective components of the Chinese traditional medicinal herb Ligusticum Chuanxiong Hort, has been reported plenty of biological activities, such as protect cardiovascular and cerebrovascular, neuroprotection and anti-tumor, et al. Because of its remarkable effects, studies on structural modification of ligustrazine have attracted much attention. Ligustrazine synthetic derivatives reported in recent decades are mainly derived from four primary intermediates (TMP-COOH, TMP-OH, TMP-NH2, HO-TMP-OH). To explore the neuroprotection activitiy of ligustrazine intermediates, six ligustrazine intermediates (2, 5, 8, 11, 12, 13) were synthesized and their protective effects against CoCl2-induced neurotoxicity in differentiated PC12 cells were studied. The target compounds were prepared via different chemical methods, including oxidation, substitution, esterification and amidation without changing the structure nucleus of ligustrazine. Compared with TMP (EC50 = 56.03 micromol x L(-1)), four compounds (2, 5, 12 and 13) exhibited higher activity (EC50 < 50 micromol x L(-1)) respectively, of which, compound 2 displayed the highest protective effect against the damaged PC12 cells (EC50 = 32.86 micromol x L(-1)), but target compounds 8 and 11 appeared lower activity (EC50 > 70 micromol x L(-1)). By structure-activity relationships analysis, the introduction of carboxyl, amino to the side chain of ligustrazine and appropriately increase the proportion of ligustrazine may contribute to enhance its neuroprotective activity, which provides a reference for the design, synthesis and activity screening of relevant series of ligustrazine derivatives in the future.
Animals
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Cell Differentiation
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drug effects
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Chemistry Techniques, Synthetic
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Cobalt
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toxicity
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Drugs, Chinese Herbal
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chemistry
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Neuroprotective Agents
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chemical synthesis
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chemistry
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pharmacology
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Neurotoxins
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toxicity
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PC12 Cells
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Pyrazines
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chemical synthesis
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chemistry
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pharmacology
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Rats
9.Effects of CNTF on the nuclear translocation of PKC following NMDA administration in primary hippocampal neurons.
Fang LIU ; Jin YAN ; Zong-lai JIANG ; Xue-qi WANG ; Xuan BAO ; Chang-lin LU
Chinese Journal of Applied Physiology 2003;19(2):145-148
AIMTo investigate the effect of ciliary neurotrophic factor (CNTF) on the nuclear translocation of protein kinase C (PKC) following NMDA administration in the primary cultured hippocampal neurons.
METHODS(1) PKCGAMMA or PKCepsilon- immunocytochemistry staining method was used after treating neurons with NMDA or CNTF. (2) The gray of the nucleus of the PKC-positive neurons were measured under the image pattern analysis system.
RESULTS(1) After NMDA administration of different concentration and time, Nucleus appear PKCgamma and PKCepsilon activities, especially the 100 micromol/L NMDA 30 min group. (2) The gray of nucleus in CNTF + 500 micromol/L NMDA group is similar to control group.
CONCLUSIONNMDA can induce nuclear translocation of PKC in the primary cultured hippocampal neurons, and CNTF can inhibit the translocation. It suggests that the inhibition of PKC translocation induced by NMDA is one of the important reasons for the neuro-protective effects of CNTF.
Animals ; Cells, Cultured ; Ciliary Neurotrophic Factor ; pharmacology ; Hippocampus ; cytology ; N-Methylaspartate ; pharmacology ; Neurons ; drug effects ; metabolism ; Protein Kinase C ; metabolism ; Protein Transport ; Rats ; Rats, Sprague-Dawley
10.Effect of angelicanaphtha on proliferation, apoptosis, collagen synthesis of human umbilical vein endothelial cells.
Kai LIU ; Xuan-Fen ZHANG ; Jin ZHANG ; Ming-Hua CAO ; Lin ZHONG ; Yong FAN
Chinese Journal of Plastic Surgery 2007;23(3):248-250
OBJECTIVETo investigate the effects of angelicanaphtha on proliferation, cell cycle, apoptosis, and collagen synthesis of human umbilical vein endothelial cells (HUVEC).
METHODSHUVEC was cultured and passaged in Dulbecco's modified Eagle's medium (DMEM) and treated with angelicanaphtha 1 mg/ L, 4 mg/L, and 16 mg/L at 1, 3, 5, and 7 day respectively. The proliferation was measured with MTT method. The cell cycle and apoptosis were analyzed with flow cytometry and collagen synthesis was determined with radioimmunoassay.
RESULTSThe proliferation of the HUVEC was accelerated by angelicanaphtha < or =4 mg/L and inhibited by angelicanaphtha at 16 mg/L (P < 0.05). Lower concentration (< or = 4 mg/L) of Angelicanaphtha decreased cells in G0/G1 phase and increased significantly cells in S phase and inhibited the apoptosis (P < 0.05). However, angelicanaphtha at 16 mg/L increased cells in G0/G1 phase and decreased cells in S phase and induced the apoptosis (P < 0.05). The collagen synthesis of HUVEC was inhibited by angelicanaphtha in concentration-dependent manner (P < 0.05 or 0.01).
CONCLUSIONThe proliferation effects of angelicanaphtha on HUVEC had dualistic regulation of increase by lower-concentration and inhibition by higher-concentration. Collagen synthesis of HUVEC was inhibited by angelicanaphtha in concentration-dependent manner.
Angelica sinensis ; Apoptosis ; drug effects ; Cell Proliferation ; drug effects ; Cells, Cultured ; Collagen Type III ; biosynthesis ; Endothelial Cells ; cytology ; drug effects ; metabolism ; Humans ; Oils, Volatile ; pharmacology ; Umbilical Veins ; cytology