2.Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment
Yang-mi CHEN ; Yan AN ; Xiang-tao DONG ; Zi-cong LU ; Jia-qiang YANG
Acta Pharmaceutica Sinica 2024;58(1):161-165
Based on the principle of molecular hybridization, fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment. The results showed that these compounds had better inhibitory effects on the tested bacteria. In particular, the activities of compounds
3.The treatment effect of ISCOM leukemia vaccine combination with 1-methyl tryptophan on tumor burden mice
Yan HUANG ; Sun WU ; Youmei ZI ; Yuan ZHANG ; Man YANG ; Dong MA ; Lishan HE
Chongqing Medicine 2016;(1):37-39
Objective Investigated the treatment effect of ISCOM leukemia vaccine combination with 1-methyl tryptophan on tumor burden mice .Methods Saponin was added lipase protein (1 mg/mL) 7 ℃ for 12 h ,adding 80 μL lipid mixed solution and 5 mL saponin solution (1 mg/mL ) to prepare ISCOM leukemia vaccine .C57BL /6 mice were randomly divided into model group , ISCOM leukemia vaccine group ,1-methyl tryptophan group and combination group ,Mice were injected FBL-3 cell to built leukemia tumor-burdened mice model .After treatment for 4 weeks ,tumors weight ,NK and Mφ and CTL cell killing activity ,serum levels of IL-10 ,IL-12 were detected .Results Tumor weight in combination group was less than 1-methyl tryptophan and ISCOM leukemia group [(0 .64 ± 0 .26)g vs .(2 .49 ± 0 .91)g ,P< 0 .01 ,(0 .64 ± 0 .26)g vs .(1 .28 ± 0 .73)g ,P< 0 .05] ;NK cell killing activity in com-bination group was higher than 1-methyl tryptophan group[(38 .41 ± 8 .27)% vs .(67 .22 ± 12 .74)% ,all P< 0 .01)] ;M φ activity in combination group was significantly higher than 1-methyl tryptophan group[(55 .69 ± 13 .69)% vs .(69 .47 ± 14 .79)% ,P< 0 .01] ;CTL activity in combination group was significantly higher than 1-methyl tryptophan group and ISCOM leukemia group[(43 .77 ± 8 .89)% vs .(69 .68 ± 11 .44)% ,P< 0 .01 ,(58 .87 ± 9 .45)% vs .(69 .68 ± 11 .44)% ,P < 0 .05] ;IL-10 in combination group were significantly lower than 1 - methyl tryptophan group and ISCOM leukemia group [(76 .2 ± 6 .82)pg /L vs .(98 .3 ± 13 .4)pg/L ,P<0 .01 ,(76 .2 ± 6 .82)pg/L vs .(202 .3 ± 44 .5)pg/L ,P < 0 .01] ;IL-12 in combination group were significantly higher than 1-methyl tryptophan group and ISCOM leukemia group[(381 .2 ± 47 .3)pg/L vs .(332 .1 ± 30 .2)pg/L ,P < 0 .05 ,(381 .2 ± 47 .3)pg /L vs . (291 .2 ± 17 .3)pg/L ,P< 0 .01] .Conclusion Combination with 1-methyl tryptophan and ISCOM leukemia vaccine has a well anti-tumor effect ,its mechanism may be through mediated and the expression of IL-12 and IL-10 .
4.Establishment and Evaluation of Hypertensive Rat Model with Excessive Accumulation of Phlegm-dampness Syndrome.
Sai WU ; Yue-hua JIANG ; Chuan-hua YANG ; Xian-qing MENG ; Dong HAO ; Ying-zi QI
Chinese Journal of Integrated Traditional and Western Medicine 2016;36(2):222-228
OBJECTIVETo observe mainfestations of syndrome and biochemical indices of hypertensive model rats with excessive accumulation of phlegm-dampness syndrome (EAPDS), and to explore its possible pathological mechanism.
METHODSEAPDS rat model was prepared in 50 Wistar rats by feeding with high fat forage. Meanwhile, a normal control group consisting of 10 Wistar rats was set up by feeding with normal forage. After 25-week continuous feeding, 22 rats with body weight (BW) and blood pressure (BP) exceeding 25% those of the control group were selected as a model group. BW, BP, blood lipids, and related serological indicators were detected in all rats. Morphological changes of target organs were observed. mRNA expression levels of leptin receptor (LepR), Janus kinase2 (Jak2), signal transducer and activator of transcription 3 (Stat3), suppressor of cytokine signaling-3 (Socs3), angiotensin II receptor type 1 (AT1), angiotensin II receptor type 2 (AT2), phosphatidylinositol 3 kinase (P13K), serine threonine kinase (Akt), nuclear factor of kappa B (NF-κBp65), inhibitor of nuclear factor kappa-B kinase α (IKKα), NF-kappa-B inhibitor β (lKKβ), NF-kappa-B inhibitor α (IKBα), and AMP-activated protein kinase (AMPK) were detected by quantitative real-time PCR (qPCR). Expression levels of AT1 and LepR in aorta were detected by immunohistochemical assay and Western blot respectively.
RESULTSCompared with the control group, BW, BP, and blood lipids increased; serum levels of leptin (Lep) , Ang II, Hcy, ET-1, TNF-α, IL-6, and p2-MG increased, but NO decreased in the model group (P < 0.05, P < 0.01). Aortal endothelial injury and smooth muscle cell proliferation occurred in the model group, accompanied with heart and renal injury. Compared with the control group, mRNA expression levels of LepR, Jak2, Stat3, Socs3, AT1 , PI3K, Akt, NF-κB p65, IKKβ, IKBα, and AMPK in aorta were up-regulated significantly (P < 0.05), while the expression of IKKa decreased (P < 0.05). Immunohistochem- ical staining showed, brownish yellow deposit of AT1 and LepR was obviously increased, with more extensively positive distribution. Western blot results showed, as compared with the control group, protein expression levels of AT1 and LepR obviously increased in the model group (P < 0.05).
CONCLUSIONSModel rats exhibited typical syndromes of EAPDS. They put up weight with fat abdomen, gloomy hair, poor appetite, hypersomnia, lowered activities , reduced food intake, loose stool, dark red tongue, white tongue with white, thick, greasy fur. Lep could be taken as one of objective indicators for evaluating hypertension rat model with EAPDS.
Animals ; Aorta ; Cell Proliferation ; Disease Models, Animal ; Hypertension ; physiopathology ; I-kappa B Proteins ; Interleukin-6 ; Leptin ; blood ; NF-KappaB Inhibitor alpha ; NF-kappa B ; Phosphatidylinositol 3-Kinases ; Rats ; Rats, Wistar ; Suppressor of Cytokine Signaling Proteins ; Transcription Factor RelA ; Tumor Necrosis Factor-alpha
5.Is nationwide special campaign on antibiotic stewardship program effective on ameliorating irrational antibiotic use in China? Study on the antibiotic use of specialized hospitals in China in 2011-2012.
Xiao-Xu, ZOU ; Zi, FANG ; Rui, MIN ; Xue, BAI ; Yang, ZHANG ; Dong, XU ; Peng-Qian, FANG
Journal of Huazhong University of Science and Technology (Medical Sciences) 2014;34(3):456-63
With dwindling number of new antibiotics and inappropriate use of antibiotics, the emergence and spread of antibiotics resistance occurs commonly in healthcare institutions worldwide. In China, antibiotics are commonly overprescribed and misused. This study is to assess the effect of the nationwide special campaign on antibiotic stewardship program (ASP) at specialized hospitals in China by investigating prescription information from 2011 to 2012. Data on the hospital consumption and prescription of systemic antibiotics were obtained from four specialized hospitals, including maternity, children's, stomatological and cancer hospitals. Systematic random sampling was used to select outpatient prescriptions and inpatient cases. A total of 105 specialized hospitals in 2011 and 121 specialized hospitals in 2012 were analysed. The defined daily doses (DDDs) per 100 inpatient days, the percentage of antibiotic use in outpatient prescriptions, and the percentage of antibiotic use in inpatient cases were used as measurements of antibiotic use. The overall antibiotic use density in the selected hospitals decreased between 2011 and 2012 from 39.37 to 26.54 DDD/100 inpatient days (P<0.001). The percentage of antibiotic use in outpatient prescriptions (range: 24.12%-18.71%, P=0.109) and inpatient cases (64.85%-60.10%, P=0.006) also decreased within the two years. Significant changes were observed among regions and different hospitals within the two years. And antibiotic consumption was correlated with the type and size of specialized hospital in 2012, but not with the regions. This analysis of antibiotic consumption of specialized hospitals allows relevant comparisons for benchmarking and shows that national ASP has improved antibiotic rational use in China. The data will assist policymakers in formulating effective strategies to decrease antibiotic overuse and identify areas that require further work.
6.Study on causes and treatment of repeated vulvovaginitis in girlhood
Di-Kai ZHANG ; Xiu-Yun LI ; Dong-Zi YANG ; Jian-Quan KUANG ;
Chinese Journal of Obstetrics and Gynecology 2001;0(07):-
Objective To explore the causes and treatment of repeated vulvovaginitis in girlhood in order to improve its prevention and treatment.Methods Fifty-one girls with repeated vulvovaginitis(age≤10 years)admitted to The Second Affiliated Hospital of Sun Yat-sen University from Jan.1990 to Nov.2004 were reviewed retrospectively.Results We found 28 girls(55%)suffering from non-specific vulvovaginitis and 14 ones(27%)suffering from posterior recto-vaginal fistula with in 51 patients.Five girls(10%)were smitten with vulval ulcer and 3 ones(6%)had been were found with vaginal foreign bodies.One girl(2%) was smitten with adhesion of labia minora.The vaginal discharges taken from 21 girls were cultured. Seventeen cases found bacteria.The positive rate of bacteria culture in the 21 cases reached 81%,in which, E.coli accounted for 5 cases(24%),staphylococcus and streptococcus accounted for 3 cases(14%) respectively.Patients suffered from non-specific vulvovaginitis and vulval ulcer accepted external lotion, antibiotic ointment or combining with antibiotics.Patients suffered from posterior recto-vaginal fistula accepted fistulectomy.Three girls who found vaginal foreign bodies took out of foreign bodies by hysteroscopo.Fifty-one girls all were cured after appropriate therapy.Conclusions Vulvovaginitis is the most common gynecologic diagnosis in girlhood.The principal cause of repeated invasion is non-specific vulvovaginitis and the secondly one is posterior recto-vaginal fistula.It need overhaul during the diagnosis.It is very availability to use hysteroscopy and do bacteria culture+antibiotic sensitivity test for repeated pediatric vulvovaginitis.
7.Diagnostic value of ovarian morphology by ultrasonography in pubertal polycystic ovary syndrome
Ya-Xiao CHEN ; Dong-Zi YANG ; Lin LI ; Xiao-Li CHEN ; Yu LI ;
Chinese Journal of Obstetrics and Gynecology 2000;0(09):-
0.05).Setting the threshold of MOV at 6.4 cm~3 offered the best compromise between sensitivity (84.8%)and specificity(87.5%),and setting the threshold of MaxOV at 8.6 cm~3 offered the best compromise between sensitivity(75.8%)and specificity(95.2%)and setting the threshold of MFN at 8 offered the best compromise between sensitivity(86.7%)and specificity(78.3%).Conclusions Ovarian morphology by ultrasonography yields satisfactory diagnostic accuracy for adolescent PCOS.Taking MOV≥ 6.4 cm~3 or MaxOV≥8.6 cm~3 or MFN≥8 as an ultraphonic criterion for pubertal PCOS offer the best compromise between sensitivity and specificity.
8.Examination of point mutations within the ABL kinase domine region of BCR/ABL in patients with chronic myeloid leukemia who develop imatinib resistance
Dong-Guang YANG ; Ri ZHANG ; Jian-Nong CEN ; Zi-Ling ZHU ;
Chinese Journal of Laboratory Medicine 2003;0(11):-
Objective To investigate the point mutations within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia who develop imatinib resistance.Methods We collected a total of 17 bone marrow samples obtained from 11 patients who showed hematology resistance (n = 7)or cytogenetic refractoriness(n = 4).A long semi-nest PCR method was used to amplify the ABL kinase domain of the BCR/ABL allele.After two rounds of PCR reactions,we got a fragment of 863 bases The PCR products were purified and followed by sequencing.Results In total,we find three point mutations presented in all patients tested G250E,E255K and T315I.The mutation rate of hematology resistance is 4/ 7,and 95% confidence interval was 8%-90%,while mutation rate of cytogenetic refractoriness 1/4,95% confidence interval 1%-81%.For those patients whose samples were available,no single mutation were determined before imatinib resistance emerged.Conclusions There is high frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia.It's good for patients to switch to another therapeutic strategy when the mutations are detected.
9.Construction of recombinant gene adenovirus encoding enhanced green fluorecence protein-peroxisome proliferator-activated receptor gamma2 fusion protein and its expression in bone marrow mesenchymal stem cells.
Li-zi LIAO ; Jin-gang XIAO ; Miao-miao YANG ; Zi-ren KONG ; Qin-ce SUN ; Wei-dong TIAN
West China Journal of Stomatology 2010;28(4):430-434
OBJECTIVETo construct mouse enhanced green fluorecence protein (EGFP) -peroxisome proliferator-activated receptor (PPAR)gamma2, and to detect EGFP-PPARgamma2 expression in infected mouse bone marrow mesenchymal stem cells (BMSC).
METHODSCut the fragment of PPARgamma2 from the expression plasmid pcDNA flag PPARgamma2, then cloned the gene fragment into pEGFP-C1 and pEGFP-N1 vector. Subsequently, subclone the fragment EGFP-PPARgamma2 from pEGFP-C1-PPARgamma2 into the shuttle plasmid DC315. HEK293 cells were co-transfected with the constructed recombinant shuttle plasmid DC315-EGFP-PPARgamma2 and large adenovirus helper plasmid pBHGlox deltaE1, 3Cre in mediation of liposome. The obtained replication-defective recombinant adenovirus Ad-EGFP-PPARgamma2 was confirmed. Then it was propagated in HEK293 cells. After the BMSC were transfected for 72 h, adipogenic differentiation was demonstrated.
RESULTSHEK293 cells were transfected with the pEGFP-C1-PPARgamma2 or pEGFP-N1-PPARgamma2 in mediation of liposome. The former green fluorescence protein was better than the latter by fluorescence microscope. The recombinant plasmids were digested and identified. Western blot analysis showed the expression of EGFP-PPARgamma2 in vitro. EGFP-PPARgamma2 protein was detectable in the nucleus of BMSC.
CONCLUSIONThe recombinant adenovirus encoding EGFP-PPARgamma2 fusion protein was successfully constructed, which provided a basis for application of EGFP-PPARgamma2 gene to adenovirus-mediated gene therapy.
Adenoviridae ; Animals ; Bone Marrow Cells ; metabolism ; Genetic Vectors ; Green Fluorescent Proteins ; metabolism ; HEK293 Cells ; Humans ; Mesenchymal Stromal Cells ; metabolism ; Mice ; PPAR gamma ; metabolism ; Recombinant Proteins ; metabolism ; Transfection
10.Modified Graeb criteria for predicting the post-hemorrhagic hydrocephalus in intraventricular hemorrhage.
Zhi SONG ; Qi-Dong YANG ; Xiao-Hong ZI ; Xuejun FAN
Chinese Medical Sciences Journal 2004;19(2):138-141
OBJECTIVETo set up a new grading system of intraventricular hemorrhage (IVH) and determine the value of predicting the probability of post-hemorrhagic hydrocephalus (PHH) in IVH.
METHODSWe first modified the Graeb criteria, then compared the value of prediction for PHH assessed by the Graeb criteria with the modified Graeb criteria. One hundred and thirty one IVH patients were divided into two groups: the upper group (n = 67) and the lower group (n = 64). Gold standard of PHH was assessed by CT scan or by out-drainage. The diagnostic parameters such as sensitivity (SE), specificity (SP) were analyzed. In the cutoff point of SE and SP curves, diagnostic efficiency (DE), and Kappa value (K) were analyzed. The probability of PHH was estimated by binary logistic regressions.
RESULTSIn all ventricular group, to Graeb criteria in the cutoff point, SE, SP, and K was 0.78, 0.84, and 0.60; and to modified Graeb criteria SE, SP, and K was 0.90, 0.84, and 0.74 respectively. The probability of PHH from point of 3-12 was 0.011, 0.032, 0.085, 0.212, 0.435, 0.689, 0.865, 0.949, 0.981, and 0.994 respectively according to modified Graeb criteria.
Aged ; Cerebral Hemorrhage ; complications ; diagnostic imaging ; Female ; Humans ; Hydrocephalus ; diagnosis ; diagnostic imaging ; etiology ; Logistic Models ; Male ; Middle Aged ; Sensitivity and Specificity ; Tomography, X-Ray Computed