1.Synthesis and Anti-HIV-1 Activity of One Schiff Base Derivative with Glucosamine of Gossypol
Jian YANG ; Wei ZHAO ; Jingxiang YANG ; Zhenhua JING ; Xianxi GUO
China Pharmacist 2017;20(5):787-790
Objective: To confirm the structure and preferential conformation of the Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine and explore its anti-HIV-1 activity.Methods: The Schiff base of gossypol with 11, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine was synthesized and identified by FT-IR, NMR spectroscopy and the PM6 semi-classical calculation.The inhibitory activity of the novel compound against the laboratory-adapted HIV-1IIIB strain was examined using the HIV-1IIIB/TZM-bl indicator cell culture system.Results: The 1H and 13C-NMR signals of the new Schiff base were assigned.The PM6 semi-classical calculation indicated that enamine-enamine tautomeric form of the new Schiff base was more stable,which was stabilized by the intramolecular hydrogen bonds.The anti-HIV-1 test showed that the compound could block the entry of HIV-1IIIB into the target cells.Conclusion: The Schiff base of gossypol with 1, 3, 4, 6-tetra-O-acetyl-β-D-glucosamine exhibits enamine-enamine tautomeric form in solution, which shows potential anti-HIV-1 activity.
2.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.
3.Gravity frequency and its monitoring application of EEG spectrum in the vigilance operation.
Jianping YANG ; Deqian ZHANG ; Jingxiang LU ; Xiaoyong SHUAI
Journal of Biomedical Engineering 2014;31(2):257-261
It is an important means to study the electrical activity of the brain's nerve cells by exploring physiological information of the EEGs from the frequency domain. The gravity frequency is one of the global parameters with using this method. We used the multitaper spectrum method (MTM) spectrum estimation method of good performance to calculate the EEG spectrum and its gravity frequency of subjects under vigilance and vigilance decrement state. The results showed that the gravity frequency of vigilance state was higher than that of vigilance decrement state, the gravity frequency became smaller along with the vigilance decrement, and the location of the gravity frequency shifted to the left in the spectrum. Finally, the monitoring curve of the gravity frequency was acquired by designing an algorithm, and it was used to online monitoring vigilance operators.
Algorithms
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Brain
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physiology
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Electroencephalography
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Humans
4.Main points of complete mesoeolic excision for right-hemi colorectal cancer and comparation with traditional surgery in the efficacy
Yang HE ; Xiaohuang TU ; Jingxiang SONG ; Zaizhong ZHANG
International Journal of Surgery 2014;41(2):97-101,封3
Objective To compare the clinical safety and efficacy of complete mesoeolic excision (CME) for right-hemi colorectal cancer with traditional surgical treatment.Methods Collectting the clinical data of 69 cases,who randonly divided into two groups,A group induced 38 cases and were implemented regular CME,and B group induded 31 cases which were implemented traditional surgery of right-hemi colorectal cancer patients from the Department of General surgery,Fuzhou General Hospital of Nanjing Military Region from Jan.1 2010 to Oct.1 2010,and comparing the safety and efficacy.Results The differences between and traditional surgery in terms of operation time,blood loss,exhaust and defecation time,hospitalization time,the rate of postoperative complication,the number of removed lymph node of Ⅰ and Ⅱ phase,3-year recurrence rate of Ⅱ phase,3-year survival rate of Ⅱ phase and the number of removed lymph node of Ⅲ phase in mesentery root were not significant.The differences in terms of the number of removed lymph node of Ⅲ phase(22.76 ± 6.94,15.11 ± 7.85),3-year recurrence rate of Ⅲ phase(5.88%,45.45%),3-year survival rate of Ⅲ phase (94.12%,63.64%),the total number of removed lymph node(20.56 ± 7.11,13.92 ± 6.62),3-year overall recurrence rate(7.89%,29.03%)and 3-year overall survival rate (94.74%,77.42%) were significant.Conclusions Comparing with traditional surgery,CME significantly benefits the patients of right-hemi colorectal cancer with stage Ⅲ,but not for patients with stage Ⅰ and Ⅱ.
5.Effect of clarithromycin on pharmacokinetics of aminophylline at steady state in rabbits
Chengchun SUN ; Xiaoyuan ZHAO ; Yang CAO ; Jingxiang WANG ;
Chinese Journal of Clinical Pharmacology and Therapeutics 2000;0(01):-
AIM: To investigate the effect of oral clarithromycin on serum concentrations of aminophylline at steady state and its pharmacokinetics in New Zealand rabbits. METHODS: The serum concentration of aminophylline was determined by FPIA in rabbits given(po) aminophylline or aminophylline combined with clarithomycin. The experiment was divided into 2 stages: (Ⅰ)the subjects only received a four day course of oral aminophylline until steady state;(Ⅱ)aminophylline and clarithromycin were coadministrated from the d 5 to d 10. The dose of aminophylline was 30 mg?kg -1 and the dose of clarithromycin was 50 mg?kg -1 for each rabbit. The two series of pharmacokineticis parameters were tested by statistic analysis. RESAULTS: There was no significant variation in pharmacokinetic parameters between two stages. CONCLUSION: It is not necessary to change the therapeutic dose of aminophylline when the drug is taken in combination with clarithromycin.
6.Cartilage construction in nude mice with microencapsulated stem cells derived from human umbilical cord Wharton’s jelly
Jianhua YANG ; Shuyun LIU ; Peng ZHAO ; Shibi LU ; Li ZHANG ; Jingxiang HUANG ; Bin ZHAO ; Wenjing XU ; Quanyi GUO
Chinese Journal of Tissue Engineering Research 2014;(8):1179-1184
BACKGROUND:Cartilage extracelular matrix with a large number of signaling molecule proteins and factors is likely to be an ideal material for tissue engineering cartilage.
OBJECTIVE: To investigate the possibility of calcium alginate and cartilage extracelular matrix combined with microencapsulated stem cels derived from human umbilical cord Wharton’s jely to construct ectopic tissue-engineered cartilage in nude mice.
METHODS: Microfilament suspension of the cartilage extracelular matrix was prepared. Human stem cels derived from Wharton’s jely of the umbilical cord were inoculated in to calcium alginate and cartilage extracelular matrix gel microspheres as experimental group. Stem cels derived from human umbilical cord Wharton’s jely were incubated in simple alginate gel microspheres as control group. After in vitro culture, the microspheres wereimplanted into the dorsal subcutaneous tissue of nude mice. Samples were taken after 4 weeks, respectively, for gross and histological observation.
RESULTS AND CONCLUSION:The stem cels exhibited paralel-chondrocyte morphology in microspheres, which grew and proliferated quite wel during in vitro culture. A new paralel-cartilaginous tissue was found in the subcutaneous tissue 4 weeks after surgery in the experimental group, and the tissue was positive for hematoxylin-eosin, safranine O, toluidine blue and colagen II. A large number of paralel-chondrocytes and cartilage lacuna-like structures were observed under a microscope with no obvious inflammatory reaction around the microspheres. The control group showed the partial degradation of microspheres, surrounded by only a smal number of inflammatory cels and lymphocytes. Calcium alginate and cartilage extracelular matrix microspheres have a rather good histocompatibility which can be used to construct paralel-cartilaginous tissues by implanting stem cel-microspheric compound into the subcutaneous tissue of nude mice.
7.Liposomal paclitaxel in combination with cisplatin as a first line of chemotherapy in treatment of advanced NSCLC with regional lymph node metastasis:A randomized controlled trial
Hu LUO ; Jingxiang YANG ; Liang GONG ; Yongfeng CHEN ; Chunlan TANG ; Heping YANG ; Wei XIONG ; Jianlin HU ; Ying HUANG ; Guangming LUO ; Hailing DUAN ; Xiangdong ZHOU
China Oncology 2013;(12):995-1000
Background and purpose: Regional lymph node metastasis was significantly associated with the prognosis of patients with non-small cell lung cancer (NSCLC). This study was designed to compare paclitaxel liposome plus cisplatin (LP) with gemcitabine and cisplatin (GP) in patients with regional lymph node metastasis of advanced NSCLC as a ifrst-line treatment. Methods:A total of 55 patients were randomly assigned to receive either liposomal paclitaxel (175 mg/m2) and cisplatin (75 mg/m2) or gemcitabine (1 000 mg/m2) and cisplatin (75 mg/m2) every 3 weeks. Results:Objective response rate (ORR) of lung primary foci was 37.9%in the LP arm and 30.8%in the GP arm (P>0.05) and the disease control rate (DCR) was 91.3%and 80.8%respectively (P>0.05);ORR of regional metastasis lymph node was higher in the LP arm (44.8%vs 15.4%, P<0.05).There was no signiifcant difference in DCR (93.1%vs 73.1%, P=0.101), although slight trends favoring paclitaxel liposome were seen;There was signiifcant difference in median overall survival (17.0 vs 12.0 months, P<0.05). LP was associated with significantly less thrombocytopenia and gastrointestinal side effects (P<0.05), but no signiifcant difference was observed in hyphemia, leucopenia, hepatotoxicity, renal toxicity and allergic reactions (P>0.05). Conclusion: Liposomal paclitaxel plus cisplatin is superior to gemcitabine plus cisplatin with less toxicity and better tolerated, it deserves further research and clinic application for patients with regional lymph node metastasis of advanced NSCLC.
8.A new assembly of locking compression plate for treatment of femoral shaft comminuted fracture:a biomechanical study
Qianhuan GUI ; Min ZHAO ; Chunlin XIAO ; Jiangjun ZHOU ; Zhuanyi YU ; Qiuxin CHENG ; Jingxiang CHEN ; Meiqing FU ; Jun YANG ; Bona SI
Chinese Journal of Trauma 2018;34(5):426-431
Objective To compare the biomechanical characteristics of new assembly of locking compression plate (NALCP) and locking compression plate (LCP) in internal fixation of femoral shaft comminuted fractures.Methods The preparation of a femoral shaft wedge fracture model (AO type 32-C2.1),six pairs of (12) femoral specimens were collected and divided into two groups randomly,with six in each group.The Group A was made up of the new assembly of locking compression plate fixation model (NALCP),and Group B the locking compression plate fixation model (LCP).The biomechanical properties of steel plates in two groups were tested by axial loading and torsional loading tests.The relative maximum displacement of fracture blocks in two groups on the X,Y and Z axes (the coronal axis was set as X axis,through the medial and lateral femur;the transverse axis was set as Z axis,through the femoral intercondylar fossa,perpendicular to the X axis;the sagittal axis was set as Y axis,perpendicular to the X and Z axis),the maximum strain,and the average strain of the steel plate were recorded.Strain distribution nephogram was produced,and the axial loading fatigue test results of Group A were recorded.Results Axial loading test:the relative maximum displacement of fracture in Group A on X,Y and Z axis were smaller than those in Group B (P <0.05 or 0.01);the main strain of Group A was greater than that of Group B (P <0.01);there was no significant difference in the average strain between Group A and Group B (P > 0.05).Torsional loading test:The relative maximum displacement of fracture in Group A on X and Z axis was smaller than that of Group B (P < 0.01);there was no statistically significant difference between the two groups on the Y axis (P > 0.05);the main strain of plate in Group A was greater than that in Group B (P < 0.01);there was no statistically significant difference in the average strain between Group A and Group B (P > 0.05).There was no obvious difference in strain distribution between the two groups.In Group A,the fatigue test of axial cyclic loading was performed for 1 million times,and the NALCP was intact without deformation,loosening,or rupture.Conclusion NALCP can provide strong mechanical stability for comminuted femoral fracture.The design of bridge steel plate is reasonable,which can effectively avoid stress concentration,reduce the stress shielding of steel plate,and facilitate bone healing.
9.The structural characterization and antigenicity of the S protein of SARS-CoV.
Jingxiang LI ; Chunqing LUO ; Yajun DENG ; Yujun HAN ; Lin TANG ; Jing WANG ; Jia JI ; Jia YE ; Fanbo JIANG ; Zhao XU ; Wei TONG ; Wei WEI ; Qingrun ZHANG ; Shengbin LI ; Wei LI ; Hongyan LI ; Yudong LI ; Wei DONG ; Jian WANG ; Shengli BI ; Huanming YANG
Genomics, Proteomics & Bioinformatics 2003;1(2):108-117
The corona-like spikes or peplomers on the surface of the virion under electronic microscope are the most striking features of coronaviruses. The S (spike) protein is the largest structural protein, with 1,255 amino acids, in the viral genome. Its structure can be divided into three regions: a long N-terminal region in the exterior, a characteristic transmembrane (TM) region, and a short C-terminus in the interior of a virion. We detected fifteen substitutions of nucleotides by comparisons with the seventeen published SARS-CoV genome sequences, eight (53.3%) of which are non-synonymous mutations leading to amino acid alternations with predicted physiochemical changes. The possible antigenic determinants of the S protein are predicted, and the result is confirmed by ELISA (enzyme-linked immunosorbent assay) with synthesized peptides. Another profound finding is that three disulfide bonds are defined at the C-terminus with the N-terminus of the E (envelope) protein, based on the typical sequence and positions, thus establishing the structural connection with these two important structural proteins, if confirmed. Phylogenetic analysis reveals several conserved regions that might be potent drug targets.
Amino Acid Sequence
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Antigens, Viral
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immunology
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Base Composition
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Computational Biology
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Enzyme-Linked Immunosorbent Assay
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Membrane Glycoproteins
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genetics
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Molecular Sequence Data
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Mutation
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genetics
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Phylogeny
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Protein Structure, Tertiary
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SARS Virus
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genetics
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immunology
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Sequence Analysis, DNA
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Sequence Homology
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Spike Glycoprotein, Coronavirus
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Viral Envelope Proteins
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genetics
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metabolism
10.A new assembly of locking compression plate of low elastic modulus for fixation of femoral comminuted fractures: a biomechanical study
Bin CHENG ; Baina SHI ; Jiangjun ZHOU ; Meiqing FU ; Jun YANG ; Zhuanyi YU ; Jingxiang CHEN ; Qiuxin CHENG ; Min ZHAO ; Chunlin XIAO
Chinese Journal of Orthopaedic Trauma 2018;20(9):798-802
Objective To compare the stress and its distribution between our self-designed new assembly of locking compression plate (NALCP) of low elastic modulus versus conventional locking compression plate (LCP) in fixation of femoral comminuted fractures.Methods Six pairs of cadaveric femur were used to create models of middle femoral comminuted fracture.The femoral fracture models were fixated respectively by NALCP of Ti2448 with low elastic modulus (E =30 Gpa) (NALCP group) and conventional LCP of Ti-6Al-4V with high elastic modulus (E =110 Gpa) (LCP group).Axial and torsion loads were applied on the models in the 2 groups to simulate those on one leg when a person slowly walks.The relative maximum displacements on the X,Y and Z axes of fracture fragments,and the maximum and average strains of the plate were recorded in the 2 groups.Nephograms of strain distribution were made for the 2 groups.The results of fatigue test under axial loads were recorded for NALCP group.Results Both the axial and torsion loading tests showed significantly larger principal and average strains in NACLP group than in LCP group (P < 0.05).However,there were no significant differences between the 2 groups in the relative maximum displacements of fracture fragments on X,Y or Z axis (P > 0.05).The plate strain nephograms for the 2 groups showed consistent strain distributions.The plates in NALCP group survived 1,000,000 fatigue tests under axial loads,without any deformation,loosening or breakage.Conclusion As our NALCP of low elastic modulus may be better in stress transmission and distribution,it can effectively reduce the effect of stress-shielding and promote bone healing.