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Synthesis of 6-Alkyloxyl-3,4-dihydro-2(1H)-quinoliones and Their Anticonvulsant Activities
Quan, Zhe Shan,Wang, Jun-Min,Rho, Jung-Rae,Kwak, Kyung-Chell,Kang, Hee-Cheol,Jun, Chang-Soo,Chai, Kyu-Yun Korean Chemical Society 2005 Bulletin of the Korean Chemical Society Vol.26 No.11
A series of 6-alkyloxyl-3,4-dihydro-2(1H)-quinoliones (5a-5n) were synthesized through nitration, reduction, diazotization, hydrolysis and alkylation from 3,4-dihydro-2(1H)-quinolione. Their structures were characterized by IR, $^1H$-NMR and MS. The anticonvulsant activity was evaluated by the Maximal electroshock test (MES) and the subcutaneous pentylenetetrazole (Metrazole) test (sc-Met). The neurotoxicity was measured by the Rotarod test (Tox). The result showed that 6-hexyloxy-3,4-dihydro-2 (1H)-quinolinone (5c) was potent in anti-MES and anti-scMet test with $ED_{50}$ of 24.0 mg/kg and 21.2 mg/kg, respectively, albeit its $TD_{50}$ (67.6 mg/kg) revealed the high neurotoxicity. 6-Benzyloxy-3,4-dihydro-2(1H)-quinolinone (5f) was less effective against MES induced seizure with $ED_{50}$ of 29.6 mg/kg, but no neurotoxicity was observed even under 300 mg/kg. Its Protective index (PI) was greater than 10 preferable to Phenytoin, Carbamazepin, Phenobarbital and Valproate.
RPSA Gene Mutants Associated with Risk of Colorectal Cancer among the Chinese Population
Zhang, Shan-Chun,Jin, Wen,Liu, Hui,Jin, Ming-Juan,Chen, Ze-Xin,Ding, Zhe-Yuan,Zheng, Shuang-Shuang,Wang, Li-Juan,Yu, Yun-Xian,Chen, Kun Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.12
The primary aim of this study was to evaluate the relationship of single nucleotide polymorphisms (SNPs) in ribosomal protein SA (RPSA) gene with colorectal cancer (CRC). A case-control study including 388 controls and 387 patients with CRC was conducted in a Chinese population. Information about socio-demography and living behavior factors was collected by a structured questionnaire. Three SNPs (rs2133579, rs2269349, rs7641291) in RPSA gene were genotyped by Illumina SnapShot method. Multiple logistic regression models were used for assessing the joint effects between tea consumption and SNPs on CRC. The subjects with rs2269349 CC genotype had a decreased risk for CRC (OR=0.60; 95%CI = 0.37-0.99), compared with TT/CT genotype after adjustment for covariates. A similar association of rs2269349 with rectal cancer was observed (OR=0.49; 95%CI=0.24-1.00). Further analyses indicated that this SNP could modify the protective effect of tea drinking on CRC. Among the subjects with rs2269349 TT/CT or rs2133579 AA/GA, there was a marginal significantly lower risk of CRC (OR and 95%CI: 0.63 and 0.39-1.01 for rs2269349; 0.64 and 0.40-1.02 for rs2133579) in tea-drinking subjects in comparison to non-tea-drinking subjects. Mutants in the RPSA gene might be associated with genetic susceptibility to CRC and influence the protective effect of tea consumption in the Chinese population.
Reliability analysis for lateral stabilityof tongwamen bridge
Pan Sheng-Shan,Shi Lei,Tan Yong-Gang,Zhang Zhe 국제구조공학회 2011 Steel and Composite Structures, An International J Vol.11 No.5
Tongwamen Bridge is a critical link between Dongmen Island and the land in Shipu town, Zhejiang province, China. It is a 238 m span, half-through, concrete-filled steel tubular (CFST) X-type arch bridge. The width of the deck is only 10 m, yielding a width-to-span ratio of 1/23.8. The plane truss type section rib was adopted, which made of two CFST chords and web member system. The lateral stability is the key issue to this bridge. However, the existing researches on Tongwamen Bridge’s lateral stability are all the deterministic structural analysis. In this paper, a new strategy for positioning sampling points of the response surface method (RSM), based on the composite method combining RSM with geometric method for structural reliability analysis, is employed to obtain the reliability index of lateral stability. In addition the correlated parameters were discussed in detail to find the major factors. According to the analysis results, increasing the stiff of lateral braces between the arch ribs and setting the proper inward-incline degree of the arch rib can enhance obviously the reliability of lateral stability. Moreover, the deck action of non-orienting force is less than the two factors above. The calculated results indicate that the arch ribs are safe enough to keep excellent stability, and it provides the foundation that the plane truss rib would be a competitive solution for a long-span, narrow, CFST arch bridge.
반추가축영양 : 발효 미역부산물이 반추위 발효특성에 미치는 영향
홍중산 ( Zhong Shan Hong ),이홍구 ( Hong Gu Lee ),이철호 ( Zhe Hu Lee ),김영성 ( Yong Cheng Jin ),이상범 ( Sang Bum Lee ),강한석 ( Han Sck Kang ),최윤재 ( Yun Jaie Choi ) 한국동물자원과학회(구 한국축산학회) 2011 한국축산학회지 Vol.53 No.4
DS-01 균주 접종에 의한 미역부산물 발효산물이 분해 정도, 영양소 변화 및 미생물오염 정도에 관한 관찰과 반추위 발효성상에 미치는 영향을 관찰하여 미역부산물의 저장성 확보와 반추동물의 사료로서의 이용가능성을 발효단계에 따라 조사하였다. DS-01 균주와 함께 배양된 미역부산물은 발효 1개월부터 현저한 분해율을 보이기 시작했다. 미역부산물중의 영양성분 함량은 발효와 함께 커다란 변화를 나타내지 않았으며 모든 처리에서 반추동물에 병원성을 가지는 미생물은 검출되지 않았다. In vitro 실험에서는 발효시간 및 첨가농도에 따른 pH 변화, 암모니아태 질소와 휘발성지방산의 생성에 대한 영향을 조사하였다. pH의 경우 6% FBSW는 1개월 및 2개월 발효조건에서 대조구, 2% 및 4% FBSW 보다 pH 값이 증가한 것을 나타내었다. 암모니아태 질소의 생성에 미치는 영향을 보면 1개월 FBSW 경우 실험 3시간 경과 후가 대조구에 비해 높은 농도를 나타내었지만 시간이 경과에 따라 대조구보다 감소한 경향을 보인다. 2개월 FBSW의 경우 4% 첨가량만 24시간 경과 후 타 처리구에 비해 높은 농도를 나타내었다. 특히, 전 발효기간 동안 6% FBSW 처리구가 발효 3시간과 24시간 경과 후 타 처리구에 비하여 낮게 나타나는 경향을 보였다. 휘발성지방산의 경우 발효 1개월 미역부산물의 4, 6% FBSW 첨가구가 6시간 경과 후 총 VFA의 농도가 현저하게 증가하는 양상을 나타내었고(p<0.05), 발효 2개월 미역부산물의 2, 4% FBSW 첨가구가 9시간 경과 후 총 VFA 농도가 6% FBSW 첨가구에 비해 현저하게 증가하는 양상을 나타냈다(p<0.05). This study was conducted to investigate the effects of brown seaweed waste (BSW) fermented with DS-01 microbe on in vitro rumen microbial fermentation. In in vitro trial, three different diets supplemented with 2%, 4%, 6% BSW fermented with DS-01 either for one month or two months was tested at 3 h, 6 h, 9 h, 12 h, and 24 h incubation. The chemical composition (CP, EE, CF, and ash) between brown seaweed waste (BSW) and fermented BSW (FBSW) were not different. The contamination of pathogenic microbes was not detected in FBSW. The pH value tended to be higher with 6% level of supplementation of FBSW for one month than other treatments. The pH at 24 h was significantly higher in FBSW than that of treatments without FBSW (p<0.05). In FBSW for two months, the pH value in 6% FBSW at 3 h in vitro fermentation tended to be higher than 2% or 4% FBSW treatments (p=0.0540), but there were no differences in other fermentation times. Although the concentration of NH3-N of BSW fermented for one month was higher than control at 3h (p<0.05), the volatile fatty acid values were significantly increased in 4 and 6% FBSW fermented for one month at 6 h incubation (p<0.05). In BSW fermented for two months, the volatile fatty acid values were significantly decreased in 6% treatment at 9h (p<0.05). As a result of in vitro trial, it was recommended that the 2~4% supplementation level of brown seaweed waste fermented with DS-01 microbe for two months could be utilized for in vivo trial in ruminants.
Wei Chao Yu,Zhe Li,Bao Shan Sun,Yan Cui 한국식품과학회 2020 Food Science and Biotechnology Vol.29 No.8
Commercial enological tannins from variousorigins have been widely used in modern wine making. Inorder to investigate the diverse quality of tannin products, aquick, accurate and simple UPLC method was developed,which could simultaneously determine 11 principle characteristiccomponents of hydrolysable tannins and condensedtannins. The optimum resolution of the tannins wasachieved on a Waters Acquity UPLC-BEH C18 column(2.1 mm 9 50 mm, 1.7 lm) at 280 nm with gradient elution. The method was validated to achieve desired specificity,linearity, precision, accuracy and stability. Thedeveloped method was successfully applied to 30 commercialenological tannins from different origins for theirquality evaluation. The 30 tannin samples were qualitativelydistinguished into hydrolysable, condensed or mixturetannins, and quantificationally classified into fourlevels of excellent, good, fair and poor products. Themethod could be used for quick evaluating the quality ofenological tannins in practical use.
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.
Jie Ma,Kam Sing Wong,Shan Li,Zhe Chen,Jianying Zhou,Yongchun Zhong 한국광학회 2015 Current Optics and Photonics Vol.19 No.1
A one-step fabrication of a photonic crystal (PC) with functional defects is demonstrated. Using multi-beamphase-controlled holographic lithography with a diffracting optical element, large area one dimensional (1D)and two dimensional (2D) PCs with periodic defects were fabricated. The uniform area is up to 2 mm2,and tens of defect channels have been introduced in the 1D and 2D PC structure. This technique givesrise to substantial reduction in the fabrication complexity and significant improvement in the spatialaccuracy of introducing functional defects in photonic crystals. This method can also be used to designand fabricate three dimensional (3D) PCs with periodic defects.