• 제목/요약/키워드: DR-3

검색결과 1,333건 처리시간 0.028초

Molecular Mechanism Underlying Hesperetin-induced Apoptosis by in silico Analysis and in Prostate Cancer PC-3 Cells

  • Sambantham, Shanmugam;Radha, Mahendran;Paramasivam, Arumugam;Anandan, Balakrishnan;Malathi, Ragunathan;Chandra, Samuel Rajkumar;Jayaraman, Gopalswamy
    • Asian Pacific Journal of Cancer Prevention
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    • 제14권7호
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    • pp.4347-4352
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    • 2013
  • Aim: To investigate the molecular mechanisms underlying triggering of apoptosis by hesperetin using in silico and in vitro methods. Methods: The mechanism of binding of hesperetin with NF-${\kappa}B$ and other apoptotic proteins like BAX, BAD, $BCL_2$ and $BCL_{XL}$ was analysed in silico using Schrodinger suite 2009. In vitro studies were also carried out to evaluate the potency of hesperetin in inducing apoptosis using the human prostate cancer PC-3 cell line. Results: Hesperetin was found to exhibit high-affinity binding resulting from greater intermolecular forces between the ligand and its receptor NF-${\kappa}B$ (-7.48 Glide score). In vitro analysis using MTT assay confirmed that hesperetin reduced cell proliferation ($IC_{50}$ values of 90 and $40{\mu}M$ at 24 and 48h respectively) in PC-3 cells. Hesperetin also downregulated expression of the anti-apoptotic gene $BCL_{XL}$ at both mRNA and protein levels and increased the expression of pro-apoptotic genes like BAD at mRNA level and BAX at mRNA as well as protein levels. Conclusion: The results suggest that hesperetin can induce apoptosis by inhibiting NF-${\kappa}B$.

1-Benzyl-3-Methyl Imidazolium Hydrogen Sulphate [bnmim][HSO4] Promoted Synthesis of α-Aminophosphonates

  • Sadaphal, Sandip A.;Sonar, Swapnil S.;Kategaonkar, Amol H.;Shingare, Murlidhar S.
    • Bulletin of the Korean Chemical Society
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    • 제30권5호
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    • pp.1054-1056
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    • 2009
  • We have demonstrated a one-pot three component coupling of an aldehydes, an amines, and triethyl phosphite using 1-benzyl-3-methyl imidazolium hydrogen sulphate [bnmim][][$HSO_{4}$] as an efficient catalyst. All the reactions proceed under solvent-free conditions at room temperature. This methodology afforded the corresponding $\alpha$-aminophosphonates in shorter reaction times with excellent yields.

유희춘이 판각을 주도한 서적에 관한 연구 (A Study on the Books Engraved under the Auspices of Yu Heui-Chun)

  • 배현숙
    • 한국도서관정보학회지
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    • 제34권3호
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    • pp.277-295
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    • 2003
  • 본고는 조선조 중기의 관료이며 학자인 미암 유희춘의 일기를 통해 당시 서적 간행의 양상을 살펴보고자 하였다. 미암 유희춘은 만년에 관직생활을 하면서 일기를 남겼으니 이 $\boxDr$미암일기$\boxUl$에 일상의 일이 매우 자세하게 기록되어 있다. 이를 통하여 당시의 정치, 경제, 사회, 문화, 서적, 가정사까지도 알 수 있다. 본고는 이 일기를 통해 미암의 서적과 관련된 여러 일 가운데 미암이 주도적으로 간행하려고 노력한 서적을 밝혔다. 아울러 당시에 편성된 책판목록에 수록되었는지의 여부도 확인하였다. 미암이 개인적으로 간행하고자 한 서적은 2종류로 나눌 수 있다. 하나는 외조부 금남 최부의 문집인 $\boxDr$금남집$\boxUl$과 중국기행문인 $\boxDr$표해록$\boxUl$이다. 다른 하나는 아동용 도서로 문해용의 $\boxDr$신증류합$\boxUl$과 도덕교육용의 $\boxDr$속몽구$\boxUl$이다. 이들 서적을 인출하기 위해 판각한 당시의 책판은 당대의 책판목록에 수록되어 있어야한다. 그러나 거의 대부분 누락되어 있다. $\boxDr$미암일기$\boxUl$를 통해 책판목록에 누락된 서적을 보완할 수 있으므로 $\boxDr$미암일기$\boxUl$의 중요성을 알 수 있다.

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An Expeditious Room Temperature Stirring Method for the Synthesis of Isoxazolo[5,4-b]quinolines

  • Niralwad, Kirti S.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • 대한화학회지
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    • 제55권5호
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    • pp.805-807
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    • 2011
  • The synthesis of different derivatives of isoxazolo[5,4-b]quinoline by the cyclization reaction of various substituted oximes of quinoline using mild base at ambient temperature. The formation of isoxazolo[5,4-b]quinoline, as a consequence of cheaper and more readily available $K_2CO_3$ and DMF participating in the reaction, is documented.

이중 모드 GPS/DR 통합 칼만필터 (A GPS/DR Integration Kalman Filter with Integration Mode)

  • 서흥석;이재호;성태경;이상정
    • 제어로봇시스템학회논문지
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    • 제7권3호
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    • pp.269-275
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    • 2001
  • In land navigation applications, two kinds of GPS/DR integration schemes are commonly used; the loosely-coupled integration scheme and the tightly-coupled one. The loosely-coupled integration filter has a simple structure and is easy to implement. When the number of visible satellites is insufficient, however, it cannot calibrate the errors of the DR sensors. On the contrary the tigthly-coupled integration filter can sup-press the growth of the error in the DR output even when the visibility is poor. However, it has larger com-putation load due to the state dimension and is inconsistent because of the variation in the measurement dimension. This paper presents a GPS/DR integration scheme with dual integration mode. During when the number of visible satellites is sufficient, the proposed scheme operates in a loosely-coupled integration mode. When the visibility becomes poor, it is switched into a tightly-coupled integration mode. Consequently, the pro-posed scheme can calibrate the DR sensors even when the visibility is poor. In addition, its computation time remains constant even if the number of visible satellites increases. Field experiment results show that the performance of the proposed integration method is almost similar to that of the tightly-coupled one.

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속단(續斷)의 RAW264.7 세포에서 LPS에 의해 유도되는 염증반응에 대한 효과 (Effect of Dipsaci Radix Water Extract on LPS-induced Inflammatory Response in RAW264.7 Mouse Macrophages)

  • 민지영;박용기
    • 대한본초학회지
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    • 제24권4호
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    • pp.189-195
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    • 2009
  • Objectives : In this study, the effect of Dipsaci Radix(DR, Dipsacus asperoides C.Y. Cheng et T. M. Ai) water extract on LPS-induced inflammatory response in RAW264.7 cells were investigated. Methods : Dried roots of DR was extracted with water for 3 h(DR-W extract). RAW264.7 cells, a mouse macrophage line, were incubated with different concentrations of DR-W extract for 30 min and then stimulated with LPS at indicated times. Cell toxicity was determined by MTT assay. The concentrations of nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) were measured by Griess assay and enzyme immunoassay (EIA), respectively. The expression of inducible nitric oxide synthease (iNOS) and cyclooxyganase (COX)-2 mRNA and protein was determined by RT-PCR and Western blot, respectively. Results : DR-W extract was significantly inhibited LPS-induced productions of NO and PGE2 in RAW264.7 cells. DR-W extract was not suppressed the expressions of iNOS mRNA and protein in LPS-stimulated RAW264.7 cells. Conclusions : This study suggests that DR-W extract can attenuate inflammatory response via inhibition of the NO and PGE2 production in activated macrophages.

Comparative Evaluation of Two-dimensional Radiography and Three Dimensional Computed Tomography Based Dose-volume Parameters for High-dose-rate Intracavitary Brachytherapy of Cervical Cancer: A Prospective Study

  • Madan, Renu;Pathy, Sushmita;Subramani, Vellaiyan;Sharma, Seema;Mohanti, Bidhu Kalyan;Chander, Subhash;Thulkar, Sanjay;Kumar, Lalit;Dadhwal, Vatsla
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권11호
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    • pp.4717-4721
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    • 2014
  • Background: Dosimetric comparison of two dimensional (2D) radiography and three-dimensional computed tomography (3D-CT) based dose distributions with high-dose-rate (HDR) intracavitry radiotherapy (ICRT) for carcinoma cervix, in terms of target coverage and doses to bladder and rectum. Materials and Methods: Sixty four sessions of HDR ICRT were performed in 22 patients. External beam radiotherapy to pelvis at a dose of 50 Gray in 27 fractions followed by HDR ICRT, 21 Grays to point A in 3 sessions, one week apart was planned. All patients underwent 2D-orthogonal and 3D-CT simulation for each session. Treatment plans were generated using 2D-orthogonal images and dose prescription was made at point A. 3D plans were generated using 3D-CT images after delineating target volume and organs at risk. Comparative evaluation of 2D and 3D treatment planning was made for each session in terms of target coverage (dose received by 90%, 95% and 100% of the target volume: D90, D95 and D100 respectively) and doses to bladder and rectum: ICRU-38 bladder and rectum point dose in 2D planning and dose to 0.1cc, 1cc, 2cc, 5cc, and 10cc of bladder and rectum in 3D planning. Results: Mean doses received by 100% and 90% of the target volume were $4.24{\pm}0.63$ and $4.9{\pm}0.56$ Gy respectively. Doses received by 0.1cc, 1cc and 2cc volume of bladder were $2.88{\pm}0.72$, $2.5{\pm}0.65$ and $2.2{\pm}0.57$ times more than the ICRU bladder reference point. Similarly, doses received by 0.1cc, 1cc and 2cc of rectum were $1.80{\pm}0.5$, $1.48{\pm}0.41$ and $1.35{\pm}0.37$ times higher than ICRU rectal reference point. Conclusions: Dosimetric comparative evaluation of 2D and 3D CT based treatment planning for the same brachytherapy session demonstrates underestimation of OAR doses and overestimation of target coverage in 2D treatment planning.

Growth Inhibitory Effect of (E)-2,4-bis(p-hydroxyphenyl)-2-Butenal Diacetate through Induction of Apoptotic Cell Death by Increasing DR3 Expression in Human Lung Cancer Cells

  • Lee, Ung-Soo;Ban, Jung Ok;Yeon, Eung Tae;Lee, Hee Pom;Udumula, Venkatareddy;Ham, Young Wan;Hong, Jin Tae
    • Biomolecules & Therapeutics
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    • 제20권6호
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    • pp.538-543
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    • 2012
  • The Maillard Reaction Products (MRPs) are chemical compounds which have been known to be effective in chemoprevention. Death receptors (DR) play a central role in directing apoptosis in several cancer cells. In our previous study, we demonstrated that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal, a MRP product, inhibited human colon cancer cell growth by inducing apoptosis via nuclear factor-${\kappa}B$ (NF-${\kappa}B$) inactivation and $G_2$/M phase cell cycle arrest. In this study, (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate, a new (E)-2,4-bis(p-hydroxyphenyl)-2-butenal derivative, was synthesized to improve their solubility and stability in water and then evaluated against NCI-H460 and A549 human lung cancer cells. (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate reduced the viability in both cell lines in a time and dose-dependent manner. We also found that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate increased apoptotic cell death through the upregulation of the expression of death receptor (DR)-3 and DR6 in both lung cancer cell lines. In addition to this, the transfection of DR3 siRNA diminished the growth inhibitory and apoptosis inducing effect of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate on lung cancer cells, however these effects of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate was not changed by DR6 siRNA. These results indicated that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal diacetate inhibits human lung cancer cell growth via increasing apoptotic cell death by upregulation of the expression of DR3.

The Prevalence and Risk Factors for Diabetic Retinopathy in Shiraz, Southern Iran

  • Ghaem, Haleh;Daneshi, Nima;Riahi, Shirin;Dianatinasab, Mostafa
    • Diabetes and Metabolism Journal
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    • 제42권6호
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    • pp.538-543
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    • 2018
  • Globally, diabetic retinopathy (DR) is one of the leading causes of blindness, that diminishes quality of life. This study aimed to describe the prevalence of DR, and its associated risk factors. This cross-sectional study was carried out among 478 diabetic patients in a referral center in Fars province, Iran. The mean${\pm}$standard deviation age of the participants was $56.64{\pm}12.45$ years old and DR prevalence was 32.8%. In multivariable analysis, lower education levels (adjusted odds ratio [aOR], 0.43; 95% confidence interval [CI], 0.24 to 0.76), being overweight (aOR, 1.70; 95% CI, 1.02 to 2.83) or obese (aOR, 1.88; 95% CI, 1.09 to 3.26), diabetes duration of 10 to 20 years (aOR, 2.35; 95% CI, 1.48 to 3.73) and over 20 years (aOR, 5.63; 95% CI, 2.97 to 10.68), receiving insulin (aOR, 1.99; 95% CI, 1.27 to 3.10), and having chronic diseases (aOR, 1.71; 95% CI, 1.02 to 2.85) were significantly associated with DR. In conclusion, longer diabetes duration and obesity or having chronic diseases are strongly associated with DR suggesting that control of these risk factors may reduce both the prevalence and impact of retinopathy in Iran.

[1,3] Oxazine 유도체 합성을 위한 효율적인 One-Pot 합성 (An Efficient One-Pot Strategies for the Synthesis of [1,3] Oxazine Derivatives)

  • Sapkal, Suryakant B.;Shelke, Kiran F.;Shingate, Bapurao B.;Shingare, Murlidhar S.
    • 대한화학회지
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    • 제54권4호
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    • pp.437-442
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    • 2010
  • 수용액 속에서 $NaHSO_4$, TBAB (phase transfer catalyst), ionic liquid (IL) (1-butyl-3-methyl imidazolium hydrogen sulphate [bmim]$HSO_4$)를 사용하여, formalin, ${\beta}$-naphthol, aromatic amines을 반응시켜서 대응하는 2,3-dihydro-2-phenyl-1Hnaphtho-[1,2-e] [1,3] oxazine 유도체를 합성할 수 있는 보다 친환경적이고, 수율이 좋고, 크로마토그래피 분리 방법을 사용하지 않는 합성 방법을 개발하였다.