1.Effect of Wenyang Huoxue Lishul Recipe Containing Serum on Expression of Cathepsin L in Puromycin Aminonucleoside-induced Injury of Mouse Glomerular Podocytes.
Wen-wen QIU ; Jun YUAN ; Liu YANG
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(5):602-607
OBJECTIVETo observe the effect of Wenyang Huoxue Lishui Recipe (WHLR) containing serum on the expression of cathepsin L (CatL) in puromycin aminonucleoside-induced injury of mouse glomerular podocytes.
METHODSMouse podocyte cells (MPCs) in vitro cultured were divided into the normal control group, the model group, the dexamethasone (DEX) group, 10% WHLR containing serum group, 20% WHLR containing serum group, the vehicle serum control group. MPCs in the normal control group were cultured at 37 degrees C culture solution for 24 h. 45 mg/L puromycin was acted on MPCs in the model group for 24 h. On the basis of puromycin intervention, 1 limol/L DEX was co-incubated in MPCs of the DEX group for 24 h; 10% or 20% WHLR containing serum was co-incubated in MPCs of the 10% WHLR containing serum group and 20% WHLR containing serum group for 24 h. The vehicle serum control group was also set up by incubating with WHLR containing serum alone for 24 h. The expression of CatL and its substrate Synaptopodin in podocytes were detected by cell immunofluorescence staining. FITC-conjugated phalloidin was used to stain F-actin. A cortical F-actin score index (CFS index) was designed to quantify the degree of cytoskeletal reorganization in cultured podocytes.
RESULTSCompared with the normal control group, the expression of synaptopodin significantly decreased and the expression of CatL significantly-increased in the model group. F-actin arranged in disorder, gradually forming pericellular F-actin ring. CFS index was obviously elevated (P < 0.01). Compared with the model group, the epression of synaptopodin increased, the expression of CatL decreased, and CFS index also decreased in the DEX group, 10% WHLR containing serum group, and 20% WHLR containing serum group (P < 0.05, P < 0.01). Compared with the DEX group, the expression of synaptopodin decreased in 10% WHLR containing serum group, CFS index also decreased in 20% WHLR containing serum group (P < 0.05).
CONCLUSIONSWHLR could up-regulate the expression of synaptopodin, down-regulate the expression of CatL, and alleviate cytoskeletal reorganization of F-actin. It was helpful to stabilize the cytoskeleton of F-actin and improve the merging of podocytes.
Actins ; metabolism ; Animals ; Cathepsin L ; metabolism ; Cells, Cultured ; Down-Regulation ; Drugs, Chinese Herbal ; pharmacology ; Kidney Glomerulus ; cytology ; Mice ; Microfilament Proteins ; metabolism ; Podocytes ; drug effects ; pathology ; Puromycin Aminonucleoside ; adverse effects ; Up-Regulation
4.Design, synthesis and pharmacological investigation of isoindoline derivatives as 5-HT/NE double reuptake inhibitors.
Hui WEN ; Yuan SHI ; Jing-wen DONG ; Yan-shen GUO ; Jian-Jun ZANG ; Guang-zhong YANG
Acta Pharmaceutica Sinica 2015;50(9):1148-1155
A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents
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chemical synthesis
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chemistry
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Biological Transport
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Drug Design
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Isoindoles
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chemical synthesis
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chemistry
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Serotonin Uptake Inhibitors
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chemical synthesis
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chemistry
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Structure-Activity Relationship
5.The efficacy of 18F-FDG PET/CT, 99Tcm-MDP bone scintigraphy, and combination of the two techniques for detecting malignant bone metastasis
De-jun, LIU ; Yan-lin, FENG ; Feng-wen, YU ; Xiao-hong, HE ; Jian-wei, YUAN ; Guang-hua, WEN ; Ming, YANG
Chinese Journal of Nuclear Medicine 2011;31(1):25-28
Objective To compare the efficacy of 18F-FDG PET/CT, 99Tcm-MDP bone scintigraphy (BS), and combination of the two techniques (PET/CT + BS) for detecting bone metastasis by ROC curve analysis. Methods All 296 patients with various cancers, who underwent both 99Tcm-MDP BS and 18F-FDG PET/CT within two months, were retrospectively analyzed. These images were interpreted according to 5-point scale (0: definitely negative, 1: probably negative, 2: equivocal, 3: probably positive, 4:definitely positive for bone metastasis), and the scale of PET/CT + BS was the sum of PET/CT and BS. In light of the confirmed diagnosis derived from pathology or follow-up, ROC curve analysis was performed.The area under the ROC curve (AUC) was compared by z-test. Results Of 296 cases, 61 (20.6%) were confirmed as bone metastases and 235 (79.4%) were negative. The AUC were 0. 919 (95% confidence interval (95% CI) :0. 867 - 0. 971) for BS, 0. 949 (95% CI: 0. 906 - 0. 991) for PET/CT, and 0. 994 (95% CI: 0.988-0.999) for PET/CT + BS, rctrospectively. The AUC of PET/CT + BS was statistically significantly larger than that of BS (z=2. 866, P=0.004) or PET/CT (z =2.027, P=0.043), while the AUC of PET/CT was larger than that of BS, but no statistically significance (z = 0. 881, P = 0. 378) was showed. The optimal sensitivity, specificity, accuracy, positive predictive value (PPV), negative predictive value(NPV) were 90. 2% (55/61), 85. 1% (200/235), 86. 1% (255/296), 61. 1% (55/90), 97. 1%(200/206) for BS, 88.5% (54/61), 97.0% (228/235), 95.3% (282/296), 88.5% (54/61), 97.0% for PET/CT, and 98.4% (60/61), 95.7% (225/235), 96.3% (285/296), 85.7% (60/70) for PET/CT + BS,respectively. The specificity (χ2 = 19.862, P<0. 001), accuracy (χ2 = 23. 361, P<0.001) and PPV (χ2 =11. 791, P =0.001) of PET/CT + BS were significantly higher than those of BS, the sensitivity of PET/CT +BS was significantly higher than that of PET/CT (χ2 =4.167, P=0.031). Compared with BS, PET/CT had a higher specificity (χ2 = 19.600, P<0. 001), accuracy (χ2 = 13. 755, P <0. 001), PPV (χ2 = 13. 608, P <0. 001), but their sensitivity showed no statistically significant difference (χ2 = 0, P = 1. 000). Conclusions The efficacy of 18F-FDG PET/CT for detecting malignant bone metastasis was superior to that of 99Tcm-MDP BS alone. The detection ability can be obviously improved by combination of the two techniques.
6.Treatment of renal lower caliceal calculi with minimally invasive percutaneous nephrolithotomy
Guo-Hua ZENG ; Xun LI ; Wen ZHONG ; Jian YUAN ; Chi-Chang SHAN ; Kai-Jun WU ; Wen-Zhong CHEN
Chinese Journal of Urology 2001;0(06):-
Objective To investigate the clinical outcomes of minimally invasive percutaneous nephrolithotomy(MPCNL)in the treatment of lower caliceal calculi.Methods We retrospectively re- viewed the clinical outcomes and complications of 33 patients who underwent MPCNL for lower caliceal cal- culi from March 2001 to April 2005.The average diameter of the calculi was 2.8 cm.Single tract nephrosto- my was performed in all 33 cases;among them renal access was obtained through a middle calyx in 10 cases and a lower calyx in 23.Nine cases had F14 renal access;and 24 cases,F16.Results Of 33 cases,28 (85%)achieved stone-free at 1 session.A second-look was needed in 3 cases due to intraoperative bleed- ing;ESWL,in 1 case with residual,calculi;no treatment,in 1 case with residual calculi<4 ram.The mean operative time was 93 min;mean blood loss was 113 ml;mean hospital stay was 11 d.Blood transfusion was needed in 1 patient who suffered from hepatic cirrhosis preoperatively;another experienced severe bleeding 7 d after operation and was cured with hyperselective spongia gelatinosa embolization of the renal artery.Fol- low-up was available in 19 cases for 2-48 months,and no recurrence of renal calculi was noted.Conclu- sions Minimally invasive percutaneous nepbrolithotomy has advantages of safety,less invasion,and easy re- covery for the treatment of lower caliceal calculi.
7.Preliminary processing, processing and usage of Dendrobii Caulis in history.
Wen-yu YANG ; Sheng TANG ; Dong-jun SHI ; Xiang-gui CHEN ; Ming-yuan LI ; Xian-fu TANG ; Chang-jiang YUAN
China Journal of Chinese Materia Medica 2015;40(14):2893-2897
On account of the dense cuticles of the fresh stem and the light, hard and pliable texture of the dried stem, Dendrobii Caulis is difficult to dry or pulverize. So, it is very important to the ancient doctors that Dendrobii Caulis should be properly treated and applied to keep or evoke its medicinal effects. The current textual research results about the preliminary processing, processing and usage methods of Dendrobii Caulis showed that: (1) In history the clinical use of fresh or processed Dendrobii Caulis as teas and tinctures were very common. (2) Its roots and rhizomes would be removed before using. (3) Some ancillary approaches were applied to shorten drying times, such as rinsing with boiling mulberry-ash soup, washing or soaking with liquor, mixing with rice pulp and then basking, etc. (4) According to the ancients knowledge, the sufficient pulverization, by means of slicing, rasping, hitting or pestling techniques, was necessary for Dendrobii Caulis to take its effects. (5) The heat processing methods for Dendrobii Caulis included stir-baking, stir-frying, steaming, decocting and stewing techniques, usually with liquor as an auxiliary material. Among above mentioned, steaming by pretreating with liquor was most commonly used, and this scheme was colorfully drawn in Bu Yi Lei Gong Pao Zhi Bian Lan (Ming Dynasty, 1591 CE) ; moreover, decocting in advance or long-time simmering so as to prepare paste products were recommended in the Qing Dynasty. (6) Some different processing programs involving stir-baking with grit, air-tightly baking with ondol (Kangs), fumigating with sulfur, which appeared in modern times and brought attractive outward appearance of the drug, went against ancients original intentions of ensuring drug efficacy.
Dendrobium
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History, Ancient
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Medicine, Chinese Traditional
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history
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Technology, Pharmaceutical
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history
8.Asymmetry of optic disc hemifield retinal nerve fiber layer in early primary open angle glaucoma
Wen, LI ; Yuan, DENG ; Dan, ZHOU ; Jun, LI ; Ding, LIN ; Chang-Hua, YE
International Eye Science 2015;(7):1204-1206
AlM: To examine the retinal nerve fiber layer ( RNFL ) changes in early primary open angle glaucoma ( POAG ) by comparing the superior half of the optic disc with the inferior disc half.METHODS: lt was a clinical observational study. The study included 30 patients ( 39 eyes ) with POAG and 20 normal subjects ( 40 eyes ) . Visual field was tested by Zeiss Humphrey750 and the optic disc topographic parameters and RNFL thickness were measured by Zeiss Cirru HD-OCT. Collecting information included visual field mean defect ( MD ) , glaucoma hemifield test ( GHT ) , intraocular pressure ( lOP ) , C/D ratio and RNFL thickness. Data were analyzed by statistic software SPSS18. 0. The differences between two groups were assessed using t test.RESULTS: The differences of superior RNFL minus inferior RNFL thichness on the corresponding clock-hour locations were caculated in two groups. There was a significant difference in superonasal- inferonasal RNFL thickness between two groups (t=2. 526, P=0. 014), and there were no significant differences in the others ( all P>0. 05).CONCLUSlON: The asymmetry of optic disc hemifield RNFL is found in early primary open angle glaucoma patients. The superonasal RNFL ( 1 o’clock for right eye, and 11 o’clock for left eye ) is more fragile to loss than inferonasal RNFL (5 o’clock for right eye, and 7 o’clock for left eye) .
9.An experimental study of motor evoked potentials of the diaphragm elicited by transcranial electric stimulation
Xu-Hui ZHOU ; Yong ZHANG ; Feng PAN ; Wang-Jun YAN ; Lian-Shun JIA ; Wen YUAN ;
Chinese Journal of Physical Medicine and Rehabilitation 2003;0(08):-
Objective To study the characteristics of the transcranial electric stimulation(TES)-elicited motor evoked potentials(MEP)recorded from different points of the diaphragm,and to determine the optimal record- ing site in the diaphragm.Methods One EEG electrode was placed subcutaneously in the midline of the skull as stimulation electrode and another EEG electrode was inserted into hard palate submucously as cathode in 30 male rats.And single square wave electrical pulse was used for stimulation.The stimulation intensity was 15 mA,the du- ration of the pulse was 0.2 ms,and the stimulating interval was 200 ms.The concentric needle electrode were insert- ed into the following eight sites:the medial,intermediate,lateral crura of the diaphragm,the junction of the posterior axilla line and the inferior border of the eleventh rib,the junction of the anterior axilla line and the inferior border of the ninth rib,the junction of the intermediate line of the clavicle and the inferior border of the eighth rib,the junction of the para-sternal line and the inferior border of the seventh rib,the pars sternalis.The MEP was recorded from each point,respectively.The optimal sites of the diaphragm MEP were found and recorded.Results The MEPs were re- corded from each of the 8 sites of the diaphragm in all the rats after TES.There was no statistically significant differ- ence among the latencies of every site.But the amplitude varied from 6.08?0.46 mV in maximum along the inferior border of the ninth rib at the anterior line of the axilla to the minimum of O.91?0.03 mV at the pars sternalis. Conclusion It is safer to insert the needle along the inferior border of the ninth rib at the anterior line of the axilla, because there was certain distant from the folding part of the pleura and the amplitude of the recorded wave at this point is maximal.
10.Inhibitory effect of 5-fluorouracil encapsulated by galactosylceramide liposomes on drug resistance and its mechanisms
Yong JIN ; Jun LI ; Yuan-Hai LI ; Xiong-Wen LV ; Jin-Fang GE ; Shu-Yun XU ;
Chinese Pharmacological Bulletin 2003;0(08):-
Aim To study inhibitory effect of 5-fluorouracil encapsulated by galactosylceramide liposomes (5-Fu-GCL)on 5-Fu-resistent HepG_2 cells and its mechanisms. Methods Inhibitory effect of 5-Fu-GCL on established model of 5-Fu-resistant HepG_2 cells was assessed with MTT assay in vitro. The concentration-time course of 5-Fu-GCL in intracellular fluid was detected with high performance liquid chromatography (HPLC). Thymidylic acid synthase (TS) expression was observed with immunohistochemical method,and NO content was determined with chemical method. Results Obvious inhibitory effects of 5-Fu-GCL (75,150,300,600,1200?mol?L-1) on 5-Fu-resistant HepG_2 cells were observed with IC_ 50 of 158.6 ?mol?L-1,far lower than that of free 5-Fu (400.9 ?mol?L-1). 5-Fu-GCL (300 ?mol?L-1) inhibited 5-Fu-resistant HepG_2 cells in a time-dependent manner,and the inhibitory effect of 5-Fu-GCL was stronger than that of free 5-Fu during 12~48 h. Compared with free 5-Fu,5-Fu-GCL (300 ?mol?L-1) increased the content of intracellular fluid in 5-Fu-resistant HepG_2 cells. 5-Fu-GCL(62.5,300,1200 ?mol?L-1) not only inhibited the expression of TS,but also increased the production of NO in 5-Fu-resistant HepG_2 cells,and these effects of 5-Fu-GCL(300,1200 ?mol?L-1) were stronger than those of free 5-Fu. Conclusion 5-Fu-GCL has inhibitory effect on 5-Fu-resistant HepG_2 cells. The effect may be related to the increased concentration of 5-Fu-GCL in intracellular fluid,inhibited expression of TS and increased production of NO.