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Synthesis of New 4-Oxo-2-Thioxo-1,2,3,4-Tetrahydropyrimidine Derivatives with an Incorporated Thiazolidinone Moiety and Testing Their Possible Serine Protease and Cercarial Elastase Inhibitory Effects with a Possible Prospective to Block Penetration of Schistosoma mansoni Cercariae into the Mice Skin

  • Bahgat Mahmoud Mohamed;Maghraby Amany Sayed;Heiba Mogeda Emam;Ruppel Andreas;Fathalla Omar Abd-elfattah Mohamed
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1002-1012
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    • 2005
  • 5-Substituted 4-oxo-2-thioxo-1,,2,3,4-tetrahydropyrimidine were synthesized by interaction of 4­oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonylhydrazide with some aldehydes to give the corresponding Schiff-bases, which after cyclization gave corresponding thiazolidinones. For some of the thiazolidinones, Mannich bases reaction was carried out. All the derivatives were tested for their possible inhibitory effect on Schistosoma mansoni cercarial elastase (CE). Only, N'-(4-methylbenzyledine)-4-oxo-2-thioxo-1,2 ,3,4-tetrahydropyrimidine-5-sulfonylhydrazide was found to have potent inhibitory effect on the CE activity with $IC_{50} = 264{\mu}M.$ Upon its use as a paint for mice tails before infection with S. mansoni cercariae, the compound formulated in jojoba oil caused a significant reduction ($93\%$; P-value = 0.0002) in the worm burden. IgG & IgM in mice sera were measured by using several S. mansoni antigens by ELISA. Sera from treated infected mice (TIM) 2, 4, and 6 weeks (W) post infection (PI) showed 1.2 folds lower, 1.2 folds higher, 1.7 folds lower IgM reactivity against soluble cercarial antigenic preparation (CAP), respectively, when compared with sera collected from infected untreated mice (IUM). Sera from TIM 2, 4, and 6WPI showed 1.3, 1.6, and 1.7 folds higher IgG reactivity, respectively against CAP than the IgG reactivity from IUM. Sera from TIM 2, 4 and 6WPI showed 1.5, 1.2 folds lower and 1.4 folds higher IgM reactivity, respectively against soluble worm antigenic preparation (SWAP) when compared with sera collected from IUM. Sera from TIM 2, 4, and 6WPI showed 1.4, 1 folds lower and 1 fold higher IgG reactivity, respectivley to SWAP when compared with sera from IUM. Sera from TIM 2, 4, and 6WPI had generaly lower IgM and IgG reactivities against soluble egg antigen (SEA) when compared with sera from IUM.

Application of AFLPs to Phylogenetic Analysis of Aegilops (AFLPs에 의한 Aegilops의 계통발생학적 재평가)

  • Park, Yong-Jin;Shim, Jae-Wook
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.42 no.6
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    • pp.790-799
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    • 1997
  • Aegilops genus is known to include the donor species of the Band D genome of the bread wheat(ABD). An effort to establish a better strategy for phylogenetic relationships about Aegilops polyploids by AFLPs(Amplified Fragment Length Polymorphisms) was conducted using the 19 Aegilops sPP. and T. aestivum. The 207 polymorphic bands from the amplified products on the 6% acrylamide denaturing sequencing gels were obtained with the 7 AFLP primer combinations, and used to account for the genetic similarities and cluster analysis using NTSYS program. According to the genome analysis, the $M^h$-genome of Ae. heldreichii was estimated as an intermediate genome between the M-genome of Ae. comosa and N-genome of Ae. uniaristata and supposed to be incorporated in the establishing process of UM-genome as a possible diploid donor. And Ae. ventricosa(DN) was more close to Ae. umbellulata(U) than Ae. squarrosa(D). The close relationship between Ae. squarrosa and T. aestivum was perceived as a diploid donor of D-genome. As for the polyploid species, hexaploid Ae. triaristata was more closely related to Ae. columnaris rather than tetraploid Ae. triaristata. The clustered groups were, basically same to the previous Gihara's sections based on phenotypes and pairing analysis of interspecific hybrids. AFLP was evaluated as an efficient and powerful method in the genome evaluation of closely related species.

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Comparing the Service Coverages of Subways and Buses and Estimating the Walking Distances of Their Users (지하철과 버스의 서비스권역 비교 및 이용자들의 도보거리 추정 - 부산시를 중심으로 -)

  • Kim, Kyung Whan;Lee, Deok Hwan;Choi, Jong Moon;Oh, Il Sung
    • KSCE Journal of Civil and Environmental Engineering Research
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    • v.30 no.6D
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    • pp.541-552
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    • 2010
  • The light rail transit (LRT) having bus lines as subsystem is being constructed or planned in the suburban area of metropolitans and medium size cities. However, there is difficulty in establishing the service coverage (SC) of the LRT because the LRT is a completely new transit mode in Korea. The purpose of this study is to provide the basic data and techniques to be used for establishing the SC of the future LRT by understanding the SC characteristics of buses and subways and building models to estimate the walking distances of their users. Busan City is selected as the study city and the SC's of buses and subways are surveyed simultaneously. A total of 9 variables for 82 stations are collected and the cluster analysis is conducted about the variables. The station areas are divided to three types of CBD (Central Business District), sub-CBD and regional center based on the analysis. A station in each area is selected as the study station. At the walking distance (WD) analysis for each mode, the 80 percentile WD of the subway is 672 m and that of the bus is 472 m. In comparing the SC's of both modes by the type of station areas, there are not significant differences between the SC's of sub-CBD and regional center except CBD. At analysis of the relationship between the personal attributes and the WD, for subway users the WD of female is longer than that of male and apartment residents use subway more positively than single house residents do. For the models to estimate the walking distances, the simple regression models were built employing the income as independent variable by dividing the stations into CBD abd non-CBD stations.

Automated Analysis for PDC-R Technique by Multiple Filtering (다중필터링에 의한 PDC-R 기법의 자동화 해석)

  • Joh, Sung-Ho;Rahman, Norinah Abd;Hassanul, Raja
    • KSCE Journal of Civil and Environmental Engineering Research
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    • v.30 no.3C
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    • pp.141-148
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    • 2010
  • Electrical noises like self potential, burst noises and 60-Hz electrical noises are one of the causes to reduce reliability of electrical resistivity survey. Even the PDC-R (Pseudo DC resisitivity) technique, recently developed, is suffering from the problem of low reliability due to electrical noises. That is, both DC-based and AC-based resistivity technique is subject to reliability problem due to electrical noises embedded in urban geotechnical sites. In this research, a new technique to enhance reliability of the PDC-R technique by minimizing influence of electrical noises was proposed. In addition, an automated procedure was also proposed to facilitate data analysis and interpretation of PDC-R measurements. The proposed technique is composed of two steps: 1. to extract information only related with the input current by means of multiple-filter technique, and 2. to undertake a task to sort out signal information only to show stable and reliable characteristics. This automated procedure was verified by a synthetic harmonic wave including DC shift, burst random noises and 60-Hz electrical noises. Also the procedure was applied to site investigation at urban areas for proving its feasibility and accuracy.

Anti-inflammatory Effects of Quercetin and Vitexin on Activated Human Peripheral Blood Neutrophils - The effects of quercetin and vitexin on human neutrophils -

  • Nikfarjam, Bahareh Abd;Hajiali, Farid;Adineh, Mohtaram;Nassiri-Asl, Marjan
    • Journal of Pharmacopuncture
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    • v.20 no.2
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    • pp.127-131
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    • 2017
  • Objectives: Polymorphonuclear neutrophils (PMNs) constitute the first line of defense against invading microbial pathogens. Early events in inflammation involve the recruitment of neutrophils to the site of injury or damage where changes in intracellular calcium can cause the activation of pro-inflammatory mediators from neutrophils including superoxide generation, degranulation and release of myeloperoxidase (MPO), productions of interleukin (IL)-8 and tumor necrosis factor ${\alpha}$ ($TNF-{\alpha}$), and adhesion to the vascular endothelium. To address the anti-inflammatory role of flavonoids, in the present study, we investigated the effects of the flavonoids quercetin and vitexin on the stimulus-induced nitric oxide (NO), $TNF-{\alpha}$, and MPO productions in human neutrophils. Methods: Human peripheral blood neutrophils were isolated, and their viabilities were determined by using the Trypan Blue exclusion test. The polymorphonuclear leukocyte (PMNL) preparations contained more than 98% neutrophils as determined by morphological examination with Giemsa staining. The viabilities of cultured neutrophils with various concentrations of quercetin and vitexin ($1-100{\mu}M$) were studied using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays. Neutrophils were cultured in complete Roswell Park Memorial Institute (RPMI) medium, pre-incubated with or without quercetin and vitexin ($25{\mu}M$) for 45 min, and stimulated with phorbol 12-myristate 13-acetate (PMA) ($10^{-7}M$). NO production was carried out through nitrite determination by using the Griess method. Also, the $TNF-{\alpha}$ and the MPO productions were measured using enzyme-linked immunosorbent assay (ELISA) kits and MPO assay kits. Results: Neutrophil viability was not affected up to a concentration of $100{\mu}M$ of quercetin or vitexin. Both quercetin and vitexin significantly inhibited $TNF-{\alpha}$, NO, and MPO productions in human neutrophils (P < 0.001). Conclusion:The present study showed that both quercetin and vitexin had significant anti-inflammatory effects. Thus, treatment with either quercetin or vitexin may be considered as a therapeutic strategy for treating patients with neutrophil-mediated inflammatory diseases.

An Extrapolation from Crop Classifications Based on Pesticide Residues Trial Data within Vegetables in Minor Crops (소면적 재배작물의 농약 잔류성 시험 후 작물 그룹화를 통한 외삽적용)

  • Park, Jong-Hyouk;Mamun, M.I.R.;El-Aty, A.M.Abd;Choi, Jeong-Heui;Im, Geon-Jae;Oh, Chang-Hwan;Shim, Jae-Han
    • The Korean Journal of Pesticide Science
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    • v.13 no.1
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    • pp.28-38
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    • 2009
  • An extrapolation of residue data of seven commonly used pesticides namely bifenthrin, chlorothalonil, cypermethrin, diazinon, fenvalerate, phenthoate and procymidone on a total of 22 minor crops has been carried out in an experimental field trial. The pesticides were applied to 11 leafy-, 5 root- and 6 stem-crops grown in the experimental green-house and the crops and plants were randomly collected at 1, 3, 5, 7 days after application. The average recoveries of applied pesticides were ranged from 72.0 to 117.0% in leafy crops, from 81.3 to 105.0% in stem crops and from 70.1 to 108.1% in the root-crops. Limits of detection (LODs) were 0.005-0.1 mg/kg in the leafy crops and 0.001-0.005 mg/kg in both the stem & root crops. Based on the results of residual dissipation pattern and their morphology, all crops were classified into high and low residual groups. The results showed that it might be possible to extrapolate residual data of stem-crops to root-crops within the same group. Crops that have currently no registered pesticide for use, would be possible to use the pesticides which are already been registered for the similar crops.

Exploring Preservice Science Teachers' Views of the Nature of Science: Biology vs. Non-Biology Teachers (예비 과학교사의 과학의 본성에 대한 인식 조사: 생물과 비생물 교사와의 비교)

  • Kim, Sun-Young
    • Journal of The Korean Association For Science Education
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    • v.30 no.2
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    • pp.206-217
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    • 2010
  • This study aims to explore preservice teachers' overall views of nature of science and compare their views by gender and certificate area (biology vs. non-biology teachers). In addition, a comparison with American preservice teachers' views was also implemented. The Views of Nature of Science (Abd-El-Khalick, 1998), an openended questionnaire, is utilized to explore participants' views of nature of science. Along with 'definition of science', six aspects of the nature of science, (1) theories and laws, (2) tentativeness, (3) social and cultural embeddedness, (4) creativity, (5) theory-laden, and (6) inference, were investigated. The qualitative result indicates that the participants' first image of science was about the method of science such as observations and experiments. Furthermore, these preservice science teachers particularly have a difficulty in differentiating between scientific theories and laws, and understanding the importance of creation and imagination in developing scientific knowledge. In addition, compared to American preservice teachers' view of the nature of science, Korean preservice teachers possess naive views in creative and imaginative aspect. Interestingly, biology teachers demonstrated lower understanding in theories and laws as well as tentativeness of scientific knowledge. However, there is no difference by gender.

Treatment with Rutin - A Therapeutic Strategy for Neutrophil-Mediated Inflammatory and Autoimmune Diseases - Anti-inflammatory Effects of Rutin on Neutrophils -

  • Nikfarjam, Bahareh Abd;Adineh, Mohtaram;Hajiali, Farid;Nassiri-Asl, Marjan
    • Journal of Pharmacopuncture
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    • v.20 no.1
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    • pp.52-56
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    • 2017
  • Objectives: Neutrophils represent the front line of human defense against infections. Immediately after stimulation, neutrophilic enzymes are activated and produce toxic mediators such as pro-inflammatory cytokines, nitric oxide (NO) and myeloperoxidase (MPO). These mediators can be toxic not only to infectious agents but also to host tissues. Because flavonoids exhibit antioxidant and anti-inflammatory effects, they are subjects of interest for pharmacological modulation of inflammation. In the present study, the effects of rutin on stimulus-induced NO and tumor necrosis factor $(TNF)-{\alpha}$ productions and MPO activity in human neutrophils were investigated. Methods: Human peripheral blood neutrophils were isolated using Ficoll-Hypaque density gradient centrifugation coupled with dextran T500 sedimentation. The cell preparations containing > 98% granulocytes were determined by morphological examination through Giemsa staining. Neutrophils were cultured in complete Roswell Park Memorial Institute (RPMI) medium, pre-incubated with or without rutin ($25{\mu}M$) for 45 minutes, and stimulated with phorbol 12-myristate 13-acetate (PMA). Then, the $TNF-{\alpha}$, NO and MPO productions were analyzed using enzyme-linked immunosorbent assay (ELISA), Griess Reagent, and MPO assay kits, respectively. Also, the viability of human neutrophils was assessed using tetrazolium salt 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT), and neutrophils were treated with various concentrations of rutin ($1-100{\mu}M$), after which MTT was appended and incubated at $37^{\circ}C$ for 4 hour. Results: Rutin at concentrations up to $100{\mu}M$ did not affect neutrophil viability during the 4-hour incubation period. Rutin significantly decreased the NO and $TNF-{\alpha}$ productions in human peripheral blood neutrophils compared to PMA-control cells (P < 0.001). Also, MPO activity was significantly reduced by rutin (P < 0.001). Conclusion: In this in vitro study, rutin had an anti-inflammatory effect due to its inhibiting NO and $TNF-{\alpha}$ productions, as well as MPO activity, in activated human neutrophils. Treatment with rutin may be considered as a therapeutic strategy for neutrophil-mediated inflammatory/autoimmune diseases.

Comparison of the Change in the Prevalence and Intensity of Schistosoma haematobium Infection Between High and Low Prevalence Areas of White Nile State, Sudan

  • Cha, Seungman;Hong, Sung-Tae;Lee, Jin-Su;Jeong, Hoo Gn;Kwon, In-Sun;Saed, Abd Al Wahab;Elhag, Mousab Siddig;Ismail, Hassan Ahmed Hassan Ahmed;Amin, Mutamad;Lee, Young-Ha
    • Parasites, Hosts and Diseases
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    • v.58 no.4
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    • pp.421-430
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    • 2020
  • This study aimed to investigate whether mass drug administration (MDA) intervention has an equivalent effect on reducing the prevalence and intensity of Schistosoma haematobium infection regardless of the baseline values. A repeated cross-sectional survey was performed targeting students of 12 primary schools in Al Jabalain and El Salam districts of White Nile State, Sudan, at both 1 week before and 8 months after the MDA. Prior to the baseline survey, schoolaged children in Al Jabalain had received MDA interventions twice in 4 years, while those in El Salam had not. The baseline prevalence was 9.1% in Al Jabalain and 35.2% in El Salam, which were reduced to 1.8% and 5.5% at 8 months after the MDA, respectively. The corresponding reduction rates were 80.3% and 84.4%, not significant difference between both districts. However, changes in the geometric mean intensity (GMI) of egg counts were significantly different between both districts. The baseline GMIs were 14.5 eggs per 10 ml of urine (EP10) in Al Jabalain and 18.5 EP10 in El Salam, which were reduced to 7.1 and 11.2 EP10 after treatment, respectively. The corresponding reduction rates were 51.0% and 39.5%. In conclusion, MDA interventions were found to bring about similar relative reduction in prevalence regardless of the baseline value; however, the relative reduction in infection intensity was more salient in the district with a low baseline value for both prevalence and intensity. This clearly points to the importance of repeated MDA interventions in endemic areas, which will eventually contribute to schistosomiasis elimination.

Appropriate Timing of Surgery after Neoadjuvant Chemo-Radiation Therapy for Locally Advanced Rectal Cancer

  • Garrer, Waheed Yousry;Hossieny, Hisham Abd El Kader El;Gad, Zeiad Samir;Namour, Alfred Elias;Amer, Sameh Mohammed Ahmed Abo
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.9
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    • pp.4381-4389
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    • 2016
  • Background: Surgery is the corner stone for the management of rectal cancer. The purpose of this study was to demonstrate the optimal time of surgical resection after the completion of neoadjuvant chemo-radiotherapy (CRT) in treatment of locally advanced rectal cancer. Materials and Methods: This study compared 2 groups of patients with locally advanced rectal cancer, treated with neoadjuvant CRT followed by surgical resection either 6-8 weeks or 9-14 weeks after the completion of chemo-radiotherapy. The impact of delaying surgery was tested in comparison to early surgical resection after completion of chemo-radiotherapy. Results: The total significant response rate that could result in functional preservation was estimated to be 3.85% in group I and 15.4% in group II. Some 9.62% of our patients had residual malignant cells at one cm surgical margin. All those patients with positive margins at one cm were in group I (19.23%). There was less operative time in group II, but the difference between both groups was statistically insignificant (P=0.845). The difference between both groups regarding operative blood loss and intra operative blood transfusion was significantly less in group II (P=0.044). There was no statistically significant difference between both groups regarding the intra operative complications (P=0.609). The current study showed significantly less post-operative hospital stay period, and less post-operative wound infection in group II (P=0.012 and 0.017). The current study showed more tumor regression and necrosis in group II with a highly significant main effect of time F=61.7 (P<0.001). Pathological TN stage indicated better pathological tumor response in group II (P=0.04). The current study showed recurrence free survival for all cases at 18 months of 84.2%. In group I, survival rate at the same duration was 73.8%, however none of group II cases had local recurrence (censored) (P=0.031). Disease free survival (DFS) during the same duration (18 months) was 69.4 % for patients in group I and 82.3% for group II (P=0.429). Conclusions: Surgical resection delay up to 9-14 weeks after chemo-radiation was associated with better outcome and better recurrence free survival.