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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.
Tang, Xiao-Yan,Igarashi, Atsushi,Sun, Wen-Hua,Inagaki, Akiko,Liu, Jingyu,Zhang, Wenjuan,Li, Yue-Sheng,Nomura, Kotohiro American Chemical Society 2014 Organometallics Vol.33 No.4
<P>A series of (imido)vanadium(V) dichloride complexes containing 8-(2,6-dimethylanilide)-5,6,7-trihydroquinoline ligands of the type V(NR)Cl<SUB>2</SUB>[8-(2,6-Me<SUB>2</SUB>C<SUB>6</SUB>H<SUB>3</SUB>)N(C<SUB>9</SUB>H<SUB>10</SUB>N)] (R = Ad (<B>3</B>), 2-MeC<SUB>6</SUB>H<SUB>4</SUB> (<B>4</B>), 2,6-Me<SUB>2</SUB>C<SUB>6</SUB>H<SUB>3</SUB> (Ar, <B>5</B>)) have been prepared and identified, and their structures have been determined by X-ray crystallographic analysis. The ethylene dimerization catalyst generated from complex <B>3</B> upon treatment with an excess amount of MAO exhibited remarkable catalytic activities (e.g. TOF = 9600000 h<SUP>–1</SUP> (2670 s<SUP>–1</SUP>), Al/V = 4000 (molar ratio)), affording 1-butene as the major product (95.0–99.4%). The activities of <B>3</B> and <B>4</B> were higher than those exhibited by the corresponding 2-(anilide)methylpyridine analogues; <B>3</B> showed higher 1-butene selectivity than the others and the activity did not decrease remarkably at 50 °C. Complex <B>5</B> afforded a mixture of polymer and oligomers with low activities, suggesting that a fine tuning of both the imido and the anionic donor ligands plays an essential role in this catalysis.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orgnd7/2014/orgnd7.2014.33.issue-4/om401119y/production/images/medium/om-2013-01119y_0004.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/om401119y'>ACS Electronic Supporting Info</A></P>
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.
Roles of Immunohistochemical Staining in Diagnosing Pulmonary Squamous Cell Carcinoma
Yan, Yue,Zhang, Ya-Xiong,Fang, Wen-Feng,Kang, Shi-Yang,Zhan, Jian-Hua,Chen, Nan,Hong, Shao-Dong,Liang, Wen-Hua,Tang, Yan-Na,He, Da-Cheng,Wu, Xuan,Zhang, Li Asian Pacific Journal of Cancer Prevention 2015 Asian Pacific journal of cancer prevention Vol.16 No.2
Background: Differentiating morphologic features based on hematoxylin-eosin (HE) staining is the most common method to classify pathological subtypes of non-small-cell lung cancer (NSCLC). However, its accuracy and inter-observer reproducibility in pathological diagnosis of poorly differentiated NSCLC remained to be improved. Materials and Methods: We attempted to explore the role of immunohistochemistry (IHC) staining in diagnosing pulmonary squamous cell carcinoma (SQCC) with poorly differentiated features by HE staining or with elevated serum adenocarcinoma-specific tumor markers (AD-TMs). We also compared the difference of epidermal growth factor receptor (EGFR) mutation rate between patients with confirmed SQCC and those with revised pathological subtype. Logistic regression analyses were used to test the association between different factors and diagnostic accuracy. Results: A total of 132 patients who met the eligible criteria and had adequate specimens for IHC confirmation were included. Pathological revised cases in poor differentiated subgroup, biopsy samples and high-level AD-TMs cases were more than those with high/moderate differentiation, surgical specimens and normal-level AD-TMs. Moreover, biopsy sample was a significant factor decreasing diagnostic accuracy of pathological subtype (OR, 4.037; 95% CI 1.446-11.267, p=0.008). Additionally, EGFR mutation rate was higher in patients with pathological diagnostic changes than those with confirmed SQCC (16.7% vs 4.4%, p=0.157). Conclusions: Diagnosis based on HE staining only might cause pathological misinterpretation in NSCLC patients with poor differentiation or high-level AD-TMs, especially those with biopsy samples. HE staining and IHC should be combined as pathological diagnostic standard. The occurrence of EGFR mutations in pulmonary SQCC might be overestimated.
Tang, Shuang-Yan,Le, Quang-Tri,Shim, Jae-Hoon,Yang, Sung-Jae,Auh, Joong-Huck,Park, Cheonseok,Park, Kwan-Hwa Blackwell Publishing Ltd 2006 FEBS JOURNAL Vol.273 No.14
<P>DNA shuffling was used to improve the thermostability of maltogenic amylase from <I>Bacillus thermoalkalophilus</I> ET2. Two highly thermostable mutants, III-1 and III-2, were generated after three rounds of shuffling and recombination of mutations. Their optimal reaction temperatures were all 80 °C, which was 10 °C higher than that of the wild-type. The mutant enzyme III-1 carried seven mutations: N147D, F195L, N263S, D311G, A344V, F397S, and N508D. The half-life of III-1 was about 20 times greater than that of the wild-type at 78 °C. The mutant enzyme III-2 carried M375T in addition to the mutations in III-1, which was responsible for the decrease in specific activity. The half-life of III-2 was 568 min while that of the wild-type was <1 min at 80 °C. The melting temperatures of III-1 and III-2, as determined by differential scanning calorimetry, increased by 6.1 °C and 11.4 °C, respectively. Hydrogen bonding, hydrophobic interaction, electrostatic interaction, proper packing, and deamidation were predicted as the mechanisms for the enhancement of thermostability in the enzymes with the mutations.</P>
Two new tirucallane triterpenoids from the leaves of Aquilaria sinensis
Jin Tang Cheng,Ya Qiong Han,Juan He,Xing De Wu,Liao Bin Dong,Li Yan Peng,Yan Li,Qin Shi Zhao 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.9
Two new tirucallane triterpenoids, aquilacallanesA–B (1–2), together with 15 known compounds(3–17) were isolated from the leaves of Aquilaria sinensis. The structures of these new compounds were elucidated onthe basis of extensive spectroscopic analyses. All compoundswere evaluated for their cytotoxic activity againstfive human cancer cell lines. The known compounds,ursolic acid (7) and 5,7,40-trimethoxyflavone (14), exhibitedweak cytotoxic activity against some cells.
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.