• Title/Summary/Keyword: Drug Development

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Excavation of Lead Compounds that Inhibit Mast Cell Degranulation by Combinatorial Chemistry and Activity-Guided

  • Hahn, Hoh-Gyu;Oh, Heong-Sub;Cheon, Seung-Hoon;Oak, Min-Ho;Kim, Young-Ran;Kim, Kyeong-Man
    • Archives of Pharmacal Research
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    • v.27 no.5
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    • pp.518-523
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    • 2004
  • An allergic reaction ensues after antigen binds to mast cell or basophil high affinity IgE receptor, Fc$\varepsilon$RI, resulting in degranulation of various inflammatory mediators that produce various allergic symptoms. In this study, i) we isolated the active component for the inhibition of mast cell degranulation from the extract of leaves of Castanea crenata and identified it as quercetin; ii) we established the total synthesis procedure of quercetin; iii) using quercetin as positive control, we excavated some lead compounds that possess inhibitory activities for mast cell degranulation by screening the chemical libraries of 1,3-oxazolidine derivatives prepared by solid phase combinatorial chemistry. Some of 1,3-oxazolidine compounds possessing acetyl and 3',4'-dichlorophenyl group displayed strong inhibitory activities on Fc$\varepsilon$RI-mediated mast cell degranulation, suggesting that they can be used as lead compounds for the development of anti-allergic agents.

Development of analytical method of DMDM hydantoin, Sorbic acid, Phenoxy ethanol in Cosmetics

  • Kim, Young-Ok;Jang, Jung-Yun;Lee, Jeong-Pyo;Yang, Seong-Jun;Lee, Kyung-Shin;Yang, Won-Jun;Kim, Chong-Kap;Choi, Sang-Sook
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.280.3-281
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    • 2003
  • A high-performance liquid chromatographic method for the simultaneous quantitative analysis of DMDM hydantoin, sorbic acid, phenoxy ethanol in cosmetics was studied by using a X-terra C18 column and 0.75mM KH2PO4 in 0.85% sulfuric acid and methanol mixture(7:3) at 214nm. Calibration curves were found to be linear in the 20-100$\mu\textrm{g}$/mL range (DMDM hydantoin), 50-250$\mu\textrm{g}$/mL range (sorbic acid) and 10-50$\mu\textrm{g}$/mL range (phenoxy ethanol). The result of recovery test were 96.6% - 104.2%. This HPLC method can be applied quality control of cosmetics.

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DEVELOPMENT OF ANALYYICAL METHOD OF DMDM HYDANTOIN, SORBIC ACID, PHENOXY ETHANOL IN COSMETICS

  • K. H. Son;Kim, Y. O.;J. Y. Jang;Lee, J. P.;S. J. Yang;Lee, K. S.;W. J. Yang;Kim, C. K.;Park, S. S.
    • Proceedings of the SCSK Conference
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    • 2003.09b
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    • pp.527-527
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    • 2003
  • A high-performance liquid chromatographic method for the simultaneous quantitative analysis of DMDM hydantoin, sorbic acid, phenoxy ethanol in cosmetics was studied by using a X-terra C$\sub$18/ column and 0.75mM KH$_2$PO$_4$ in 0.85% sulfuric acid and methanol mixture(7:3) at 214nm. Calibration curves were found to be linear in the 20-100 $\mu\textrm{g}$/mL range (DMDM hydantoin), 50-250 $\mu\textrm{g}$/mL range (sorbic acid) and 10-50 $\mu\textrm{g}$/mL range (phenoxy ethanol). The result of recovery test were 96.6% ∼ 104.2%. This HPLC method can be applied quality control of cosmetics.

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Development of the Portable Drug Delivery Systems with a Piezoelectric Micropump (압전 마이크로펌프 방식의 휴대용 약물전달장치 개발)

  • Kim, Sei Yoon;Kim, Young Tae;Seo, Hyun Bae
    • Journal of Drive and Control
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    • v.12 no.4
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    • pp.71-76
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    • 2015
  • The therapy of injecting a fixed amount of a prescribed drug for a predetermined time is an effective treatment in relieving pain during anticancer treatments. Due to recent medical technology development, cancer is currently classified as a disease that can be managed in the patient's lifetime. If patients were able to use a drug delivery system that was portable, sustainable and had an accurate flow control, they would be able to inject medication whenever they need. In this study we developed a piezoelectric micropump for a drug delivery system by designing a pump chamber, check valve and diaphragm. We also developed a driving circuit that consumes low power and to which we applied a variety of signals. We fabricated a portable drug delivery system with this piezoelectric micropump and driving circuit. In addition, through a performance test, we confirmed that the system can precisely control the drug flow rate.

Cytotoxic Components in an Extract from the Leaves and Stems of Stauntonia hexaphylla

  • Zhao, Jing;Yim, Soon-Ho;Um, Jung-In;Park, Si-Hwan;Oh, Eun-Sang;Jung, Da-Woon;Williams, Darren R.;Lee, Ik-Soo
    • Natural Product Sciences
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    • v.20 no.2
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    • pp.130-134
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    • 2014
  • An investigation was carried out to identify novel anti-cancer compounds from Korean indigenous plant extracts. Bioassay-guided fractionation and chemical investigation of the EtOAc extract from the leaves and stems of Stauntonia hexaphylla resulted in the isolation of two active compounds, hederagenin 3-O-${\alpha}$-L-arabinoside (1) and quercetin (2). The structures of these compounds were elucidated by spectroscopic methods, including UV, IR, MS, NMR techniques and compared with previous spectroscopic data. The cytotoxic effects of fractions and compounds on HCT116 human colon cancer cells were evaluated using the MTT assay. Quercetin showed a stronger anti-cancer effect when compared to hederagenin 3-O-${\alpha}$-L-arabinoside.

A Study on Improvement Issues to Activate the Statistics Utilization of the Ministry of Food and Drug Safety (식품의약품안전처 통계 활용 활성화를 위한 개선과제 도출)

  • Jung, Daeun;Kim, Jinmin
    • Journal of Korea Society of Digital Industry and Information Management
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    • v.17 no.4
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    • pp.133-146
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    • 2021
  • In the field of food and drug, the role of the Ministry of Food and Drug Safety is becoming more important for national and public safety as well as national development and improvement of public welfare. Food and drug statistics are being used to determine the priorities and directions of policy for the promotion of public health and the development of the health industry. This study focuses on statistics from the MFDS. Through the analysis of the MFDS's statistics, the current status of the MFDS's production statistics was identified, and the survey of utilization and satisfaction of the MFDS's statistics was conducted on food and drug experts who actually use the statistics of the MFDS. In order to identify problems of the MFDS statistics, environmental factors affecting the MFDS statistics were derived, and the priorities of improvement tasks for its statistics were identified using AHP and IPA. In addition, the current situation of the statistical system, which serve as the basic coordinate for the establishment and execution of domestic food and drug policies, was identified and implications were provided.

A Study on the Prediction of Drug Efficacy by Using Molecular Structure (분자구조 유사도를 활용한 약물 효능 예측 알고리즘 연구)

  • Jeong, Hwayoung;Song, Changhyeon;Cho, Hyeyoun;Key, Jaehong
    • Journal of Biomedical Engineering Research
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    • v.43 no.4
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    • pp.230-240
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    • 2022
  • Drug regeneration technology is an efficient strategy than the existing new drug development process, which requires large costs and time by using drugs that have already been proven safe. In this study, we recognize the importance of the new drug regeneration aspect of new drug development and research in predicting functional similarities through the basic molecular structure that forms drugs. We test four string-based algorithms by using SMILES data and searching for their similarities. And by using the ATC codes, pair them with functional similarities, which we compare and validate to select the optimal model. We confirmed that the higher the molecular structure similarity, the higher the ATC code matching rate. We suggest the possibility of additional potency of random drugs, which can be predicted through data that give information on drugs with high molecular similarities. This model has the advantage of being a great combination with additional data, so we look forward to using this model in future research.

Experimental model and novel therapeutic targets for non-alcoholic fatty liver disease development

  • Yujin Jin;Kyung-Sun Heo
    • The Korean Journal of Physiology and Pharmacology
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    • v.27 no.4
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    • pp.299-310
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    • 2023
  • Non-alcoholic fatty liver disease (NAFLD) is a complex disorder characterized by the accumulation of fat in the liver in the absence of excessive alcohol consumption. It is one of the most common liver diseases worldwide, affecting approximately 25% of the global population. It is closely associated with obesity, type 2 diabetes, and metabolic syndrome. Moreover, NAFLD can progress to non-alcoholic steatohepatitis, which can cause liver cirrhosis, liver failure, and hepatocellular carcinoma. Currently, there are no approved drugs for the treatment of NAFLD. Therefore, the development of effective drugs is essential for NAFLD treatment. In this article, we discuss the experimental models and novel therapeutic targets for NAFLD. Additionally, we propose new strategies for the development of drugs for NAFLD.

Development and Validation of a Simultaneous Analytical Method for the Detection of Mefentrifluconazole and Triticonazole Fungicide in Agricultural Crops (농산물 중 메펜트리플루코나졸 및 트리티코나졸 살균제의 동시 분석법 개발 및 검증)

  • Park, Ji-Su;Lee, Han Sol;Lee, Su Jung;Shin, Hye-Sun;Shim, Jae-Han;Yun, Sang Soon;Jung, Yong-hyun;Oh, Jae-Ho
    • Korean Journal of Environmental Agriculture
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    • v.39 no.2
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    • pp.130-137
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    • 2020
  • BACKGROUND: Mefentrifluconazole and triticonazole are the triazole fungicides. The maximum residue levels for agricultural products need to be set up. Therefore, development of the official analytical method for determination of mefentrifluconazole and triticonazole residues from agricultural crops was necessary due to safety management, and then a simultaneous analytical method was developed for the determination of mefentrifluconazole and triticonazole in agricultural crops. METHODS AND RESULTS: Samples were extracted using acetonitrile and purified using dispersive solid phase extraction, and then detected with liquid chromatograph-tandem mass spectrometry (LC-MS/MS). Matrix-matched calibration curves (0.0025-0.25 ㎍/mL) were linear into a sample extract with r2>0.99. For validation, the recovery test was carried out at three fortification levels (LOQ, 10 LOQ and 50 LOQ) from agricultural samples. The results for mefentrifluconazole and triticonazole ranged between 92.3 to 115.3% and 91.4 to 108.5%, respectively and RSD (relative standard deviation) values were also below 6.0%. Furthermore, inter-laboratory was conducted to validate the method. CONCLUSION: All values were corresponded with the criteria ranges requested by both the CODEX (CAC/GL 40-1993, 2003) and MFDS guidelines (2016). Therefore, the proposed method can be used as an official analytical method for determination of mefentrifluconazole and triticonazole (triazole fungicides) in the Republic of Korea.

Computer-Aided Drug Discovery in Plant Pathology

  • Shanmugam, Gnanendra;Jeon, Junhyun
    • The Plant Pathology Journal
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    • v.33 no.6
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    • pp.529-542
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    • 2017
  • Control of plant diseases is largely dependent on use of agrochemicals. However, there are widening gaps between our knowledge on plant diseases gained from genetic/mechanistic studies and rapid translation of the knowledge into target-oriented development of effective agrochemicals. Here we propose that the time is ripe for computer-aided drug discovery/design (CADD) in molecular plant pathology. CADD has played a pivotal role in development of medically important molecules over the last three decades. Now, explosive increase in information on genome sequences and three dimensional structures of biological molecules, in combination with advances in computational and informational technologies, opens up exciting possibilities for application of CADD in discovery and development of agrochemicals. In this review, we outline two categories of the drug discovery strategies: structure- and ligand-based CADD, and relevant computational approaches that are being employed in modern drug discovery. In order to help readers to dive into CADD, we explain concepts of homology modelling, molecular docking, virtual screening, and de novo ligand design in structure-based CADD, and pharmacophore modelling, ligand-based virtual screening, quantitative structure activity relationship modelling and de novo ligand design for ligand-based CADD. We also provide the important resources available to carry out CADD. Finally, we present a case study showing how CADD approach can be implemented in reality for identification of potent chemical compounds against the important plant pathogens, Pseudomonas syringae and Colletotrichum gloeosporioides.