1.Recent advances in the structure-activity relationship study of small-molecule sodium channel blockers with analgesic effects.
Wen LI ; You ZHOU ; Hong-Min LIU ; Qi-Dong YOU
Acta Pharmaceutica Sinica 2009;44(2):101-108
Pain is one of the common clinical symptom, previous studies have implicated sodium channels as a key constituent in pain signaling. Sodium channel blockers with efficient sodium channel blockade effect play an important role in analgesic treatment. However, most drugs used in clinic have many drawbacks and can not meet the demand of the clinical use. Therefore, for the development of new generation of sodium channel blockers, it is of great significance to find small molecule sodium channel blocking lead compounds with novel chemical scaffolds and new structures, sodium channel blocking activity and structure-activity relationship are discussed in detail, and current problems and trends in future research are also emphasized.
Analgesics
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chemistry
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pharmacology
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therapeutic use
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Animals
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Drug Design
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Humans
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Molecular Structure
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Neuralgia
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drug therapy
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Pain
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drug therapy
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Pain Measurement
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Sodium Channel Blockers
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chemistry
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pharmacology
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therapeutic use
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Sodium Channels
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drug effects
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Structure-Activity Relationship
2.Study of the therapeutic effects of free radical scavenger edaravone on cerebral hemorrhage in rats
Ling-Lin DONG ; Fu-Qiang GUO ; You-Song YANG ; Hong-Yuan DAI ; Wen-Bin WU ;
Chinese Journal of Neurology 2001;0(01):-
Objective To explore therapeutic effects and mechanisms of radical scavenger edaravone on experimental cerebral hemorrhage.Methods Two hundred-forty male SD rats were divided randomly into four groups:control group,cerebral hemorrhage group,edaravone treatment group before operation (A) and edaravone treatment group after operation (B).Experimental cerebral hemorrhage model was made according to the method reported by Rosenberg.Water quantity contained in brain and nervous missing sign were observed,meanwhile the levels of superoxide dismutase (SOD) and malondialdehyde (MDA) in brain tissue were measured.Results Compared with cerebral hemorrhage group,nervous missing sign and water quantity contained in brain obviously changed in edaravone treatment group (P
3.Application of minimally invasive, decompression bone graft implantation combined with metal trabecular bone reconstruction system for early stage osteonecrosis of femoral head.
Xian-tao CHEN ; Xu-yi TAN ; You-wen LIU ; Xiao-dong ZHANG ; Li-yun LIU ; Yu-dong JIA
China Journal of Orthopaedics and Traumatology 2015;28(5):422-425
OBJECTIVETo observe the application effect of minimally invasive decompression, bone graft implantation and metal trabecular bone reconstruction system for early stage osteonecrosis of femoral head and discuss the treatment of hip-salvage operation in early stage osteonecrosis of femoral head;
METHODSFrom January 2010 to June 2011, 50 patients (62 hips) Which were osteonecrosis of femoral head of early stake,were treated with minimally invasive decompression, bone graft implantation and metal trabecular bone reconstruction system, including 31 males (40 hips), 19 females (22 hip) with an average age of 36.2 years old ranging from 22 to 54 years old. The course of disease was from 6 to 15 months (averaged 10.5 months). Among them, 19 cases (23 hips) were steroid-induced, 25 cases (33 hips) were alcohol-induced, 6 cases (6 hips) were idiopathic; According to ARCO stage, 28 hips were at stage I, 34 hips were at stage II. All of them were diagnosed as femoral head necrosis by imaging examination before operation. Then each patient was followed to assess by Harris hip score, curative effect, and conduct the femoral head survival analysis during the postoperation.
RESULTSAll patients had finished operation, the operation time was between 30 and 85 min, intraoperative blood loss was 50 to 220 ml, and 47 cases (58 hips) were follow-up from 24 to 46 months with an average of 34.05 months. As compared with preoperative, the Harris hip score at the last follow-up was improved, the difference was statistically significant (P<0.01). The Harris hip score, curative effect and survival time of femoral head in ARCO stage I was superior to these in ARCO Stage II, the difference was statistically significant (P< 0.05).
CONCLUSIONEffect of minimally invasive decompression,bone graft implantation combine with the metal trabecular bone reconstruction system for early stage osteonecrosis of femoral head was good,it could significantly improve the Harris hip score, increase the femoral head survival time, delay the hip replacement, and performance better in ARCO stage I.
Adult ; Bone Transplantation ; Decompression, Surgical ; Female ; Femur Head ; injuries ; pathology ; surgery ; Femur Head Necrosis ; surgery ; Follow-Up Studies ; Humans ; Male ; Middle Aged ; Prostheses and Implants ; Reconstructive Surgical Procedures ; Young Adult
4.Study on three different species tibetan medicine sea buckthorn by 1H-NMR-based metabonomics.
Yong-Wen SU ; Er TAN ; Jing ZHANG ; Jia-Li YOU ; Yue LIU ; Chuan LIU ; Xiang-Dong ZHOU ; Yi ZHANG
China Journal of Chinese Materia Medica 2014;39(21):4234-4239
The 1H-NMR fingerprints of three different species tibetan medicine sea buckthorn were established by 1H-HMR metabolomics to find out different motablism which could provide a new method for the quality evaluation of sea buckthorn. The obtained free induction decay (FID) signal will be imported into MestReNova software and into divide segments. The data will be normalized and processed by principal component analysis and.partial least squares discriminant analysis to perform pattern recognition. The results showed that 25 metabolites belonging to different chemical types were detected from sea buckthorn,including flavonoids, triterpenoids, amino acids, carbohydrates, fatty acids, etc. PCA and PLS-DA analysis showed three different varietiest of sea buckthorn that can be clearly separated by the content of L-quebrachitol, malic acid and some unidentified sugars, which can be used as the differences metabolites of three species of sea buckthorn. 1H-NMR-based metabonomies method had a holistic characteristic with sample preparation and handling. The results of this study can offer an important reference for the species identification and quality control of sea buckthorn.
Hippophae
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metabolism
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Magnetic Resonance Spectroscopy
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methods
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Medicine, Tibetan Traditional
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Metabolomics
5.Establishment and identification of A new HPV positive esophageal cancer cell line.
Jin-Tao LI ; Fu-You ZHOU ; Wen-Ping DONG ; Li-Dong WANG ; Yi ZENG
Chinese Journal of Virology 2013;29(2):119-125
In order to explore the relationship between human papilloma virus ( HPV) and upper gastrointestinal cancer(esophageal cancer), An esophageal squamous cell carcinoma(ESCC) tissue was obtained from a 76 year old Chinese female patient from Anyang city, a high-incidence area for esophageal cancer, in China. Transplanted tumor was formed through direct SCID mouse tumorigenicity experiment and cultured monolayer cells were obtained after several passages and screenings Immunofluorescence test, cell growth curve, soft agar assay, chromosome analysis and tissues HE staining were also performed to confirm the epithelial cell origin. Cell DNA STR typing results showed that no three alleles was observed,indicating no contamination of human cells. DNA analysis revealed the presence of HPV type 18 DNA in this cell line. DOLINK test found the E6 protein expression of HPV virus. We concluded that the established cell line is a new esophageal squamous cell-origincarcinoma cell line with HPV DNA positive and expression of viral oncoprotein. It provides new cytologic material for performing etiology studies on the occurrence and development of esophageal cancer.
Aged
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Animals
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Carcinoma, Squamous Cell
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virology
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Cell Proliferation
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China
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Esophageal Neoplasms
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virology
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Female
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Human papillomavirus 18
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genetics
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isolation & purification
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Humans
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Male
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Mice
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Mice, SCID
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Papillomavirus Infections
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virology
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Tumor Cells, Cultured
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cytology
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virology
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Tumor Virus Infections
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virology
6.Computerized three-dimensional reconstruction and morphologic measurement of adult acetabulum bone structure.
Jian-dong DONG ; You WANG ; Zhen-an ZHU ; Dong-yun GU ; Wen-dong XUE ; Ke-rong DAI
Chinese Journal of Surgery 2005;43(24):1583-1586
OBJECTIVETo set up three-dimensional reconstruction of acetabulum bone structure from CT scanned image in computer with software of CAD and study quantitatively the morphologic features of the acetabulum.
METHODSThrough the process of CT scanning, and edge recording of the CT image, we made use of CAD software and Unigraphics software to reconstruct the 40 normal acetabulum bones for the radius of acetabulum (R), minimum thickness of medial wall of acetabulum (L), depth of Harris fossa (D) and maximum opening rim width in cross-sectional plane (W).
RESULTSThe average R was 30.48 +/- 2.05 mm. The average L was 2.35 +/- 1.13 mm. The average D was 5.71 +/- 1.21 mm. The average W was 63.06 +/- 2.05 mm. There was a linear relationship between the R and the W, but no correlation between the R, the L and the D.
CONCLUSIONSThere was a significance linear relationship between the R and the W in normal adult acetabulum. However no correlation between the R, the L and the D.
Acetabulum ; anatomy & histology ; diagnostic imaging ; Adult ; Humans ; Imaging, Three-Dimensional ; methods ; Pelvimetry ; methods ; Tomography, X-Ray Computed
7.S2 iliosacral screw insertion technique.
Hong-min CAI ; You-wen LIU ; Hong-jun LI ; Xue-jian WU ; Hong-tao TANG ; Ying ZHANG ; Yu-dong JIA ; Wu-yin LI
China Journal of Orthopaedics and Traumatology 2015;28(10):910-914
OBJECTIVETo introduce a technique pertaining to S2 iliosacral screw insertion.
METHODSThe screw pathway was first measured on the preoperative pelvic CT scan or the standard sacral lateral radiograph to make sure the existence of the "safe zone" in the S2 segment for screw insertion. Under general anesthesia, patients were positioned supine or prone, depending on the injury pattern of pelvic ring or associated injuries requiring concomitant operation. The operation field was routinely sterilized using iodine and subsequent alcohol solution and draped. The tip of a guide wire was inserted through a stab wound to the posterior outer iliac table, manipulated in the "safe zone" being enclosed by the anterior aspect of the S2 nerve root tunnel, the anterior aspect of the sacral vertebrae, and the inferior aspect of the S1 foramen under the guidance of the standard sacral lateral fluoroscopy, and then the tip was hammered one to two millimeters into the iliac cortex. The guide wire progressed along the trajectory between the inferior aspect of the S1 foramen and the superior aspect of the S2 foramen on the pelvic outlet fluoroscopic view, and then along the posterior to the anterior aspect of the S2 sacral vertebrae and alae on the pelvic inlet fluoroscopic view with a predetermined length. At that moment, in order to ensure the safety, another standard sacral lateral view was imaged to detect the guide wire's tip which should locate posterior to the anterior aspect of the sacral vertebrae and anterior to the anterior aspect of the S2 nerve root tunnel. Subsequently, the depth was measured, the trajectory was drilled and tapped, and the screw was inserted. Following the removal of the guide wire, the wound was irrigated and sutured.
RESULTSUtilizing this insertion technique, there were 30 S2 iliosacral screws in total being placed to stabilize the injured and unstable posterior pelvic ring in 27 patients. Each S2 screw was accompanied by an ipsilateral S1 screw. The S2 screw location was completely intraosseous in all patients, which was verified by postoperative pelvic outlet and inlet radiographs and CT scans. The insertion accuracy was 100 percent in the present series.
CONCLUSIONThe S2 iliosacral screw insertion technique is safe and reproducible to guide the placement of the S2 screw, enhancing the stability for the compromised posterior pelvic ring.
Adult ; Bone Screws ; Female ; Fractures, Bone ; surgery ; Humans ; Ilium ; injuries ; surgery ; Male ; Sacrum ; injuries ; surgery
8.Aortic elastic properties and its clinical significance in intracranial aneurysms.
Zhao-xia PU ; Xiang-dong YOU ; Wen-chao WENG ; Jian-an WANG ; Jian SHI
Journal of Zhejiang University. Medical sciences 2011;40(5):550-554
OBJECTIVETo investigate the aortic elastic properties and its clinical significance in intracranial aneurysms (IAs).
METHODSOne hundred and seven IAs patients (57 with hypertension) and 108 healthy subjects were recruited. The internal aortic diameters in systole and diastole were measured by the M-mode echocardiography, the aortic elasticity indexes were calculated and compared.
RESULTSThe aortic distensibility (DIS) was lower and the aortic stiffness index (SI) was higher in IAs patients than those in controls (both P <0.001). DIS was lower and SI was higher in IAs patients with hypertension (IAs-HP) than those in IAs with no hypertension (P <0.001). Similar results were obtained when the aortic elasticity index were adjusted for body surface area and body mass index.
CONCLUSIONAbnormal aortic elasticity is a common finding in IAs patients and hypertension is closely related to the severity of aortic elasticity.
Adult ; Aged ; Aorta ; diagnostic imaging ; physiopathology ; Case-Control Studies ; Elasticity ; Female ; Humans ; Intracranial Aneurysm ; physiopathology ; Male ; Middle Aged ; Ultrasonography
9.Role of HPV16/18/45 DNA testing of cervical specimens as a triage testing in cervical cancer screening.
Jing LI ; Wen CHEN ; Le-ni KANG ; Feng CHEN ; Dong-ping GUO ; Ba-yi LI ; You-lin QIAO
Acta Academiae Medicinae Sinicae 2013;35(3):254-259
OBJECTIVETo evaluate the clinical performance of careHPV16/18/45 DNA testing of cervical specimens as a triage testing for women with positive findings during the cervical cancer screening.
METHODSEligible women aged 25-65 years were enrolled from two high-risk communities in Yangcheng County,Shanxi Province.After providing written informed consent on a voluntary base,women underwent questionnaire-based interview,gynecological examination,and sample collection.Hybrid capture 2 technology(HC2),careHPV,Avantage HPV E6 test,and visual inspection with acetic acid(VIA)were conducted as the primary screening tests at the enrollment visit.Women with any positive finding were invited to receive a second VIA and colposcopy.careHPV16/18/45 was performed as a triage testing.Any visible lesion under colposcopy was directly biopsied.Women with pathology confirmed cervical intraepithelial neoplasia grade 2 and worse(CIN2+)were treated with standard procedures.
RESULTSFor the self-collected and doctor-collected samples,the application of careHPV16/18/45 as a triage testing decreased the colposcopy referral to 3.2% and 3.1%,respectively.Meanwhile,the sensitivity,specificity,and positive predictive value(PPV)for CIN2+were 50.0%,97.6%,and 26.7% for women with positive self-sampling careHPV results and 63.0%,97.9%,and 34.0% for women with positive doctor-sampling careHPV results.
CONCLUSIONcareHPV16/18/45 is promising as a triage testing among women with positive screening findings in low-resource settings.
Adult ; Aged ; Colposcopy ; DNA, Viral ; analysis ; Early Detection of Cancer ; methods ; Female ; Human papillomavirus 16 ; genetics ; isolation & purification ; Human papillomavirus 18 ; genetics ; isolation & purification ; Humans ; Mass Screening ; methods ; Middle Aged ; Uterine Cervical Neoplasms ; diagnosis ; virology ; Vaginal Smears