Exosome-mediated lnc-ABCA12-3 promotes proliferation and glycolysis but inhibits apoptosis by regulating the tolllike receptor 4uclear factor kappa-B signaling pathway in esophageal squamous cell carcinoma

Esophageal squamous cell carcinoma (ESCC) is a kind of malignant tumor with high incidence and mortality in the digestive system. The aim of this study is to explore the function of lnc-ABCA12-3 in the development of ESCC and its unique mechanisms. RT-PCR was applied to detect gene transcription levels in tissues or cell lines like TE-1, EC9706, and HEEC cells. Western blot was conducted to identify protein expression levels of mitochondrial apoptosis and toll-like receptor 4 (TLR4)uclear factor kappa-B (NF-κB) signaling pathway. CCK-8 and EdU assays were carried out to measure cell proliferation, and cell apoptosis was examined by flow cytometry. ELISA was used for checking the changes in glycolysis-related indicators.Lnc-ABCA12-3 was highly expressed in ESCC tissues and cells, which preferred it to be a candidate target. The TE-1 and EC9706 cells proliferation and glycolysis were obviously inhibited with the downregulation of lnc-ABCA12-3, while apoptosis was promoted. TLR4 activator could largely reverse the apoptosis acceleration and relieved the proliferation and glycolysis suppression caused by lnc-ABCA12-3 downregulation. Moreover, the effect of lnc-ABCA12-3 on ESCC cells was actualized by activating the TLR4/NF-κB signaling pathway under the mediation of exosome. Taken together, the lnc-ABCA12-3 could promote the proliferation and glycolysis of ESCC, while repressing its apoptosis probably by regulating the TLR4/NF-κB signaling pathway under the mediation of exosome.

The establishment of a prognostic model of thyroid cancer based on alternative splicing events and the study of its regulatory network / 中华检验医学杂志

Objective:To analyze the alternative splicing (AS) events of patients with thyroid carcinoma (THYC) and explore the correlation between AS events and the prognosis of THYC.Methods:The clinical data and the Percent Splice In (PSI) value of AS events of THYC were downloaded from The Cancer Gene Atlas (TCGA) database and the TCGA SpliceSeq database respectively. The occurrence of seven kinds of AS events including AA, AD, AF, AP, ME, ES and RI in THYC was investigated and the matrix of AS events and survival data was constructed. Univariate Cox regression analysis was used to screen AS events related to prognosis of THYC. To avoid over-fitting, the least absolute shrinkage and selection operator (LASSO) regression analysis was performed. Then Multivariate Cox regression analysis was used to construct prognosis model. Kaplan-Meier curve and receiver operating characteristic (ROC) curve were performed to evaluate the prognosis ability of the risk model. We also used Pearson correlation analysis to select splicing factors (SF) which were correlated with survival associated AS events. Above SF genes were enrolled to gene ontology (GO) enrichment and KEGG pathway analysis.Results:A total of 10 447 genes and 45 150 AS events in 507 THYC patients were found in the present study. Among them, ES was the main type (38.84%) and ME was the type with the least frequency (0.51%). Totally 1 842 AS events associated with prognosis of THYC patients were identified. Three AS events including USHBP1-48249-AA、CACNB1-40626-AT and BEX5-89679-AP were selected to construct the prognosis model. The risk score of 0.807 was indicated as the best cut-off value of prognosis model. The patients were divided into high-risk group (240 cases) and low-risk group (241 cases) based on the risk score. The results demonstrated that the risk model could be used as a valuable prognostic factor for THYC ( P<0.001, AUC=0.929). The SF-AS network was constructed and several SF genes, including CDK12, RBM25, DDX39B, SRRM2 and DDX46 were identified as hub genes. Conclusions:The risk model based on 3-AS events was valuable prognosis predictor of THYC. The SF-AS network provided new insight for the exploration of tumorigenesis and development of THYC.

Research Advances in the Effect of Mechanical Regulation of Long-Chain Non-Coding RNAs on Osteogenic Differentiation of Mesenchymal Stem Cells / 医用生物力学

With the development of the 3rd-generation high-throughput sequencing technology and tissue engineering, recent studies show that many long-chain non-coding RNAs (LncRNAs) have played an important role in osteogenic differentiation of mesenchymal stem cells (MSCs). LncRNAs, which are involved in the regulation of mechanical regulation, further regulate bone-related cell functions and play a regulatory role at multiple levels, including transcription, post-transcriptional and epigenetic. LncRNAs may be involved in the osteogenic differentiation and bone remodeling of MSCs, the regulation of bone-related cell functions as a mechanical response molecule, as well as the pathological process of skeletal diseases.

Research progress of comprehensive assessment tools in home care service / 中华全科医师杂志

A comprehensive assessment tool for home care can help to determine the service needs.This article summarizes some of the advanced assessment scales that have been internationally applied for the home health care and to discuss the direction for development of the assessment tools in China.

Measurement of effective constituents contents in rhubarb by capillary electrophoresis / 重庆医学

Objective To adopt the capillary electrophoresis(HPCE) for detecting the contents of emodin,chrysophanol and rhein in the extract of rheum officinale.Methods The detection was executed with a fused-silica capillary column(67.4 cm× 75.0 μm,effective length 51.0cm) as the separation column.The buffer solution consisted of 60 mmol/L Na2B4O7,40 mmol/L Na2CO3 and 40 mmol β-cyclodextrin(pH 8.9).The detection wavelength was 254 nm.Results RSD of precision in emodin,chrysophanol and rhein was 1.79％,4.46％ and 2.30％.respectively The linear range of 3 components was 1.1-19.0 mg/mL;the average recovery rates of emodin,chrysophanol and rhein were 100.14 ％,99.65 ％ and 98.44 ％ respectively,RSD was 2.43 ％,2.54 ％ and 2.02％ respectively(n=3).Conclusion The method can be used in the content determination of rheum officinale extract.

Degradation behavior and compatibility of micro, nanoHA/chitosan scaffolds with interconnected spherical macropores.

Hydroxyapatite/Chitosan (HA/CS) composite have significant application in biomedical especially for bone replacement. Inorganic particle shape and size of composite affect the scaffold mechanical property, biological property, and degradation. The aim of this study was to fabricate HA/CS scaffold with good pore connectivity and analyze their biological, degradation properties. Microhydroxyapatite/chitosan (mHA/CS) and nanohydroxyapatite/chitosan (nHA/CS) composite scaffolds with interconnected spherical pore architectures were fabricated. Composite scaffolds structure parameters were analyzed using micro CT. Cell proliferation and morphology were tested and compared between two scaffolds using mouse osteoblastic cell line MC3T3-E1. To research the composite degradation in lysozyme PBS solution, degradation rate and reducing sugar content were tested, and scaffolds morphology were observed by SEM. The results showed that microHA and nanoHA were fabricated by being calcined and synthesis methods, and their infrared spectra are very similar. EDAX composition analysis demonstrated that both of microHA and nanoHA were calcium deficiency HA. Micro-CT results demonstrated the scaffolds had interconnected spherical pores, and the structure parameters were similar. Cell viabilities were significant increased with cultured time, but there were no significant difference between microHA/CS and nanoHA/CS scaffolds. Scaffold structure was gradually destroyed and inorganic composition HA particles are more prominent with degradation time. SIGNIFICANCE: (1) Inorganic particle shape and size of composite affect the scaffold mechanical property, biological property, and degradation. NanoHA/CS and microHA/CS scaffolds with good pore connectivity were fabricated and their biological, degradation properties were studied in this manuscript. (2) The scaffold with interconnected porosity construct provides the necessary support for cells to proliferate and maintain their differentiated function, and its architecture related to the structure and morphology of new bone. Polymer scaffolds were fabricated by the technique of compression molding and particulate leaching method, and paraffin microspheres were used as the porogen. (3) MicroHA/CS and nanoHA/CS composite scaffolds are potential materials for use in bone tissue engineering.

Bibliometric Analysis of Drug Therapy of Rheumatoid Arthritis Based on WoS Core Collection / 中国药房

OBJECTIVE:To investigate the development of drug therapy of rheumatoid arthritis,and to provide reference for the study of this field in China. METHODS:All literatures were retrieved during 2005-2016 using Web of ScienceTM(called"WoS"for short)core collection as database,"Rheumatoid arthritis""Rheumatoid-arthritis""Drug therapy""Medication"as subjects,set-ting literature type as"Article""Review". Bibliometric analysis method was used to list and analyze literatures about drug therapy of rheumatoid arthritis by annual number of articles published,source journals,subjects,agencies,authors and hot issues. RE-SULTS:A total of 2 528 literatures were retrieved from WoS core collection. The number of literatures showed an overall trend of growth.Those literatures came from more than 800 journals,among which top 10 journals published 689 literatures about drug ther-apy of rheumatoid arthritis(27.25%).A total of 18 subjects were involved,and the number of literatures in"Clinical medicine"was the largest,with 1 884 literatures(74.53%).A total of 3 431 research institutions were involved,and the largest number of literatures were issued by the Harvard University,with 68 literatures in total(2.69%). A total of 14 325 researchers were in-volved,and top 10 researchers published 240 literatures about drug therapy of rheumatoid arthritis(9.49%). The frequency of 25 keywords was greater than or equal to 100 times,that of 12 was greater than or equal to 150 times."Rheumatoid-arthritis"had the highest frequency(1 740 times). In basic scientific index(ESI)database,there were 35 literatures with high citation fre-quency. CONCLUSIONS:With the literatures of rheumatoid arthritis therapy increasing year by year,the focus of research in this field is focused on the diagnosis of rheumatoid arthritis and clinical efficacy. In China,no institution or author enters the world front rank in this research field.Attention should be paid to the clinical study on drug therapy of rheumatoid arthritis.

The mechanical and biological responses of MC3T3-E1 cells under hypergravity / 医用生物力学

Objective To explore the effect of hypergravity on morphology and osteogenesis function of preosteoblast MC3T3-E1 ceils.Methods The cultured MC3T3-E1 cells under hypergravity by different loading forces were divided into five groups,including control group,5 g group,10 g group,15 g group and 20 g group.The experimental groups were loaded for 30 min each time in 3 successive days,and the control group with no g-value was synchronously exposed to the same surrounding.The morphology of cytoskeletal protein was observed by phalIoidin staining,The alkaline phosphatase (ALP) content was examined by ALP activity assay kit,the gene expression of ALP,collagen Ⅰ (Col Ⅰ),osteocalcin (OC),runt-related transcription factors (Runx2) was measured by real-time quantitative PCR,and the protein expression of Col Ⅰ and OC was tested by Western blotting.Results Under the condition of hypergravity,cell body of osteoblast became thinner,but its surface area increased significantly;with the structure of skeletal arrangement becoming loose,actin microfilament structure reduced so that the orderly arrangement of actin-like dispersion lowered.The gene expressions of related indicators of osteogenic differentiation including ALP,Col][,OC,Runx2 were significantly up-regulated,which was the same as Col Ⅰ protein and OC protein after hypergravity loading.A very minute quantity of small red-orange nodules was found in the control group,while the cells in experimental groups after hypergravity loading obviously formed various sizes of red-orange nodules.Conclusions Under hypergravity,changes in osteoblast morphology can be triggered by rearrangements of skeletal structure.Furthermore,osteoblast maturation and differentiation can be stimulated effectively by up-regulating differentiation-related gene and protein expressions.

Clinical characteristics of patients with hyperthyroidism complicated with acute cerebral infarction and evaluation on prognosis and safety of intravenous thrombolysis treatment / 吉林大学学报(医学版)

Objective:To analyze the clinical characteristics of the patients with hyperthyroidism complicated with acute cerebral infarction, and to evaluate the prognosis and safety of intravenous thrombolysis treatment in the patients with hyperthyrodism complicated with acute cerebral infarctron within time window for thrombolysis. Methods:The clinical materials of patients with acute cerebral infarction treated with intravenous tissue plasminogen activator (rt-pA)were retrospectively analyzed.All patients were divided into hyperthyroidism group (n=41) and non-hyperthyroidismin group (n=160) according to whether complicated with hyperthyroidism.The general imformation,the area of cerebral infarction and intracranial hemorrhage of the patients in two groups were analyzed.Results:The NHISS score of the patients in hyperthyroidism group was higher than that in non-hyperthyroidism group for the first time(P0.05).The proportions of the different infarction sizes had significant differences between two groups (P 0.05).Conclusion:The patients with acute cerebral infarction complicated with hyperthyroidism could benefit from intravenous thrombolysis, without the increasing of incidence of spontaneous intracranial hemorrhage (sICH) and SHA.

Detection of acute cellular rejection in heart transplantation at the early stage using two-dimensional speckle tracking imaging and ICAM-1-targeted myocardial contrast echocardiography / 中华超声影像学杂志

Objective To investigate whether two-dimension speckle tracking imaging(2D-STI) and ICAM-1-targeted myocardial contrast echocardiography could detect the acute cellular rejection of heart transplantation at the early stage.Methods The abdominal heterotopic heart transplantation model was successfully established using Wistar and SD rats.Forty-eight rats were divided into allografts (ALLO) group (n =24) and isografts(ISO) group (n =24).Echocardiography,2D-STI and ICAM-1 targeted myocardial contrast echocardiography were performed at 1,3,5 day after transplantation respectively.After ultrasound imaging,transplanted hearts were harvested for Hematoxylin-eosin staining and immunofluorescence histochemistry to evaluate acute cellular rejection and ICAM-1 expression.Results There were obvious difference between ALLO group and ISO group in echocardiographic parameters at 5 days after transplantation surgery (all P ＜0.05).Compared with those in ISO group,global circumferential strain and strain rate (GCS,GCSr),and circumferential strain of endo-myocardium (CSendo) decreased in ALLO group at day 3 post-transplantation (all P＜0.05).Compared with those in ISO group,all strain parameters in ALLO decreased significantly at postoperative day 5 (all P＜ 0.05).Myocardial contrast echocardiography using ICAM-1-targeted microbubbles showed that the video intensity in ALLO group was significant higher than that in ISO group at postoperative day 3 and day 5 (all P＜0.05).Conclusions 2D-STI and myocardial contrast echocardiography using ICAM-1-targeted microbubbles are sensitive and useful for detecting heart transplant acute rejection at the early stage.

Utilization and satisfaction of family doctor service among contract-signing residents in Beijing urban area and related influencing factors / 中华全科医师杂志

Objective To investigate the utilization and satisfaction of family doctor service among contract-signing residents in Beijing urban area,and the related influencing factors.Methods Total 740 contract-signing residents visiting community health service centers of two urban districts in Beijing from June to September of 2015 were selected with purposive sampling as study subjects.All participants completed a questionnaire survey on the utilization and satisfaction of the service provided by family doctors.The influencing factors related to satisfaction were analyzed by chi-square test and multivariate Logistic regression.Results The survey showed that 73.9％ (547/740) of the participants would seek service in community health service centers first when their illness was mild;while 56.2％ (416/740) of the participants would seek service in secondary or tertiary hospitals directly.Four out of 8 contracted services were mostly utilized:personalized health counseling (732/740,98.9％),chronic disease management (721/740,97.4％),health promotion guidance (626/740,84.6％),and health education (614/740,83.0％).The satisfaction rates for service attitude of family doctor,the contents of contracted service,the competence of family doctor and the environment of clinical setting were 82.7％ (612/740),75.4％ (558/740),72.8％ (539/740) and 70.4％ (521/740),respectively.The satisfaction rates of service contents were 85.4％ (164/192) for home visit,81.3％ (248/305) for appointment of experts in tertiary hospital,76.8％ (562/732) for personalized health counseling,76.3％ (550/721) for chronic disease management,75.2％ (471/626) for health promotion guidance,74.4％ (457/614) for health education,72.8％ (302/415) for referral service,and 65.7％ (305/464) for appointment of next visit.Logistic regression showed that the quality of family doctor service in the community health service institutions (OR =2.693,P =0.000) and education levels of residents (OR =0.680,P =0.008) were the factors related to the satisfaction of the patients.Conclusion The contract-signing residents in Beijing urban area are willing to go to the community health service institutions,and generally satisfied with the service.But the service contents and service quality need to be further improved.

Quercetin Inhibited ADMA-induced Endoplasmic Reticulum Stress Responses and HUVECs Apotosis / 医学研究杂志

Objective To study the effect of quercetin on ADMA induced endoplasmic reticulum stress responses (ER stress).Methods Human umbilical veins endothelial cells (HUVECs) were cultured,and left untreated or challenged for 24h with 100μmol/L ADMA in the absence and presence of 20μmol/L quercetin,the PERK and IRE1 was determined by Western blot.ATF4 and CHOP mRNA was detected by RT-PCR.Cells apoptosis was detected by flow cytometry.Results ADMA induced HUVECs apoptosis.Quercetin inhibited ADMA-induced PERK and IRE1 protein expression and ATF4 and CHOP mRNA expression.At last,Quercetin inhibited ADMA-induced cells apoptosis.Conclusion ADMA induced ER stress and HUVECs apotosis while quercetin inhibited ADMA-induced ER stress and apoptosis.

Evaluation scales for doctor-patient communication in general practice / 中华全科医师杂志

Communication skills are the basic requirement for general practitioners,the continuous improvement of communication skills is the guarantee of the service quality.It is crucial to establish an effective evaluation system in the training of communication skills for general practitioners.This article reviews the current status of evaluation scales of doctor-patient communication skill commonly used in China and other countries to provide reference for the establishment of the communication skill evaluation system for general practitioners which is suitable for China's condition.

Bibliometric Analysis of Drug Therapy of Rheumatoid Arthritis Based on WoS Core Collection / 中国药房

OBJECTIVE:To investigate the development of drug therapy of rheumatoid arthritis,and to provide reference for the study of this field in China. METHODS:All literatures were retrieved during 2005-2016 using Web of ScienceTM(called"WoS"for short)core collection as database,"Rheumatoid arthritis""Rheumatoid-arthritis""Drug therapy""Medication"as subjects,set-ting literature type as"Article""Review". Bibliometric analysis method was used to list and analyze literatures about drug therapy of rheumatoid arthritis by annual number of articles published,source journals,subjects,agencies,authors and hot issues. RE-SULTS:A total of 2 528 literatures were retrieved from WoS core collection. The number of literatures showed an overall trend of growth.Those literatures came from more than 800 journals,among which top 10 journals published 689 literatures about drug ther-apy of rheumatoid arthritis(27.25%).A total of 18 subjects were involved,and the number of literatures in"Clinical medicine"was the largest,with 1 884 literatures(74.53%).A total of 3 431 research institutions were involved,and the largest number of literatures were issued by the Harvard University,with 68 literatures in total(2.69%). A total of 14 325 researchers were in-volved,and top 10 researchers published 240 literatures about drug therapy of rheumatoid arthritis(9.49%). The frequency of 25 keywords was greater than or equal to 100 times,that of 12 was greater than or equal to 150 times."Rheumatoid-arthritis"had the highest frequency(1 740 times). In basic scientific index(ESI)database,there were 35 literatures with high citation fre-quency. CONCLUSIONS:With the literatures of rheumatoid arthritis therapy increasing year by year,the focus of research in this field is focused on the diagnosis of rheumatoid arthritis and clinical efficacy. In China,no institution or author enters the world front rank in this research field.Attention should be paid to the clinical study on drug therapy of rheumatoid arthritis.

Collagen/silk fibroin nerve conduits used for repairing peripheral nerve defect:application and development / 中国组织工程研究

BACKGROUND:Peripheral nerve defect due to limb dysfunction has always been the difficulty faced by the medical profession. Ideal materials and processing technology for constructing a tissue engineering scaffold targeting peripheral nerve repair are stil in research stage. OBJECTIVE:To review the research progress in peripheral nerve repair using col agen/silk fibroin nerve conduits. METHODS:In this paper, the first author retrieved the PubMed and CNKI from 2003 to 2016 to search articles regarding methods of constructing artificial nerve scaffolds and selection of raw materials. Data from these articles were col ected, summarized and analyzed. RESULTS AND CONCLUSION:Forty-six articles were included for final analysis. Col agen and its degradation products trigger no inflammatory response in the host because of high biocompatibility and biodegradability. However, its use is largely limited by its rapid degradation and poor physical performance. Silk fibroin has a high flexibility and biocompatibility, and exhibits a slow degradation in vivo. As a rapid prototyping technique, three-dimensional printing can print various forms of scaffolds within a short time, characterized as high-quality pore structure and large-scale production. Given these, the col agen/silk fibroin nerve conduit prepared using the three-dimensional printing technology can maintain the biocompatibility and even improve the mechanical properties of the raw materials. Until now, more investigations on nerve repair using col agen or silk fibroin have been done, and we have never stopped improving the production process of these scaffolds. Therefore, the col agen/silk fibroin scaffold prepared using the three-dimensional printing technology is expected to become the main candidate for the repair of peripheral nerve defects.

Experimental animal models of intervertebral fusion-induced adjacent segment degeneration / 中国组织工程研究

BACKGROUND:Upright rat intervertebral disc degeneration model can prove that intervertebral fusion can aggravate the adjacent-segment intervertebral disc degeneration, but cannot affirm that spinal non-fusion technology has more advantages. OBJECTIVE:Base on the affirmed intervertebral disc degeneration models of Beagle dog, we performed intervertebral fusion to affirm whether or not the intervertebral fusion can aggravate the adjacent-segment intervertebral disc degeneration. METHODS:Twelve Beagle dogs were randomly divided into two groups. The control group animals were stabbed percutaneous to injure L5/6 disc. The experimental group animals were stabbed percutaneous to injur L5/6 disc. One month later, we made L4/5 intervertebral fusion. At 3 and 6 months postoperatively, lumbar MRI was conducted. L5/6 discs were harvested and subjected to histological observation and PCR. RESULTS AND CONCLUSION:(1) MRI:in the experimental group, 3 and 6 months after fusion, different degrees of intervertebral disk herniation appeared. In the control group, no obvious intervertebral disk herniation appeared. (2) Histological observation:6 months after fusion, in the experimental group, intervertebral disc annulus and nucleus pulposus were disordered;there was a gap in the fold, and the number of nucleus pulposus cel s decreased. In the control group, nucleus pulposus and anulus fibrosus boundary was clear;col agen was loose and arranged regularly. Cel number was more. Anulus fibrosus was close to normal. Col agen fibers were regular and dense. In the experimental group, 3 and 6 months after fusion, type II col agen-positive cel s were less than the control group (P<0.05). Moreover, type II col agen-positive cel s were less at 6 months than at 3 months in the experimental group (P<0.05). (3) PCR:Bone morphogenetic protein 15 and tissue inhibitor of matrix metal oproteinase 1 gene expression was higher in the experimental group than in the control group at 3 and 6 months after fusion (P<0.05). Bone morphogenetic protein 15 and tissue inhibitor of matrix metal oproteinase 1 gene expression was higher in the experimental group at 6 months than that at 3 months (P<0.05). (4) These results suggest that intervertebral fusion can aggravate the adjacent-segment intervertebral disc degeneration.

Influence of interleukin-1beta on microRNA-27b and matrix metalloproteinase-13 expression in rat chondrocytes / 中国组织工程研究

BACKGROUND:Matrix metal oproteinase-13 is most active in the degradation of col agen type II in the extracel ular matrix of cartilage. Interleukin-1 (IL-1) is thought to be the inducer of matrix metal oproteinases, and participates in the degradation and degeneration of articular cartilage. OBJECTIVE:To study the influence of IL-1βon microRNA-27b (miR-27b) and matrix metal oproteinase-13 expression of chondrocytes in rats. METHODS:Chondrocytes isolated from seven male Wistar rats were cultured and divided into IL-1βstimulation group and control group. No stimulus was given in the control group;10μg/L of serum free medium was used to culture rat chondrocytes in the IL-1βstimulation group. Cel growth was observed at 0, 24, and 48 hours under an inverted microscope. miR-27b and matrix metal oproteinase-13 expression in the cultured chondrocytes were detected. RESULTS AND CONCLUSION:The relative expression of matrix metal oproteinase-13 in rat chondrocytes was gradual y increased when induced by IL-1βat 0, 24, and 48 hours (P<0.05). Expression of miR-27b and miR-31 in rat chondrocytes at 24 and 48 hours induced by IL-1βgradual y decreased (P<0.05);conversely, expression of MiR-26a, miR-26b, miR-23, and miR-204 gradual y increased (P<0.05). After 48 hours of IL-1βinduction, expression of miR-27b was the lowest in rat chondrocytes (P<0.05). These findings suggest that IL-1βinhibits miR-27b expression, strengthens the expression of matrix metal oproteinase-13, and damages chondrocytes, contributing to both the onset and progression of osteoarthritis.

Synthesis and antitumor activity of fluoroquinolon-3-yl-s-triazole sulfide ketones and their derivatives from ciprofloxacin / 药学学报

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.

Synthesis and antitumor activity of C-3 thiazolo 3 2-b 1 2 4 triazole-substituted pefloxacin derivatives / 中国药科大学学报

To search for fluoroquinolones(FQs)with antitumor activity;the C-3 carboxylic acid group of peflox-acin (1)was replaced by fused heterocyclic core;and twelve novel thiazolo[3;2-b][1;2;4]triazole heterocycles(6a-6l)were designed and synthesized.The structures of target compounds were characterized by elemental anal-ysis and spectral data.The results of the in vitro antiproliferative effect on SMMC-7721;L1210 and HL60 cell lines showed that the title compounds exhibited more significant antitumor activity than both of the pefloxacin and the corresponding opening-ring intermediates(5 a-5 l).Among them;the target compounds which possess a ben-zene ring bearing a hydroxyl group (6e)or a fluorine atom (6j)exhibited more potent antiproliferative effect on SMMC-7721 cells than other compounds.Therefore;the antitumor fluoroquinolones can be designed by replacing the C-3 carboxylic acid group of fluoroquinolones with the thiazolo[3;2-b][1;2;4]triazole moiety.

Preparation and characterization of self-assembled thiolated chitosan derivatives and gold nanoparticles / 国际生物医学工程杂志

Objective To prepare self-assembled thiolated chitosan derivatives gold nanoparticles (CS-GNRs) and carry out the feature tests.Methods CS-GNRs was prepared by chitosan derivatives and GNRs through strong metal sulfur chemical bond between thiols and gold on GNRs surface.Morphology features was tested by transmission electron microscope,dynamic light scattering was adopted to observe the size of nanoparticles.Ultraviolet-visible spectrophotometer was used to detect the optical properties and the property change.Meanwhile,the surface-enhanced Raman scattering (SERS) activity of CS-GNRs was investigated by using crystal violet (CV) as a probe molecular.Results CS-GNRs were in good shape,uniform particle size and good dispersion.The SERS of CV was enhanced,and the enhancement factor of CV adsorbed on CS-GNRs was up to 2×103.Conclusions The nanoparticles have potential application in molecular detection and Raman spectra detection.