• Title/Summary/Keyword: NSC

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Synthesis of Novel Benzofuran and Related Benzimidazole Derivatives for Evaluation of In Vitro Anti-HIV-1, Anticancer and Antimicrobial Activities

  • Rida, Samia M.;El-Hawash, Soad A.M.;Fahmy, Hesham T.Y.;Hazzaa, Aly A.;El-Meligy, Mostafa M.M.
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.826-833
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    • 2006
  • Previously, we synthesized and evaluated several benzofuran derivatives containing heterocyclic ring substituents linked to the benzofuran nucleus at C-2 by a two- to four-atom spacer as potential anti-HIV-1, anticancer and antimicrobial agents. Among these derivatives, NSC 725612 and NSC 725716 exhibited interesting anti-HIV-1 activity. To further investigate the structure-activity relationship, we synthesized several new benzofuran derivatives derived from 2-acetylbenzofuran (2, 3a-c) and 2-bromoacetylbenzofuran (6; 7a,b; 8a,b). The compounds were designed to comprise the heterocyclic substituents directly linked to the benzofuran nucleus at C-2. Moreover, various related benzimidazoles derived from 2-acetylbenzimidazole and from 2-cyanomethylbenzimidazole (12a,b; 13a,b; 15; 16a,b) were also prepared as isosteres. The synthesized compounds were preliminarily evaluated for their in vitro anti-HIV-1, anticancer and antimicrobial activity. Compounds 2, 3a, 3b, and 12b showed weak anti-HIV-1 activity. Compound 6 exhibited mild activity against S. aureus, while compound 15 had mild activity towards S. aureus and C. albicans. However, no significant anticancer activity was observed with any of the tested compounds. From these results, we conclude that the presence of the spacer between the heterocyclic substituent and the benzofuran nucleus may be essential for the biological activity.

Numerical Investigation on Cracking of Bridge Deck Slabs with Latex Modified Concrete Overlays (라텍스 개질 콘크리트 교량 교면 포장부 균열에 대한 수치해석 연구)

  • Choi, Kyoung-Kyu
    • Journal of the Korea Concrete Institute
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    • v.22 no.1
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    • pp.77-84
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    • 2010
  • Latex modified concrete (LMC) exhibits improved material properties including high tensile strength and durability compared with conventional concrete, and hence LMC has been used as protective layers over the bridge deck slabs to increase their service life with underlying assumption of excellent bond behavior between the LMC overlay and the concrete substrate. In this study, the effect of the primary parameters of the concrete substrate (i.e., shrinkage, stiffness and cracking capacity) as well as the LMC overlay thickness on the probability of cracking of the bridge deck slabs using LMC overlays was investigated by carrying out the finite element analysis that simulated the bond behavior of LMC overlays on normal strength concrete (NSC) and HPC bridge deck slabs. Based on the results of the numerical analysis, it is concluded that the relatively high shrinkage strains and stiffness of HPC slabs can increase its probability of cracking in bridge deck slabs using LMC overlay.

Application of Precast Concrete Products of Non-Sintered Cement Mortar based on Industrial by-Products (산업부산물을 이용한 비소성 시멘트 모르타르의 프리캐스트콘크리트 제품 적용성 평가)

  • Na, Hyeong-Won;Moon, Kyoung-Ju;Hyung, Won-Gil
    • Journal of the Korea Institute of Building Construction
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    • v.20 no.1
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    • pp.19-26
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    • 2020
  • This study aimed to develop non-sintered cement that could replace portland cement which emits large amount of carbon dioxide during firing process. For this purpose, ground granulated blast furnace slag, type c fly ash and slaked lime were used. In addition, through the experimental results, the characteristics of the non-sintered cement binders according to the mixing ratios will be identified, and the utilization plans for the precast concrete products will be presented. In this experiment, non-sintered cement binders using industrial by-products were prepared to compare the flexural strength and compressive strength of each of the 3, 7 and 28 days. As a result, the results satisfy the KS of the target product proposed in this study. Therefore, this study presents the possibility of using precast concrete products by developing non-sintered cement binders using industrial by-products.

Binding Mode Studies of Indenoisoquinoline Analogues into Human Topoisomerase I-DNA Complex Using Flexible Docking (Human Topoisomerase I-DNA 절개가능 복합체에 대한 Indenoisoquinoline 유도체들의 결합양상 연구)

  • Park, In-Seon;Kim, Bo-Yeon;Kim, Choon-Mi;Choi, Sun
    • YAKHAK HOEJI
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    • v.53 no.4
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    • pp.228-234
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    • 2009
  • Topoisomerase I (Topo I) participates in the DNA replication, transcription, and repair. Binding of Topo I inhibitor to the Topo I-DNA cleavage complex forms stabilized ternary complex which blocks DNA religation and ultimately causes cell death. Camptothecin (CPT) and its derivatives have been among the most effective anticancer drugs by inhibition of topo I. However, efforts to synthesize non-CPT drugs have been actively going on because the CPT derivatives have several limitations such as poor solubility, short half-life, and side effects. As an indenoisoquinoline, NSC314622 is not as potent as CPT, but its chemical stability and slower reversibility of the cleavage complex made it a good lead compound. Recently, a series of indenoisoquinoline analogues were synthesized with substituted dimethoxy or methylenedioxy on the aromatic ring and alkylamino on the lactam nitrogen. Some of them showed quite good Topo I inhibitory activity. Using the computer docking program, Surflex-Dock, indenoisoquinoline analogues were docked into the human Topo I-DNA cleavable complex. The docking results showed that the compounds with activity better than NSC314622 intercalated between the -1 and +1 base pairs at the cleavage site, but those with little or no activities did not appear to intercalate. These results could be useful to design new Topo I inhibitors improved than CPT.

Building a Nonlinear Relationship between Air and Water Temperature for Climate-Induced Future Water Temperature Prediction (기후변화에 따른 미래 하천 수온 예측을 위한 비선형 기온-수온 상관관계 구축)

  • Lee, Khil-Ha
    • Journal of Environmental Policy
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    • v.13 no.2
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    • pp.21-38
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    • 2014
  • In response to global warming, the effect of the air temperature on water temperature has been noticed. The change in water temperature in river environment results in the change in water quality and ecosystem, especially Dissolved Oxygen (DO) level, and shifts in aquatic biota. Efforts need to be made to predict future water temperature in order to understand the timing of the projected river temperature. To do this, the data collected by the Ministry of Environment and the Korea Meteororlogical Administration has been used to build a nonlinear relationship between air and water temperature. The logistic function that includes four different parameters was selected as a working model and the parameters were optimized using SCE algorithm. Weekly average values were used to remove time scaling effect because the time scale affects maximum and minimum temperature and then river environment. Generally speaking nonlinear logistic model shows better performance in NSC and RMSE and nonlinear logistic function is recommendable to build a relationship between air and water temperature in Korea. The results will contribute to determine the future policy regarding water quality and ecosystem for the decision-driving organization.

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An Evaluation on Punching Shear Capacity of R/C Flat Plate Slab (RC 플랫 플레이트 슬래브의 뚫림전단성능평가)

  • Kim, Jong-Keun;Shin, Sung-Woo;Yang, Ji-Soo;Lee, Li-Hyung
    • Journal of the Korea institute for structural maintenance and inspection
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    • v.7 no.3
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    • pp.205-213
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    • 2003
  • The primary purpose of this study is to investigate punching shear capacity of flat plate slab using high strength concrete in column. It may be much contributed to economy efficiency and structural advantages that High Strength Concrete(HSC) used for vertical member and Normal Strength Concrete(NSC) for horizontal member. Therefore, six plate flat slab specimens with HSC column and NSC slab had been made and tested with real scale. The major variables were compressive strength of concrete(fck=285, $460kgf/cm^2$), extended length of HSC from column face and amount of shear reinforcements. As the result of this test, the maximum load and punching shear capacity of specimens is affected by extended length and shear reinforcements.

An Aminopropyl Carbazole Derivative Induces Neurogenesis by Increasing Final Cell Division in Neural Stem Cells

  • Shin, Jae-Yeon;Kong, Sun-Young;Yoon, Hye Jin;Ann, Jihyae;Lee, Jeewoo;Kim, Hyun-Jung
    • Biomolecules & Therapeutics
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    • v.23 no.4
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    • pp.313-319
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    • 2015
  • P7C3 and its derivatives, 1-(3,6-dibromo-9H-carbazol-9-yl)-3-(p-tolylamino)propan-2-ol (1) and N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-hydroxypropyl)-N-(3-methoxyphenyl)-4-methylbenzenesulfonamide (2), were previously reported to increase neurogenesis in rat neural stem cells (NSCs). Although P7C3 is known to increase neurogenesis by protecting newborn neurons, it is not known whether its derivatives also have protective effects to increase neurogenesis. In the current study, we examined how 1 induces neurogenesis. The treatment of 1 in NSCs increased numbers of cells in the absence of epidermal growth factor (EGF) and fibroblast growth factor 2 (FGF2), while not affecting those in the presence of growth factors. Compound 1 did not induce astrocytogenesis during NSC differentiation. 5-Bromo-2'-deoxyuridine (BrdU) pulsing experiments showed that 1 significantly enhanced BrdU-positive neurons. Taken together, our data suggest that 1 promotes neurogenesis by the induction of final cell division during NSC differentiation.

Induced neural stem cells from human patient-derived fibroblasts attenuate neurodegeneration in Niemann-Pick type C mice

  • Hong, Saetbyul;Lee, Seung-Eun;Kang, Insung;Yang, Jehoon;Kim, Hunnyun;Kim, Jeyun;Kang, Kyung-Sun
    • Journal of Veterinary Science
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    • v.22 no.1
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    • pp.7.1-7.13
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    • 2021
  • Background: Niemann-Pick disease type C (NPC) is caused by the mutation of NPC genes, which leads to the abnormal accumulation of unesterified cholesterol and glycolipids in lysosomes. This autosomal recessive disease is characterized by liver dysfunction, hepatosplenomegaly, and progressive neurodegeneration. Recently, the application of induced neural stem cells (iNSCs), converted from fibroblasts using specific transcription factors, to repair degenerated lesions has been considered a novel therapy. Objectives: The therapeutic effects on NPC by human iNSCs generated by our research group have not yet been studied in vivo; in this study, we investigate those effects. Methods: We used an NPC mouse model to efficiently evaluate the therapeutic effect of iNSCs, because neurodegeneration progress is rapid in NPC. In addition, application of human iNSCs from NPC patient-derived fibroblasts in an NPC model in vivo can give insight into the clinical usefulness of iNSC treatment. The iNSCs, generated from NPC patientderived fibroblasts using the SOX2 and HMGA2 reprogramming factors, were transplanted by intracerebral injection into NPC mice. Results: Transplantation of iNSCs showed positive results in survival and body weight change in vivo. Additionally, iNSC-treated mice showed improved learning and memory in behavior test results. Furthermore, through magnetic resonance imaging and histopathological assessments, we observed delayed neurodegeneration in NPC mouse brains. Conclusions: iNSCs converted from patient-derived fibroblasts can become another choice of treatment for neurodegenerative diseases such as NPC.

Heat stress effects on fertility and reproductive health problems of dairy cows in a selected area of Bangladesh

  • Rifat J. Sumi;Ziban C. Das;Mohammad N. Hoque;Abu N. M. A. Rahman;Mohammad T. Islam;Anup K. Talukder
    • Journal of Animal Reproduction and Biotechnology
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    • v.37 no.4
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    • pp.266-275
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    • 2022
  • The impact of heat stress (HS) on reproductive performance and its problems in cows remains to be investigated in Bangladesh. The study was, therefore, aimed to evaluate the effect of HS on fertility and reproductive health problems of dairy cows in a selected area of Bangladesh. A total of 1,095 cows from 500 farms were included in this study. The climate-related data were recorded daily basis for every month in a year and temperature-humidity index (THI) values were calculated to determine the level of HS. Concurrently, data on fertility parameters [number of services per conception (NSC), conception rate (CR) and calving to the first service interval (CFSI)], and reproductive problems were collected through a pre-defined questionnaire. The results show that crossbred [Native x Holstein-Friesian, (HF)] cows were more vulnerable (p < 0.05) to a magnitude of HS effects considering physiological parameters of cows [age, body condition score (BCS), parity and milk yield]. Regarding fertility, HS had no effect on NSC, CR and CFSI in both native and crossbred cows (p > 0.05). The findings on the reproductive problems indicate that HS had significant influence on the prevalence of anestrus (χ2 = 21.814, p < 0.05) and retained placenta (χ2 = 24.632, p < 0.05) in cows. Of note, the prevalence of repeat breeding syndrome was 2.5 folds higher in stress condition than in no stress condition. Abortion and dystocia were not influenced by HS. In conclusion, HS does not influence the fertility parameters of cows studied; however, anestrus and retained placenta are likely to occur under HS conditions in cows.

Effects of Namhae Specialized Crops Water Extract on Lipid Metabolism in Rats Fed a Cholesterol Diet (남해군 특용작물 열수 추출분말이 콜테스테롤 급이 흰쥐의 혈청 및 장기 중 지질성분에 미치는 영향)

  • Shin, Jung-Hye;Kang, Min-Jung;Yang, Seung-Mi;Lee, Soo-Jung;Sung, Nak-Ju
    • Korean journal of food and cookery science
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    • v.27 no.5
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    • pp.599-610
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    • 2011
  • This study was performed to investigate the effect of water extracts from Namhae special crops (NSC) on improved serum lipid composition using rats fed a 1% cholesterol diet for 4 weeks. Male Wister rats (200-210 g) were divided into six groups: Normal cholesterol diet group (Normal), 1% cholesterol diet group (Control), 1% cholesterol and NSC water extract powder supplemented groups, including, turmeric (Tu-EP), cactus (Ba-EP), aloe vera (Al-EP) and asparagus (As-EP). No significant differences were observed for food intake or body weight gain between the control and experimental groups. However, food efficiency ratio (FER) was the lowest in the As-EP group. The serum levels of total cholesterol and triglycerides in the NSC water powder extract supplement groups were lower than those in the control group. The serum high density lipoprotein (HDL)-cholesterol content in the Tu-EP group was higher than that in the other experimental groups. Very low density lipoprotein (VLDL)-cholesterol content in the As-EP group was similar to that in normal group. Furthermore, the VLDL content in the Al-EP group was lower than that in the normal group. Serum antioxidant activity by TBARS level and DPPH radical scavenging were significantly higher in the Ba-EP group than that in the control group. Hepatic total cholesterol and lipid content in the Al-EP group decreased significantly compared to that in the control group. These results suggest that the NSC water extract may reduce serum cholesterol and prevent oxidative stress by stimulating antioxidative systems in rats fed a 1% cholesterol diet.