1.Design, synthesis and biological evaluation of the novel trehalose derivatives.
Acta Pharmaceutica Sinica 2015;50(6):725-732
Using brartemicin as the leading compound, fifteen novel trehalose derivatives were designed and synthesized, and the structures were determined by 11H NMR, MS and element analysis. Inhibitory effects of the target compounds on the proliferation of A549, HepG2 and HUVEC cells were detectec by MTT assay. The abilities of adhesion, invasion and migration of A549 and HepG2 cells inhibited by the synthesized compounds were evaluated through Matrigel experiment and Transwell assay. The results showed that, the target compounds had no significant cytotoxicity (compared with the control, P>0.05) to A549, HepG2 and HUVEC cells at the dose range of 1-32 µmol.L-1. At the above dose range, the inhibitory effects of A549 cells adhesion, invasion and migration and HepG2 cells adhesion and invasion by compounds 79 and 82 are better than brartemicin.
Antineoplastic Agents
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chemical synthesis
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pharmacology
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Cell Adhesion
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Cell Line, Tumor
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drug effects
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Drug Design
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Hep G2 Cells
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drug effects
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Human Umbilical Vein Endothelial Cells
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drug effects
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Humans
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Trehalose
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analogs & derivatives
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chemistry
2.Design, synthesis and biological evaluation of the novel trehalose derivatives.
Acta Pharmaceutica Sinica 2015;50(6):725-32
Using brartemicin as the leading compound, fifteen novel trehalose derivatives were designed and synthesized, and the structures were determined by 11H NMR, MS and element analysis. Inhibitory effects of the target compounds on the proliferation of A549, HepG2 and HUVEC cells were detectec by MTT assay. The abilities of adhesion, invasion and migration of A549 and HepG2 cells inhibited by the synthesized compounds were evaluated through Matrigel experiment and Transwell assay. The results showed that, the target compounds had no significant cytotoxicity (compared with the control, P>0.05) to A549, HepG2 and HUVEC cells at the dose range of 1-32 µmol.L-1. At the above dose range, the inhibitory effects of A549 cells adhesion, invasion and migration and HepG2 cells adhesion and invasion by compounds 79 and 82 are better than brartemicin.
3.Comparison and Analysis of Rational Use of Antineoplastic Chinese Patent Medicine before ;and after Intervention in the Tumor Ward of Nantong First People’s Hospital
Chinese Journal of Information on Traditional Chinese Medicine 2017;24(2):117-119
Objective To evaluate the effect of the assessment of intervention of rational use and special initiative of antineoplastic Chinese patent medicine in tumor ward of Nantong First People’s Hospital (hereinafter referred to as “the hospital”); To facilitate the rational use of medicine in clinical setting. Methods Medical records of discharged patients in April and October 2015 were collected, and various types of irrational use of Chinese patent medicine was analyzed and put into statistical analysis. Results The proportion of medical records of irrational use of Chinese patent medicine declined from 39.45% to 18.49%; the percent of irrational prescription order sheet declined from 11.49%to 3.45%;the differences of variors irrational medicine use before and after the intervention were statistically significant. Conclusion The status of the rational use of antineoplastic Chinese patent medicine in tumor ward is improved after half-year special intervention and correction initiative.
4.The effects of the 150 m heliox saturation -182 m excursion diving in the open sea on the serum and urine CRH, beta-EP content of divers.
Yi-Qum FANG ; Ji XU ; Yong CHEN
Chinese Journal of Applied Physiology 2003;19(4):371-382
Adult
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Corticotropin-Releasing Hormone
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blood
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urine
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Diving
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physiology
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Helium
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Humans
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Male
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Oxygen
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beta-Endorphin
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blood
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urine
5.Clinical significance of early diagnosis and prognostic value of serum cell-free DNA on patients with cervical carcinoma
Yong HU ; Chunhua CHEN ; Fang NAN
Clinical Medicine of China 2015;(4):359-362
Objective To explore the clinical significance of the serum cell-free DNA on early diagnosis and prognostic value of patients with cervical carcinoma. Methods Forty-five patients with cervical carcinoma and 50 healthy women from May 2012 to February 2014 were selected from the Central Hospital of Ezhou. Serum cell-free DNA(cf-DNA),carbohydrate antigen125(CA125),carbohydrate antigen19-9(CA19-9), squamous cell carcinoma antigen( SCC ),β-human chorionic gonadotropin( β--HCG ) were detected by electrochemiluminescence analyzer. Results The levels of serum cf-DNA,SCC,β-HCG of patients in the cervical carcinoma group were(178. 8 ± 43. 4)μg/ L,(0. 7 ± 0. 3)μg/ L,(1. 3 ± 0. 4)kU/ L respectively, higher than those in health women((1 354. 7 ± 267. 2)μg/ L,(1. 4 ± 0. 4)μg/ L,(5. 2 ± 0. 6)kU/ L),and the differences were significant(t = 30. 690,9. 709,37. 614;P < 0. 001). Serum cf-DNA level of patients with Ⅱ-Ⅲperiod cervical carcinoma was(2 538. 8 ± 775. 3)μg/ L,higher than patients with Ⅰ period((1 244. 7 ± 253. 6)μg/ L;t = 8. 191,P < 0. 001). The area under the curve of ROC of serum cf-DNA,CA125,CA19-9, SCC,β-HCG were 0. 951 6,0. 638 2,0. 614 4,0. 805 7,0. 753 1 respectively and the AUC of serum cf-DNA was the largest. The sensibility,specificity,accuracy of cf-DNA were 75. 56% ,99. 13% ,93. 36% and 28. 32% , 93. 24% ,64. 26% in terms of CA125. Meanwhile,the sensibility,specificity,accuracy of CA19-9 were 19. 75% , 94. 47% ,67. 28% and 38. 87% ,88. 53% ,80. 16% in terms of SCC. The sensibility,specificity,accuracy of β-HCG were 43. 28% ,86. 21% ,77. 83% respectively. Conclusion Serum cf-DNA has high sensibility, specificity and accuracy in early diagnosis and prognostic value of patients with cervical carcinoma and it is worthy of clinical promotion.
6.Thoraco-abdominal two-field lymphadenectomy combined with adjuvant chemotherapy in the management of thoracic esophageal carcinoma
Wentao FANG ; Wenhu CHEN ; Yong JIANG
Chinese Journal of Thoracic and Cardiovascular Surgery 1995;0(05):-
Objective To increase the radical resection rate and decrease local-regional relapse rate in thoracic esophageal carcinoma. Methods One-hundred and four patients were prospectively randomized to receive esophagectomy with thoraco-abdominal 2-field lymphadenectomy (48 cases) or with lymph node sampling (56 cases). In 101 patients who survived after surgery, 29 received adjuvant chemotherapy with cisplatin and fluorouracil (FP). Results Comparing with lymph node sampling, the operation time for lymphadenectomy was prolonged. However, there was no increase in blood loss, surgical morbidity, or mortality. Mean stations of lymph node dissected (10.5 stations vs. 3.2 stations,P
7.Determination of forsythin in Shuanghuanglian Oral Liquid by RP-HPLC
Yong CHEN ; Binghui ZHU ; Jihui FANG ;
Chinese Traditional Patent Medicine 1992;0(10):-
Objective: To establish a method for determination of forsythin in Shuanghuanglian Oral (Flos Lonicerae, Radix Scutellariae, Fructus Forsythiae, etc.) Methods: After processing by RP SPE (reverse phase solid phase extraction), the sample solution was measured by RP HPLC. The chromatographic conditions were: Prodigy ODS (3) (150?4.6mm,5?m) column as analytic column; MeOH H 2O HAc(40∶60∶1,V/V) as mobile phase; detection wavelength at 227nm; column temperature at 35?C ; flow rate at 1.0mL?min -1 . Results: The linear range of forsythin was 0.1~2.0?g, r =0.9997. The average recovery was 102.2%, RSD =0.61%( n =6). Conclusion: The method is simple, accurate, reproducible and can be used to enhance the quality control of this drug.
8.The relationship between respiratory-circulatory changes and pulmonary complications in elderly patients after thoracotomy
Wentao FANG ; Yong CHEN ; Xiangyu ZHANG
Chinese Journal of Thoracic and Cardiovascular Surgery 2003;0(04):-
Objective To study the respiratory and circulatory changes in elderly patients, and their relationship with pulmonary complications after thoracotomy. Methods 58 elderly patients either aged over 75 years, with major organ dysfunction or underwent highly invasive procedures (group 1). Respiratory and circulatory status, including arterial blood gas under room air, water balance, urine gravity, and hemodynamics monitoring through pulmonary artery catheter were documented. The results were compared with those from 56 young patient controls receiving thoracotomy in the same period (group 2). Results All 12 patients having pulmonary complications were from group 1 (group 1A). Ten of them presented on the 2nd or 3rd postoperative day with hypoxemia. The other 2 died of type II respiratory failure after severe infection. Preoperative pulmonary co-morbidity (P=0.026, Exp(B)=5.4) and obesity (P=0.043, Exp(B)=4.9) were identified as independent risk factors for pulmonary complications after thoracotomy in elderly patients. During the first 3 postoperative days, PaO_2 of group 1A was significantly lower than group 2 as well as the other elderly patients who did not develop pulmonary complications after surgery (Group 1B). PaCO_2 of group 1A and 1B were significantly lower than group 2. There were also significant differences between the three groups in water balance on the first postoperative day (group 1A +832ml, P=0.006 vs. group 1B +109ml, P=0.004 vs. group 2 -243ml ). Urine gravity in group 1A was also significantly higher than in group 2 in the first 3 postoperative days. Pulmonary artery catheter monitoring revealed increased cardiac output and decreased systemic vascular resistance, showing a hyperdynamic status, in elderly patients after surgery. Pulmonary vascular resistance was elevated in the same time. Conclusion Pulmonary co-morbidities commonly seen in elderly patients are responsible for pulmonary complications, the major cause of surgical mortality after thoracotomy. Hypoxemia in the early postoperative period is mainlycaused by relative volume overloading from trauma induced interstitial edema. Close monitoring of arterial blood gas under room air, water balance, and urine gravity after thoracotomy may identify elderly patients at risk of developing pulmonary complication and prompt timely intervention.
9.HPLC combined with PCA technology for analysis of five gingerol compounds in different processing degrees of ginger charcoal.
Jiang-yong YU ; Qiu-fang CHEN ; Guo-yong LU
China Journal of Chinese Materia Medica 2015;40(21):4200-4204
To establish a new method for simultaneously determining the content of five gingerol compounds in different processing degrees of ginger charcoal and PCA principal component analysis was conducted for analysis. Samples were analyzed on Ultimate TM XB-C18 column (4.6 mm x 250 mm, 5 μm) , with acetonitrile (A) -0.1% phosphoric acid solution (B) as mobile phase for gradient elution. Detection wavelength was set at 280 nm. The flow rate was 0.6 mL x min(-1) and the column temperature was 30 degrees C. The five compounds were separated well and showed good linearity (r ≥ 0.999 7) within the concentration ranges tested. The average value for recoveries was between 98.86% - 101.5% (RSD 1.4% - 2.9%). The contents of five compounds showed difference among different processing degrees of ginger charcoal. Zingiberone had the highest content in the standard carbon, and the content of gingerol was decreased as the deepening of processing degree. Different processing degrees of ginger charcoal were classified into three groups with PCA, and provided scientific basis for establishing the quality standards of ginger charcoal.
Catechols
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chemistry
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Charcoal
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chemistry
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Chemistry, Pharmaceutical
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methods
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Chromatography, High Pressure Liquid
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methods
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Drugs, Chinese Herbal
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chemistry
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Fatty Alcohols
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chemistry
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Ginger
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chemistry
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Principal Component Analysis
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methods
10.Association of the expressions of glomerular nephrin, vascular endothelial growth factor and its receptor with proteinuria in preeclampsia rats
Fang FANG ; Lin TAO ; Jianying NIU ; Guixiang CHEN ; Yunjiao ZHOU ; Jing CHEN ; Minmin ZHANG ; Yong GU
Chinese Journal of Nephrology 2010;26(6):460-465
Objective To investigate the association of the expressions of glomerular nephrin, vascular endothelial growth factor (VEGF) and its receptor (VEGFR) with proteinuria in preeclampsia rats. Methods A rat model of preeclampsia was developed by inhibitor of nitric oxide synthase (L-NAME). The systolic blood pressure (SBP) and 24 h urine protein were compared among the normal female group (n=6), the normal pregnant group (n=8), nonpregnant control group (n=6) and preeclampsia group(n=8). The kidney biopsies of each group were observed by light and electron microscopy. The glomerular nephrin was detected by Western blotting and real-time PCR. Immunofluorescence was used to detect the expression of WT1. The level of glomerular VEGF and VEGFR (Flt-1 and Flk-1) were evaluated by Western blotting. Results The level of glomerular nephrin protein in the rats with preeclampsia (0.0726±0.0074) was significantly lower compared with normal female group (0.3795±0.0509), normal pregnant group (0.2361±0.0437) and nonpregnant control group (0.7265±0.0503) (P<0.01, respectively), while the levels of nephrin mRNA were not significantly different among 4 groups. The expression of WT1 was not significantly different among 4 groups as well. The level of glomerular VEGF in preeclampsia group (1.5429±0.0898) was significantly higher compared with normal female group (1.1870±0.1160), normal pregnant group (1.3741 ±0.1165) and nonpregnant control group (1.0155±0.0742)(P<0.01,respectively). VEGFR (Flt-1 and Flk-1) was also significantly higher in preeclampsia rats compared with other control groups (P<0.05, respectively). Conclusions In preeclampsia rats, nephrin is decreased significantly and the glomerular VEGF-VEGFR is increased significantly compared with the other control groups. The abnormal expression of nephrin and VEGF-VEGFR may be involved in the preeclampsia proteinuria. The underlying mechanism of this phenomenon needs further research.