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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.
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.
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.
Xian-Qing Deng,Cheng-Xi Wei,Ming-Xia Song,채규윤,Zhi-Gang Sun,Zhe-Shan Quan 대한화학회 2010 Bulletin of the Korean Chemical Society Vol.31 No.2
A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.
( Xian Min Piao ),( Eun Kyu Jang ),( Jong Wook Chung ),( Gi An Lee ),( Ho Sun Lee ),( Jung Sook Sung ),( Young Ah Jeon ),( Jung Ro Lee ),( Yeon Gyu Kim ),( Sok Young Lee ) 한국육종학회 2013 Plant Breeding and Biotechnology Vol.1 No.4
Tomato was considered as one of the most widely cultivated vegetable crops in the world. Tomato plant has high antioxidant capacity which can be attributed to the high levels of carotenoids, phenols, vitamins C and E. However, most of tomato plants have been discarded as waste after fruit harvesting. In order to identify genetic resources with high antioxidant level for use infood or as feed additives, we investigated the ABTS, DPPH antioxidant activity and polyphenol content in tomato leaves and stems. A total of 112 tomato accessions were classified into three groups by latitude of their collected countries: 30°~60° North (50 accessions), 0°~30° North (40 accessions), and 0°~30° South (22 accessions). Stem and leaf extracts showed wide variation in ABTS antioxidant activity ranging from 1.6±1.0 to 48.4±6.1 μg Trolox mg-1 dw. The antioxidant activity of DPPH was in the range of 6.±0.2 to 40.0±0.3 μg ASC mg-1 dw. Total polyphenol content ranged from 6.1±0.2 to 38.9±0.7 μg GAE mg -1 dw. ABTS, DPPH antioxidant activities and polyphenol content in accessions from 30°~60°N latitude were significantly higher (P<0.05) than those from 0°~30°N latitude. ABTS values showed a significant positive correlation (r = 0.700**) with DPPH activity. IT100506 (KOR) and 702959 (UKR) were recommended as potential sources of natural antioxidants due to their highest antioxidant activity among accessions. This study will provide valuable information for tomato breeders in developing and producing functional food or feed additives resources.
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.