1.Experimental study on the apoptosis of gastric cancer cells induced by adenovirus mediated fusion gene system driven by KDR promoter
Qiang LI ; Zonghai HUANG ; Guoqiang SU
Medical Journal of Chinese People's Liberation Army 2001;0(10):-
Objective To study the selective tumoricidal effect of adenovirus (Ad)-mediated fusion gene system driven by kinase domain-containing (KDR) promoter on human stomach adenocarcinoma SCG7901 cells, and to observe its apoptosis induction effect. Methods Both the AdEasy-KDR-CDglyTK cells with KDR-expressing SCG7901 cells and non KDR-expressing HepG2 cells were reconstructed, and then they were treated with the pro-drugs 5-FC and/or GCV at different concentrations. The killing effects of the transfection on the cells were evaluated. Flow cytometry was employed to determine the cell cycle distribution, and Hooechest/PI stain and electron microscopy performed to observe the pathological changes of cells. Results The green fluorescent protein (GFP) was observed in 95% of the infected SCG7901 and HepG2 cells when the multiple of infection (MOI) of the Ads was 100. No significant difference on the growth feature was found among the transfected SCG7901, HepG2 and untransfected SCG7901 and HepG2 cells. The infected cells exhibited different sensitivities to the two pro-drugs: SCG7901 cells infected with rAd were highly sensitive to the pro-drugs, while the infected HepG2 cells were not (P
2.Synthesis and antitumor activity of fluoroquinolone C-3 s-triazole Schiff-base carboxylic acid derivatives from pefloxacin (X)
Huili ZHANG ; Ke LI ; Hui ZHAO ; Guoqiang HU ; Wenlong HUANG
Journal of China Pharmaceutical University 2017;48(2):167-171
To explore a new strategy for further optimization to the C-3 bioisteric heterocyclic ring of fluoroquinolones,twelve novel fluoroquinolone C-3 s-triazole Schiff-base carboxylic acid derivatives(7a-71) were designed and synthesized with both functionalized sulfanylacetic acid and Schiff-base moieties as the modified side-chain for the C-3 bioisosteric s-triazole ring of pefloxacin(1).The structures were characterized by elemental analysis and spectral data,and the in vitro anti-tumor activity of the title compounds against SMMC-7721,L1210 and HL60 cell lines was evaluated.The preliminary pharmacological results demonstrated that the title compounds possessed more significantly anti-proliferative activity than either the parent 1 or the corresponding amine intermediates(6).In particular,the title compound bearing a fluorine atom (7j) and compound bearing a nitro group attached to benzene ring (71) were comparable to the control doxorubicin against SMMC-7721 cells with an IC50 value of micro-molar concentration,respectively.It suggests that s-triazole ring modified with functional side-chain moieties instead of the C-3 carboxylic group is favorable to the improvement of antitumor activity.
3.Use of rats mesenchymal stem cells modified with mHCN2 gene to create biologic pacemakers.
Jin, MA ; Cuntai, ZHANG ; Shen, HUANG ; Guoqiang, WANG ; Xiaoqing, QUAN
Journal of Huazhong University of Science and Technology (Medical Sciences) 2010;30(4):447-52
The possibility of rats mesenchymal stem cells (MSCs) modified with murine hyperpolarization-activated cyclic nucleotide-gated 2 (mHCN2) gene as biological pacemakers in vitro was studied. The cultured MSCs were transfected with pIRES2-EGFP plasmid carrying enhanced green fluorescent protein (EGFP) gene and mHCN2 gene. The identification using restriction enzyme and sequencing indicated that the mHCN2 gene was inserted to the pIRES2-EGFP. Green fluorescence could be seen in MSCs after transfection for 24-48 h. The expression of mHCN2 mRNA and protein in the transfected cells was detected by RT-PCR and Western blot, and the quantity of mHCN2 mRNA and protein expression in transfected MSCs was 5.31 times and 7.55 times higher than that of the non-transfected MSCs respectively (P<0.05, P<0.05). I(HCN2) was recorded by whole-cell patch clamp method. The effect of Cs(+), a specific blocker of pacemaker current, was measured after perfusion by patch clamp. The results of inward current indicated that there was no inward current recording in non-transfected MSCs and a large voltage-dependent inward and Cs(+)-sensitive current activated on hyperpolarizations presented in the transfected MSCs. I(HCN2) was fully activated around -140 mV with an activation threshold of -60 mV. The midpoint (V(50)) was -95.1+/-0.9 mV (n=9). The study demonstrates that mHCN2 mRNA and protein can be expressed and the currents of HCN2 channels can be detected in genetically modified MSCs. The gene-modified MSCs present a novel method for pacemaker genes into the heart or other electrical syncytia.
4.Case-control Study on Small Splint and Plaster External Fixation after Closed Manipulative Reduction in the Treatment of Elderly Type C Colles Fractures
Ayong HUANG ; Guoqiang LI ; Yuzhong SUN ; Qingsheng WU
Chinese Journal of Information on Traditional Chinese Medicine 2014;(7):25-27,28
Objective To compare the clinical effects of small splint fixation after closed manipulative reduction with plaster external fixation in the treatment of elderly type C Colles fractures.Methods Totally 96 elderly patients with type C Colles fractures were randomly divided into two groups, 48 patients in each group. Both groups were treated with closed manipulative reduction. The fractures were externally fixed with splint in the treatment group, and those were externally fixed with pipe plaster in the control group. The figure of radius length, palmar tilt and ulnar deviation were detected respectively in pre-reduction, the same day with reduction, and the day when external fixation was removed (6th week), in order to evaluated the drop of anatomical position. The therapeutic effects were evaluated according to Gartland-Werley wrist score when external fixation was taken off after 6 months.Results In both groups, figures of radius length, palmar tilt and ulnar deviation evidently increased in the day after reduction and the day of external fixation removal, compared with pre-reduction (P<0.05). Compared with the day after reduction, the radius length, palmar tilt and ulnar deviation of the day of external fixation removal all dropped in both groups (P<0.05). But the drop degree in control group was significantly higher than treatment group (P<0.05). For the joint function, 9 cases for excellent, 26 for good, 6 for fair, and 4 for bad in the therapy group. The excellent and good rate was 77.8% (35/45). In the control group, 4 cases for excellent, 22 for good, 10 for fair and 9 for bad. The excellent and good rate was 57.8% (26/45). The curative effect of treatment group was remarkably superior to control group (P<0.05).Conclusion Closed manipulative reduction combined with splint external fixation is more effective than pipe plaster in treatment of elderly type C Colles fractures.
5.Drug-resistance of Enterobacter cloacae and Its Genes Encoding Aminoglycosides Modifying Enzymes
Hezan HUANG ; Guoqiang ZHANG ; Wenqing ZHANG ; Yiming MAO
Chinese Journal of Nosocomiology 2009;0(19):-
OBJECTIVE To investigate the drug-resistance of Enterobacter cloacae(ECL) and its carrying rate of gene encoding aminoglycosides modifying enzymes(AMEs).METHODS Totally 132 clinically isolated ECL strains were identified with VITEK-32.Their drug susceptibility was tested with K-B disc diffusion.The presence of ESBLs and AmpC was tested with three dimensional test.The genes encoding AMEs were detected with PCR and confirmed by sequence.RESULTS All strains of ECL were susceptible to IMP and MER.The resistance rate to AMK,LVX,FEP,CFS and CIP was 21.2%,35.6%,37.9%,46.2% and 48.5%,respectively with gradually increasing.Their resistance rate to other antibiotics ranged from 50.0% to 87.7%.Among 132 strains of ECL,45 strains producing ESBLs,accounted for 34.1%,27 strains producing AmpC,accounted for 20.5%,11 strains producing ESBLs and AmpC,accounted for 8.3% and 49 strains producing neither ESBLs nor AmpC,accounted for 37.1%.Seven strains without positive detection of ESBLs were resistant to CTX and CAZ,but carried the genes of resistance to TEM and SHV.The detection rate of genes encoding AMEs was about 62.1%,among which subtypes of aac(6′)-Ⅰb dominated with detection rate of 51.5%.Meanwhile the detection rate of subtype aac(3)-Ⅰ,aac(3)-Ⅱ,aac(6′)-Ⅱ,ant(3″)-Ⅰ,ant(2″)-Ⅰ and aph(3′)-Ⅵ was 15.9%,12.9%,18.9%,37.1%,6.8% and 9.8%,respectively.The detection rate of carrying more than two types of AMEs was about 89.0%.There were 5 strains of presenting phenotypic resistance without detection of genes encoding AMEs.CONCLUSIONS The clinically isolated ECL strains are not only severe resistant to drug and but also multi-drug resistant.The carrying rate of genes encoding ESBLs,AmpC and AMEs is higher than estimated which is the leading cause of resistance to antibiotics.
6.An analysis of victim's help-seeking behavior of domestic violence
Yuping CAO ; Yalin ZHANG ; Shichang YANG ; Guoqiang WANG ; Guoping HUANG
Chinese Journal of Behavioral Medicine and Brain Science 2011;20(3):264-266
Objective To analysis the victim's help-seeking behavior of domestic violence. Methods Using a multi-stage sampling strategy,306 victims of domestic violence were randomly selected and face-to-face interviewed. A self-designed help-seeking questionnaire of domestic violence was administered. Results 33.7%victims felt nowhere to seek help. The three leading helpers they seek were the other family member (34.6%),neighbor and friend( 17.0% ) and community office ( 12.5% ) ,and the community office had highest prevalence of effect (71. 1% ). The prevalence of seeking help from other family member and Women's Federation were highest in urban victims (P<0.01) ,and seeking help from community office was highest in rural victims (P<0.01). The three leading helpers were other family member (27.3%) ,community office ( 15.8% ) and neighbor and friend ( 10.9% ) by male victims, and other family member ( 38.0% ), neighbor and friend ( 20.0% ) and community office ( 10.8% ) by female victims. The prevalence of seeking help from neighbor and friend was higher in female than in male ( 20.0% vs 10.9%, x2 = 3. 980, P< 0.05 ). Adult victims seek help from other family member were less than children and the elderly (31.6% vs 42.0% and 46.9%, x2 =5.993, P<0.05),and the elderly seek help from community office were more than adults and children (28.1% vs 12. 1% and 4.0%, x2 =9.930, P<0.01 ). The victims with higher level of education were with higher prevalence of feeling nowhere to seek help (47.8%). Seeking help from other family member and community office were most in victims with lower level of education( 38.5% and 24.0% ,respectively) and were least in victims with higher level of education ( 17.4% and 0,respectively, P < 0.05, P < 0. 01 ). Conclusion Help-seeking behaviors of victims of domestic violence are varied by geographic settings,age,gender and education levels.
7.The effects of enhanced external counterpulsation on arterial elasticity in patients with cerebral ischemic stroke
Guoqiang ZHOU ; Zongqing HUANG ; Jianwei XIAO ; Yuguang WANG ; Xiaokun YAN
Chinese Journal of Nervous and Mental Diseases 2014;(7):385-389
Objectives To examine the effects of enhanced external counterpulsation on arterial elasticity in stroke patients to provide clinical evidence for secondary prevention of patients with cerebral ischemic stroke. Methods Total 192 patients with ischemic stroke were enrolled and then divided into the EECP (n=107) and control (n=85) group. Auto-matic measurement synchronous atherosclerosis detector was use to measure brachial-ankle pulse wave velocity (BaP-WV) and cardio-ankle vascular index (CAVI). The difference of BaPWV and CAVI were evaluated before, at 36 hours and one month after EECP. Results The BaPWV and CAVI significantly decreased at 36 hours and 1 month after treat-ment in EECP groups compared to either pre-therapy or control groups (all P<0.05). Conclusions EECP can signifi-cantly reduce the BaPWV and CAVI and improve the arterial elasticity in patients with cerebral ischemic stroke. Thus, arterial elasticity may be an important index to evaluate the effects of EECP on cerebral ischemic stroke.
8.Design, synthesis, antibacterial and anti-cell proliferation activities of 1,2,4triazino3,4-h 1,8naphthyridine-8-one-7-carboxylic acid derivatives.
Liuzhou GAO ; Tao LI ; Wenlong HUANG ; Hui ZHAO ; Guoqiang HU
Acta Pharmaceutica Sinica 2015;50(3):332-6
To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.
9.Synthesis, antitumor activity and SAR of C-3 oxadiazole sulfanylacetylhydrazone-substituted fluoroquinolone analogues.
Liuzhou GAO ; Yusuol XIE ; Tao LI ; Wenlong HUANG ; Guoqiang HU
Acta Pharmaceutica Sinica 2014;49(12):1694-8
To explore an efficient strategy for the conversion of antibacterial fluoroquinolones into antitumor fluoroquinolones, an azole heterocyclic ring of oxadiazole instead of the C-3 carboxylic acid group with a functionalized hydrazone group as a modified side-chain, fifteen novel 2-(fluoroquinolon-3-yl)-oxadiazole-5- sulfanylacetylhydrazone derivatives 7a-7o were designed and synthesized on the basis of the pharmacophore hybridization principle from pefloxacin, separately. The structures for fifteen title compounds were characterized by elemental analysis, 1H NMR and MS, and their in vitro antitumor activity against Hep-3B cell line was evaluated by a MTT assay. The results showed that the title compounds exhibited more significantly inhibitory activity than that of the parent pefloxacin, in which compounds with electron-withdrawing group attached on aryl ring had more potency than that of compounds with electron donating group, especially compounds with a carboxylic substituent were comparable to comparison doxorubicin. It suggests that it is favorable for an improvement of antitumor activity to remain a carboxylic acid unit at the aromatic ring.
10.The size of thyroid nodules contributing to the accuracy of fine-needle aspiration cytology
Bin LU ; Xiangdong YOU ; Pintong HUANG ; Guoqiang MO ; Minqiang PAN
Chinese Journal of Ultrasonography 2014;23(9):778-781
Objective To evaluate the association of the size of thyroid nodules and accuracy of fineneedle aspiration cytology in diagnose of thyroid nodules.Methods 691 thyroid nodules in 630 patients pathologically confirmed were retrospectively analyzed in our hospital.All imaging data of preoperative ultrasound-guided FNAC were collected in our review.Yields of FNAC were divided into six levels according to the classification criteria of the Bethesda system(level Ⅰ,insufficient material or nondiagnosed;level Ⅱ,benign ; level Ⅲ,atypical hyperplasia; level Ⅳ,follicular neoplasm ; level Ⅴ,suspicious for malignancy; level Ⅵ,malignant),>level Ⅳ was the malignant cytologic criteria for diagnosis of thyroid nodules.According to the maximal diameter of thyroid nodules,the nodules were divided into group A(L≤0.5 cm),group B(0.5 cm<L<1.0 cm) and group C(L≥1.0 cm).Postoperative pathologic results were taken as the gold standard.Results Of 691 nodules,there were 176(25.47%),298(43.13%) and 217(31.40%) in group A,group B and group C respectively.Among the three groups,accuracy of ultrasound-guided FNAC in group B (90.94 %) was higher than in group A(80.11%) and group C(83.41 %),with statistically significant(P <0.05).There was not statistically different between group A and group C(P >0.05).The specificity,positive predictive value and negative predictive value were not statistically different among three groups(P >0.05).Conclusions The size of thyroid nodules was partly associated with accuracy of ultrasound-guided FNAC.