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Xian-Yu Sun,Yun-Zhe Jin,Fu-Nan Li,Gao Li,Kyu-Yun Chai,Zhe-Shan Quan 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.12
A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3- a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4] triazole[4,3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having ED50 values of 17.17 mg/kg and 24.55 mg/kg and protective index (PI = TD50/ED50) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having ED50 values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.
Sun, Xian-Yu,Jin, Yun-Zhe,Li, Fu-Nan,Li, Gao,Chai, Kyu-Yun,Quan, Zhe-Shan The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.12
A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.
Jing, Jie-Xian,Wang, Yan,Xu, Xiao-Qin,Sun, Ting,Tian, Bao-Guo,Du, Li-Li,Zhao, Xian-Wen,Han, Cun-Zhi Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.23
To evaluate the value of combined detection of serum CEA, CA19-9, CA24-2, AFP, CA72-4, SCC, TPA and TPS for the clinical diagnosis of upper gastrointestinal tract (GIT) cancer and to analyze the efficacy of these tumor markers (TMs) in evaluating curative effects and prognosis. A total of 573 patients with upper GIT cancer between January 2004 and December 2007 were enrolled in this study. Serum levels of CEA, CA19-9, CA24-2, AFP, CA72-4, SCC, TPA and TPS were examined preoperatively and every 3 months postoperatively by ELISA. The sensitivity of CEA, CA19-9, CA24-2, AFP, CA72-4, SCC, TPA and TPS were 26.8%, 36.2%, 42.9%, 2.84%, 25.4%, 34.6%, 34.2% and 30.9%, respectively. The combined detection of CEA+CA199+CA242+CA724 had higher sensitivity and specificity in gastric cancer (GC) and cardiac cancer, while CEA+CA199+CA242+SCC was the best combination of diagnosis for esophageal cancer (EC). Elevation of preoperative CEA, CA19-9 and CA24-2, SCC and CA72-4 was significantly associated with pathological types (p<0.05) and TNM staging (p<0.05). Correlation analysis showed that CA24-2 was significantly correlated with CA19-9 (r=0.810, p<0.001). The levels of CEA, CA19-9, CA24-2, CA72-4 and SCC decreased obviously 3 months after operations. When metastasis and recurrence occurred, the levels of TMs significantly increased. On multivariate analysis, high preoperative CA72-4, CA24-2 and SCC served as prognostic factors for cardiac carcinoma, GC and EC, respectively. combined detection of CEA+CA199+CA242+SCC proved to be the most economic and practical strategy in diagnosis of EC; CEA+CA199+CA242+CA724 proved to be a better evaluation indicator for cardiac cancer and GC. CEA and CA19-9, CA24-2, CA72-4 and SCC, examined postoperatively during follow-up, were useful to find early tumor recurrence and metastasis, and evaluate prognosis. AFP, TPA and TPS have no significant value in diagnosis of patients with upper GIT cancer.
Rui Liu,Zhang-Long Yu,Yuan-Lin Sun,Li-Tao Tong,Li-Ya Liu,Li-Li Wang,Xian-Rong Zhou,Su-Mei Zhou 한국식품과학회 2021 Food Science and Biotechnology Vol.30 No.6
To investigate the effects of electrolyzed watertreatment on the qualities of rice noodles prepared withsemidry- milled rice flour, pasting properties and thermalproperties of rice flour, and the cooking and texturalproperties of rice noodles were determined. Higher peakviscosity and lower melting enthalpy were observed inelectrolyzed water (EW) treated rice flour. The hardness,gumminess and chewiness of rice noodle in slightly acidicelectrolyzed water treated rice noodles with availablechlorine concentration (ACC) 20.32 mg/L were increasedsignificantly (p\0.05). The cooking loss decreased significantlyin strong acidic electrolyzed water treated noodleswith ACC 10.09 mg/L treatment (p\0.05). Theresults indicated that EW could promote the gelatinizationof rice flour, and improve the textural qualities of ricenoodles. Therefore EW was appropriate to be used in ricenoodle production.
Xian Jing,Kaixuan Wang,Jieqiong Lin,Peng Liu,Yudi Kan,Xu Zheng,Jie Sun,Yingchun Li 성균관대학교(자연과학캠퍼스) 성균나노과학기술원 2019 NANO Vol.14 No.1
Slicing reference data and adaptive slicing algorithm are the key issues to find out appropriate layer thicknesses of three-dimensional (3D) microstructures with free-form surface in two photon polymerization (TPP). In the present work, an adaptive slicing method (ASM) was proposed to improve the fabricating efficiency of 3D microstructures with free-form surface in TPP microfabrication. In the proposed method, slicing reference data were obtained by intersecting a series of vertical planes with the triangular patch format along characteristic directions. Maximum acceptable chordal height played a role as judging criteria to obtain appropriate layer thicknesses. What's more, typical 3D microstructures with free-form surfaces were fabricated with uniform slicing method (USM) and the proposed ASM, respectively. The comparison results showed that the proposed method effectively improved fabricating efficiency, guaranteeing an acceptable surface quality at the same time. This work was expected to provide references for improving fabrication efficiency of complex 3D microstructures in TPP.
Mu, Xian-Min,Shi, Wei,Sun, Li-Xin,Li, Han,Wang, Yu-Rong,Jiang, Zhen-Zhou,Zhang, Lu-Yong Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.4
Background/Aim: Pristimerin isolated from Celastrus and Maytenus spp can inhibit proteasome activity. However, whether pristimerin can modulate cancer metastasis is unknown. Methods: The impacts of pristimerin on the purified and intracellular chymotrypsin proteasomal activity, the levels of regulator of G protein signaling 4 (RGS 4) expression and breast cancer cell lamellipodia formation, and the migration and invasion were determined by enzymatic, Western blot, immunofluorescent, and transwell assays, respectively. Results: We found that pristimerin inhibited human chymotrypsin proteasomal activity in MDA-MB-231 cells in a dose-dependent manner. Pristimerin also inhibited breast cancer cell lamellipodia formation, migration, and invasion in vitro by up-regulating RGS4 expression. Thus, knockdown of RGS4 attenuated pristimerin-mediated inhibition of breast cancer cell migration and invasion. Furthermore, pristimerin inhibited growth and invasion of implanted breast tumors in mice. Conclusion: Pristmerin inhibits proteasomal activity and increases the levels of RGS4, inhibiting the migration and invasion of breast cancer cells.