1.Study on the effect of cluster needling of scalp acupuncture on the plasticity protein MAP-2 in rats with focal cerebral infarction.
Wen-zeng ZHU ; Jin-xia NI ; Qiang TANG ; Gui-rong DONG ; Hong-ying LI
Chinese Acupuncture & Moxibustion 2010;30(1):46-50
OBJECTIVETo investigate the material base and underlying mechanism of the effect of cluster needling of scalp acupuncture on the neuronal plasticity in rats with focal cerebral infarction.
METHODSThe model rats with acute cerebral infarction were made by blocking the middle cerebral artery with monofilament. One hundred and thirty two Wistar rats were randomly divided into 4 groups: sham-operation group (A), model group (B), point-to-point scalp acupuncture group (C) and cluster-needling of scalp acupunture group (D). Puncturing from "Baihui (GV 20)" to "Qubin (GB 7)" was used in group C. Cluster needling of scalp acupuncture was used in group D, in which needles were inserted forward and slantingly into "Baihui (GV 20)" and its left and right sides at 4 mm. In both groups, the treatment was carried out with rapid twirling reinforcing-reducing for 1 min then retaining needle for 30 min, once a day, 6 days in one course, for treating 4 courses. There was no treatment for group A and B. The change of neurological function was evaluated with Bederson score, while the expression of microtubule-associated protein 2 (MAP-2) in the ischemic penumbra was examined with immunohistochemistry (streptavidin-peroxidase method).
RESULTSIn comparison,with group B, the score of neurological function in group D decreased on 7th day (P<0.05), while the scors in group C and D also decreased on 14th and 28th days (both P<0.05). As compared with group C, the score of neurological function in group D obviously decreased on 28th days (P<0. 05). Comparing with group B, the expression of MAP-2 on the ischemic cortex was significantly increased in group D and C on 7th, 14th and 28th days (all P<0. 05), however, this expression in group D was higher than that in group C on 14th and 28th days (P<0. 05).
CONCLUSIONCluster needling of scalp acupuncture can improve the neurological function of rats with focal cerebral infarction, and increase the expression of MAP-2 in the ischemic penumbra.
Acupuncture Therapy ; methods ; Animals ; Cerebral Infarction ; ethnology ; metabolism ; physiopathology ; therapy ; Disease Models, Animal ; Male ; Microtubule-Associated Proteins ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Scalp
2.Synthesis and anti-proliferative activity of fluoroquinolone (rhodanine unsaturated ketone) amide derivatives.
Liu-zhou GAO ; Yu-suo XIE ; Qiang YAN ; Shu-min WU ; Li-li NI ; Hui ZHAO ; Wen-long HUANG ; Guo-qiang HU
Acta Pharmaceutica Sinica 2015;50(8):1008-1012
To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.
Amides
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chemical synthesis
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pharmacology
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Antineoplastic Agents
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chemical synthesis
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pharmacology
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Cell Line, Tumor
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Fluoroquinolones
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chemical synthesis
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pharmacology
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HL-60 Cells
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Humans
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Ketones
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chemical synthesis
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pharmacology
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Rhodanine
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chemical synthesis
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pharmacology
3.Synthesis and anti-proliferative activity of fluoroquinolone C-3 fused heterocyclic α,β-unsaturated ketones derived from ciprofloxacin.
Taol LI ; Zhou Gao LIU ; Yu-suo XIE ; Yan-fei FENG ; Qiang YAN ; Shu-min WU ; Li-li NI ; Hui ZHAO ; Wen-long HUANG ; Guo-qiang HU
Acta Pharmaceutica Sinica 2015;50(5):569-573
To discover novel antitumor fluoroquinolone lead compounds from a rational modification for antibacterial fluoroquinolones, a fused heterocyclic ketone corresponding to thiazolo[2,3- b][1,2,4]triazolone used as a bioisosteric replacement of the C-3 carboxylic acid group of ciprofloxacin 1, and further modification by a Claisen condensation reaction with substituted benzaldehydes formed novel fluoroquinolone C-3 fuse heterocyclic α, β-unsaturated ketones as the title compounds (6a-6r), separately. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS, and the in vitro anti-proliferative activity against human hepatoma Hep-3B cells, pancreatic Capan-1 cells and leukemia HL60 cells was evaluated by a MTT assay. The preliminary results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. In particular, compounds carrying an electron-withdrawing carboxyl (6k, 6m) or sulfonamide substituent (6q, 6r) attached to benzene ring were comparable to or better than constractive drug doxorubicin against Capan-1 cells. As such, it suggests that it is favorable for a fused heterocyclic α, β-unsaturated ketone scaffold instead of the C-3 carboxylic acid group to improve the antitumor activity of fluoroquinolones.
Anti-Bacterial Agents
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Antineoplastic Agents
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chemical synthesis
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pharmacology
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Cell Line, Tumor
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Ciprofloxacin
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analogs & derivatives
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Fluoroquinolones
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chemical synthesis
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pharmacology
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HL-60 Cells
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Humans
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Ketones
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pharmacology
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Structure-Activity Relationship
4.Synthesis and antitumor activity of fluoroquinolon-3-yl-s-triazole sulfide ketones and their derivatives from ciprofloxacin.
Li-li NI ; Qiang YAN ; Shu-min WU ; Yu-suo XIE ; Liu-zhou GAO ; Ying-jie LIU ; Wen-long HUANG ; Guo-qiang HU
Acta Pharmaceutica Sinica 2015;50(10):1258-1262
To discover an efficient strategy for the conversion of the antibacterial activity of fluoroquinolones into the antitumor activity, the three series of C-3 s-triazole-based derivatives including sulfide ketones (6a-6g), thiosemicarbazones (7a-7g) and fused heterocyclic thiazolotriazoles (8a-8g) were synthesized from ciprofloxacin (1), respectively. The structures were characterized by elemental analysis and spectral data. The antitumor activity was tested against three tumor cell lines (Hep-3B, Capan-1 and HL60) using the MTT assay. The three types of compounds all exhibited stronger anti-proliferative activities than ciprofloxacin in the test. The order of their activities was in compounds 7>8>6, and the order of selectivity against cancer cell lines was Capan-1, Hep-3B and HL60. Meanwhile, the SAR revealed that some compounds with electron-drawing group substituted such as fluoro- and nitro-phenyl compounds (6f, 7f, 8f) and (6g, 7g, 8g) displayed more significant activity than the control compounds, especially the IC50 values of thiosemicarbazone compounds 7f and 7g against Capan-1 was comparable to doxorubicin. Thus, a five-membered triazole as the C-3 bioisostere modified with the functionalized side-chain of sulfide-ketone thiosemicarbazone warrants special attention and further investigation.
Anti-Bacterial Agents
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chemistry
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Antineoplastic Agents
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pharmacology
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Cell Line, Tumor
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Ciprofloxacin
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chemistry
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Doxorubicin
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pharmacology
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HL-60 Cells
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Humans
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Ketones
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pharmacology
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Sulfides
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pharmacology
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Triazoles
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pharmacology
5.Study of cochlear hydrops analysis masking procedure in patients with Meniere's disease and otologically normal adults.
Ying-ying SHANG ; Wen-wen DIAO ; Dao-feng NI ; Zhi-qiang GAO ; Chun-xiao XU ; Feng-rong LI
Chinese Medical Journal 2012;125(24):4449-4453
BACKGROUNDThe cochlear hydrops analysis masking procedure (CHAMP) is a new diagnostic technique for Meniere's disease (MD). But its value has not been well proven. This study aimed to evaluate the diagnostic value of CHAMP for MD.
METHODSCHAMP test was taken in three populations using the Auditory Evoked Potential system delivered by Bio-logic Systems Corporation: (1) otologically normal subjects; (2) patients clinically diagnosed with definite MD; (3) patients clinically diagnosed with probable and possible MD.
RESULTSAccording to the comparison between the normal and definite MD group, if the abnormal criterion of CHAMP was defined as latency delay less than 0.3 ms, then the corresponding sensitivity was only 52%. However, if the abnormal criterion was defined as latency delay between 0.6 and 3.8 ms, then a sensitivity of 93% and a specificity of 100% can be achieved. The complex amplitude ratio showed a significant overlap between normal and definite MD group. If the abnormal criterion was defined as a complex amplitude ratio less than 0.95, the corresponding specificity was only 50%. However, if the abnormal criterion was defined as less than 0.80, the corresponding sensitivity was 60%, and the specificity was 97%. If the abnormal criterion of CHAMP was defined as latency delay less than 0.6 ms or the complex amplitude ratio less than 0.80, CHAMP result can be obtained in all subjects with good sensitivity and specificity.
CONCLUSIONSCHAMP can differentiate patients with Meniere's disease from otologically normal subjects with high sensitivity and specificity. The recommended criterion of abnormal CHAMP was a latency delay less than 0.6 ms or a complex amplitude ratio less than 0.80.
Adolescent ; Adult ; Aged ; Audiometry, Evoked Response ; Endolymphatic Hydrops ; diagnosis ; physiopathology ; Female ; Humans ; Male ; Meniere Disease ; diagnosis ; physiopathology ; Middle Aged ; Young Adult
6.The expression and significance of structural proteins, VEGF and Ang-1 in cavernous venous malformations of the body surface.
Tian-xiang OUYANG ; Si-ming YUAN ; Xin XING ; Can-rong NI ; Wei-qiang ZHENG ; Ping WEN
Chinese Journal of Plastic Surgery 2003;19(1):47-50
OBJECTIVETo study the expression and significance of structural proteins, VEGF and Ang-1 in cavernous venous malformations of the body surface.
METHODSTissue samples came from 25 cases of cavernous venous malformations, 12 cases of normal moderate veins and 12 cases of normal small veins. Envision immunohistochemical stain was used to investigate the expression of IV collagen, fibronectin, laminin, VEGF and Ang-1. The results were analyzed semi-quantitatively.
RESULTSThe distribution of structural proteins in cavernous venous malformations is similar to moderate and small veins, but the expression in venous malformations is less obviously. VEGF expression in cavernous venous malformations and small veins is stronger obviously than moderate veins. Ang-1 expression in small veins is stronger remarkably than cavernous venous malformations and moderate veins.
CONCLUSIONThe abnormal expression of structural proteins may be an important factor in etiopathology and progress of cavernous venous malformations. There is disturbance of blood vessel remodelling in the sinusoid of cavernous venous malformations, with which the less expression of Ang-1 may be related.
Angiopoietin-1 ; metabolism ; Collagen Type IV ; metabolism ; Fibronectins ; analysis ; Hemangioma, Cavernous ; metabolism ; Humans ; Laminin ; metabolism ; Vascular Endothelial Growth Factor A ; metabolism ; Veins ; abnormalities ; metabolism
7.The effects of functional magnetic resonance imaging on motor cortex function in patients with cerebral ischemic stroke
Zi-Qian CHEN ; Ping NI ; Hui XIAO ; You-Qiang YE ; Gen-Nian QIAN ; Xi-Zhang YANG ; Jin-Liang WANG ; Shang-Wen XU ; Mei NIE ; Yu SONG ; Biyun ZHANG ;
Chinese Journal of Physical Medicine and Rehabilitation 2003;0(12):-
Objective To investigate the effects of functional magnetic resonance imaging (fMRI)with acute ischemic stroke (AIS) patients,and to evaluate the relationship between brain reorganization and motor recovery.Methods Nine AIS patients and 9 healthy volunteers were assessed by fMR1 during passive finger clenching at a pace of 1 Hz.The fMRI results were analyzed using SPM2 software.Lateral indices (LIs) and activated regions were calculated,and the relationship between LI and muscle strength was examined.Results In the control group,activation was observed in the contralateral sensorimotor cortex (SMC) and the bilateral supplementary area (SMA) during the passive movement.In the AIS group,similar results were recorded dur- ing unaffected hand movement,but the ipsilateral activation areas were greater than those on the eontralateral side during movement of the affected hand.LI results confirmed that movement of the affected hand mainly elici- ted activation in the ipsilateral hemisphere.Conclusion The different fMRI manifestations of patients and nor- mal subjects reflect brain compensation,and fMRI is valuable for studying the correlation between motor function and brain reorganization.
8.A clinical pathological study on cavernous venous malformation of the body surface.
Si-ming YUAN ; Tian-xiang OUYANG ; Xin XING ; Can-rong NI ; Wei-qiang ZHENG ; Ping WEN
Chinese Journal of Plastic Surgery 2003;19(5):350-353
OBJECTIVETo investigate the clinical pathology of cavernous venous malformations of the body surface.
METHODSTissue samples of cavernous venous malformations from 42 cases were stained with hematoxylin and eosin to observe the pathologic structure. The clinical manifestations and case history were summarized accordingly.
RESULTSThere was no distribution difference of the malformation in sex and body sides, but with obvious difference in anatomic sites. The malformation occurred most frequently at the head and neck, more frequently at extremities and least frequently at the trunk. According to pathologic structure, cavernous venous malformations of the body surface can be divided into three types: the cellular, the canaliform and the mixed.
CONCLUSIONThe cause of distribution difference in anatomic sites remains unclear. Internal hemorrhage and infection may account for the increased growth and ache of the lesion. The different pathologic structure of the malformation may cause different clinical manifestations.
Adolescent ; Adult ; Aged ; Arteriovenous Malformations ; complications ; pathology ; Child ; Child, Preschool ; Female ; Humans ; Infant ; Infection ; etiology ; Male ; Middle Aged ; Pain ; etiology ; Sex Factors ; Skin ; blood supply ; pathology ; Veins ; abnormalities
9.Utility of waist-to-height ratio in detecting central obesity and related adverse cardiovascular risk among normal weight adults.
Wen-Feng SONG ; Xiao-Ni ZHONG ; Rong LUO ; Yong-Hong WANG ; Yong-Qiang LI ; Kao-Cong TIAN
Chinese Journal of Preventive Medicine 2010;44(12):1102-1105
OBJECTIVETo detect central obesity and related adverse cardiovascular disease risk factors by waist-to-height ratio (WHR) among normal weight adults in Chongqing area.
METHODSA total of 20 000 participants aged 18 - 59 from one hour economic cycle of Chongqing area were selected by group sampling method. We measured the height, waist circumference (WC), body weight, blood pressure, blood lipid and blood sugar. Body Mass Index (BMI) and WHR were computed. We analyzed the differences of the correlated indexes between non-central obesity group (WHR < 0.5) and central obesity group (WHR ≥ 0.5) of those had normal weight (18.5 ≤ BMI (kg/m(2)) < 24). And we used logistic regression method to analyze the relation between central obesity and related adverse cardiovascular risk factors.
RESULTSAmong 11 612 normal weight subjects, 1801 (15.51%) participants were normal weight central obesity. Of non-central obesity group and central obesity group, the levels of waist WC were (73.71 ± 5.91) and (84.47 ± 4.58) cm (F = 328.74, P < 0.01); diastolic blood pressure levels were (72.85 ± 10.30) and (78.22 ± 11.90) mm Hg (1 mm Hg = 0.133 kPa, F = 23.62, P < 0.01); triglyceride levels were (1.22 ± 0.95), (1.97 ± 1.91) mmol/L (F = 114.70, P < 0.01); total cholesterol levels were (4.66 ± 0.84) and (5.04 ± 0.92) mmol/L (F = 13.10, P < 0.01); high density lipoprotein levels were (1.41 ± 0.31), (1.25 ± 0.29) mmol/L (F = 29.44, P < 0.01); low density lipoprotein levels were (2.65 ± 0.74) and (3.03 ± 0.77) mmol/L (F = 9.98, P < 0.01); glycemia levels were (4.94 ± 0.82) and (5.25 ± 1.37) mmol/L (F = 47.21, P < 0.01). The results of the logistic regression analysis showed the central obesity normal weight group was 1.28 (1.02 - 1.60), 1.49 (1.20 - 1.84), 2.24 (1.92 - 2.60), 1.77 (1.53 - 2.05), 1.58 (1.15 - 2.16) and 1.31 (1.06 - 1.63) times more likely than the normal group to have significantly elevated levels of systolic blood pressure, diastolic blood pressure, triglyceride, high density lipoprotein, low density lipoprotein and blood glucose.
CONCLUSIONWHR can effectively reflect the normal weight central obesity and the risk factors of cardiovascular disease;the adverse cardiovascular disease risk was high among normal weight central obesity adults.
Adolescent ; Adult ; Body Height ; Body Mass Index ; Body Weight ; Cardiovascular Diseases ; epidemiology ; China ; epidemiology ; Female ; Humans ; Male ; Middle Aged ; Obesity ; Obesity, Abdominal ; epidemiology ; Risk Factors ; Waist Circumference ; Young Adult
10.Animal model of facial neuritis induced by herpes simplex virus.
Wen LIU ; Zhi-Qiang GAO ; Ping SHEN ; Dao-Feng NI ; Shi-Ming QUAN ; An-Ping NI ; Yun ZHANG
Chinese Journal of Otorhinolaryngology Head and Neck Surgery 2006;41(1):17-21
OBJECTIVETo study the role of herpes simplex virus type 1 ( HSV-1 ) in facial paralysis by developing an experimental animal model of viral facial paralysis.
METHODSBoth sides of posterior auricular branch of facial nerve were anatomies and incised in 66 mice. The HSV-1 was inoculated into right ear branch and fetal bovine serum was inoculated into left ear branch as control. The symmetry of mouse face was observed and scored. The temporal bones were serially sectioned and stained with hematoxylin and eosin. The extratemporal facial nerves were stained with osmium tetroxide. HSV-1 DNA in bilateral facial nerve, brain stem, trigeminal ganglion and spinal cord was detected by the polymerase chain reaction.
RESULTSTwenty-eight (42. 42%) mice developed right facial paralysis between 2 and 5 days after inoculation. Continuing 3-6 days, the facial paralysis recovered spontaneously. Thirty-eight mice had no signs of facial paralysis. Compared with the left, nerve swelling, inflammatory cell infiltration were manifested in right temporal facial nerve of paralyzed mice. The ratio of the cross-sectional area of the facial nerve to the facial canal ( FN/FC ) was significantly higher than that on the control side (P < 0.01). Demyelinated nerve fibers were seen in the right extratemporal facial nerve. Not only in paralyzed mice, but also in non-paralyzed mice, HSV DNA was detected in some nerve tissues.
CONCLUSIONSInoculating HSV-1 into posterior auricular branch of facial nerve can produce an acute and transient facial paralysis in mice. The possible pathophysiologic mechanism of the facial paralysis is viral invasion and transportation from distal branch to main trunk. Then the viral facial neuritis causes facial paralysis.
Animals ; Disease Models, Animal ; Facial Nerve ; virology ; Facial Nerve Diseases ; virology ; Female ; Herpes Simplex ; physiopathology ; Herpesvirus 1, Human ; Mice ; Mice, Inbred BALB C