• 제목/요약/키워드: Chemical library

검색결과 195건 처리시간 0.027초

2-(Trimethylammonium) Ethyl (R)-3-Methoxy-3-oxo-2-Stearamidopropyl Phosphate Suppresses Osteoclast Maturation and Bone Resorption by Targeting Macrophage-Colony Stimulating Factor Signaling

  • Park, So Jeong;Park, Doo Ri;Bhattarai, Deepak;Lee, Kyeong;Kim, Jaesang;Bae, Yun Soo;Lee, Soo Young
    • Molecules and Cells
    • /
    • 제37권8호
    • /
    • pp.628-635
    • /
    • 2014
  • 2-(Trimethylammonium) ethyl (R)-3-methoxy-3-oxo-2-stearamidopropyl phosphate [(R)-TEMOSPho], a derivative of an organic chemical identified from a natural product library, promotes highly efficient megakaryopoiesis. Here, we show that (R)-TEMOSPho blocks osteoclast maturation from progenitor cells of hematopoietic origin, as well as blocking the resorptive function of mature osteoclasts. The inhibitory effect of (R)-TEMOSPho on osteoclasts was due to a disruption of the actin cytoskeleton, resulting from impaired downstream signaling of c-Fms, a receptor for macrophage-colony stimulating factor linked to c-Cbl, phosphoinositol-3-kinase (PI3K), Vav3, and Rac1. In addition, (R)-TEMOSPho blocked inflammation-induced bone destruction by reducing the numbers of osteoclasts produced in mice. Thus, (R)-TEMOSPho may represent a promising new class of antiresorptive drugs for the treatment of bone loss associated with increased osteoclast maturation and activity.

오갈피나무의 정유성분 GC-MS 분석 (GC-MS Analysis of Volatile Constituents from Acanthopanax sessiliflorus)

  • 임순성;이연실;이설림;김종기;조선행;신국현;이상현
    • 생약학회지
    • /
    • 제39권1호
    • /
    • pp.7-18
    • /
    • 2008
  • The chemical composition of the volatile constituents from the leaves, stems, and roots of Acanthopanax sessiliforus growing wild in Mt. Deok-Yu was determined by GC and GC-MS spectrometric analysis with the aid of NBS, Wiley Library and RI indice searches. The major constituents identified were ${\delta}-3-carene$ (7.24%), limonene (8.10%), ${\beta}-thujene$ (17.85%), trans-bicyclic hydrocarbon (13.35%) and ${\delta}-cadinene$ (4.28%) in the leaves from one year-grown plants, tricyclene (7.21%), ${\beta}-myrcene$ (7.62%), limonene (10.23%), ${\beta}-thujene$ (15.61%) and dihydroedulan I (6.12%) in the leaves from three years-grown plants, ${\delta}-3-carene$ (4.96%), limonene (5.93%), ${\beta}-phellandrene$ (17.31%) and naphthalene (7.79%) in the stems from one year-grown plants, ${\alpha}-pinene$ (5.21%), limonene (5.12%) and ${\beta}-phellandrene$ (9.82%) in the stems from three years-grown plants, ${\alpha}-pinene$ (12.73%), ${\beta}-pinene$ (11.16%), ${\delta}-3-carene$ (6.16%) and ${\gamma}-cadinene$ (23.39%) in the roots from one year-grown plants, and ${\alpha}-pinene$ (17.25%), ${\beta}-pinene$ (9.35%), ${\delta}-3-carene$ (7.26%) and ${\gamma}-cadinene$ (17.95%) in the roots from three years-grown plants.

삼 인피섬유 혼합율이 종이의 보존 특성에 미치는 영향 (Permanent Characteristics of the Handsheet Mixed with Hemp Bast Fiber)

  • 김준규;최경화;이명구
    • 펄프종이기술
    • /
    • 제46권6호
    • /
    • pp.71-77
    • /
    • 2014
  • Despite the ubiquity of electronic media, paper is still the most generally readable carrier of information. Because paper materials are deteriorated by chemical, biological and physical factors over time, there have been major concerns about the decay of large collections of books, publications, old maps, historical artifacts, and written records. Therefore, manufacture of permanent paper has been a highly debated issue in paper conservation research. Through the use of permanent paper, our new records, journals, library books, art works, and all culturally and historically important documents can be preserved. In this study, handsheets were made of mixture of hemp bast fiber produced by soda pulping and HwBKP varying the amount of hemp. Physical, mechanical and optical properties of each handsheet were examined. As the ratio of hemp bast fiber increased, mechanical properties were improved significantly, but opacity decreased. After aging, the optical properties of the handsheets mixed with the hemp bast fiber more decreased than those of the non-mixed handsheet. The more mixture ratio of hemp bast fiber increased, the more decreasing rate of optical properties increased. As a result, it was confirmed that hemp bast fiber is a very promising resource for the manufacturing of permanent paper.

한국산 오미자로부터 디벤조사이클로옥타디엔 계열 리그난 화합물 정성 및 정량 분석 (Qualitative and Quantitative Analysis of Dibenzocyclooctadiene Lignans for the Fruits of Korean "Omija" (Schisandra chinensis))

  • 김헌웅;신재형;이민기;장가희;이성현;장환희;정석태;김정봉
    • 한국약용작물학회지
    • /
    • 제23권5호
    • /
    • pp.385-394
    • /
    • 2015
  • Background : Dibenzocyclooctadiene lignans are secondary metabolites present abundantly in the fruits belonging to the genus Schisandra. According to previous studies, Schisandra lignans exhibit anti-inflammatory, anti-cancer and anti-diabetic properties, as well as an inhibitory effect on platelet aggregation. Therefore, establishing the Korean "Omija" (Schisandra chinensis) as a lignan-rich source, in addition to identifying and quantifying the lignans, is extremely valuable. Methods and Results : Dibenzocyclooctadiene lignans were analyzed with liquid chromatography using diode array detection/mass spectrometry, from methanol extracts subsequently identified by a constructed chemical library of 50 lignans. A total of 27 components of lignan including gomisin S were identified, of which schisandrin, gomisin A, gomisin N, deoxyschisandrin, ${\gamma}$-schisandrin, and schisandrin C were identified as the major components in the Korean Omija, Schisandra chinensis. These compounds were divided into two groups, S-biphenyl and R-biphenyl based on the configurations of the stereoisomers structures with contents of 661.7 and 1350.1mg per 100 g dry weight, respectively. The total lignan content averaged 2011.4mg per 100 g dry weight, of which schisandrin and gomisin N comprised the majority (771.8 and 420.5mg per 100 g dry weight respectively). Conclusions : Lignans which are present in high quantities in the ripe fruit of Schisandra chinensis are important functional compounds that play a major role in the prevention and treatment of human diseases.

IQGAP1, a signaling scaffold protein, as a molecular target of a small molecule inhibitor to interfere with T cell receptor-mediated integrin activation

  • Li, Lin-Ying;Nguyen, Thi Minh Nguyet;Woo, Eui Jeon;Park, Jongtae;Hwang, Inkyu
    • 농업과학연구
    • /
    • 제47권2호
    • /
    • pp.361-373
    • /
    • 2020
  • Integrins such as lymphocyte function-associated antigen -1 (LFA-1) have an essential role in T cell immunity. Integrin activation, namely, the transition from the inactive conformation to the active one, takes place when an intracellular signal is generated by specific receptors such as T cell receptors (TCRs) and chemokine receptors in T cells. In an effort to explore the molecular mechanisms underlying the TCR-mediated LFA-1 activation, we had previously established a high-throughput cell-based assay and screened a chemical library deposited in the National Institute of Health in the United States. As a result, several hits had been isolated including HIKS-1 (Benzo[b]thiophene-3-carboxylic acid, 2-[3-[(2-carboxyphenyl) thio]-2,5-dioxo-1-pyrrolinyl]-4,5,6,7-tetrahydro-,3-ethyl ester). In an attempt to reveal the mode of action of HIKS-1, in this study, we did drug affinity responsive target stability (DARTS) assay finding that HIKS-1 interacted with the IQ motif containing GTPase activating protein 1 (IQGAP1), a 189 kDa multidomain scaffold protein critically involved in various signaling mechanisms. Furthermore, the cellular thermal shift assay (CETSA) provided compelling evidence that HIKS-1 also interacted with IQGAP1 in vivo. Taken together, it can be concluded that HIKS-1 interferes with the TCR-mediated LFA-1 activation by interacting with IQGAP1 and thereby disrupting the signaling pathway for LFA-1 activation.

상록활엽수 정유성분의 GC/MS 분석 (GC/MS Analysis of Volatile Constituents from Broad-Leaved Indeciduous Trees)

  • 임순성;이연실;김혜민;안영희;신국현;이상현
    • 한국자원식물학회지
    • /
    • 제21권4호
    • /
    • pp.237-248
    • /
    • 2008
  • 자생 상록활엽수의 부위별 재료에서 추출한 주요 정유성분으로 광나무의 꽃에는 hotrienol(9.21%), 돈나무의 잎에는 undecane(32.12%), 붓순나무의 잎에는 1,8-cineole(45.32%), 새덕이나무의 잎에는 ${\gamma}$-terpinene(15.62%), 생달나무의 잎에는 1,8-cineole(14.66%), 차나무의 잎에는 2-acetyl-5-methylfuran(54.51%), 황칠나무의 잎에는 ${\gamma}$-elemene(18.59%) 등의 성분함량이 특히 높음을 알 수 있었다.

Identification of a Gene Involved in the Negative Regulation of Pyomelanin Production in Ralstonia solanacearum

  • Ahmad, Shabir;Lee, Seung Yeup;Khan, Raees;Kong, Hyun Gi;Son, Geun Ju;Roy, Nazish;Choi, Kihyuck;Lee, Seon-Woo
    • Journal of Microbiology and Biotechnology
    • /
    • 제27권9호
    • /
    • pp.1692-1700
    • /
    • 2017
  • Ralstonia solanacearum causes bacterial wilt in a wide variety of host plant species and produces a melanin-like blackish-brown pigment in stationary phase when grown in minimal medium supplemented with tyrosine. To study melanin production regulation in R. solanacearum, five mutants exhibiting overproduction of melanin-like pigments were selected from a transposon (Tn) insertion mutant library of R. solanacearum SL341. Most of the mutants, except one (SL341T), were not complemented by the original gene or overproduced melanins. SL341T showed Tn insertion in a gene containing a conserved domain of eukaryotic transcription factor. The gene was annotated as a hypothetical protein, given its weak similarity to any known proteins. Upon complementation with its original gene, the mutant strains reverted to their wild-type phenotype. SL341T produced 3-folds more melanin at 72 h post-incubation compared with wild-type SL341 when grown in minimal medium supplemented with tyrosine. The chemical analysis of SL341T cultural filtrate revealed the accumulation of a higher amount of homogentisate, a major precursor of pyomelanin, and a lower amount of dihydroxyphenylalanine, an intermediate of eumelanin, compared with SL341. The expression study showed a relatively higher expression of hppD (encoding hydroxyphenylpyruvate dioxygenase) and lower expression of hmgA (encoding homogentisate dioxygenase) and nagL (encoding maleylacetoacetate isomerase) in SL341T than in SL341. SL341 showed a significantly higher expression of tyrosinase gene compared with SL341T at 48 h post-incubation. These results indicated that R. solanacearum produced both pyomelanin and eumelanin, and the novel hypothetical protein is involved in the negative regulation of melanin production.

Efficacy of intralipid administration to improve in vitro fertilization outcomes: A systematic review and meta-analysis

  • Han, E Jung;Lee, Hye Nam;Kim, Min Kyoung;Lyu, Sang Woo;Lee, Woo Sik
    • Clinical and Experimental Reproductive Medicine
    • /
    • 제48권3호
    • /
    • pp.203-210
    • /
    • 2021
  • We performed a systematic review and meta-analysis to evaluate whether intralipid administration improved the outcomes of in vitro fertilization. Online databases (PubMed, Cochrane Library, Medline, and Embase) were searched until March 2020. Only randomized controlled trials (RCTs) that assessed the role of intralipid administration during in vitro fertilization were considered. We analyzed the rates of clinical pregnancy and live birth as primary outcomes. Secondary outcomes included the rates of chemical pregnancy, ongoing pregnancy, and missed abortion. We reviewed and assessed the eligibility of 180 studies. Five RCTs including 840 patients (3 RCTs: women with repeated implantation failure, 1 RCT: women with recurrent spontaneous abortion, 1 RCT: women who had experienced implantation failure more than once) met the selection criteria. When compared with the control group, intralipid administration significantly improved the clinical pregnancy rate (risk ratio [RR], 1.48; 95% confidence interval [CI], 1.23-1.79), ongoing pregnancy rate (RR, 1.82; 95% CI, 1.31-2.53), and live birth rate (RR, 1.85; 95% CI, 1.44-2.38). However, intralipid administration had no beneficial effect on the miscarriage rate (RR, 0.75; 95% CI, 0.48-1.17). A funnel plot analysis revealed no publication bias. Our findings suggest that intralipid administration may benefit women undergoing in vitro fertilization, especially those who have experienced repeated implantation failure or recurrent spontaneous abortion. However, larger, well-designed studies are needed to confirm these findings.

어린이 활동양상 설문분석을 통한 신규관리 활동공간 검토 (Selection of New High-maintenance Children's Activity Spaces based on Children's Life Patterns)

  • 김호현;최인석;남의현;이정훈;유시은;박충희;이정섭
    • 한국환경보건학회지
    • /
    • 제45권2호
    • /
    • pp.164-172
    • /
    • 2019
  • Objectives: This study's purpose is finding children's activity spaces that demand environmental safety management. Methods: The method of this study is analysing children's life patterns based on a questionnaire survey. Results: This study analyzed children's life patterns through a questionnaire survey. In total, 2,447 questionnaires were provided to analyze children's life patterns. The results of the questionnaire indicated a highly simple form because many children generally stayed in their home (66%) or nursery facility (2%). In the case of other facilities, playground was ranked first and amusement park was ranked second. In addition, kids cafe (including play facilities installed in shopping centers, etc.), library, and internet cafe were among the responses. Conclusions: The priority for new high-maintenance children's activity spaces are academy (rank 1), kids cafe (rank 2), indoor playground (rank 3).

Prediction of pollution loads in the Geum River upstream using the recurrent neural network algorithm

  • Lim, Heesung;An, Hyunuk;Kim, Haedo;Lee, Jeaju
    • 농업과학연구
    • /
    • 제46권1호
    • /
    • pp.67-78
    • /
    • 2019
  • The purpose of this study was to predict the water quality using the RNN (recurrent neutral network) and LSTM (long short-term memory). These are advanced forms of machine learning algorithms that are better suited for time series learning compared to artificial neural networks; however, they have not been investigated before for water quality prediction. Three water quality indexes, the BOD (biochemical oxygen demand), COD (chemical oxygen demand), and SS (suspended solids) are predicted by the RNN and LSTM. TensorFlow, an open source library developed by Google, was used to implement the machine learning algorithm. The Okcheon observation point in the Geum River basin in the Republic of Korea was selected as the target point for the prediction of the water quality. Ten years of daily observed meteorological (daily temperature and daily wind speed) and hydrological (water level and flow discharge) data were used as the inputs, and irregularly observed water quality (BOD, COD, and SS) data were used as the learning materials. The irregularly observed water quality data were converted into daily data with the linear interpolation method. The water quality after one day was predicted by the machine learning algorithm, and it was found that a water quality prediction is possible with high accuracy compared to existing physical modeling results in the prediction of the BOD, COD, and SS, which are very non-linear. The sequence length and iteration were changed to compare the performances of the algorithms.