• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.212.2-212.2
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• 2003

In the course of searching for BACE1 (${\beta}$-secretase) inhibitors from natural products, the ethyl acetate soluble fraction of green tea, which was suspected to be rich in catechin content, showed potent inhibitory activity. (-)-Epigallocatechin gallate, (-)-epicatechin gallate, and (-)-gallocatechin gallate ware isolated with IC$\_$50/ values of 1.6${\times}$10$\^$-6/ M, 4.5${\times}$10$\^$-6/ M, and 1.8${\times}$10$\^$-6/ M, respectively. Seven additional authentic catechins were tested for a fundamental structure-activity relationship. (-)-Catechin gallate, (-)-gallocatechin, and (-)-epigallocatechin significantly inhibited BACE1 activity with IC$\_$50/ values of 6.0${\times}$10$\^$-6/ M, 2.5${\times}$10$\^$-6/ M, and 2.4${\times}$10$\^$-6/ M, respectively. (omitted)

• Archives of Pharmacal Research
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• 제29권8호
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• pp.657-665
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• 2006

We recently reported that dimethylsphingosine (DMS), a metabolite of sphingolipids, increased intracellular pH and $Ca^{2+}$ concentration in U937 human monocytes. In the present study, we found that dimethylphytosphingosine (DMPH) induced the above responses more robustly than DMS. However, phytosphingosine, monomethylphytosphingosine or trimethylsphingosine showed little or no activity. Synthetic C3 deoxy analogues of sphingosine did show similar activities, with the C16 analogue more so than C18. The following structure-activity relationships were observed between DMS derivatives and the intracellular pH and $Ca^{2+}$ concentrations in U937 monocytes; 1) dimethyl modification is important for the DMS-induced increase of intracellular pH and $Ca^{2+}$, 2) the addition of an OH group on C4 enhances both activities, 3) the deletion of the OH group on C3 has a negligible effect on the activities, and 4) C16 appears to be more effective than C18. We also found that W-7, a calmodulin inhibitor, blocked the DMS-induced pH increase, whereas, KN-62, ML9, and MMPX, specific inhibitors for calmodulin-dependent kinase II, myosin light chain kinase, and $Ca^{2+}$-calmodulin-dependent phosphodiesterase, respectively, did not affect DMS-induced increases of pH in the U937 monocytes.

• 한국전문물리치료학회지
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• 제30권2호
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• pp.136-143
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• 2023

Background: The International Classification of Functioning, Disability and Health (ICF) model, created by the World Health Organization, provides a theoretical framework that can be applied in the diagnosis and treatment of various disorders. Objects: Our research purposed to ascertain the relationship between structure/function, activity, and participation domain variables of the ICF and pain, pain-associated disability, activities of daily living (ADL), and quality of life in patients with chronic low back pain (LBP). Methods: Two-hundred patients with chronic LBP (mean age: 35.5 ± 8.8 years, females, n = 40) were recruited from hospital and community settings. We evaluated the body structure/function domain variable using the Numeric Pain Rating Scale (NPRS) and Roland-Morris disability (RMD) questionnaire. To evaluate the activity domain variable, we used the Oswestry Disability Index (ODI) and Quebec Back Pain Disability Scale (QBDS). For clinical outcome measures, we used Short-form 12 (SF-12). Pearson's correlation coefficient was used to ascertain the relationships among the variables (p < 0.05). All the participants with LBP received 30 minutes of conventional physical therapy 3 days/week for 4 weeks. Results: There were significant correlations between the body structure/function domain (NPRS and RMD questionnaire), activity domain (ODI and QBDS), and participation domain variables (SF-12), rending from pre-intervention (r = -0.723 to 0.783) and postintervention (r = -0.742 to 0.757, p < 0.05). Conclusion: The identification of a significant difference between these domain variables point to important relationships between pain, disability, performance of ADL, and quality in participants with LBP.

• The Korean Journal of Physiology and Pharmacology
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• 제14권6호
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• pp.441-447
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• 2010

B13, a ceramide analogue, is a ceramidase inhibitor and induces apoptosis to give potent anticancer activity. A series of thiourea B13 analogues was evaluated for their in vitro cytotoxic activities against human renal cancer Caki-2 and leukemic cancer HL-60 in the MTT assay. Some compounds (12, 15, and 16) showed stronger cytotoxicity than B13 and C6-ceramide against both tumor cell lines, and compound (12) gave the most potent activity with $IC_{50}$ values of 36 and $9\;{\mu}M$, respectively. Molecular modeling of thiourea B13 analogues was carried out by comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). We obtained highly reliable and predictive CoMSIA models with cross-validated $q^2$ values of 0.707 and 0.753 and CoMSIA contour maps to show the structural requirements for potent activity. These data suggest that the amide group of B13 could be replaced by thiourea, that the stereochemistry of 1,3-propandiol may not be essential for activity and that long alkyl chains increase cytotoxicity.

• Applied Biological Chemistry
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• 제40권5호
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• pp.447-450
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• 1997

18 종의 N-치환 phenyl 1,3,5-trimethylpyrazole-4-carboxamide 를 합성하여 벼 잎집무늬 마름병균 Rhizoctonia solani $K{\ddot{u}}hn$ 에 대한 균사생육억제력 $(pEC_{50})$ 과 이 균에서 분리한 succinate dehydrogenase (SDH)의 효소활성 저해력 $(pI_{50})$ 을 측정하였다. 구조-활성 상관연구를 통해 균사생육억제력이 SDH 효소저해력과 소수성인자인 chromatographic capacity factor $(\acute{k})$ 에 의해 79%까지 유의성 있게 해석되었으며 이는 합성한 화합물의 주작용점이 SDH 이고 생체내에서 작용점까지 도달하는데 필요한 소수성성질이 살균력의 발현에 중요한 인자임을 보여준다.

• 한국콘텐츠학회논문지
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• 제12권4호
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• pp.304-314
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• 2012

본 연구는 서울에 거주하면서 여가-신체활동에 참여하는 60세 이상의 노인 여성 211명을 대상으로 삶의 의미, 낙관성 및 행복의 관계를 살펴보았다. 분석은 SPSS WIN 15.0과 AMOS 6.0 프로그램을 이용하여 탐색적-확인적 요인분석, 신뢰도분석, 상관관계 분석, 구조모형분석을 통해 결과를 도출하였다. 그 결과를 제시하면 다음과 같다. 첫째, 삶의 의미를 구성하는 의미발견은 낙관성에 통계적으로 유의미한 정적 영향을 미치는 것으로 나타나 삶의 의미발견을 추구할수록 낙관성도 높아지는 것으로 조사되었다. 의미추구도 낙관성에 통계적으로 유의미한 정적 영향을 미치는 것으로 나타나 삶의 의미발견을 추구할수록 낙관성도 높아지는 것으로 나타났다. 둘째, 낙관성은 행복을 구성하는 긍정적 정서에 통계적으로 유의미한 정적 영향을 미치는 것으로 나타나 여가-신체활동에 참여하는 노인이 낙관적일수록 긍정적 정서도 높아지는 것으로 조사되었다. 또한 여가-신체활동에 참여하는 노인의 낙관성은 부정적 정서에 부적 영향을 미치는 것으로 낙관적일수록 부정적 정서가 감소하는 것으로 조사되었다.

• Archives of Pharmacal Research
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• 제22권6호
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• pp.592-607
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• 1999

2-(1-Aryl-1-hydroxymethyl)-and 2-aroyl-DHAQ derivatives (DHAQ, 1,4-dihydroxy-,10-anthraquinone), and 2-(1-aryl-1-hydroxymethyl)-ATO derivatives (ATO, anthraceneactivity (T/C 125~128%), though their cytotoxicity was not further improved compared to that of 2-(1-aryl-1-dydroxymethyl)-1,4-dihydroxy-9,10-anthraquinones. They manifested no correlation between the cytotoxicity and the antitumor activity. In case of 2-[1-hydroxy-1-(4-propylphenyl)-methyl]-ATO, the most bioactive one in viv-1,4,9,10-tetraone) were synthesized and their antitumor activities were determined. 2-(1-Aryl-1-hydroxymethyl)-DHAQ derivatives showed a stronger cytotoxicity compared to the series of 2-(1-hydroxyalkyl)-1,4-dihydroxy-9,10-anthraquinone derivatives. It was suggested that the presence of aryl group at the side chain accelerated the bioreductive activation leading to cell death. 2-Aroyl-DHAQ derivatives, despite their higher electrophilicity, revealed smaller cytotoxicity and antitumor activity (expressed by T/C value) than 2-(1-aryl-1-hydroxymethyl)-DHAQ derivatives. Thus, no consistent relationship between the electronic effect on aromatic side chain and the cytotoxicity was observed. ATO series exhibited a higher antitumor o among the same series, it showed an $ED_{50}$ value of 10.2 mg/mL and a T/C value of 218%. It is assumed that the anthrancene1,4,9,10-tetraones after uptake into cellular tissues might be transformed to a cytotoxic metabolite(s).

• Bulletin of the Korean Chemical Society
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• 제34권7호
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• pp.2006-2010
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• 2013

Leukocyte common antigen-related phosphatase (LAR) has been considered a promising target for the development of therapeutics for neurological diseases. Here, we report the first example for a successful application of the structure-based virtual screening to identify the novel small-molecule LAR inhibitors. Five of these inhibitors revealed micromolar inhibitory activities with the associated $IC_{50}$ values ranging from 2 to 6 ${\mu}M$. Because the newly identified inhibitors were also screened for having desirable physicochemical properties as a drug candidate, they may serve as a starting point of the structure-activity relationship study to optimize the medical efficacy. Structural features relevant to the stabilization of the new inhibitors in the active site of LAR are discussed in detail.

• 한국환경성돌연변이발암원학회:학술대회논문집
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• 한국환경성돌연변이발암원학회 2003년도 추계학술대회
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• pp.64-67
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• 2003

• 한국미생물생명공학회:학술대회논문집
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• 한국미생물생명공학회 2002년도 학술발표대회
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• pp.35-35
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• 2002