• Archives of Pharmacal Research
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• 제19권1호
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• pp.62-65
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• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.

• 약학회지
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• 제54권2호
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• pp.112-121
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• 2010

The cytotoxic activity of 33,4,5-trihydroxybenzoic acid methylester and related compounds on the growth of normal cell lines, human skin melanoma cells and human oral epithelioid cell line were evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and 2,3-bis-[2-methoxy-4-nitro-5-sulfo-phenyl]-2-H-tetrazolium-5-caboxanilide (XTT) methods. 3,4,5-Trihydroxybenzoic acid methylester decreased the cell viability of human skin melanoma cells and human oral epithelioid cells shown by the MTT method and the cell adhesion activity of human skin melanoma cells and human oral epithelioid cells shown by the XTT method. In light microscopy, 100 ${\mu}M$ 3,4,5-trihydroxybenzoic acid methylester showed the highest cytotoxic activity. These results suggest that 3,4,5-trihydroxybenzoic acid methylester has a potential anticancer activity.

• 약학회지
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• 제50권4호
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• pp.278-286
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• 2006

Classical dihydropyrrole[3,4-f]quinazoline antifolates 7,8 and 9, in which the tricyclic ring is structurally similar to the pteridine ring of $CH_2-THF(1)$, the cofactor of thymidylate synthase (TS), were synthesized, and their in vitro antitumor activity was evaluated by measuring the cell growth inhibitory activity against cancer cell lines. The target compounds were cytotoxic against CCRF-CEM, human T-cell acute lymphoblastic leukemia, with the cell growth inhibitory activity $(IC_{50})$ of $0.8{\sim}8.3\;{\mu}M$. Among the three compounds, 3-amino analog 7 was 10- and 3.5-fold more cytotoxic compared to the 3-methyl analogs 8 and 9, and its cytotoxicity was similar to that of the reference compound with the $IC_{50}$ value of $0.83\;{\mu}M$. This result was supposed as the consequence of the fact that dihydropyrroloquinazolinone ring with amino group was able to bind well in the active site of TS. In the case of 3-methyl analogs, analog 9, which has two-carbon bridge between the dihydropyrroloquinazolinone ring and benzoyl-L-glutamic acid, was 3-times more potent in cytotoxicity than analog 8 which has one-carbon bridge, and this result indicates that the distance and conformational orientation of the benzoyl-L-glutamic acid moiety with respect to the tricyclic ring may also be a crucial determinant of cell growth inhibitory activity.

• Bulletin of the Korean Chemical Society
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• 제27권9호
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• pp.1353-1358
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• 2006

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

• 약학회지
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• 제35권5호
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• pp.401-415
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• 1991

Effects of quercetin on the specific and non-specific immune responses were studied in vivo. Quercetin at a dose of 2.5, 5, 10, 20 and 40 mg/kg were orally administered to ICR male mice once daily for 28 consecutive days. Cyclophosphamide was injected intraperitoneally to ICR mice with a single dose of 5 mg/kg 2 days before secondary immunization. Mice were sensitized and challenged with sheep red blood cells (S-RBC). Immune responses were evaluated by humoral and cellular immune reponses and non-specific immune response. The results of this study were summarized as followings; 1. Quercetin significantly decreased the body weight, and introduced the atrophy of liver, spleen and thymus gland dose-dependently, but increased the numbers of white blood cell. 2. Querectin significantly depressed the hemagglutination titer, Arthus reaction and hemolytic plaque forming cell. 3. Quercetin significantly depressed the delayed type hypersensitivity and rosette forming cell. 4. Quercetin at a dose of 2.5, 5 and 40 mg/kg significantly depressed phagocytic activity. 5. Quercetin at a dose of 10 and 20 mg/kg significantly increased natural killer cell activity.

• The Korean Journal of Physiology and Pharmacology
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• 제7권5호
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• pp.275-278
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• 2003

Antioxidative activity is an important factor in inhibiting oxidative stress. The usual methods for determining antioxidative activity are time-consuming and cumbersome. They are also indirect processes that use biological material such as brain or liver microsome. This study therefore proposed a new method. Redoxpotential was determined using galvanic cell with or without the addition of various antioxidants or herbal extracts in zinc sulfate solution. The result was compared with the results from the TBA method and the peroxide value from sodium thiosulfate titration. All methods showed significant and dose-dependent enhancement of antioxidative activity by adding ascorbic acid, quercetin, ginseng, or gingko biloba extract. The result of redox potential using galvanic cell showed the smallest standard deviation and took the shortest time among the three methods. Therefore, the antioxidative potential of chemical substances and herbal extracts can be determined simply, directly and accurately in a short period of time using galvanic cell.

• 생약학회지
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• 제35권1호통권136호
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• pp.62-79
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• 2004

Cell-scattering is a phenotypic change easily observed in most epithelial cells treated with Hepatocyte Growth Factor /scatter Factor (HGF/SF) or phorbol esters (PKC-activators). Recent studies have shown the possibilities to use as therapeutic materials of HGF/SF or non tumor promoting phorbol esters for liver disease, cancer and AIDS. In this study, we tested a cell-scattering activity of 534 methanol extracts from plants inhabiting in Korean peninsula using the phenotype-based assay system. Nine Active extracts were detected : Daphne genkwa, Daphne kiusiana, and Aleurites fordii showed high activity (+++), Euphorbia sieboldiana and Rhodotypos scandens showed medium activity (++), Sambucus sieboldiana var. pendula, Catalpa bignonioides, Sambucus sieboldiana and Lycoris squamigera showed low activity (+). Furthermore, the effects of these active materials in the culture cells were investigated with biochemical studies.

• Restorative Dentistry and Endodontics
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• 제24권1호
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• pp.76-87
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• 1999

The effect of retrograde root-end filling materials(IRM, Super-EBA, Vitremer, MTA) on human periodontal ligament fibroblasts and osteoblasts was observed. The cell activities were evaluated by MTT assay, protein assay and alkaline phosphatase activity examination. The results as follows ; 1. After 24hrs culture, both E1 cells & PDL fibroblast adding root-end filling materials were suppressed cell activities but after 48hrs, cell activities were recovered. 2. Cell activity was lowest in Vitremer followed by IRM, MTA, Super-EBA. 3. Cell activity depression by Vitremer was not concerned with pH changes. 4. Protein synthesis by root-end filling materials were not significant difference in Both E1 cell & PDL fibroblasts but protein synthesis were a little increased by Super-EBA. 5. Alkaline phosphatase activity was increased in E1 cell by Super-EBA & MTA but was not significant differences in E1 cell by IRM & Vitremer. Alkaline phosphatase activity was a little depressed in PDL fibroblast by Vitremer. This findings suggest that these root-end filling materials may have important roles in promotion of PDL healing and consequently may be useful for clinical application in apical surgery.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2001년도 추계학술발표대회
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• pp.66-69
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• 2001

Previously we developed a CHO cell line (CHO-OTC1-A19) expressing the first two enzymes of urea cycle. This cell line showed higher ammonia removal activity and faster growth rate than the vector controlled CHO cells (CHO-neo-5). The purpose of this study was to develop a cell line with higher ammonia removal activity than the cell line developed previously. To accomplish this, we constructed stable CHO cell lines expressing the first three, the first four, or all five enzymes of urea cycle by the stable transfection method. We finally selected CHO-AL-19 cell line expressing the first three, the first four enzymes of the cycle with higher ammonia activity than CHO-OTC1-A19 and CHO-n대-5 cell lines: 40% and 15% higher than those of CHO-neo-5 and CHO-OTC1-A19 cell lines 72 hour after culture started, respectively. It also showed 44% and 10% higher cell viability than CHO-neo-5 and CHO- OTC1-A19 cell lines at higher cell density. In addition, CHO-AL-19 cells showed 45%-60% and about 20% lower ammonia concentration per cell than those of CHO-neo-% and CHO-OTC1-A19 cell lines, respectively. These results indicate that CHO-AL-19 could be used in the production of human therapeutic proteins with higher efficiency.

• 공업화학
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• 제9권6호
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• pp.857-863
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• 1998

Beer의 법칙을 이용하여 lysozyme-M. lysodeikticus cell의 용해반응속도 및 lysozyme의 활성을 측정할 수 있는 간단하고 새로운 실험방법을 제시하였다. M.lysodeikticus cell의 농도에 따라 용액의 UV 투과도를 측정하였으며 이것은 Beer의 법칙에 따르는 것으로 나타났다. 또한 용액 내의 lysozyme 농도 및 용해반응에 의해 생성되는 생성물은 UV 투과도에 전혀 영향을 미치지 않는 것으로 실험적으로 증명되었다. 따라서 lysozyme의 용해반응이 진행되는 동안 용액내에 존재하는 M. lysodeikticus cell의 농도는 UV-분광광도계를 이용하여 in-situ로 측정될 수 있었다. 이렇게 얻어진 M. lysodeikticus cell의 농도변화를 Michaelis-Menten식을 이용하여 lysozyme-M. lysodeikticus cell의 용해 반응속도 상수들을 결정하였다. 최대반응속도상수 $k_3$은 약 $0.1734sec^{-1}$로 나타났으며 Michaelis-Menten 상수는 약 $9.83{\times}10^{-6}M$으로 나타났다. Lysozyme의 용해반응속도가 활성에 의존하므로 이와 같은 측정을 통해 lysozyme의 활성도도 측정할 수 있었다.