• Title/Summary/Keyword: $IC_{I}$

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Antiplatelet Activity of 2-(4-Cyanophenyl) amino-1,4-naphthalenedione-3-pyridinium perchlorate (PQ5) (2-(4-시아노페닐) 아미노 -1,4-나프탈렌디온-3-피리디니움 퍼클로레이트 (PQ5)의 항혈소판작용)

  • 김도희;이수환;최소연;문창현;문창현;김대경;유충규
    • YAKHAK HOEJI
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    • v.43 no.6
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    • pp.809-817
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    • 1999
  • The effect of 2-(4-cyanophenyl)amino-1,4-naphthalenedione-3-pyridinium perchlorate (PQ5) on pla-telet aggregation and its action mechanisms were investigated with rat platelet. PQ5 inhibited the platelet aggregation induced by collagen ($6{\;}{\mu\textrm{g}}/ml$), thrombin (0.4 U/ml) and A23187 ($3{\mu}M$) in concentration-dependent manner with $IC_{50}$ values of 5.50, 25.89 and $37.12{\;}{\mu}M$, respectively. PQ5 also significantly reduced the thromboxane $A_2$ (TXA2) formation in a concentration dependent manner. The collagen-induced arachidonic acid (AA) release in [-3H]-AA incorporated platelet, an indication of the phospholipase $A_2$ activity, was decreased by PQ5 pretreatment PQ5 significantly inhibited the activity of thormboxane synthase only at high concentration ($100{\mu}M$), but did not affect the cyclooxygenase activity at all. Collagen-induced ATP release was significantly reduced by PQ5. Calcium-induced platelet aggregation experiment suggests that the elevation of intracellular free $Ca^{2+}$ concentration ($[Ca^{2+}]_i$) by collagen stimulation is decreased by the pretreatment of PQ5, which is due to the inhibition of calcium release from intracellular store and influx from outside of the cell. PQ5 did not showed the effect of anticoagulation as prothrombin time (PT) or activated partial thromboplastin time (APTT). Form these results, it is suggested that PQ5 exerts its antiplatelet activity through the inhibition of the intracellular $Ca^{2+}$ mobilization and the decrease of the $TXA_2$ synthesis.

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Anti-Diabetic and Anti-Inflammatory Effects of Green and Red Kohlrabi Cultivars (Brassica oleracea var. gongylodes)

  • Jung, Hyun Ah;Karki, Subash;Ehom, Na-Yeon;Yoon, Mi-Hee;Kim, Eon Ji;Choi, Jae Sue
    • Preventive Nutrition and Food Science
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    • v.19 no.4
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    • pp.281-290
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    • 2014
  • The aim of the present study was to evaluate the anti-diabetic, anti-inflammatory, antioxidant potential, and total phenolic content (TPC) of green and red kohlrabi cultivars. Anti-diabetic and anti-inflammatory activities were evaluated via protein tyrosine phosphatase (PTP1B) and rat lens aldose reductase inhibitory assays and cell-based lipopolysaccharide (LPS)-induced nitric oxide (NO) inhibitory assays in RAW 264.7 murine macrophages. In addition, scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical, and peroxynitrite ($ONOO^-$) were used to evaluate antioxidant potential and TPC was selected to assess phytochemical characteristics. Between the two kohlrabi cultivars, red kohlrabi (RK) had two times more TPC than green kohlrabi (GK) and showed significant antioxidant effects in DPPH, ABTS, and $ONOO^-$ scavenging assays. Likewise, methanol (MeOH) extracts of RK and GK inhibited LPS-induced NO production in a dose dependent manner that was further clarified by suppression of iNOS and COX-2 protein production. The MeOH extracts of RK and GK exhibited potent inhibitory activities against PTP1B with the corresponding $IC_{50}$ values of $207{\pm}3.48$ and $287{\pm}3.22{\mu}g/mL$, respectively. Interestingly, the RK MeOH extract exhibited significantly stronger anti-inflammatory, anti-diabetic, and antioxidant effects than that of GK MeOH extract. As a result, our study establishes that RK extract with a higher TPC might be useful as a potent anti-diabetic, antioxidant, and anti-inflammatory agent.

Separation and Purification of Angiotensin Converting Enzyme Inhibitory Peptides derived from Goat's Milk Whey Hydrolysates (산양유 Whey로부터 ACE 억제 Peptide의 분리 및 정제)

  • Lee, K.J.;Kim, S.B.;Ryu, J.S.;Shin, H.S.;Lim, J.W.
    • Journal of Animal Science and Technology
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    • v.47 no.1
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    • pp.83-90
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    • 2005
  • ACE-inhibitory peptides derived from goat's whey hydrolyzed by various proteolytic enzymes were separated and purified for antihypertension materials. The highest ACE-inhibitory activity of goat's whey hydrolysates was 85.5 % by pepsin for 72 hrs. Also the highest ACE-inhibitory activity of goat's whey hydrolysates was F-4 by pepsin for 72 hrs by Sephadex G-25 gel chromatograms. F-4e and F-4ed from F-4 by RP-HPLC to first and second purification were the highest in ACE-inhibitory activity, respectively. The most abundant amino acid was leucine(I 8.54 %) in F-4ed of ACE-inhibitory peptides after second purification. Amino acid sequence of F-4ed of ACE-inhibitory peptides showed Leu-Lys-Asp-Tyr-Gly-GlyVal- Ser-Leu and Leu-Gly-Asp-Gly-Ala-Gly- Asp-Val-Ala-Phe. $IC_{50}$ calibrated in peptic hydrolysates(72 hrs), F-4, F-4e and F-4ed from goat's whey hydrolysates by pepsin for 72 hrs were 33.93, 28.75, 11.74 and 1.09 mg/ml, respectively. From the results of this experiment, goat's whey hydrolysate by pepsin was shown to have ACE-inhibitory activity.

Pretreatment for Recycling of Domestic Aluminum Dross (국내 알루미늄 드로스의 처리공정에 관한 연구)

  • 박형규;이후인;김준수;윤의박
    • Resources Recycling
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    • v.5 no.1
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    • pp.14-20
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    • 1996
  • For recycl~ng alumhx~rn dross, the cbaraclcrislics of dross and ils reutll~zalin~af~te r plocsssing should he considered. Nurn~llumd ross was classified according to iB sire in this shldy. Tbe dross larger Illan 3001~1w as directly re-meltcd to recover aluminum, and the s~nallerd ~ossw as leachcd and riln~tedl o scparalc 111s eri~lerls alt and to oxidize the rnelals contained in the dross. As a rcwlt, amount of the dross uscd lo be dircarded ahcr processing could hc reduced Also, lhc chem~cal culnposit~ons of a domzstic alumlnum dross and the changes in con~posilii~ndsu ring processings were investigated. and Cound that most mctaU'ic aluminum in the dross was changed inlu alu~n~numox ide lhruugli the roasting. Tile processed dross would he ulillzed for malerials such as alumina, alumma cemenl or tilcs.

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Enantiospecific separation in biphasic Membrane Reactors

  • Giorno, Lidietta
    • Proceedings of the Membrane Society of Korea Conference
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    • 1998.10a
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    • pp.15-18
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    • 1998
  • Membrane reactors are systems which combine a chemical reactor with a membrane separation process allowing to carry out simultaneously conversion and product separation. The catalyst can be immobilized on the membrane or simply compartmentalized in a reaction space by the membrane. Membrane reactors are today investigated to produce optically pure isomers and/or resolve racemic mixture of enantiomers. The interest towards these systems is due to the increasing demand of enantiomerically pure compounds to be used in the pharmaceutical, food, and agrochemical industries. In fact, enantiomers can have different biological activities, which often influence the efficacy or toxicity of the compound. On the basis of current literature there are basically two schemes on the use of membrane technology to produce enantiomers. In one case, the membrane itseft is intrinsically enantioselective: the membrane is the chiral system which selectively separates the wanted isomer on the basis of its conformation. In the other, a kinetic resolution using an enantiospecific biocatalyst is combined with a membrane separation process; the membrane separates the product from the substrate on the basis of their relative chemical properties (i.e. solubility). This kind of configuration is widely used to carry out kinetic resolutions of low water soluble substrams in biphasic membrane reactors [Giomo, 1995, 1997; Lopez, 1997]. These are systems where enzyme-loaded membranes promote reactions between two separate phases thanks to the properties of enzymes, such as lipases, to catalyse reactions at the org ic/aqueous interface; the two phases are maintained in contact and separated at the membrane level by operating at appropriate transmembrane pressure. A schematic representation of biphasic membrane reactor is shown in figure 1, while an example of enantiospecific reaction and product separation carried out with these systems is reported in figure 2.

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Antiplatelet Actions of 2-Bromo-3-(.3,5-tert-butyl-4-hydroxylphenyl)-1,4-naphthaleneflione (TPN2) (2-Bromo-3-(3,5-tert-butyl-4-hydroxylphenyl)-1,4-naphthalenedione (TPN2)의 항혈소판 작용)

  • 최소연;김민화;이수환;정이숙;백은주;유충규;문창현
    • Biomolecules & Therapeutics
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    • v.7 no.3
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    • pp.227-233
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    • 1999
  • The effects of 2-bromo-3-(3,5-tert-butyl-4-hydroxylphenyl)-1,4-naphthalenedione(TPN2), a synthetic vitamin K derivative, on platelet aggregation and its action mechanisms were investigated in rat platelet. TPN2 inhibited the platelet aggregation induced by collagen($10\mu\textrm{g}$/ml), thrombin(0.1 U/ml), A23187($10\mu\textrm{M}$) and arachidonic acid($100\mu\textrm{M}$) in concentration-dependent manner with $IC_{50}$ values of 6.5$\pm$1.3, 59.3$\pm$4.5, 13.0$\pm$2.37 and 2.9$\pm$$1.0\mu\textrm{M}$, respectively. Collagen-induced serotonin release was significantly reduced by TPN2. The elevation of intracellular free $Ca^{2+}$ concentration ([$Ca^{2+}$]i) by collagen stimulation was greatly decreased by the pretreatment of TPN2, which was due to the inhibition of calcium release from intracellular store and influx from outside of the cell. TPN2 also significantly reduced the thromboxane $A_2$($TXA_2$) formation in a concentration-dependent manner. The collagen-induced arachidonic acid (AA) release in [$^3H$]-AA incorporated platelet, an indicative of the phospholipase $A_2$ activity, was decreased by TPN2 pretreatment. TPN2 significantly inhibited the activity of thromboxane synthase, but did not affect the cyclooxygenase activity. From these results. it is suggested that TPN2 exert its antiplatelet activity through the inhibition of the intra-cellular $Ca^{2+}$ mobilization and the decrease of the $TXA_2$ synthesis.

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Inhibitory Effects of Flavonoids Isolated from Leaves of Petasites japonicus on $\beta$-Secretase (BACE1)

  • Song, Kyung-Sik;Choi, Sun-Ha;Hur, Jong-Moon;Park, Hyo-Jun;Yang, Eun-Ju;MookJung, In-Hee;Yi, Jung-Hyun;Jun, Mi-Ra
    • Food Science and Biotechnology
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    • v.17 no.6
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    • pp.1165-1170
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    • 2008
  • The deposition of the amyloid $\beta}$ ($A{\beta}$)-peptide following proteolytic processing of amyloid precursor protein (APP) by $\beta$-secretase (BACE1) and $\gamma$-secretase is critical feature in the progress of Alzheimer's disease (AD). Consequently, BACE1, a key enzyme in the production of $A{\beta}$, is a prime target for therapeutic intervention in AD. In the course of searching for BACE1 inhibitors from natural sources, the ethyl acetate fraction of Petasites japonicus showed potent inhibitory activity. Two BACE1 inhibitors quercetin (QC) and kaempferol 3-O-(6"-acetyl)-$\beta$-glucopyranoside (KAG) were isolated from P. japonicus by activity-guided purification. QC, in particular, non-competitively attenuated BACE1 activity with $IC_{50}$ value of $2.1{\times}10^{-6}\;M$ and $K_i$ value of $3.7{\times}10^{-6}\;M$. Both compounds exhibited less inhibition of $\alpha$-secreatase (TACE) and other serine proteases including chymotrypsin, trypsin, and elastase, suggesting that they ere relatively specific and selective inhibitors to BACE1. Furthermore, both compounds significantly reduced the extracellular $A{\beta}$ secretion in $APP_{695}$-transfected B103 cells.

Synthesis, Radiolabeling and Gastrin Releasing Peptide Receptor Binding Affinity of a Novel Bombesin Antagonist-Based Peptide, DOTA-Ala(SO3H)-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-NH2

  • Lim, Jae Cheong;Choi, Sang Mu;Cho, Eun Ha;Kim, Jin Joo
    • Journal of Radiation Industry
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    • v.7 no.2_3
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    • pp.127-134
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    • 2013
  • Bombesin receptors are overexpressed in many kinds of human tumors. In particular, the gastrin releasing peptide receptor (GRPR) which is also called bombesin receptor subtype 2, has been identified in prostate cancer. In the present study, we developed a bombesin antagonist-based $^{177}Lu$-labeled peptide, $^{177}Lu$-DOTA-$Ala(SO_3H)$-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-$NH_2$ (DOTA-sBBNA). DOTA-sBBNA was prepared using a solid phase synthesis method. It was labeled with $^{177}Lu$ by a high radiolabeling yield (>98%), and its Log P value was -2.05. The radiolabeled peptide was highly stable in serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-Bombesin on the PC-3 human prostate carcinoma cells revealed that the $IC_{50}$ value of the peptide was 6.76 nM indicating a highly nanomolar binding affinity for GRPR. These results suggest that $^{177}Lu$-DOTA-sBBNA can be a potential candidate for targeting prostate cancer, and further studies to evaluate its biological characteristics are needed.

Novel Bombesin Analogues Conjugated with DOTA-Ala(SO3H)-4 aminobenzoic acid and DOTA-Lys(glucose)-4 aminobenzoic acid: Synthesis, Radiolabeling, and Gastrin Releasing Peptide Receptor Binding Affinity

  • Lim, Jae Cheong;Choi, Sang Mu;Cho, Eun Ha;Kim, Jin Joo
    • Journal of Radiation Industry
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    • v.7 no.2_3
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    • pp.191-200
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    • 2013
  • In this study, a novel bombesin (BBN) analogues, DOTA-Ala($SO_3H$)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-sBBN) and DOTA-Lys(glucose)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-gluBBN), were synthesized and radiolabeled, and their binding affinities were evaluated. Peptides were prepared by a solid phase synthesis method and their purities were over 98%. DOTA is the chelating agent for $^{177}Lu$-labeling, and the DOTA-conjugated peptides were radiolabeled with $^{177}Lu$ by a high radiolabeling yield (>98%). The Log P values of DOTA-sBBN and DOTA-gluBBN were -2.20 and -2.79, respectively. 50.41% of $^{177}Lu$-DOTA-sBBN and 72.97% of $^{177}Lu$-DOTA-gluBBN were left undegraded by the serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-BBN on the PC-3 human prostate carcinoma cells revealed that 50% inhibitory concentration ($IC_{50}$) were 1.46 nM of DOTA-sBBN and 4.67 nM of DOTA-gluBBN indicating a highly nanomolar binding affinity for GRPR. Therefore, it is concluded that $^{177}Lu$-DOTA-sBBN and $^{177}Lu$-DOTA-gluBBN can be potential candidates as a targeting modality for the Gastrin-releasing peptide receptor (GRPR)-over-expressing tumors, and further studies to evaluate their biological and pharmacological characteristics are needed.

A Case Study on the Intensive Semester Operation of Online-based Project Learning Using Python : Focusing on S Women's University (파이썬을 활용한 온라인 기반 프로젝트의 집중학기제 운영사례 : S 여대를 중심으로)

  • Kyun, Suna;Jang, Jiyoung
    • Journal of Engineering Education Research
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    • v.24 no.5
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    • pp.3-14
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    • 2021
  • This study deals with the case of online-based project learning, which was designed for the purpose of university educational innovation and enhancing learners' competencies required by society, operated during the COVID-19 pandemic. The course was applied Python programming language, team-based project learning, and intensive course system, which is required by our society and companies in the era of the 4th industrial revolution. Also it was operated as a non-face-to-face online class, which would have been operated in an offline class if it had not been for Covid 19 pandemic, to explore the possibilities and educational effects of online learning. To do this, 32 university students participated in online-based project learning during 8 weeks, and then conducted a survey. The survey results were analyzed in terms of i) non-face-to-face online learning, ii) team-based project learning, and iii) application of the intensive course system. Results say that most of the learners were satisfied with the online learning, team-based project learning, and the intensive semester system applied in this course at a high level, and also they clearly presented the reasons. Thereby, it has been confirmed that the learners were already well aware of the pros and cons of each learning method. Based on these results, the implications were discussed.