1.Design, Synthesis and Antiviral Activity of Novel EV71 3C Protease Inhibitors
Jian YANG ; Fang ZHANG ; Jingxiang YANG ; Rui YU ; Xianxi GUO
China Pharmacist 2015;18(10):1638-1642
Objective:To explore novel compounds with anti-EV71 activity. Methods: A series of oligopeptides were designed based on the active groove of the EV71 3C protease using molecular simulation technology. Furthermore, some oligopeptides were syn-thesized and tested for the inhibition ability against EV71 in vitro. Results:Pentapeptides had higher binding affinity to the EV71 3C protease than the other oligopeptides, such as compounds 25 and 16. Therefore, compounds 25 and 16 were synthesized and tested in vitro for the anti-EV71 activity, and compound 25 exhibited potent anti-EV71 activity(EC50 =1. 36 μmol·L-1, CC50 =211. 94 μmol ·L-1, SI=155. 84), while compound 16 had no evident effect on EV71. Conclusion: It is worthy of further investigation on com-pound 25 as a novel scaffold of anti-EV71inhibitor.
2.Interaction and Molecular Simulation between Gossypol and Human Serum Albumin
Jian YANG ; Jurong LI ; Xianxi GUO ; Zhifeng DU ; Fang ZHANG
China Pharmacist 2015;(6):881-883,887
Objective:To explore the interaction between gossypol and human serum albumin ( HSA) . Methods:The interaction of gossypol and HSA under physiological conditions was studied by fluorescence spectroscopy, and the molecular docking software was used to simulate the interaction. Results:The binding constant of gossypol and HSA at 293K and 303K was 2. 390 6 × 105 L·mol-1 and 3. 576 8 × 103 L·mol-1 , respectively. There was one binding site on HSA for gossypol. Hydrogen bond and Van Der Waals inter-actions were involved in the binding process. The binding of gossypol and HAS was closer to tyrosine residue in HSA. The molecular simulation analysis verified the above results. Conclusion: The gossypol-induced fluorescence quenching of HSA belongs to a static quenching procedure.
3.Six to Ten Years Follow-Up Survey of Triancinolone Acetonide Therapy in Children with Nephrotic Syndrome
fang, YANG ; guo-ling, HE ; wen-jian, LIU
Journal of Applied Clinical Pediatrics 2006;0(17):-
Objective To observe the long term effects of triancinolone acetonide(T-A)as a substitution for prednisone,a maintenance therapy in treating children with nephrotic syndrome(NS).Methods Twenty-five children with idiopathic NS(10 children with simple type NS and 15 children with nephritic type NS).Prednisone treatment for 4-8 weeks would bring remission,and immunosupression was added if remission failed.Then oral prednisone was reduced to 2 mg/kg per alternate day for 2 weeks,followed by a small dose of T-A(0.5-1.0 mg/kg)intramuscular injection,once a year per month for the first year,and every other month for the second year,as for the 8 frequently relapse cases,it would be every 3 months for the third year,other 17 cases stopped T-A intramuscular injection in the third year.Two weeks after T-A treatment stopped using prednisone.The relapse and the side-effects was observed through the observation of 25 NS children's clinical manifestation,routine urine test,and biochemistry variation before and during the T-A treatment,along with a 6 to 10 years follow-up survey after T-A therapy stopped.Statistical analysis was performed by using SPSS 10.0 software.Results 1.Median dose of T-A was 0.97 mg/kg per time,total doses of T-A was 18.1 mg/kg(13.5-24.4 mg/kg).2.There were 16 relapse cases by prednisone treatment,while 7 relapse cases by T-A treatment for 2 years,there existed a significant comparison(P0.05).4.There were only 4 relapsed cases in the 6-10 years of follow-up observation,the difference was sharp compared with the 16 relapsed cases before T-A treatment(P
4.Evaluation of maxillary protraction in treatment of skeletal class Ⅲ malocclusions in early mixed dentition
zhi-fang, CAI ; jian-guo, WANG ; min, HOU
Journal of Shanghai Jiaotong University(Medical Science) 2006;0(07):-
Objective To evaluate the outcomes of maxillary protraction in the treatment of skeletal class Ⅲ malocclusions in early mixed dentition. Methods Fourteen patients with skeletal class Ⅲ malocclusions in early mixed dentition were treated with maxillary protraction for one year with oral active appliance bonded face mask.Cephalometric records were analyzed to assess the changes of maxillo-facial structure of the hard tissue before and after treatment. Results The anterior crossbite was unlocked in all the patients,and the maxilla moved downwards and forwards.Point A moved forwards,and angle SNA and ANB significantly increased.The mandible rotated downward and backward,and the Wits values significantly increased,which led to the correction of a skeletal class Ⅲ relationship.Maxillary length and protrusion significantly increased,and facial profile improved obviously. Conclusion Maxillary protraction works well in the treatment of skeletal class Ⅲ malocclusions in early mixed dentition,and can reduce the chances of later orthognathic surgery.
5.Application of Color Doppler Ultrasonography by Bed Side in the Early Diagnosis of Hypoxic-Ischemic Encephalopathy in Full Term Neonates
yi-jin, SU ; lian-fang, DU ; jin, XIA ; min, FANG ; xian-ming, XU ; jian-guo, HONG
Journal of Applied Clinical Pediatrics 2004;0(12):-
Objective To explore the value of color doppler ultrasonography by bed side in the early diagnosis of HIE in full term neonates.Methods The changes of cerebral parenchymal and cerebral arterial blood stream parameter on 35 cases of neonates clinically diagnosed HIE of mild and moderate degree and 40 cases of normal newborns on the 24,48 and 72 hours after birth were observed by color doppler ultrasonography by bed side.Results 1.The cerebral parenchyma was even echo in normal newborns,but it was maldistributed and reinforced in mild asphyxia neonates and it was more serious in moderate degree.The echo of cerebral parenchyma in mild degree was near normal in 48 hours after birth,while the echo of cerebral parenchyma in moderate degree was still maldistributed and reinforced in 48 and 72 hours after birth.2.There was obvious changes in the cerebral arterial blood stream parameter and hemodynamics of the asphyxia newborns compared with normals.The systolic peak velocity(Vs)and end diastolic velocity(Vd)of the cerebral arteries in mild and moderate degree were obviously lower than that of control group in 24,48 hours after birth(Pa0.05).3.Resistance index(RI)of the cerebral arteries in mild and moderate degree were higher than that of control group in 24,48 hours after birth(Pa0.05).Conclusion Color doppler ultrasonography by bed side is a convenient,noninvasive method for diagnosing HIE.
6.TAXONOMY OF PLANT PATHOGENIC CORYNEFORM BACTERIA
Jian-Hua GUO ; Yong-Jian CAI ; Yong-Fang CHEN ; Yun-Ying GE ;
Microbiology 1992;0(01):-
There are many different opinions about the taxonomy of plant pathogenic coryneform bacteria since they were departed from genus of Corynebacteria. In recent years, they were classified into 5 genus, including Clav-ibacter, Curtobacterium, Arthrobacter, Rhodococcus and Rathayibacter. Some new points of view about their taxonomy have been published thereafter. The changing of taxonomy is maily because of the methods'altering from old to new molecular and polyphasic taxonomy, and the latter is in continuously development. Taxonomy of plant pathogenic coryneform bacteria somehow depends on the cooperation of phytopathologists, microbilogists and other scientists.
7.Screening, Identification and Fermentation Optimization of Aminotransferase-producing Strain
Jing WANG ; Jiang-Hua LI ; Jun FANG ; Jian LU ; Guo-Cheng DU ; Jian CHEN ;
Microbiology 2008;0(09):-
A strain named as WJ44 with capability of producing branched-chain aminotransferase was isolated from the soil, the enzyme activity is especially high when used leucine as a substrate. According to the physiological characteristics, biochemical characteristics and 16S rRNA sequence of WJ44, the strain was identified as Bacillus cereus. The optimal carbon source and nitrogen source were also determined as 20 g/L glucose, 15 g/L tryptone and 5 g/L beef extract, respectively. The optimal proportion of other component in the medium is corn steep liquor 15 g/L, KH2PO4 3 g/L, MgSO4?7H2O 0.5 g/L. The optimum original pH value is 7.0, the cultural temperature is 37℃, liquid volume is 20 mL/250 mL, the shaker’s rotating speed is 200 r/min. The highest leucine transferase activity of 45.787 U/mL was achieved after 10 h under the opti- mal condition, and the dry weight of cell is 8.643 g/L, increased by 54% and 10% respectively. This result shows that WJ44 is a branched-chain aminotransferase-production strain with fine capability.
8.Evaluation on outcome of iodine deficiency disorders control in Hubei Provinvce in 2007
Ming-jian, LI ; Qing, SHI ; Jian, YIN ; Bao-guo, HUANG ; Fang, ZHOU ; Pei-sheng, XIONG ; Xin-guo, GONG
Chinese Journal of Endemiology 2008;27(5):541-542
Objective To investigate the current situation of the prevention and contml of iodine deficiency disorders(IDD)in Hubei Province,SO as to provide a policy.making basis for controlling work of IDD. Methods Using the method of proportional population sampling(PPS),30 eounties were seiected in Hubei Province.In each selected county,1 primary school was chosen.In every primary school,40 pupil8 aged 8~10 years were selected to examine thyroid size,intelligent quotient(IQ),and salt iodine contents at their home.In the selected pupils,2 boys and 2 girls were chosen to determine their urinary iodine contents in each age grouD.Twenty pupils in the above school and 5 housewives ileal"to this school were tested in health education questionnaire. Results The median of salt iodine was 30.1 mg/kg,and the rate of comsuming qualified iodized salt was 96.2% (1154/1200).The rates ofchild goiter were 6.5%(78/1200)by palpation and 4.1%(49/1200)by B ultrasound.The median of urinary iodine Was 358.4μg/L and mean of the IQ was 105.3±14.4.The rate of qualified scores of both students and housewives Was 25.5%(153/600)、90.7%(136/150).Conclusions The current Bituation of iedine nutrition is good.The goal of eliminating IDD has been achieved in Hubei Province.
10.Identification and Function of Acid-sensing Ion Channels in RAW 264.7 Macrophage Cells
Lan NI ; Peng FANG ; Zhuang-Li HU ; Hai-Yun ZHOU ; Jian-Guo CHEN ; Fang WANG ; You JIN
Journal of Huazhong University of Science and Technology (Medical Sciences) 2018;38(3):436-442
Activation of acid-sensing ion channels (ASICs) plays an important role in neuroinflammation.Macrophage recruitment to the sites of inflammation is an essential step in host defense.ASIC 1 and ASIC3 have been reported to mediate the endocytosis and maturation of bone marrow derived macrophages.However,the expression and inflammation-related functions of ASICs in RAW 264.7 cells,another common macrophage,are still elusive.In the present study,we first demonstrated the presence of ASIC 1,ASIC2a and ASIC3 in RAW 264.7 macrophage cell line by using reverse transcriptase polymerase chain reaction (RT-PCR),Western blotting and immunofluorescence experiments.The non-specific ASICs inhibitor amiloride and specific homomeric ASIC 1 a blocker PcTx 1 reduced the production of iNOS and COX-2 by LPS-induced activating RAW 264.7 cells.Furthermore,not only amiloride but also PcTx 1 inhibited the migration and LPS-induced apoptosis of RAW 264.7 cells.Taken together,our findings suggest that ASICs promote the inflammatory response and apoptosis of RAW 264.7 cells,and ASICs may serve as a potential novel target for immunological disease therapy.