• Interdisciplinary Bio Central
• /
• v.3 no.4
• /
• pp.15.1-15.11
• /
• 2011

Background: Histone deacetylase (HDAC) 8 is one of its family members catalyzes the removal of acetyl groups from N-terminal lysine residues of histone proteins thereby restricts transcription factors from being expressed. Inhibition of HDAC8 has become an emerging and effective anti-cancer therapy for various cancers. Application computational methodologies may result in identifying the key components that can be used in developing future potent HDAC8 inhibitors. Results: Facilitating the discovery of novel and potential chemical scaffolds as starting points in the future HDAC8 inhibitor design, quantitative structure-activity relationship models were generated with 30 training set compounds using genetic function approximation (GFA) and Bayesian algorithms. Six GFA models were selected based on the significant statistical parameters calculated during model development. A Bayesian model using fingerprints was developed with a receiver operating characteristic curve cross-validation value of 0.902. An external test set of 54 diverse compounds was used in validating the models. Conclusions: Finally two out of six models based on their predictive ability over the test set compounds were selected as final GFA models. The Bayesian model has displayed a high classifying ability with the same test set compounds and the positively and negatively contributing molecular fingerprints were also unveiled by the model. The effectively contributing physicochemical properties and molecular fingerprints from a set of known HDAC8 inhibitors were identified and can be used in designing future HDAC8 inhibitors.

• Archives of Pharmacal Research
• /
• v.27 no.10
• /
• pp.1043-1047
• /
• 2004

Thirteen compounds were isolated from the $CH_2Cl_2$ fraction of Machilus thunbergii as phospholipase $C{\Upsilon}1\;(PLC{\Upsilon}1)$ inhibitors. These compounds were identified as nine lignans, two neolignans, and two flavans by spectroscopic analysis. Of these, 5,7-di-O-methyl-3',4'-methylenated (-)-epicatechin (12) and 5,7,3'-tri-O-methyl (-)-epicatechin (13) have not been reported previously in this plant. In addition, seven compounds, machilin A (1), (-)-sesamin (3), machilin G (5), (+)-galbacin (9), licarin A (10), (-)-acuminatin (11) and compound 12 showed dose-dependent potent inhibitory activities against $PLC{\Upsilon}1$ in vitro with $IC_{50}$ values ranging from 8.8 to 26.0 ${\mu}M$. These lignans, neolignans, and flavans are presented as a new class of $PLC{\Upsilon}1$ inhibitors. The brief study of the structure activity relationship of these compounds suggested that the benzene ring with the methylene dioxy group is responsible for the expression of inhibitory activities against $PLC{\Upsilon}1$. Moreover, it is suggested that inhibition of $PLC{\Upsilon}1$ may be an important mechanism for an antiproliferative effect on the human cancer cells. Therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.

• Journal of Ginseng Research
• /
• v.44 no.2
• /
• pp.215-221
• /
• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• Biomolecules & Therapeutics
• /
• v.2 no.4
• /
• pp.303-309
• /
• 1994

The analysis of membrane receptors for hormones and neurotransmitters has progressed considerably by pharmacological and biochemical means and more recently through the use of specific antibodies. Two kinds of antibodies could be produced, one is from synthetic peptides and the other from proteins such as purified receptor. Anti-peptide antibodies gave some advantages; epitope is evident and also receptor purification in quantity is not prerequisite. It can be also applied to the study of receptor structure-activity relationship. The purpose of the present study was 1) to produce and characterize a polyclonal antibody against a synthetic $\beta$2-adrenergic receptor peptide(Phe-Gly-Asn-Phe-Trp-Cys-Phe-Trp-Thr-Ser-Ile-Asp-Val-Leu) and 2) to determine the effects of this antibody on the $\beta$-adrenergic receptor ligand interaction. The peptide sequence contains an amino acid residue such as Asp-113 which was identified as one of important component for receptor-ligand interaction in site-directed mutagenesis studies. Production of antibody was performed by immunization of rabbits through popliteal lymph node with the peptide coupled with Keyhole Limpet Hemocyanin (KLH). The titer of antibody against this peptide was 1 : 1000. The anti-peptide antibody was able to detect a 67 kDa protein band in western blot corresponding to the molecular weight of the $\beta$-adrenergic receptor in partially purified receptor fraction derived from guinea pig lung. The antisera inhibited the specific binding of [$^3$H]dihydroalprenolol to $\beta$-adrenergic receptor in a concentration-dependent manner. The results from this study suggest that the peptide sequence selected in the present study is important for the receptor ligand interaction.

• The Journal of the Korea Contents Association
• /
• v.17 no.5
• /
• pp.326-336
• /
• 2017

This study investigates the relevance of stress, self factor and emotional factor, and the influence on Smartphone Addiction Level among college students. The survey was administered to 261 college students in J city from December 16th to 23rd, 2016. The structured self-administered questionaries were used. The multiple linear regression analysis revealed that the factors with explanatory powers of 52% on Smartphone Addiction Level included physical activity changes, sleep disorders, the self control about self factors, the impulsion of emotional factors. With the analysis of covariance structure, we could confirm the relationship among the four factors such as stress, self factor, emotional factor and Smartphone Addiction Level. The results of the study indicate that the efforts to manage stress, self factors and emotional factors, are required to reduce the Smartphone Addiction Level of the college students. The results are expected to be useful for the development of programs and policy to decrease the Smartphone Addiction Level. In the following study, structural equation modeling about additional factors, which influences on Smartphone Addiction Level, will be needed.

• Journal of Radiation Industry
• /
• v.10 no.4
• /
• pp.181-187
• /
• 2016

Selective ${\beta}_1$-agonist and antagonists are used for the treatment of cardiac diseases including congestive heart failure, angina pectoris and arrhythmia. Selective ${\beta}_1$-antagonists including nebivolol have high binding affinity on ${\beta}_1$-adrenergic receptor, not ${\beta}_2$-receptor mainly expressed in smooth muscle. Nebivolol is one of most selective ${\beta}_1$-blockers in clinically used ${\beta}_1$-blockers including atenolol and bisoprolol. We tried to develop clinically useful cardiac PET tracers using a selective ${\beta}_1$-blocker. Nebivolol is $C_2$-symmetric and has two chromane moiety with a secondary amino alcohol and aromatic fluorine. We adopted the general synthetic strategy using epoxide ring opening reaction. Unlike formal synthesis of nebivolol, we prepared two chromane building blocks with fluorine and iodine which was transformed to diaryliodonium salt for labelling of $^{18}F$. Two epoxide building blocks were readily prepared from commercially available chromene carboxylic acids (1, 8). Then, the amino alcohol building block (15) was prepared by ammonolysis of epoxide (14) followed by coupling reaction with the other building block, epoxide (7). Diaryliodonium salt, a precursor for $^{18}F$-aromatic substitution, was synthesized in moderate yield which was readily subjected to $^{18}F$-aromatic substitution to give $^{18}F$-labelled nebivolol.

• Korean Journal of Poultry Science
• /
• v.48 no.4
• /
• pp.255-265
• /
• 2021

Global warming and scorching summer seasons affect the growth ability of broilers and animal welfare. In modern broilers, vital organs, such as the heart and lungs, grow disproportionally under intensive selection, making it difficult to adapt to warmer climates. Changes in environmental temperature can affect muscle formation during embryonic development and the early posthatching period. Satellite cells are highly sensitive to heat stress. Heat stress affects the proliferation and differentiation activity of satellite cells and muscle growth and structure. Therefore, thermal manipulation during broiler chick embryogenesis and environmental temperature management at the beginning of hatching are critical for the development and growth of broiler muscles. This review focuses on the thermoregulation mechanism of birds, the muscle development process of broilers, and the function of satellite cells, the relationship between heat stress and muscle development of chicks shortly after hatching, and studies on heat resistance and muscle growth of broilers.

• Journal of Korean Library and Information Science Society
• /
• v.53 no.4
• /
• pp.25-44
• /
• 2022

The purpose of this study is to examine how the content components of information literacy textbooks develop and is to find implications for improving of textbook publication. Three kinds of information literacy textbooks were published sequentially over time. The content components of 『Information and media』(1996) and 『Library and information skills』(2011) are processed by filament structure and 『Information and library』(2002) has a topic-driven project activity. Generally, a small lesson unit of the textbook consisted of three components (learning goals, learning contents, learning activities) and each component in the unit have to make semantic close relationships. However, in some information literacy textbooks, there are cases that the semantic relationship between goals, contents, and activities are cut off. This disconnection cases can be a fatal drawback for the reliability of textbooks, so sufficient attention is needed to develop information literacy textbooks later.

• Advances in nano research
• /
• v.12 no.3
• /
• pp.291-300
• /
• 2022

The behavior of hydrogen species on the surface of the catalyst during the Lewis acid transformation to form Brønsted acid sites over the spherical silica-supported WO_x catalyst was investigated. To understand the structure-activity relationship of Lewis acid transformation and hydrogen bonding interactions, we explore the potential of using the in situ diffuse reflection infrared Fourier transform spectroscopy (DRIFTS) with adsorbed ammonia and hydrogen exposure. From the results of in situ DRIFTS measurements, Lewis acid sites on surface catalysts were transformed into new Brønsted acid sites upon hydrogen exposure. The adsorbed NH₃ on Lewis acid sites migrated to Brønsted acid sites forming NH⁴⁺. The results show that the dissociated H atoms present on the catalyst surface formed new Si-OH hydroxyl species - the new Brønsted acid site. Besides, the isolated Si-O-W species is the key towards H-bond and Si-OH formation. Additionally, the H atoms adsorbed surrounding the Si-O-W species of mono-oxo O=WO₄ and di-oxo (O=)₂WO₂ species, where the Si-O-W species are the main species presented on the Inc-SSP catalysts than that of the IWI-SSP catalysts.

• Korean Journal of Social Welfare
• /
• v.58 no.1
• /
• pp.115-141
• /
• 2006

The purpose of this study is to understand the changes from adopting daily two-shift roster in child care institutions. To accomplish this purpose, we collected data mainly from depth interview with managers, child care workers, and children in child care institutions adopting daily two-shift roster, and analysed these data through qualitative case study approach. The results of this study are as follows. First, child care workers take the chance of recreation, their working conditions improved, they were participated in self-development activity, and they could make relationship with persons in social network. But, some participants worried about decrease of responsibility of workers. Second, one hand, possibility of high-quality care for child is increased, on the other hand, possibility of improving attachment relationship between workers and children is decreased. some children is confused by shift. But, most important strength is that partners have complementary parenting roles through discussion about parenting skills. They have developed communication skills by trial and error, and growed with children through sharing. Third, many qualified persons have applied for institution because of improvement of working conditions, thus institutions had the chance of adopting qualified workers. These workers have various abilities and resources, could mobilize resources from community, and could progress various programs and intervene for children. But, institutions had many difficulties in process adopting daily two-shift roster because of unstable financial support and previous structure. Most of participants worried about that local government may cut down a subsidy.