Monosaccharide as a Central Scaffold Toward the Construction of Salicylate-Based Bidentate PTP1B Inhibitors via Click Chemistry

Tang, Yan-Hui,Hu, Min,He, Xiao-Peng,Fahnbulleh, Sando,Li, Cui,Gao, Li-Xin,Sheng, Li,Tang, Yun,Li, Jia,Chen, Guo-Rong Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.3

The discovery of carbohydrate-based bioactive compounds has recently received considerable interest in the drug development. This paper stresses on the application of 1-methoxy-O-glucoside as the central scaffold, whereas salicylic pharmacophores were introduced with diverse spatial orientations probing into the structural preference of an enzymatic target, i.e. protein tyrosine phosphatase 1B (PTP1B). By employing regioselective protection and deprotection strategy, 2,6-, 3,4-, 4,6- and 2,3-di-O-propynyl 1-methoxy-O-glucosides were previously synthesized and then coupled with azido salicylate via click chemistry in forming the desired bidentate salicylic glucosides with high yields. The inhibitory assay of the obtained triazolyl derivatives leads to the identification of the 2,3-disubstituted salicylic 1-methoxy-O-glucoside as the structurally privileged PTP1B inhibitor among this bidentate compound series with micromole-ranged $IC_{50}$ value and reasonable selectivity over other homologous PTPs tested. In addition, docking simulation was conducted to propose a plausible binding mode of this authorized inhibitor with PTP1B. This research might furnish new insight toward the construction of structurally different bioactive compounds based on the monosaccharide scaffold.

Monosaccharide as a Central Scaffold Toward the Construction of Salicylate-Based Bidentate PTP1B Inhibitors via Click Chemistry

Yan-Hui Tang,Min Hu,Xiao-Peng He,Sando Fahnbulleh,Cui Li,Li-Xin Gao,Li Sheng,Yun Tang,Jia Li,Guo-Rong Chen 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.3

The discovery of carbohydrate-based bioactive compounds has recently received considerable interest in the drug development. This paper stresses on the application of 1-methoxy-O-glucoside as the central scaffold,whereas salicylic pharmacophores were introduced with diverse spatial orientations probing into the structural preference of an enzymatic target, i.e. protein tyrosine phosphatase 1B (PTP1B). By employing regioselective protection and deprotection strategy, 2,6-, 3,4-, 4,6- and 2,3-di-O-propynyl 1-methoxy-O-glucosides were previously synthesized and then coupled with azido salicylate via click chemistry in forming the desired bidentate salicylic glucosides with high yields. The inhibitory assay of the obtained triazolyl derivatives leads to the identification of the 2,3-disubstituted salicylic 1-methoxy-O-glucoside as the structurally privileged PTP1B inhibitor among this bidentate compound series with micromole-ranged IC50 value and reasonable selectivity over other homologous PTPs tested. In addition, docking simulation was conducted to propose a plausible binding mode of this authorized inhibitor with PTP1B. This research might furnish new insight toward the construction of structurally different bioactive compounds based on the monosaccharide scaffold.

Combination of Tumor Volume and Epstein-Barr Virus DNA Improved Prognostic Stratification of Stage II Nasopharyngeal Carcinoma in the Intensity Modulated Radiotherapy Era: A Large-Scale Cohort Study

Qiu-Yan Chen,Shao-Yan Guo,Lin-Quan Tang,Tong-Yu Lu,Bo-Lin Chen,Qi-Yu Zhong,Meng-Sha Zou,Qing-Nan Tang,Wen-Hui Chen,Shan-Shan Guo,Li-Ting Liu,Yang Li,Ling Guo,Hao-Yuan Mo,Rui Sun,Dong-Hua Luo,Chong Zha 대한암학회 2018 Cancer Research and Treatment Vol.50 No.3

Purpose Little is known about combination of the circulating Epstein-Barr viral (EBV) DNA and tumor volume in prognosis of stage II nasopharyngeal carcinoma (NPC) patients in the intensity modulated radiotherapy (IMRT) era. We conducted this cohort study to evaluate the prognostic values of combining these two factors. Materials and Methods By Kaplan-Meier, we compare the differences of survival curves between 385 patients with different EBV DNA or tumor volume levels, or with the combination of two biomarkers mentioned above. Results Gross tumor volume of cervical lymph nodes (GTVnd, p < 0.001) and total tumor volume (GTVtotal, p < 0.001) were both closely related to pretreatment EBV DNA, while gross tumor volume of nasopharynx (GTVnx, p=0.047) was weakly related to EBV DNA. EBV DNA was significantly correlated with progress-free survival (PFS, p=0.005), locoregional-free survival (LRFS, p=0.039), and distant metastasis-free survival (DMFS, p=0.017), while GTVtotal, regardless of GTVnx and GTVnd, had a significant correlation with PFS and LRFS. The p-values of GTVtotal for PFS and LRFS were 0.008 and 0.001, respectively. According to GTVtotal and pretreatment EBV DNA level, patients were divided into a low-risk group (EBV DNA 0 copy/mL, GTVtotal < 30 cm3; EBV DNA 0 copy/mL, GTVtotal  30 cm3; or EBV DNA > 0 copy/mL, GTVtotal < 30 cm3) and a high-risk group (EBV DNA > 0 copy/mL, GTVtotal  30 cm3). When patients in the low-risk group were compared with those in the high-risk group, 3-year PFS (p=0.003), LRFS (p=0.010), and DMFS (p=0.031) rates were statistically significant. Conclusion Pretreatment plasma EBV DNA and tumor volume were both closely correlated with prognosis of stage II NPC patients in the IMRT era. Combination of EBV DNA and tumor volume can refine prognosis and indicate for clinical therapy.

Cyclooxygenase-2 Promoter 765C Increase of Digestive Tract Cancer Risk in the Chinese Population: a Meta-analysis

Xu, Yan-Song,Zhao, Bo,Long, Chen-Yan,Li, Hui,Lu, Xing,Liu, Gang,Tang, Xiao-Zhun,Tang, Wei-Zhong Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.11

Background: To evaluate relationship between the cyclooxygenase-2 promoter 765G/C polymorphism and digestive cancer risk in China. Materials and Methods: A literature search through February 2014 was performed using PubMed, Chinese Biomedical Literature Database (CBM) and China National Knowledge Infrastructure (CNKI) databases, and a meta-analysis was performed with RevMan 5.2 software for odds ratios and 95%CIs. Results: In total, 9 articles with 3,263 cases and 4,858 controls were included in this meta-analysis. The pooled OR (95%CIs) in the co-dominant model (GC vs GG) was 1.56 [1.19, 2.06], and in the dominant model ((CC+GC) vs GG), the pooled OR was 1.59 [1.21, 2.09] in overall cancers. In the subgroup analysis, stratified by cancer type, significant associations were found that the-765C allele had increased pancreatic cancer and gastric risk. No significant liver cancer and colorectal cancer risk of COX-2 -765G/C polymorphism was found. Conclusions: These findings suggest that COX-2-765*C is related to cancer susceptibility and may increase gastric and pancreatic cancer risk.

Pretreatment Serum Amyloid A and C-reactive Protein Comparing with Epstein-Barr Virus DNA as Prognostic Indicators in Patients with Nasopharyngeal Carcinoma: A Prospective Study

Qiu-Yan Chen,Qing-Nan Tang,Lin-Quan Tang,Wen-Hui Chen,Shan-Shan Guo,Li-Ting Liu,Chao-Feng Li,Yang Li,Yu-Jing Liang,Xue-Song Sun,Ling Guo,Hao-Yuan Mo,Rui Sun,Dong-Hua Luo,Yu-Ying Fan,Yan He,Ming-Yuan C 대한암학회 2018 Cancer Research and Treatment Vol.50 No.3

Purpose The measuring Epstein-Barr virus (EBV) DNA is an important predictor of nasopharyngeal carcinoma (NPC). This study evaluated the predictive value of pretreatment serum amyloid A (SAA) and C-reactive protein (CRP) comparing with EBV DNA in patients with NPC. Materials and Methods In an observational study of 419 non-metastatic NPC patients, we prospectively evaluated the prognostic effects of pretreatment SAA, CRP, and EBV DNA on survival. The primary endpoint was progress-free survival (PFS). Results The median level of SAA and CRP was 4.28 mg/L and 1.88 mg/L, respectively. For the high- SAA group (> 4.28 mg/L) versus the low-SAA ( 4.28 mg/L) group and the high-CRP group (> 1.88 mg/L) versus the low-CRP ( 1.88 mg/L) group, the 5-year PFS was 64.5% versus 73.1% (p=0.013) and 65.2% versus 73.3% (p=0.064), respectively. EBV DNA detection showed a superior predictive result, the 5-year PFS in the EBV DNA  1,500 copies/mL group was obviously different than the EBV DNA < 1,500 copies/mL group (62.2% versus 77.8%, p < 0.001). Multifactorial Cox regression analysis confirmed that in the PFS, the independent prognostic factors were including EBV DNA (hazard ratio [HR], 1.788; p=0.009), tumour stage (HR, 1.903; p=0.021), and node stage (HR, 1.498; p=0.049), but the SAA and CRP were not included in the independent prognostic factors. Conclusion The results of SAA and CRP had a certain relationship with the prognosis of NPC, and the prognosis of patients with high level of SAA and CRP were poor. However, the predictive ability of SAA and CRP was lower than that of EBV DNA.

Panax ginseng and its ginsenosides: potential candidates for the prevention and treatment of chemotherapy-induced side effects

Yan Wan,Jing Wang,Jin-feng Xu,Fei Tang,Lu Chen,Yu-zhu Tan,Chao-long Rao,Hui Ao,Cheng Peng 고려인삼학회 2021 Journal of Ginseng Research Vol.45 No.6

Chemotherapy-induced side effects affect the quality of life and efficacy of treatment of cancer patients. Current approaches for treating the side effects of chemotherapy are poorly effective and may causenumerous harmful side effects. Therefore, developing new and effective drugs derived from natural nontoxiccompounds for the treatment of chemotherapy-induced side effects is necessary. Experimentsin vivo and in vitro indicate that Panax ginseng (PG) and its ginsenosides are undoubtedly non-toxic andeffective options for the treatment of chemotherapy-induced side effects, such as nephrotoxicity, hepatotoxicity,cardiotoxicity, immunotoxicity, and hematopoietic inhibition. The mechanism focus on antioxidation,anti-inflammation, and anti-apoptosis, as well as the modulation of signaling pathways, suchas nuclear factor erythroid-2 related factor 2 (Nrf2)/heme oxygenase-1 (HO-1), P62/keap1/Nrf2, c-jun Nterminalkinase (JNK)/P53/caspase 3, mitogen-activated protein kinase (MEK)/extracellular signalregulatedkinases (ERK), AMP-activated protein kinase (AMPK)/mammalian target of rapamycin(mTOR), mitogen-activated protein kinase kinase 4 (MKK4)/JNK, and phosphatidylinositol 3-kinase(PI3K)/AKT. Since a systemic review of the effect and mechanism of PG and its ginsenosides onchemotherapy-induced side effects has not yet been published, we provide a comprehensive summarizationwith this aim and shed light on the future research of PG.

Research Articles : Genetic analysis of the related traits of flowering and silk for hybrid seed production in maize

( Hui Ling Xie ),( Dong Ding ),( ZI Tian Cui ),( Xin Wu ),( Yan Min Hu ),( Zong Hua Liu ),( Yu Ling Li ),( Ji Hua Tang ) 한국유전학회 2010 Genes & Genomics Vol.32 No.1

The Clamping Position Optimization and Deformation Analysis for an Antenna Thin Wall Parts Assembly with ASA, MIGA and PSO Algorithm

Ming-hui Pan,Wen-cheng Tang,Yan Xing,Jun Ni 한국정밀공학회 2017 International Journal of Precision Engineering and Vol.18 No.3

In order to reduce the deformation and assembly error in an antenna thin wall parts assembly process, the assembly location or clamping positions need to be optimized. In this paper, the effect of clamping positions and clamping force on the thin wall parts deformation is analyzed considering the gravity by finite element simulation under different clamping force. The clamping positions are optimized with the Adaptive Simulated Annealing (ASA), Multi-Island Genetic Algorithm (MIGA) and Particle Swarm Optimization (PSO) algorithm by Isight software to reduce the deformation. Comparing with MIGA and PSO method, the results show that the clamping position optimization based on ASA exhibits the better results and superior than the MIGA and PSO no matter whether it has the effect of gravity. Simultaneously, through establishing the contact force model and contact deformation model, the nonlinear relationship between contact force, contact deformation and contact area is qualitatively analyzed, and the node deformation is calculated by theoretical formula. Comparing with those results, it is shown that the theoretical value matches well with the simulation results. Finally, some clamping scheme principles are proposed so that it provides a basis for reducing the deformation and assembly error of thin wall parts in future.

Strengthening regional integration/cooperation with the Neighbourhood System of Innovation conceptual framework: the case of China and ASEAN

Mingfeng Tang,Angathevar Baskaran,Hui Yan,Mammo Muchie 기술경영경제학회 2015 ASIAN JOURNAL OF TECHNOLOGY INNOVATION Vol.23 No.2

Traditional neo-classical market approach to regional integration/cooperation mainly focuseson trade and investment. The paper proposes an innovation system approach to regionalintegration/cooperation as an alternative that focuses on knowledge, learning, innovation,and competence (KLIC) building without excluding trade and investment. The underlyingargument is that while liberal trade and investment conceptual framework takes a narroweconomic gain and loss approach, the system of innovation approach includes economic andnon-economic variables by including KLIC, and broad economic and social gain. The paperpresents the Neighbourhood System of Innovation (NeSI) conceptual framework whichcaptures the reciprocal interactions between national innovation systems (NSI) of larger‘regional economic pole’ (REP) and smaller economies (or among NSIs of the smallereconomies) in the ‘Neighbourhood’ region. The case of China and Association of SoutheastAsian Nations (REP and Neighbourhood, respectively) is used to demonstrate the usefulnessof NeSI framework and its possible application to other similar cases. The aim of the paperis not to produce a path-breaking theory, but to present a different perspective throughinnovation systems approach as an alternative to enhance understanding of regionalintegration and cooperation dynamic processes.

Over-expression of StLCYb increases b-carotene accumulation in potato tubers

Xiao-yan Song,Wen-jiao Zhu,Rui-min Tang,Jing-hui Cai,Min Chen,Qing Yang 한국식물생명공학회 2016 Plant biotechnology reports Vol.10 No.2

Lycopene b-cyclase (LCYb) is involved in the first step of the b-branch synthetic pathway of carotenoids from lycopene in plants. In this study, to explore the possibility of regulating b-carotene synthesis via the b-branchspecific pathway in potato, StLCYb gene was first isolated from potato cultivar Desiree, and its open reading frame was 1503 bp long without intron. The protein sequence of StLCYb showed high similarity with that of LCYbs in other species such as SlLCYb1, CaLCYb, NtLCYb and ApLCYb. StLCYb was expressed in all tissues and the highest level was observed in tubers followed in flowers, and the lowest level was in roots. HPLC detected an about 1.5–1.9 times increase in b-carotene content of transgenic potato tubers, in which the gene StLCYb was overexpressed, compared with the wild-type control. Besides, the expression levels of carotenoid-related genes StPSY, StPDS, StZDS, StCHYb and StZEP transcripts in the transgenic lines were significantly higher than in the wild-type control, which implied a positive regulation in promoting carotenoid synthesis. All these results suggest that b-carotene content in potato tubers could be regulated by modulating StLCYb expression.