• 제목/요약/키워드: Small molecules

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Comparative Molecular Field Analyses on the Herbicidal Activities of New 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one Derivatives (새로운 5-benzofuryl-2-[1-(alkoxyimino)alkyl]-3-hydroxycyclohex-2-en-1-one 유도체들의 제초활성에 관한 비교 분자장 분석)

  • Chung, Ki-Sung;Jang, Seok-Chan;Choi, Kyung-Seob;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.49 no.3
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    • pp.238-242
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    • 2006
  • The herbicidal activities against the pre-emergence of rice plant (Oryza sativa L.) and barnyard grass (Echinochloa crus-gall) with changing substituents $(R_1-R_4)$ of new 5-benzofuryl-2-[1-(alkoxyimino) alkyl]-3-hydroxycyclohex-2-en-1-one derivatives as substrate molecules were studied quantitatively using comparative molecular field analyses (CoMFA). The optimized CoMFA models (rice plant: A5 & barnyard grass: B3) were derived from atom based fit alignment and a combination of CoMFA fields. The two models for herbicidal activity against two plants showed the best predictability and fitness ($q^2$>0.6 & ${r^2}_{ncv.}$>0.94) for the herbicidal activities. Also, CoMFA-HINT contour maps showed that the selective herbicidal activity between rice plant and barnyard grass depends on the hydrophobicity of $R_2\;and\;R_3$ groups in molecule. Therefore, it is expected that the herbicidal activity against barnyard grass will be improved by the introduction of the steric bulk small and hydrophobic group.

The Up-Regulation of miR-199b-5p in Erythroid Differentiation Is Associated with GATA-1 and NF-E2

  • Li, Yuxia;Bai, Hua;Zhang, Zhongzu;li, Weihua;Dong, Lei;Wei, Xueju;Ma, Yanni;Zhang, Junwu;Yu, Jia;Sun, Guotao;Wang, Fang
    • Molecules and Cells
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    • v.37 no.3
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    • pp.213-219
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    • 2014
  • MicroRNAs (miRNAs) represent a class of small non-coding regulatory RNAs that play important roles in normal hematopoiesis, including erythropoiesis. Although studies have identified several miRNAs that regulate erythroid commitment and differentiation, we do not understand the mechanism by which the crucial erythroid transcription factors, GATA-1and NF-E2 directly regulate and control differentiation via miRNA pathways. In this study, we identified miR-199b-5p as a key regulator of human erythropoiesis, and its expression was up-regulated during the erythroid differentiation of K562 cells. Furthermore, the increase of miR-199b-5p in erythroid cells occurred in a GATA-1- and NF-E2-dependent manner during erythrocyte maturation. Both GATA-1 and NF-E2 bound upstream of the miR-199b gene locus and activated its transcription. Forced expression of miRNA-199b-5p in K562 cells affected erythroid cell proliferation and maturation. Moreover, we identified c-Kit as a direct target of miR-199b-5p in erythroid cells. Taken together, our results establish a functional link among the erythroid transcription factors GATA-1/NF-E2, miR-199b-5p and c-Kit, and provide new insights into the coupling of transcription and post-transcription regulation in erythroid differentiation.

Isolation of Stenotrophomonas rhizopilae Strain GFC09 with Ginsenoside Converting Activity and Anti-wrinkle Effects of Converted Ginsenosides (사포닌 전환 활성 Stenotrophomonas rhizopilae Strain GFC09 균주의 분리 동정 및 전환 사포닌의 주름 개선 효과)

  • Min, Jin Woo;Kim, Hye-Jin;Joo, Kwang-Sik;Kang, Hee-Cheol
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.4
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    • pp.375-382
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    • 2015
  • Ginsenosides (ginseng saponin) as the one of important pharmaceutical compounds of ginseng and is responsible for the pharmacological and biological activities. These ginsenoside produces diverse small molecules ginsenoside which have more pharmacological activities including anti-wrinkle, anti-cancer and anti-oxidant effects. In the present study, we isolated bacteria using esculin agar, to produce ${\beta}$-glucosidase, and we focused on the bio-transformation of ginsenoside. Phylogenetic tree analysis was performed by comparing the 16S rRNA sequences; we identified the strain as Stenotrophomonas rhizopilae strain GFC09. In order to determine the optimal conditions for enzyme activity, the crude enzyme was incubated with 1 mM ginsenoside $Rb_1$. Bioconversion of ginsenoside $Rb_1$ were analyzed using TLC and HPLC. The crude enzyme hydrolyzed the ginsenoside $Rb_1$ along the following pathway: LB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$ into compound K, TSB: $Rb_1{\rightarrow}Rd{\rightarrow}F_2$. The structure of the hydrolyzed metabolites were identified by NMR. The activity screening tests showed that the conversion product induced the production of type I procollagen in a dose-dependent manner. These results suggested that hydrolyzed ginseng product containing the ginsenoside $F_2$ and compound K could be useful as an active ingredient for wrinkle-care cosmetics.

Salicylate Can Enhance Osteogenic Differentiation of Human Periosteum-derived Mesenchymal Stem Cells (Salicylate가 성체줄기세포의 골분화에 미치는 영향)

  • Kim, Bo Gyu;Lee, A ram;Lee, Bo Young;Shim, Sungbo;Moon, Dong kyu;Hwang, Sun-Chul;Byun, June-Ho;Woo, Dong Kyun
    • Journal of Life Science
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    • v.28 no.12
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    • pp.1455-1460
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    • 2018
  • Due to a rapidly expanding aging population, the incidence of degenerative bone disease has increased, and efforts to handle the issue using regenerative medicine have become more important. In order to control various bone diseases such as osteoarthritis and osteoporosis, regenerative medicine utilizing adult stem cells has been extensively studied. And it is now clear that the mitochondrial energy metabolism, oxidative phosphorylation, is important for the process of stem cell differentiation. Interestingly, a recent study reported that salicylate promotes mitochondrial biogenesis by regulating the expression of $PGC-1{\alpha}$ in murine cells. However, the possible effects of salicylate on osteogenic differentiation through increased mitochondrial biogenesis in stem cells remain unknown. Thus, here we investigated whether salicylate could influence osteogenic differentiation and mitochondrial biogenesis of periosteum-derived mesenchymal stem cells (POMSCs). We found that salicylate treatments of POMSCs undergoing osteogenic differentiation increased the activity of alkaline phosphatase, a well-known early marker of bone cell differentiation. In addition, we observed that mitochondrial mass was increased by salicylate treatments in POMSCs. Together, these results indicate that salicylate can enhance osteogenic differentiation and mitochondrial biogenesis in POMSCs. Therefore, the findings in this study suggest that small molecules augmenting mitochondrial function such as salicylate can be a novel modulator for osteogenic differentiation and regenerative medicine.

New conceptual approaches toward dentin regeneration using the drug repositioning strategy with Wnt signaling pathways

  • Lee, Eui-Seon;Kim, Tae-Young;Aryal, Yam Prasad;Kim, Kihyun;Byun, Seongsoo;Song, Dongju;Shin, Yejin;Lee, Dany;Lee, Jooheon;Jung, Gilyoung;Chi, Seunghoon;Choi, Yoolim;Lee, Youngkyun;An, Chang-Hyeon;Kim, Jae-Young
    • International Journal of Oral Biology
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    • v.46 no.2
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    • pp.67-73
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    • 2021
  • This study summarizes the recent cutting-edge approaches for dentin regeneration that still do not offer adequate solutions. Tertiary dentin is formed when odontoblasts are directly affected by various stimuli. Recent preclinical studies have reported that stimulation of the Wnt/β-catenin signaling pathway could facilitate the formation of reparative dentin and thereby aid in the structural and functional development of the tertiary dentin. A range of signaling pathways, including the Wnt/β-catenin pathway, is activated when dental tissues are damaged and the pulp is exposed. The application of small molecules for dentin regeneration has been suggested as a drug repositioning approach. This study reviews the role of Wnt signaling in tooth formation, particularly dentin formation and dentin regeneration. In addition, the application of the drug repositioning strategy to facilitate the development of new drugs for dentin regeneration has been discussed in this study.

Development of analytical method for the isotope purity of pure D2 gas using high-precision magnetic sector mass spectrometer

  • Chang, Jinwoo;Lee, Jin Bok;Kim, Jin Seog;Lee, Jin-Hong;Hong, Kiryong
    • Analytical Science and Technology
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    • v.35 no.5
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    • pp.205-211
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    • 2022
  • Deuterium (D) is an isotope with one more neutron number than hydrogen (H). Heavy elements rarely change their chemical properties with little effect even if the number of neutrons increases, but low-mass elements change their vibration energy, diffusion rate, and reaction rate because the effect cannot be ignored, which is called an isotope effect. Recently, in the semiconductor and display industries, there is a trend to replace hydrogen gas (H2) with deuterium gas (D2) in order to improve process stability and product quality by using the isotope effect. In addition, as the demand for D2 in industries increases, domestic gas producers are making efforts to produce and supply D2 on their own. In the case of high purity D2, most of them are produced by electrolysis of heavy water (D2O), and among D2, hydrogen deuteride (HD) molecules are present as isotope impurities. Therefore, in order to maximize the isotope effect of hydrogen in the electronic industry, HD, which is an isotope impurity of D2 used in the process, should be small amount. To this end, purity analysis of D2 for industrial processing is essential. In this study, HD quantitative analysis of D2 for high purity D2 purity analysis was established and hydrogen isotope RM (Reference material) was developed. Since hydrogen isotopes are difficult to analyze with general gas analysis instrument, they were analyzed using a high-precision mass spectrometer (Gas/MS, Finnigan MAT271). High purity HD gas was injected into Gas/MS, sensitivity was determined by a signal according to pressure, and HD concentrations in two bottles of D2 were quantified using the corresponding sensitivity. The amount fraction of HD in each D2 was (4518 ± 275) μmol/mol, (2282 ± 144) μmol/mol. D2, which quantifies HD amount using the developed quantitative analysis method, will be manufactured with hydrogen isotope RM and distributed for quality management and maintenance of electronic industries and gas producers in the future.

Electrochemical Mass Transport Control in Biomimetic Solid-State Nanopores (생체모사형 나노포어를 활용한 전기화학 기반 물질전달 조절 시스템)

  • Soongyu Han;Yerin Bang;Joon-Hwa Lee;Seung-Ryong Kwon
    • Journal of the Korean Electrochemical Society
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    • v.26 no.4
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    • pp.43-55
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    • 2023
  • Mass transport through nanoporous structures such as nanopores or nanochannels has fundamental electrochemical implications and many potential applications as well. These structures can be particularly useful for water treatment, energy conversion, biosensing, and controlled delivery of substances. Earlier research focused on creating nanopores with diameters ranging from tens to hundreds of nanometers that can selectively transport cationic or anionic charged species. However, recent studies have shown that nanopores with diameters of a few nanometers or even less can achieve more complex and versatile transport control. For example, nanopores that mimic biological channels can be functionalized with specific receptors to detect viruses, small molecules, and even ions, or can be made hydrophobic and responsive to external stimuli, such as light and electric field, to act as efficient valves. This review summarizes the latest developments in nanopore-based systems that can control mass transport based on the size of the nanopores (e.g., length, diameter, and shape) and the physical/chemical properties of their inner surfaces. It also provides some examples of practical applications of these systems.

The Effects of Weekly Reports as a Method for Encouraging Student Questions in Middle School Science Instruction (중학교 과학 수업에서 학생 질문을 촉진하는 방안으로서의 주단위 보고서의 효과)

  • Kang, Hun-Sik;Lee, Sung-Mi;Kwon, Eun-Kyung;Noh, Tae-Hee
    • Journal of The Korean Association For Science Education
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    • v.26 no.3
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    • pp.385-392
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    • 2006
  • This study investigated the effects of weekly reports as a method for encouraging student questions in middle school science instruction by focusing on student conceptual understanding, achievement, concept map, and perceptions of weekly reports. Seventh graders (N=211) from a middle school were assigned to control and weekly reports (WR) groups. All students were taught about the 'three states of matter', the 'motion of molecules', and the 'change of states and thermal energy' for eighteen class hours. Students in the WR group were required to write weekly reports for six of those periods. Results revealed that conception test scores for the WR group were significantly higher than those for the control group. Compared conception test scores by learning strategy, students using a surface learning strategy in the WR group scored significantly higher than those in the control group. While students employing a deep learning strategy in the WR group also performed better than those in the control group, the difference was relatively small. The scores of an achievement test and a concept map test for the WR group were significantly higher than those for the control group. However, there were no significant interactions between instruction and students' learning strategy in the two variables. It was also found that most students in the WR group positively perceived weekly reports.

Studies on the Micelle Formation of Nonionic Surfactant(1) -1NMR Self-Diffusion and Proton Relaxation of Polyoxyethylene Alkyl Ether- (계면활성제 수용액의 미셀형성(제1보) - Polyoxyethylene Alkyl Ether의 자기확산과 프로톤 이완 -)

  • Choi, Seung-Ok;Jeong, Hwan-Kyeong;Lee, Jin-Hee;Nam, Ki-Dae
    • Applied Chemistry for Engineering
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    • v.9 no.6
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    • pp.822-828
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    • 1998
  • Binary system of water and polyoxyethylene dodecyl ether, $C_{12}H_{25}(OCH_2CH_2)nOH$, have been studied by $^1H$ NMR techniques. For n=5($C_{12}EO_5$) and n=8($C_{12}EO_8$), the self-diffusion coefficients of nonionic surfactants in the isotropic phase($L_1$) have been measured by using pulsed field gradient technique for a range of temperature and concentrations. In addition the line widths of the different proton signals have been monitored, and samples of some liquid crystalline characteristic were also studied. Dramatic Broadening of the methylene signals of the alkyl($C_{12}H_{25}$) chain is observed as the hexagonal liquid crystalline phase is approached in the $C_{12}EO_5-$water system, while only small broadening is observed in the $C_{12}EO_8-$water system. It was shown that there was a growth of $C_{12}EO_5$ micelles to rods with increasing concentrations, while the $C_{12}EO_8-$ micelles at low temperature remain small in the concentration range. The self-diffusion coefficients of the surfactants decrease rapidly with increasing concentration until a minimum is reached after which there is slow increase. The location of the minimum point occurs at lower concentrations the temperature is close to the cloud point, where the system separate into two isotropic phase. In the line width studies, broadening is found at a certain temperature interval when the concentration is increased in the $C_{12}EO_5$ system. The results indicate that the surfactant aggregates grow in size at the cloud point is approached. The aggregates seem to be flexible and probably not to be of a definite shape close to the cloud point. In the $C_{12}EO_8$ system, the micelles are much less affected by an increase in temperature and micellar growth can't be unambiguously established. The methylene signals of the ethylene oxide moieties consistantly show narrower $^1H$ signals, showing that in the aggregates they are less ordered than the chain methylenes. The various changes in aggregate size and shape are correlated with the stability ranges of the isotropic and liquid crystalline phases according to phase diagrams from the literature. Both aggregate size and phase structure are in qualitative agreement with concentration based on the effective shape of the molecules at different temperature and concentration.

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The Expression of Adhesion Molecules on BAL Cells and Serum Soluble ICAM-1 Level after the Radiotherapy for the Lung Cancer and Its Relationship to the Development of of Radiation Pneumonitis and Fibrosis (방사선 치료후 기관지-폐포세척액내 폐포대식세포 및 임파구의 접착분자발현 변화와 방사선에 의한 폐렴 및 폐섬유증발생의 예측인자로서의 의의)

  • Kim, Dong-Soon;Paik, Sang-Hoon;Choi, Eun-Kyung;Chang, Hye-Sook;Choi, Jung-Eun;Lim, Chae-Man;Koh, Yun-Suck;Lee, Sang-Do;Kim, Woo-Sung;Kim, Won-Dong
    • Tuberculosis and Respiratory Diseases
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    • v.43 no.1
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    • pp.75-87
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    • 1996
  • Background: Lung cancer is the second most frequent malignancy in man in Korea. Surgery is the best treatment modality for non-small cell lung cancer, but most patients were presented in far advanced stage. So radiation therapy(RT) with or without chemotherapy is the next choice and radiation-induced pneumonitis and pulmonary fibrosis is the major limiting factor for the curative RT. Radiation pneumonitis is manifested with fever, cough and dyspnea, 2~3 months after the termination of radiotherpy. Chest X ray shows infiltration, typically limited to the radiation field, but occasionally bilateral infiltration was reported. Also Gibson et al reported that BAL lymphocytosis was found in both lungs, even though the radiation was confined to one lung. The aim of this study is to investigate the change of adhesion molecules expression on BAL cells and serum soluble ICAM-1(sICAM-1) level after the RT and its relationship to the development of radiation pneumonitis. The second aim is to confirm the bilaterality of change of BAL cell pattern and adhesion molecule expression. Subjects: BAL and the measurement of sICAM level in serum and BALF were done on 29 patients with lung cancer who received RT with curative intention. The BAL was done before the RT in 16 patients and 1~2 month after RT in 18 patients. 5 patients performed BAL before and after RT. Result: Clinically significant radiation pneumonitis developed in 7 patients. After RT, total cell count in BAL was significantly increased from $(20.2{\pm}10.2){\times}10^6\;cells/ml$ to $(35.3{\pm}21.6){\times}10^6\;cells/ml$ (p=0.0344) and %lymphocyte was also increased from $5.3{\pm}4.2%$ to $39.6{\pm}23.4%$ (p=0.0001) in all patient group. There was no difference between ipsilateral and contraleteral side to RT, and between the patients with and without radiation-pneumonitis. In whole patient group, the level of sICAM-1 showed no significant change after RT(in serum: $378{\pm}148$, $411{\pm}150\;ng/ml$, BALF: $20.2{\pm}12.2$, $45.1{\pm}34.8\;ng/ml$, respectively), but there was a significant difference between the patients with pneumonitis and without pneumonitis (serum: $505{\pm}164$ vs $345{\pm}102\;ng/ml$, p=0.0253, BALF: $67.9{\pm}36.3$ vs $25.2{\pm}17.9\;ng/ml$, p=0.0112). The expression of ICAM-1 on alveolar macrophages (AM) tends to increase after RT (RMFI: from $1.28{\pm}0.479$ to $1.63{\pm}0.539$, p=0.0605), but it was significantly high in patients with pneumonitis ($2.10{\pm}0.390$) compared to the patients without pneumonitis ($1.28{\pm}0.31$, p=0.0002). ICAM-1 expression on lymphocytes and CD 18 (${\beta}2$-integrin) expression tended to be high in the patients with pneumonitis but the difference was statiastically not significant. Conclusion: Subclinical alveolitis on the basis of BAL finding developed bilaterally in all patients after RT. But clinically significant pneumonitis occurred in much smaller fraction and the ICAM-1 expression on AM and the sICAM-1 level in serum were good indicator of it.

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