Structure-based design, structure–activity relationship analysis, and antitumor activity of diaryl ether derivatives

Shao-Mei Yang,Fu-Nan Li,Zhi-Ning Huang,Zhong-Shi Zhou,Jin Hou,Man-Yi Zheng,Li-Juan Wang,Yu Jiang,Xin-Yi Zhou,Qiu-Yue Chen,Shan-Hua Li 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.10

To identify novel therapeutic agents to treatcancer, we synthesized a series of diaryl ether derivatives. Structure–activity relationship studies revealed that thepresence of a chlorine or hydroxyl at the para-position onthe phenyl ring (5h or 5k) significantly enhanced antitumoractivity. Compound 5h had stronger growth inhibitory activityin HepG2, A549, and HT-29 cells than compound 5k,with IC50 values of 2.57, 5.48, and 30.04 lM, respectively. Compound 5h also inhibited the growth of other cells lines,including Hep3B, PLC/PRF5, SMMC-7721, HeLa, andA375, with IC50 values of 2.76, 4.26, 29.66, 18.86, and10.21 lM, respectively. The antitumor activity of compound5h was confirmed by a colony forming assay. Further,our results indicated that the antitumor activity ofcompound 5h may be mediated by enhancing expression ofp21 and cl-caspase3, and leading to apoptosis of cancercells.

A two-stage cascaded foreground seeds generation for parametric min-cuts

( Shao-mei Li ),( Jun-guang Zhu ),( Chao Gao ),( Chun-wei Li ) 한국인터넷정보학회 2016 KSII Transactions on Internet and Information Syst Vol.10 No.11

Parametric min-cuts is an object proposal algorithm, which can be used for accurate image segmentation. In parametric min-cuts, foreground seeds generation plays an important role since the number and quality of foreground seeds have great effect on its efficiency and accuracy. To improve the performance of parametric min-cuts, this paper proposes a new framework for foreground seeds generation. First, to increase the odds of finding objects, saliency detection at multiple scales is used to generate a large set of diverse candidate seeds. Second, to further select good-quality seeds, a two-stage cascaded ranking classifier is used to filter and rank the candidates based on their appearance features. Experimental results show that parametric min-cuts using our seeding strategy can obtain a relative small pool of proposals with high accuracy.

The Synthesis and Preliminary Activity Assay In Vitro of Peptide-like Derivatives as APN Inhibitors

Li, Shao-Hua,Li, Gang,Huang, Hui-Ming,Xiong, Fang,Liu, Cheng-Mei,Tu, Guo-Gang 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.10

Both the aminopeptidase N (APN) and matrix metalloproteinase (MMP) are essential metallopeptidases in the development of tumor invasion and angiogenesis. A series of novel peptide-like derivatives were designed and synthesized as antitumor agents. Their structures were confirmed by IR, MS, and $^1H$-NMR. These compounds exhibited potent inhibitory activities against APN and low activity against MMP in vitro. The derivatives with methoxy group show better activities than those with other substituted group and could be used as lead compounds for exploring new APN inhibitors in the future.

The Presence of Open Dentinal Tubules Affects the Biological Properties of Dental Pulp Cells Ex Vivo

Mei-Ying Shao,Zhong-Sen Fu,Ran Cheng,Hui Yang,Li Cheng,Feng-Ming Wang,Tao Hu 한국분자세포생물학회 2011 Molecules and cells Vol.31 No.1

To investigate the effects of open dentinal tubules on the morphological and functional characteristics of dental pulp cells. Morphological changes in human dental pulp cells that were seeded onto dentin discs with open den-tinal tubules were investigated on days 1, 2, 4, and 10 of culture using scanning electron microscopy and fluores-cence microscopy. Samples collected on days 1, 3, 6, 8, and 10 of culture were evaluated for cell proliferation rate and alkaline phosphatase activity. Cultured human dental pulp cells developed a columnar or polygonal morphology and monopolar cytoplasmic processes that extended into the dentinal tubules. The cells formed a multilayer and secreted an extracellular matrix onto the cell surface. Scanning electron microscopy and fluorescence microscopy revealed polarized organization of odontoblasts. Cells seeded onto dentin discs prolifer-ated minimally but showed high levels of ALP activity. Dental pulp cells seeded onto treated dentin discs develop an odontoblast-like phenotype, which may be a potential alternative for use in experimental research on dentinogenesis.

Growth and Differentiation Effects of Homer3 on a Leukemia Cell Line

Li, Zheng,Qiu, Hui-Ying,Jiao, Yang,Cen, Jian-Nong,Fu, Chun-Mei,Hu, Shao-Yan,Zhu, Ming-Qing,Wu, De-Pei,Qi, Xiao-Fei Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.4

The Homer protein family, also known as the family of cytoplasmic scaffolding proteins, which include three subtypes (Homer1, Homer2, Homer3). Homer3 can regulate transcription and play a very important role in the differentiation and development for some tissues (e.g. muscle and nervous systems). The current studies showed that Homer3 abnormal expression changes in acute myeloid leukemia (AML). Forced expression of Homer3 in transfected K562 cells inhibited proliferation, influenced the cell cycle profile, affected apoptosis induced by $As_2O_3$ through inhibition of Bcl2 expression, and also promoted cell differentiation induced by 12-O-tetra decanoylphorbol-acetate (TPA). These results showed that Homer3 is a novel gene which plays a certain role in the occurrence and development of AML.

Involvement of Cdc25c in Cell Cycle Alteration of a Radioresistant Lung Cancer Cell Line Established with Fractionated Ionizing Radiation

Li, Jie,Yang, Chun-Xu,Mei, Zi-Jie,Chen, Jing,Zhang, Shi-Min,Sun, Shao-Xing,Zhou, Fu-Xiang,Zhou, Yun-Feng,Xie, Cong-Hua Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.10

Cancer patients often suffer from local tumor recurrence after radiation therapy. Cell cycling, an intricate sequence of events which guarantees high genomic fidelity, has been suggested to affect DNA damage responses and eventual radioresistant characteristics of cancer cells. Here, we established a radioresistant lung cancer cell line, A549R, by exposing the parental A549 cells to repeated ${\gamma}$-ray irradiation with a total dose of 60 Gy. The radiosensitivity of A549 and A549R was confirmed using colony formation assays. We then focused on examination of the cell cycle distribution between A549 and A549R and found that the proportion of cells in the radioresistant S phase increased, whereas that in the radiosensitive G1 phase decreased. When A549 and A549R cells were exposed to 4 Gy irradiation the total differences in cell cycle redistribution suggested that G2-M cell cycle arrest plays a predominant role in mediating radioresistance. In order to further explore the possible mechanisms behind the cell cycle related radioresistance, we examined the expression of Cdc25 proteins which orchestrate cell cycle transitions. The results showed that expression of Cdc25c increased accompanied by the decrease of Cdc25a and we proposed that the quantity of Cdc25c, rather than activated Cdc25c or Cdc25a, determines the radioresistance of cells.

5G Network Slices Embedding with Sharable Virtual Network Functions

Chengli Mei,Jiayi Liu,Jinyan Li,Lei Zhang,Menghan Shao 한국통신학회 2020 Journal of communications and networks Vol.22 No.5

Network slicing (NS) is recognized as a key technology for the 5G mobile network in enabling the network to support multiple diversified vertical markets over a shared physicalinfrastructure with efficiency and flexibility. A 5G NS instance iscomposed of a set of virtual network function (VNF) instances toform the end-to-end (E2E) virtual network for the slice to operateindependently. The deployment of a NS is a typical virtual network embedding (VNE) problem. We consider a scenario in whichVNF instances can be shared across multiple slices to further enhance the utilization ratio of the underlying physical resources. ForNSs with sharable VNF instances, the deployment of the slice instances is essentially the embedding of multiple virtual networkscoupled by the VNFs shared among slices. Hence, we formulatethis sharable-VNFs-based multiple coupled VNE problem (SVMVNE) through an integer linear program (ILP) formulation, anddesign a back-tracking coordinated virtual network mapping algorithm. Simulation results demonstrate that VNF-sharing can enhance the slice acceptance ratio with the same physical network,which represents higher physical resource utilization. Moreover,our approach achieves higher acceptance ratio by comparing to abaseline algorithm.

Design, synthesis and biological evaluation of B-region modified diarylalkyl amide analogues as novel TRPV1 antagonists

한영택,Shao-Mei Yang,Xiao-Yuan Wang,Fu-Nan Li 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.4

Design, synthesis and biological evaluation ofB-region, known to be a dipolar interacting pharmacophore,modified diarylalkyl amide analogues for novelTRPV1 (transient receptor potential channel, vanilloidsubfamily member 1) antagonists was described. A varietyof moieties including guanidines, heterocyclic rings, cinnamides,and a-substituted acetamides were introduced atthe B-region. TRPV1 antagonistic activities of these analogueswere evaluated by 45Ca2? uptake assay in rat DRGneuron. In particular, a,a-difluoroamide 53 exhibited3-fold more potent TRPV1 antagonistic activity (IC50 =0.058 lM) than the parent amide analogue 6.

Cordycepsmilitaris polysaccharide triggers apoptosis and G0/G1 cell arrest in cancer cells

Cheng Chen,Mei-LinWang,Chao Jin,Huijuan Chen,Shao-Hui Li,Shu-Ying Li,Xing-Fan Dou,Jun-Qiang Jia,Zhong-Zheng Gui 한국응용곤충학회 2015 Journal of Asia-Pacific Entomology Vol.18 No.3

Although many studies have shown the antitumor properties of Cordyceps militaris (artificial cultivated from Bombyx mori pupa) polysaccharides, little is known regarding the mechanism of its effects. This study was conducted to determine the mechanism of antitumor effects of C. militaris polysaccharide extract by evaluating apoptosis rate and cell cycle progression status in human liver cancer cell SMMC-7721, stomach cancer cell BGC-823 and breast cancer cell MCF-7. Results showed that C. militaris polysaccharides inhibited proliferation of SMMC-7721, BGC-823 and MCF-7 cells with an IC50 of 192 ± 23.2 μg/mL, 237 ± 12.7 μg/mL and 165 ± 16.3 μg/mL, respectively. We also found that C. militaris polysaccharides at increasing concentrations induced apoptosis dose dependently in those cancer cells: apoptosis rates were 48.3%, 59.4% and 70.9% for SMMC-7721, 41.3% and 57.0%, 72.2% for BGC-823 and 61.3%, 66.9% and 80.6% for MCF-7 at 110, 156 and 323 mg/mL of C. militaris polysaccharides, respectively. C. militaris polysaccharides arrested SMMC-7721, BGC-823 and MCF-7 cells at G0/G1 and G2/M phases with corresponding decrease in S-phase. This study suggests that C. militaris polysaccharides may exert its antitumor effects in those cancer cells by suppressing its growth, arresting the G0/G1-phase, reducing DNA synthesis and inducing apoptosis.

Spirometric Standards for Healthy Children and Adolescents of Korean Chinese in Northeast China

Kui Feng,Li Chen,Shao-Mei Han,Guang-Jin Zhu 대한의학회 2011 Journal of Korean medical science Vol.26 No.11

In China there are 1,923,842 Korean Chinese, who live mostly (92.27%) in the country’s three northeast provinces. In spite of this sizeable number, no spirometric data are available at present on them. The present study investigated normal spirometric reference values for the Korean Chinese children and adolescents. Spirometry was performed in 443healthy Korean Chinese children and adolescents aged 8-18 yr with measurements of forced vital capacity (FVC), forced expiratory volume in 1 second (FEV1), peak expiratory flow (PEF) and maximum mid-expiratory flow (MMEF). Reference equations for FEV1, FVC,PEF and MMEF were derived by using multiple regression analysis. All of the measured spirometric parameters correlated positively with height and age significantly (P < 0.001). The predicted values of FVC and FEV1 were higher than values obtained by using Caucasian and other Asian equations (P < 0.001). A set of spirometric reference equations has been derived using a relatively large, healthy, non-smoking young Korean Chinese population with a wide range of ages and heights, the results of which differ from those gained from several other reference equations. These reference equations should be used for evaluation of lung function in this population.