• Tribology and Lubricants
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• 제32권5호
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• pp.141-146
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• 2016

The diketopyrrolopyrrole (DPP) pigment is a bicyclic 8-π-electron system containing two lactam units. Typical DPP derivative pigments have melting points of over 350°C and very low solubility in most solvents, and show absorption in the visible region with a molar extinction coefficient of 33,000 dm²mol⁻¹ and strong photoluminescence with maxima in the range 500–600 nm. X-ray structure analyses of DPP show that the whole molecule is almost in one plane. The phenyl rings are twisted out of the heterocyclic plane and the intermolecular hydrogen bonding between neighboring lactam NH and carbonyl units influences the structure of the DPP pigment in the solid state. In this study, mono-N-alkylation and mono-N-arylation were undertaken for Pigment Red 264 or Pigment Orange 73 with alkyl halide and aryl halide, respectively, in the presence of sodium tert-butoxide as a base catalyst to improve the solubility of DPP pigments and their application as CO₂ indicators. The synthetic yield was in the range 11–88%. The indicator dyes are highly soluble in organic solvents and shows pH-dependent absorption (λ_max 501 and 572 nm for the protonated and deprotonated forms, respectively) and emission (λ_max 524 and 605 nm for the protonated and deprotonated forms, respectively) spectra. The mono-N-alkylated and mono-N-arylated DPP pigment was identified by ¹H-NMR (¹H-Nuclear Magnetic Resonance Spectrometer), FT-IR (Fourier Transform Infrared Spectroscopy), and MS (Mass Spectrometry). According to the results of color and hue properties obtained by a color matching analyzer, the synthesized DPP pigment material can be used as a CO₂ indicator.

• Molecular & Cellular Toxicology
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• 제2권3호
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• pp.151-158
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• 2006

Khal was a synthetic congener of halocidin, a heterodimeric peptide consisting of 19 and 15 amino acid residues detected in Halocynthia aurantium. This compound was considered a candidate for the development of a novel peptide antibiotic. The genotoxicity of Khal was subjected to high throughput toxicity screening (HTTS) because they revealed strong antibacterial effects. Mouse lymphoma thymidine kinase ($tk^{+/-}$) gene assay (MOLY), single cell gel electrophoresis (Comet) assay and chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. These compounds are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. Before performing the comet assay, $IC_{20}$ of Khal was determined the concentration of $25.51\;{\mu}/mL\;and\;21.99\;{\mu}g/mL$ with and without S-9, respectively. In the comet assay, Khal was not induced DNA damage in mouse lymphoma cell line. Also, the mutation frequencies in the Khal-treated cultures were similar to the vehicle controls. It is suggests that Khal is non-mutagenic in MOLY assay. And no clastogenicity was observed in Khal-treated Chinese hamster lung cells. The results of this battery of assays indicate that Khal has no genotoxic potential in bacterial or mammalian cell systems. Therefore, we suggest that Khal, as the optimal candidates with both no genotoxic potential and antibacterial effects must be chosen.

• Journal of Pharmaceutical Investigation
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• 제22권3호
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• pp.185-196
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• 1992

To assess its suitability as a prodrug of 5-fluorouracil (5-FU), 1-glycyloxymethyl-5-FU HCl (GFU), a 5-fluorouracil derivative having a glycyloxymethyl group at the N-l position was synthetized. Its physicochemical properties and hydrolysis kinetics, in aqueous solution of pH $1{\sim}10$ and in the presence of human plasma or rat liver homogenate were studied. Its acute toxicity and antitumor activity against sarcoma 180 were also examined, GFU showed higher lipid/water partition coefficient than 5-FU. The calculated $pK_{\alpha}$ values of 5-FU and GFU were 8.02 and 7,20, respectively. The decomposition rates of GFU in aqueous solution showed a pH-dependence over the pH range used, which could be ascribed to solvent catalysed hydrolysis reaction at pH lower than 4,16 and to specific hydroxide ion hydrolysis reaction at pH higher than 4,16, The half-life of GFU was 6,9 min in 80% human plasma solution and less than 3 min in rat liver homogenate at $37^{\circ}C$, The $LD_{50}$ value of 5-FU was 240 mg/kg while that of GFU was 440.6 mg/kg (226 mg as 5-FU). Both of 5FU and GFU showed a strong antitumor activity, Therapeutic ratios of 5-FU and GFU were 3.07 and 3.55, respectively.

• 한국전산구조공학회논문집
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• 제25권2호
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• pp.139-148
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• 2012

MLS(Moving Least Squares) 차분법은 무요소법의 이동최소제곱법과 Taylor 전개를 이용하여 요소망의 제약 및 수치 적분이 없이 절점만을 이용하여 미분방정식을 수치해석할 수 있는 방법이다. 본 연구에서는 고체역학 문제의 동적해석을 위하여 MLS 차분법의 시간이력해석 알고리즘을 제시한다. 개발된 알고리즘은 Newmark 방법으로 시간적분을 하였으며, 강형식을 그대로 이산화하여 해석을 수행했다. 이동최소제곱법을 이용해 Taylor 전개식을 근사하여 실제 미분계산없이 미분근사식을 얻기 때문에 고차까지 Taylor 다항식의 차수를 증가하는 것이 용이하다. 1차원과 2차원 수치예제들을 통하여 동적해석을 위한 MLS 차분법의 정확성과 효율성을 검증하였다. 수치결과들이 정확해에 잘 수렴하였으며, 유한요소법(FEM)의 해석결과와 비교하여 떨림현상(oscillation) 및 주기성(periodicity) 오차에 대해 보다 안정적인 모습을 보였다.

• 대한화학회지
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• 제22권4호
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• pp.239-244
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• 1978

Stilbene 유도체인 trans-1,2-bispyrazylethylene에 대한 분광학적 연구를 행하였다. 보통의 자외선 흡수스펙트럼에서는 $n{\rightarrow}{\pi}^*$ 흡수밴드는 에너지가 비슷한 ${\pi}{\rightarrow}{\pi}^*$ 흡수밴드에 가려져서 나타나지 않는데 2차 미분 스펙트럼과 저온(77˚K)에서의 스펙트럼으로 부터 $n{\rightarrow}{\pi}^*$ 흡수 밴드를 확인할 수가 있었다. 또한 ${\pi}{\rightarrow}{\pi}^*$ 흡수밴드들의 전이에너지를 PPP-SCF-CI MO 방법으로 계산한 결과 스펙트럼에서 얻은 값과 잘 일치했다. 형광스펙트럼, 형광편광스펙트럼, 그리고 PPP-SCF-CI MO 방법에 의한 계산으로부터 형광을 내는 상태는 $^1({\pi},\;{\pi}^*)$ 상태임을 알 수가 있었으며 이것은 형광에 대한 alkaline salt effect의 결과와 일치한다.

• Journal of the Korean Wood Science and Technology
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• 제37권3호
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• pp.239-244
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• 2009

본 연구에서는 느티나무 심재부에서 단리한 7-hydroxy-3-methoxycadalene이 나타내는 세포독성을 경감시키고 물에 대한 낮은 용해도를 향상시킬 목적으로 반응물의 7번 위치에 존재하는 수산기를 친수성이 강하고 세포 독성이 없는 글루코오스로 치환시켜 7-O-${\beta}$-D-glucopyranosyl -3-methoxycadalene을 합성하였으며, 수율은 약 55%에 이르렀다. 7-O-${\beta}$-D-glucopyranosyl -3-methoxycadalene은 반응 전 7-hydroxy-3-methoxycadalene에 비해 물에 대한 수용성이 크게 증가하였다. 카달렌-글루코오스 유도체는 정상 폐조직 세포(WI-38 cell line)와 폐암 세포주(A-549 cell line)에 대한 세포생존율, 즉 반수치사율(IC50)이 각각 $298.2{\mu}m$과 $88.6{\mu}m$로 나타났다. 이러한 결과는 7-hydroxy-3-methoxycadalene에 글루코오스 한 분자를 치환함으로써 폐암세포의 증식억제에 미치는 약리적 효과가 3배 이상으로 향상되었음을 의미한다.

• BMB Reports
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• 제51권4호
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• pp.188-193
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• 2018

Caffeoylserotonin (CaS), one derivative of serotonin (5-HT), is a secondary metabolite produced in pepper fruits with strong antioxidant activities. In this study, we investigated the effect of CaS on proliferation and migration of human keratinocyte HaCaT cells compared to that of 5-HT. CaS enhanced keratinocyte proliferation even under serum deficient condition. This effect of CaS was mediated by serotonin 2B receptor (5-HT2BR) related to the cell proliferation effect of 5-HT. We also confirmed that both CaS and 5-HT induced G1 progression via 5-HT2BR/ERK pathway in HaCaT cells. However, Akt pathway was additionally involved in upregulated expression levels of cyclin D1 and cyclin E induced by CaS by activating 5-HT2BR. Moreover, CaS and 5-HT induced cell migration in HaCaT cells via 5-HT2BR. However, 5-HT regulated cell migration only through ERK/AP-1/MMP9 pathway while additional Akt/NF-${\kappa}B$/MMP9 pathway was involved in the cell migration effect of CaS. These results suggest that CaS can enhance keratinocyte proliferation and migration. It might have potential as a reagent beneficial for wound closing and cell regeneration.

• 한국전산구조공학회논문집
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• 제26권1호
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• pp.39-48
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• 2013

본 논문은 기존의 1차원 Stefan 문제를 해석할 수 있는 이동최소제곱 차분법을 확장하여 복잡한 계면경계 형상을 갖는 2차원 문제에 적용할 수 있는 수치기법을 개발한다. 1차원 경우와 달리 2차원 영역에서 임의로 움직이는 이동경계의 위상변화를 효과적으로 모델링할 수 있는 기법을 제안했으며, 이동경계 모사시 절점만 사용하는 이동최소제곱 차분법의 강점을 그대로 살리면서 이동경계의 불연속 특이성과 kinetics 조건을 정확하게 만족시키는 이동최소제곱 미분근사식을 제시했다. 평형방정식은 implicit(음해)법으로 차분하여 수치 안정성을 확보했으며, 이동경계는 explicit(양해)법으로 update하여 계산효율성의 극대화했다. 몇 가지 수치예제를 통해 개발된 이동최소제곱 차분법이 다양한 계면경계 형상을 갖는 2차원 Stefan 문제를 정확하고 효율적으로 풀 수 있음을 검증했다.

• 한방비만학회지
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• 제20권1호
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• pp.1-9
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• 2020

Objectives: Artemisinin and its derivatives extracted from Artemisia annua, a Chinese herbal medicine, have variable biological effects due to structural differences. Up to date, the anti-obesity effect of dihydroartemisinin (DHA), a derivative of artemisinin, is unknown. The purpose of this study was to investigate the anti-adipogenic and lipolytic effects of DHA on 3T3-L1 preadipocytes. Methods: Oil Red O staining and AdipoRed assay were used to measure lipid accumulation and triglyceride (TG) content in 3T3-L1 cells, respectively. Cell count analysis was used to determine the cytotoxicity of 3T3-L1 cells. Western blot and real-time reverse transcription polymerase chain reaction analyses were used to analyze the expression of protein and mRNA in 3T3-L1 cells, respectively. Results: DHA at 5 μM markedly inhibited lipid accumulation and reduced TG content in differentiating 3T3-L1 cells with no cytotoxicity. Furthermore, DHA at 5 μM inhibited the expression of CCAAT/enhancer-binding protein-α (C/EBP-α), peroxisome proliferator-activated receptor-γ (PPAR-γ), fatty acid synthase (FAS), and perilipin A as well as the phosphorylation of signal transducer and activator of transcription-3 (STAT-3) in differentiating 3T3-L1 cells. Moreover, while DHA at 5 μM had no effect on the mRNA expression of adiponectin, it strongly suppressed that of leptin in differentiating 3T3-L1 cells. However, DHA at 5 μM had no lipolytic effect on differentiated 3T3-L1 cells, as assessed by no enhancement of glycerol release. Conclusions: These results demonstrate that DHA at 5 μM has a strong anti-adipogenic effect on differentiating 3T3-L1 cells through the reduced expression and phosphorylation of C/EBP-α, PPAR-γ, FAS, perilipin A, and STAT-3.

• 약학회지
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• 제45권5호
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• pp.468-475
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• 2001

Fenofibrate is a fibric acid derivative that is a strong reducer of triglyceride. Micronozed formulation of fenofibrate has improved bioavailability compared to non-micrornized formulation. This study performed a retrospective comparison of micrornized and non-micrornized fenofibrate (28 in micronized and 51 in non-micronized group) by comparing the means of changes in total triglyceride, total cholesterol, HDL-cholesterol and TC/HDL ratio in type 2 diabetics with dyslipidemia The result skewed that after 12 weeks of treatment both drugs produced a significant reduction in total triglyceride levels (62% with micronized, 37% with non-micronized). The mean decrease observed for total triglyceride levels were significantly lower for micronized fenofibrate (p<0.001). Both drugs showed a significant reduction for total cholesterol levels (-22% with micronized, -14% with non-micronized fenofibrate). The mean decrease observed for total cholesterol was not significantly different between the two drugs (p>0.05). HDL-cholesterol levels increased by 24% and 15%) with micronized and non-micronized, respectively and the differences from the baseline were statistically significant for both drugs (p<0.05). The mean change of HDL-cholesterol was not significantly different between the two drugs. There was a statistically significant reduction in TC/HBL-cholesterol ratio from baseline for both drugs (7.1 to 4.8 with micronized and 5.1 to 4.5 with non-micronized), and the reduction of TC/HDL-cholesterol ratio tended to be significantly greater with micronized fenofibrate (p<0.05). This study shows that short-term treatment with micronized fenofibrate is more effective than non-micronized fenosbrate in type 2 diabetes patients with dyslipidemia.