• 제목/요약/키워드: SRC-3

검색결과 210건 처리시간 0.034초

Pyrrole-Derivative of Chalcone, (E)-3-Phenyl-1-(2-Pyrrolyl)-2-Propenone, Inhibits Inflammatory Responses via Inhibition of Src, Syk, and TAK1 Kinase Activities

  • Yang, Sungjae;Kim, Yong;Jeong, Deok;Kim, Jun Ho;Kim, Sunggyu;Son, Young-Jin;Yoo, Byong Chul;Jeong, Eun Jeong;Kim, Tae Woong;Han Lee, In-Sook;Cho, Jae Youl
    • Biomolecules & Therapeutics
    • /
    • 제24권6호
    • /
    • pp.595-603
    • /
    • 2016
  • (E)-3-Phenyl-1-(2-pyrrolyl)-2-propenone (PPP) is a pyrrole derivative of chalcone, in which the B-ring of chalcone linked to ${\beta}$-carbon is replaced by pyrrole group. While pyrrole has been studied for possible Src inhibition activity, chalcone, especially the substituents on the B-ring, has shown pharmaceutical, anti-inflammatory, and anti-oxidant properties via inhibition of NF-${\kappa}B$ activity. Our study is aimed to investigate whether this novel synthetic compound retains or enhances the pharmaceutically beneficial activities from the both structures. For this purpose, inflammatory responses of lipopolysaccharide (LPS)-treated RAW264.7 cells were analyzed. Nitric oxide (NO) production, inducible NO synthase (iNOS) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) mRNA expression, and the intracellular inflammatory signaling cascade were measured. Interestingly, PPP strongly inhibited NO release in a dose-dependent manner. To further investigate this anti-inflammatory activity, we identified molecular pathways by immunoblot analyses of nuclear fractions and whole cell lysates prepared from LPS-stimulated RAW264.7 cells with or without PPP pretreatment. The nuclear levels of p50, c-Jun, and c-Fos were significantly inhibited when cells were exposed to PPP. Moreover, according to the luciferase reporter gene assay after cotransfection with either TRIF or MyD88 in HEK293 cells, NF-${\kappa}B$-mediated luciferase activity dose-dependently diminished. Additionally, it was confirmed that PPP dampens the upstream signaling cascade of NF-${\kappa}B$ and AP-1 activation. Thus, PPP inhibited Syk, Src, and TAK1 activities induced by LPS or induced by overexpression of these genes. Therefore, our results suggest that PPP displays anti-inflammatory activity via inhibition of Syk, Src, and TAK1 activity, which may be developed as a novel anti-inflammatory drug.

가열온도, 가열시간 및 부형제의 첨가량이 도축 반추위 내용물의 자일란, 셀룰로오스 및 전분 분해효소 활성에 미치는 영향 (Effects of Temperature and Time for Heating and Filler Content on the Activities of Xylanase, Cellulase and Amylase in Slaughterhouse Rumen Content)

  • 원미영;이도형;김은중
    • 한국초지조사료학회지
    • /
    • 제33권1호
    • /
    • pp.58-66
    • /
    • 2013
  • 본 연구는 도축장에서 폐기되는 도축 반추위 내용물을 사일리지 혹은 TMR (total mixed ration) 사료 첨가용 효소제로 개발하기 위한 목적으로 수행되었다. 도축 반추위 내용물에는 상당한 수분이 함유되어 있어, 적절한 건조과정을 거치지 않고서는 그 활용이 원활하지 않다. 그러나 효소는 열에 민감한 단백질로 구성되어 있기 때문에 적절한 건조 조건의 개발이 필요하다. 본 연구에서는 통계적 방법을 이용하여 가열온도(60, 75, $90^{\circ}C$), 가열시간(12, 30, 48 시간) 및 부형제의 비율(12, 22.5, 33%)이 도축 반추위 내용물에 함유된 다양한 효소활성에 미치는 효과를 분석하였다. 총 3가지 효소, xylan 분해효소, 셀룰로오스 분해효소 및 전분 분해효소를 검토하였고, 각 효소활성들에 대한 각 요인들의 효과가 매우 다양하게 나타났다(p<0.05). 셀룰로오스 분해효소와 전분 분해효소의 활성은 가열온도가 증가함에 따라 감소하였으며(p<0.05), xylan 분해해소는 열에 대한 안전성이 다른 효소들에 비하여 우수하였다. 자일란, 셀룰로오스, 전분 분해효소를 증가시키는 적정 부형제의 비율은 22.5, 12 그리고 33%로 나타났다. 비록 3가지 효소들의 제형화에 있어 공통적으로 적용될 수 있는 최적점을 도출하지는 못하였으나, 본 연구결과에서 얻어진 효소들의 반응 값들을 이용하여 목적하는 효소에 따라서 다양한 방법으로 적용이 가능할 것으로 판단된다.

SRC기둥-H형단면과 U형단면으로 구성된 합성보 접합부의 반복가력실험 (Cyclic Loading Test on Connection of SRC Column-Composite Beam Consisting of H-Section and U-Section Members)

  • 김영주;배재훈;안태상;김진원;유홍식
    • 한국강구조학회 논문집
    • /
    • 제26권4호
    • /
    • pp.263-275
    • /
    • 2014
  • 본 연구에서는 SRC 기둥-H형단면과 U형단면으로 구성된 합성보 접합부에 관해서 반복가력실험을 실시하였다. 합성보에 관한 핵심요소는 H형단면과 U형단면 간 용접접합부의 구조적 성능이다. 이 두 부재 접합부의 성능을 향상시키기 위해서는 수직스티프너와 사다리꼴 스티프너가 필요하다. 접합부의 반복적인 성능을 평가하기 위해서 5개의 실대형 실험체를 계획하였으며, 실험변수는 H형단면의 크기($H-500{\times}200{\times}10{\times}16$, $H-600{\times}200{\times}11{\times}17$), 스티프너와 상부근의 유무 및 용접접근공(WAH)의 유무 등이다. 실험결과, H-500 시리즈 및 H-600 시리즈 보가 있는 실험체의 회전각은 각각 4%와 3%로 나타났으며, 이는 특수모멘트골조와 중간모멘트골조에 요구되는 값이다. 실험결과는 스티프너와 상부근이 있는 실험체의 변형능력이 그렇지 않은 실험체에 비해서 우수한 결과를 보였다. 끝으로, 실험체의 에너지소산능력과 변형도 분포를 요약하였다.

Comparison of Milling and Flour Quality Characteristics of Foreign Wheat and Korean Wheat

  • Jinhee Park;Kyeong-Hoon Kim;Chon-Sik Kang;Go Eun Lee;Kyeong-Min Kim;Mina Kim;Han-yong Jeong;Yurim Kim;Jiyoung Shon;Jong-Min Ko
    • 한국작물학회:학술대회논문집
    • /
    • 한국작물학회 2022년도 추계학술대회
    • /
    • pp.296-296
    • /
    • 2022
  • This study was investigated to compare the milling and physicochemical characteristics of six Korean wheat cultivars (Keumkang, KK; Jokyung, JK; Goso, GS; Joongmo2008, JM; Baekkang, BK; Saekeumkang, SKK) and five foreign wheat classes (Australian standard white wheat, ASW; Australian hard, AH; US northern spring, NS; US hard red winter, HRW; Soft wheat, SW). Korea and foreign wheat grains were milled using a Buhler MLU-202. Flour moisture, ash, protein, gluten, sedimentation, particle size, solvent retention capacity (SRC) and dough properties of flour were analyzed. Results showed that the hard wheats had a greater total flour yield and reduction fraction yield than the soft wheats regardless of the country. However, there were in the milling characteristics between the US and Korean soft wheats. GS, a soft wheat in Korea, had the lowest flour yield (59.6%) and the highest bran fraction yield (21.4%). The particle sizes of flour by milling fraction were B1>B2>B3 for the largest, and the R1〈R2〈R3 for the smallest. Particle size, ash, protein contents and the values of lactic acid SRC showed highly correlated with flour yield. The gluten-performance-index (GPI) is the ratio of the lactic acid SRC value to the sum of sodium carbonate and sucrose SRC values, and it has been used as a quality indicator for overall performance potential of flour. GPI values differed depending on the wheat variety or class, JM (0.82) was the highest value, and SKK (0.56) and SW (0.59) were low. The curve pattern of the Mixolab result also gives a quality indication of the flour sample. JM and NS flour had similar pattern at water absorption and gluten strength parameters and BK and HRW had similar viscosity patterns. These results will enable further study for blending Korean wheat cultivar to improve the flour quality.

  • PDF

Human Estrogen Receptor Ligand Binding Domain (hER LBD)과 Co-activator로 구성된 효모 Two-Hybrid System을 이용한 내분비계장애물질 검출계의 구축 (Construction of the Detection System of Endocrine Disrupters using Yeast Two-Hybrid System with Human Estrogen Receptor ligand Binding Domain and Co-activators)

  • 이행석;조은민;류재천
    • 한국환경성돌연변이발암원학회지
    • /
    • 제22권3호
    • /
    • pp.175-182
    • /
    • 2002
  • Endocrine disruptors (EDs) are the chemicals that affect endocrine systems through activation or inhibition of steroid hormone response. It is necessary to have a good system to evaluate rapidly and accurately endocrine-disrupting activities of suspected chemicals and their degradation products. The key targets of EDs are nuclear hormone receptors, which bind to steroid hormones and regulate their gene transcription. We constructed a co-expression system of Gal4p DNA binding domain (DBD)- ligand binding domain of human estrogen receptor $\alpha$ or $\beta$, and Gal4p transactivation domain (TAD)-co-activator AIB-1, SRC-1 or TIF-2 in Saccharomyces cerevisiae with a chromosome-integrated lacZ reporter gene under the control of CYC1 promoter and Gal4p binding site (GAL4 upstream activating sequence, GAL4$_{UAS}$). Expression of this reporter gene was dependent on the presence of estrogen or EDs in the culture medium. We found that the two-hybrid system with combination of the hER$\beta$ LBD and co-activator SRC-1 was most effective in the xenoestrogen-dependent induction of reporter activity. The extent of transcriptional activation by those chemicals correlated with their estrogenic activities measured by other assay systems, indicating that this assay system is efficient and reliable for measuring estrogenic activity. The data in this research demonstrated that the yeast detection system using steroid hormone receptor and co-activator is a useful tool for identifying chemicals that interact with steroid receptors.s.

  • PDF

폴리에틸렌 기반 자기강화복합재료의 성형성 및 기계적 특성에 따른 최적 제직형상 수치해석적 연구 (Study of Optimal Weaving Shape according to Formability and Mechanical Properties of Polyethylene-based Self-reinforced Composite)

  • 유성훈;이필규;이종혁;김늘새롬;심지현
    • 한국염색가공학회지
    • /
    • 제34권1호
    • /
    • pp.58-67
    • /
    • 2022
  • In this study, self-reinforced composite(SRC) was prepared using HDPE(High density polyethylene) fabric(2×2 plain) and LDPE(Low density polyethylene) film. The optimal conditions were derived by manufacturing specimens according to the temperature of 100 ~ 140℃ using a hot stamping at a pressure of 100bar for 10 minutes in order to find the optimal conditions for the SRC. The manufactured SRC was analyzed for tensile properties, compressive strength and shear strength through a universal testing machine(UTM). As a result of the measurement, the P3 specimen prepared by hot stamping at a temperature of 130℃ and a pressure of 100bar for 10 minutes was found to be higher than other specimens with tensile strength and tensile modulus of 210MPa and 19GPa, compressive strength 69MPa and shear strength 13MPa and it was considered to be optimal condition. Finally, the composite material according to the fabric structure was modeled using experimental values and the physical properties of the composite material according to the fabric structure were predicted using GeoDict and Digimat.

Experimental study on seismic performance of steel reinforced concrete T-shaped columns

  • Liu, Zuqiang;Zhou, Chaofeng;Xue, Jianyang;Leon, Roberto T.
    • Steel and Composite Structures
    • /
    • 제36권3호
    • /
    • pp.339-353
    • /
    • 2020
  • This study investigates the seismic performance of steel reinforced concrete (SRC) T-shaped columns under low cyclic loading tests. Based on test results of ten half-scale column specimens, failure patterns, hysteretic behavior, skeleton curves, ultimate strength, ductility, stiffness degradation and energy dissipation capacity were analyzed. The main variables included loading angles, axial compression ratios and steel ratios. The test results show that the average values of the ductility factor and the equivalent viscous damping coefficient with respect to the failure of the columns were 5.23 and 0.373, respectively, reflecting good seismic performance. The ductility decreased and the initial stiffness increased as the axial compression ratio of the columns increased. The strength increased with increasing steel ratio, as expected. The columns displaced along the web had higher strength and initial stiffness, while the columns displaced along the flange had better ductility and energy dissipation capacity. Based on the test and analysis results, a formula is proposed to calculate the effective stiffness of SRC T-shaped columns.

Seismic behaviour of repaired superelastic shape memory alloy reinforced concrete beam-column joint

  • Nehdi, Moncef;Alam, M. Shahria;Youssef, Maged A.
    • Smart Structures and Systems
    • /
    • 제7권5호
    • /
    • pp.329-348
    • /
    • 2011
  • Large-scale earthquakes pose serious threats to infrastructure causing substantial damage and large residual deformations. Superelastic (SE) Shape-Memory-Alloys (SMAs) are unique alloys with the ability to undergo large deformations, but can recover its original shape upon stress removal. The purpose of this research is to exploit this characteristic of SMAs such that concrete Beam-Column Joints (BCJs) reinforced with SMA bars at the plastic hinge region experience reduced residual deformation at the end of earthquakes. Another objective is to evaluate the seismic performance of SMA Reinforced Concrete BCJs repaired with flowable Structural-Repair-Concrete (SRC). A $\frac{3}{4}$-scale BCJ reinforced with SMA rebars in the plastic-hinge zone was tested under reversed cyclic loading, and subsequently repaired and retested. The joint was selected from an RC building located in the seismic region of western Canada. It was designed and detailed according to the NBCC 2005 and CSA A23.3-04 recommendations. The behaviour under reversed cyclic loading of the original and repaired joints, their load-storey drift, and energy dissipation ability were compared. The results demonstrate that SMA-RC BCJs are able to recover nearly all of their post-yield deformation, requiring a minimum amount of repair, even after a large earthquake, proving to be smart structural elements. It was also shown that the use of SRC to repair damaged BCJs can restore its full capacity.

Src Family Kinase Inhibitor PP2 Induces LC3 Conversion in a Manner That is Uncoupled from Autophagy and Increases Apoptosis in Multidrug-Resistant Cells

  • Kim, Yun-Ki;Ahn, Jun-Ho;Lee, Mi-Chael
    • Biomolecules & Therapeutics
    • /
    • 제20권4호
    • /
    • pp.393-398
    • /
    • 2012
  • Recently, we reported that defective autophagy may contribute to the inhibition of the growth in response to PP2 (4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine), a selective SFK inhibitor, in multidrug-resistant v-Ha-ras-transformed NIH 3T3 cells (Ras-NIH 3T3/Mdr). In this study, we demonstrated that PP2 induces LC3 conversion via a mechanism that is uncoupled from autophagy and increases apoptosis in Ras-NIH 3T3/Mdr cells. PP2 preferentially induced autophagy in Ras-NIH 3T3 cells rather than in Ras-NIH 3T3/Mdr cells as determined by LC3-I to LC3-II conversion and GFP-LC3 fluorescence microscopy. Beclin 1 knockdown experiments showed that, regardless of drug resistance, PP2 induces autophagy via a Beclin 1-dependent mechanism. PP2 induced a conformational change in Beclin 1, resulting in the enhancement of the pro-autophagic activity of Beclin 1, in Ras-NIH 3T3 cells. Further, PI3K inhibition induced by wortmannin caused a significant increase in apoptosis in Ras-NIH 3T3 cells, as demonstrated by flow cytometric analysis of Annexin V staining, implying that autophagy inhibition through PI3K increases apoptosis in response to PP2 in Ras-NIH 3T3 cells. However, despite the fact that wortmannin abrogates PP2-induced GFP-LC3 punctae formation, some LC3 conversion remains in Ras-NIH 3T3/Mdr cells, suggesting that LC3 conversion may occur in an autophagy-independent manner. Taken together, these results suggest that PP2 induces LC3 conversion independent of PI3K, concomitant with the uncoupling of LC3 conversion from autophagy, in multidrug-resistant cells.

溫肺湯과 溫肺湯去총白의 抗알레르기效果 및 鎭痛, 解熱作用에 대한 實驗的 硏究 (Experimental sutdy on the anti-allergic effects of Onpyetang and Onpyetang-Gechongbaek)

  • 박재현;채병윤
    • 한방안이비인후피부과학회지
    • /
    • 제14권2호
    • /
    • pp.154-172
    • /
    • 2001
  • Major symptoms of al1ergic rhinitis are nasal obstruction, sneezing and watery rhinorrhea. Onpyetang has been used to treat for nasal obstruction, which is one of the symptoms of allergic rhinitis. This Experimental study was done to research effects of Onpyetang and transformed Onpyetang(Allii Radix is deducted from Onpyetang) on the anti-allergic effects. We have studied the vascular permeability response induced by serotonin and histamine, the contact dermatitis response induced by picryl chloride, the delayed type hypersensitivity response to SRC, the mice paw edema induced by carrageenin, the writhing syndrome induced by $0.7\%$ acetic acid, and the rectal temperature in febrile rats induced by yeast. The results were as follows : 1. In the vascular permeability response to intradermal serotonin and histamine. Onpyetang proved significant inhibitory effect(P<0.05, p<0.001) But transformed Onpyetang proved significant inhibitory effect only to histamine(P<0.05) 2. In the contact dermatitis response induced by picryl chloride, Onpyetang and transformed Onpyetang proved significant inhibitory effect.(P<0.05, P<0.05) 3. In the delayed type hypersensitivity response induced by SRC, Onpyetang and transformed Onpyetang proved significant inhibitory effect on mice paw edema.. (P<0.05, P<0.05) 4. In the delayed type hypersensitivity response induced by SRC, Onpyetang proved significant inhibitory effect to serum IgE.(P<0.01) But transformed Onpyetang proved insignificant inhibitory effect on serum Ig E. 5. In the mice paw edema induced by carrageenin, Onpyetang and transformed Onpyetang proved significant anti-inflammatory effect. (P<0.01, P<0.01) 6. In the writhing syndrome induced $0.7\%$ acetic acid, Onpyetang and transformed Onpyetang proved significant analgestic effect. (P<0.01, P<0.01) 7. In the rectal temperature in febrile rats induced by yeast, Onpyetang and transformed Onpyetang proved significant anti-pyretic effect.(P<0.001, P<0.01) according to this result Onpyetang was conclude to be effective on anti-allergic, anti-pyretic, anti-inflammatory and analgestic action. but transformed Onpyetang(Allii Radix is deducted from Onpyetang) was not effective on the vascular permeability response to intradermal serotonin and increasing Ig E of delayed type hypersensitivity response induced by SRC. In addition, transformed Onpyetang is not effective as Onpyetang. More study should be done about the role of Allii Radix.

  • PDF