1.Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives.
Wenhu LIU ; Shibao WANG ; Xian YU ; Xinqiang YIN ; Yi LIU
Acta Pharmaceutica Sinica 2012;47(2):194-9
To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.
2.Intralesional curettage and wide excision for treatment of giant cell tumors (GCTs) of the distal radius: A Meta-analysis.
Zhen-chun YIN ; Bing-gen LIU ; Qing-jiang PANG ; Xian-jun CHEN ; Xiao YU
China Journal of Orthopaedics and Traumatology 2016;29(1):58-64
OBJECTIVETo search all studies that had been published in the world with regarding to the effectiveness of the extent of intralesional curettage and wide excision for recurrence rate and complications and comparative functional outcomes in patients with giant cell tumours (GCT) of the distal radius and analyze them which were in high quality by means of Meta analysis, in order to give some evidences for the choice of method dealing with giant cell tumors GCT in surgery.
METHODSCochrane central register of controlled trials(Issue 8 2014), PubMed(1970-01-01/2013-01-01), Ovid (1970-01-01/2013- 01-01), Elsevier (1970-01-01/2013-01-01), CNKI (1970-01-01/2013-01-01) were searched. Including intralesional curettage and wide excision were performed to treat giant cell tumors (GCTs) of the distal radius in the literatures, selecting on meet eligibility in the standard literatures underwent strict quality assessment. The Meta-analysis was performed with software RevMan5.0 from the Cochrane collaboration. Additionally, the analysis checked the heterogeneity of data. The effectiveness of the extent of intralesional curettage and wide excision for recurrence rate and complication in patients with giant cell tumours of the distal radius were evaluated and Odds Ratio was calculated.
RESULTSSeven relevant articles were identified involving total 163 cases. Among them, 92 cases were intralesional curettage (PMMA, n = 54; bone graft, n = 33; no PMMA or bone grafts, n = 5) and 71 cases were wide excision. The patients in the intralesional curettage group had a higher recurrence rate [OR = 3.87, 95% CI (1.42, 10.53)],especially for Campanacci grade 3 GCTs [OR = 10.12, 95% CI (1.57, 65.27)], yet fewer major complications [OR = 0.13, 95% CI (0.04, 0.40)] than the wide excision group. The use of PMMA versus bone graft did not affect the recur- rence rate [OR = 0.96, 95% CI (0.26, 3.56)]. By selecting the system evaluation of MSTS, the VAS and dynamometer, the result showed that the intralesional curettage group was equivalent or preferable to wide excision in terms of function rehabilitation.
CONCLUSIONBased on data obtained from the limited number of studies available, intralesional curettage appears to be moreappropriate for the treatment of local lesions (Grade 1 and 2) than Grade 3 GCTs of the distal radius. Moreover, PMMA was not additionally effective as an adjuvant, the intralesional curettage group was found to be equivalent or preferable to wide excision in terms of function rehabilitation.
Bone Neoplasms ; surgery ; Curettage ; methods ; Giant Cell Tumor of Bone ; surgery ; Humans ; Radius ; surgery
3.Advance of Ser/Thr Kinase Pololike Kinase 1 (Plk1) Research
Fu-Yin XIONG ; Hui-Yuan LIU ; Hong-Xing CHEN ; Ji-Xian DENG ;
China Biotechnology 2006;0(05):-
Pololike kinase 1(Plk1)contain an Nterminal Ser/Thr kinase catalytic domain and a Cterminal region that contains two poloboxes.As a key regulator of multiple steps during cell cycle across eukaryotic species,many proteins interact with Plk1.Plk1 is highly expressed in malignant cells and serves as a negative prognostic marker in specific human cancer types.Plk1 is a potential target for cancer therapy.Some novel smallmolecule inhibitors of pololike kinase 1 provide novel opportunities for cancerdrug discovery,such as BI 2536,ON01910.
4.Prognostic analysis of acute motor axonal neuropathy
Shi-Fang HOU ; Xian-Hao XU ; Yin-Hong LIU ; Huo ZHANG ; Xiang WANG ; Jian YIN
Chinese Journal of Neuromedicine 2009;8(5):496-499
Objective To investigate the clinical features of Guillain-Barre syndrome (GBS) and clarify the long-term prognosis of acute inflammatory demyelinating polyneuropathy (AIDP) and acute motor axonal neuropathy (AMAN). Methods We conducted an analysis of the clinical data of 50 patients with GBS treated in our hospital between 2003 and 2007. According to the eleetrophysiological criteria, the eases were classified into AIDP (n=24) and AMAN eases (n=22), with 4 eases of unknown classification. The patients unable to walk upon discharge were followed up for more than 6 months, and the clinical features and prognosis of the two groups were compared. Results The age, gender, cranial nerve involvement, Hughes grade at the initial neurological examination and at the time of symptom peak did not differ significantly between the patients with AIDP and AMAN (P>0.05), and most of the AMAN patients had a good recovery. The number of patients capable of walking at one month after the onset was comparable between the two groups (P>0.05). In AMAN group, the percentages of patients with slow recovery and those having rapid recovery were significantly higher than those in AIDP group (P<0.05). Conclusion The clinical recovery of AMAN patients can be either rapid or prolonged, and rigorous immunotherapy should be administered to achieve early recovery and ensure more favorable outcomes of the patients.
5.Design, synthesis and activities of 4-(2-acetoxybenzoylamino) butyramide derivatives.
Wen-Hu LIU ; Shi-Bao WANG ; Xian YU ; Xin-Qiang YIN ; Yi LIU
Acta Pharmaceutica Sinica 2012;47(2):194-199
To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.
4-Aminopyridine
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Amides
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chemical synthesis
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chemistry
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therapeutic use
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Animals
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Anticonvulsants
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chemical synthesis
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chemistry
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therapeutic use
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Epilepsy
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chemically induced
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drug therapy
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Female
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Male
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Mice
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Molecular Structure
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Random Allocation
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Structure-Activity Relationship
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gamma-Aminobutyric Acid
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chemistry
6.Relationship between body mass index, waist circumference and blood pressure among 5246 residents in Chongqing area.
Xiao-bo HUANG ; Rong HU ; Jin-lian LIU ; Yong-lan HOU ; Qing-rong LE ; Kai-liang LUO ; Xian-e LU ; Qiang SHE ; Yue-hui YIN ; Xian-bin LAN
Chinese Journal of Cardiology 2007;35(7):655-658
OBJECTIVETo explore the relationship between body mass index, waist circumference and blood pressure among residents in Chongqing area.
METHODSA total of 5246 residents aged 15 and over in Chongqing area were enrolled in this study by use of stratified sampling and cluster sampling methods. Data on blood pressure (SBP, DBP), pulse, height, body weight, waist and hip circumferences as well as questionnaire survey were analyzed.
RESULTSThe level of SBP and DBP and hypertension prevalence rate were significantly positively correlated with BMI (all P < 0.01). SBP, DBP levels and hypertension prevalence rate were significantly higher in people with abdomen obesity than people with normal waist circumference (all P < 0.01). BMI, waist circumference in hypertensive residents were significantly higher than non-hypertensive residents (all P < 0.01).
CONCLUSIONBlood pressure level and hypertension prevalence rate were closely related with BMI and waist circumference among residents in Chongqing area.
Adolescent ; Adult ; Aged ; Blood Pressure ; Body Mass Index ; China ; epidemiology ; Female ; Heart Rate ; Humans ; Hypertension ; epidemiology ; physiopathology ; Male ; Middle Aged ; Prevalence ; Risk Factors ; Rural Population ; Urban Population ; Waist Circumference ; Waist-Hip Ratio ; Young Adult
7.Inhibition of ER alpha-mannosidase expression causes reduction and shortening of microvilli on rat liver epithelial cell WB-F344.
Fang-tao ZHAO ; Jing LI ; Geng-xian SHI ; Yin LIU ; Li-ping ZHU
Acta Academiae Medicinae Sinicae 2003;25(1):52-55
OBJECTIVETo study the effect of N-glycosylation on the modification of microvilli on the surface of rat liver epithelial cell WB-F344 and the growth of the cells in culture.
METHODSRecombinant adeno-associated virus (rAAV) expression vector pAGX (+) containing an antisense or a sense fragment of 6A8 cDNA encoding a human alpha-mannosidase was constructed. The recombinant vectors or the mock were transfected into WB-F344 cells by means of lipofectAmine. The transfected cells were selected in G418 medium and cloned by means of limiting dilution. Integration of the transfected DNA into host DNA was detected by neo PCR. Rat liver ER alpha-mannosidase activity in cell supernatant was measured by using P-nitrophenyl-alpha-D-mannopyranoside as a substrate. Microvilli on cell surface were observed upon a scan electron microscope. The growth curves of the cells in culture were drawn.
RESULTSThe cell clones transfected with antisense 6A8 showed reduction of ER alpha-mannosidase activity with various degrees. Clone AS1 and AS2 cell showed a pronounced reduction of the enzymatic activity. In the study on AS1 cells, Con A binding to the cells was found to be enhanced, cell growth in culture became slow from day 5. The microvilli on the cells were reduced and blunted.
CONCLUSIONSTransfection with antisense 6A8 resulted in reduction and blunting of microvilli on the surface of growing WB-F344 cells, which might be related to N-glycosylation modification.
Animals ; Cloning, Molecular ; Epithelial Cells ; cytology ; Glycosylation ; Liver ; cytology ; Microvilli ; Rats ; Transfection ; alpha-Mannosidase ; genetics ; metabolism
8.Serum levels of sVCAM-1, IL-18 and VEGF in patients with aplastic anemia and their clinical significance.
Rui-Yu LIU ; Yuan-Zhong WU ; Huo-Liang FAN ; Xian-Yin XU ; Yao-Guang LUO ; Jun HU
Journal of Experimental Hematology 2009;17(1):117-120
This study was purposed to investigate the serum levels of soluble intracellular adhesion molecule (sVCAM-1), interleukin 18 (IL-18) and vascular endothelial growth factor (VEGF) in patients with aplastic anemia (AA) and their clinical significance. Enzyme linked immunosorbent assay (ELISA) was used to detect sVCAM-1, IL-18 and VEGF in serums of 30 patients with AA and 25 normal controls. The results showed that the serum levels of sVCAM-1 and IL-18 in patients with AA [(839.08 +/- 173.97) ng/ml, (380.35 +/- 47.76) pg/ml] were significantly higher than those in normal controls [(538.16 +/- 91.21) ng/ml, (256.39 +/- 59.52) pg/ml] (p < 0.01; p < 0.01). The levels of sVCAM-1 and IL-18 in severe AA patients [(969.94 +/- 182.54) ng/ml, (388.96 +/- 46.06) pg/ml] were higher than those in chronic AA patients [(709.26 +/- 165.32) ng/ml, IL-18 (352.21 +/- 47.08) pg/ml] (p < 0.01; p < 0.05), but the level of VEGF in AA patients [(69.63 +/- 27.42) pg/ml] was lower than that in the normal controls [(125.62 +/- 32.15) pg/ml] (p < 0.01)]. The level of VEGF in severe AA patients [(51.30 +/- 29.86) pg/ml] was significantly lower than that in chronic AA patients [(80.02 +/- 25.14) pg/ml] (p < 0.01). The levels of sVCAM-1 and IL-18 in AA patients after treatment were lower than those before treatment (p < 0.01; p < 0.05), but the level of VEGF after treatment was significantly higher than that before treatment (p < 0.05). It is concluded that the high levels of sVCAM-1, IL-18 and low level of VEGF in serum may be involved in the pathogenesis and progress of AA.
Adolescent
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Adult
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Aged
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Anemia, Aplastic
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blood
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Case-Control Studies
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Female
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Humans
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Interleukin-18
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blood
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Male
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Middle Aged
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Vascular Cell Adhesion Molecule-1
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blood
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Vascular Endothelial Growth Factor A
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blood
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Young Adult
9.Adventitious root induction and in vitro culture of Panax notoginseng.
Xian-Fu GAO ; Zhao-Hui XU ; Jia-Jian LIU ; Li-Ping MA ; Long-Ping YIN ; Wei JIA
China Journal of Chinese Materia Medica 2006;31(18):1485-1488
OBJECTIVETo investigate the induction and culture of adventitious root of Panax notoginseng.
METHODThree ways, induction from the explants of three-year-old P. notoginseng. The explants of regenerated shoots and calluses, were used to induce adventitious roots. The effects of 2, 4-dichlorophenoxyacetic acid, indole-3-butyric acid and naphthylacetic acid on adventitious root induction were investigated respectively. The effects of four modes of separating adventitious roots from the parent tissues on culture in vitro were compared.
RESULTAdventitious roots were successfully induced by three methods, of which the young flower bud callus was the best material for the induction of adventitious root. Indole-3-butyric acid possessed the strongest potency for induction. The liquid culture system was established by continuous culture of adventitious roots together with their parent tissues before separated.
CONCLUSIONThe acquisition and culture in vitro in liquid culture system of adventitious roots of P. notoginseng lay a foundation for the next investigation.
2,4-Dichlorophenoxyacetic Acid ; pharmacology ; Indoles ; pharmacology ; Naphthaleneacetic Acids ; pharmacology ; Panax notoginseng ; drug effects ; growth & development ; Plant Growth Regulators ; pharmacology ; Plant Roots ; drug effects ; growth & development ; Plants, Medicinal ; drug effects ; growth & development ; Tissue Culture Techniques ; methods
10.Chemical coupling of anti-dNA antibody on collagen coating.
Lan-xia LIU ; Xi-gang LENG ; Jing-yin YUE ; Li-ping SONG ; Hai WANG ; Cun-xian SONG
Acta Academiae Medicinae Sinicae 2005;27(6):718-722
OBJECTIVETo evaluate the feasibility and stability of chemically conjugating IgM on collagen films.
METHODSIgM was labeled with 125I using the chloramine-T method. Six collagen films were randomly divided into two groups. In chemical coupling group 125I-labeled IgM was chemically coupled with the films through N-succinmiclyl-3- (2-pyridyl-dithio) propionate reaction. In control group 125I-labeled IgM was absorbed onto collagen films. The amount of IgM on the collagen films and the amount of IgM remained on the films after extensive rinsing with phosphate buffered saline were monitored by counting the radioactivity of 125I.
RESULTSThe amount of antibodies loaded onto collagen films in the chemical coupling group was 15 times higher than that on the control films, showing significant statistical difference (P < 0.01). And the stability of conjugation antibodies on collagen films was significantly better than the control films.
CONCLUSIONChemical coupling is an effective approach to immobilize antibodies on collagen for further plasmid DNA tethering.
Angioplasty, Balloon, Coronary ; instrumentation ; Animals ; Antibodies, Antinuclear ; metabolism ; Cattle ; Coated Materials, Biocompatible ; chemistry ; metabolism ; Collagen ; chemistry ; metabolism ; Genetic Vectors ; Immunoglobulin M ; metabolism ; In Vitro Techniques ; Mice ; Protein Binding ; Stents ; Surface Properties