• 제목/요약/키워드: inhibition layer

검색결과 235건 처리시간 0.03초

Pharmacodynamics of CKD-602 (Belotecan) in 3D Cultures of Human Colorectal Carcinoma Cells

  • Lee Sin-Hyung;Al-Abd Ahmed M.;Park Jong-Kook;Cha Jung-Ho;Ahn Soon-Kil;Kim Joon-Kyum;Kuh Hyo-Jeong
    • Biomolecules & Therapeutics
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    • 제14권2호
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    • pp.90-95
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    • 2006
  • CKD-602 exerts its antitumor effect via inhibition of topoisomerase I in cancer cells. Multicellular spheroid (MCS) and Multicellular layers (MCLs) are known as in vitro 3-dimensional models which closely represent tumor conditions in vivo. In order to investigate the potential of CKD-602 against human colorectal tumors, we evaluated the anti-proliferative activity and penetration ability of CKD-602 in MCS and MCL cultures of DLD-l human colorectal cancer cells, respectively. The maximum effects($E_{max}$) induced by CKD-602 were significantly lower in MCS compared to monolayers (48% vs 92%). With prolonged drug exposure, the $IC_{50's}$ of CKD-602 decreased to $23.5{\pm}1.0nM$ in monolayers after 24 h exposure and $42.3{\pm}1.7nM$ in MCS after 6 days, respectively. However, no further increase in effect was observed for exposure time longer than growth doubling time (Td) in both cultures. Activity of CKD-602 was significantly reduced after penetration through MCL and also with cell-free insert membrane. In conclusion, CKD-602 showed significantly decreased anti-proliferative activity in 3D cultures (MCS) of human colorectal cancer cells. Tumor penetration of CKD-602 could not be determined due to loss of activity after penetration through cell free insert membrane, which warrants further evaluation using a modified model.

Anti-Melanogenic Potentials of Nanoparticles from Calli of Resveratrol-Enriched Rice against UVB-Induced Hyperpigmentation in Guinea Pig Skin

  • Lee, Taek Hwan;Kang, Ji Hee;Seo, Jae Ok;Baek, So-Hyeon;Moh, Sang Hyun;Chae, Jae Kyoung;Park, Yong Un;Ko, Young Tag;Kim, Sun Yeou
    • Biomolecules & Therapeutics
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    • 제24권1호
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    • pp.85-93
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    • 2016
  • We already reported that genetically engineered resveratrol-enriched rice (RR) showed to down-regulate skin melanogenesis. To be developed to increase the bioactivity of RR using calli from plants, RR was adopted for mass production using plant tissue culture technologies. In addition, high-pressure homogenization (HPH) was used to increase the biocompatibility and penetration of the calli from RR into the skin. We aimed to develop anti-melanogenic agents incorporating calli of RR (cRR) and nanoparticles by high-pressure homogenization, examining the synergistic effects on the inhibition of UVB-induced hyperpigmentation. Depigmentation was observed following topical application of micro-cRR, nano-calli of normal rice (cNR), and nano-cRR to ultraviolet B (UVB)-stimulated hyperpigmented guinea pig dorsal skin. Colorimetric analysis, tyrosinase immunostaining, and Fontana-Masson staining for UVB-promoted melanin were performed. Nano-cRR inhibited changes in the melanin color index caused by UVB-promoted hyperpigmentation, and demonstrated stronger anti-melanogenic potential than micro-cRR. In epidermal skin, nano-cRR repressed UVB-promoted melanin granules, thereby suppressing hyperpigmentation. The UVB-enhanced, highly expressed tyrosinase in the basal layer of the epidermis was inhibited by nano-cRR more prominently than by micro-cRR and nano-cNR. The anti-melanogenic potency of nano-cRR also depended on pH and particle size. Nano-cRR shows promising potential to regulate skin pigmentation following UVB exposure.

Surface Oxidation of High Strength Automotive Steels during Continuous Annealing, and the Influence of Trace Elements of P,B, and Sb

  • Sohn, Il-Ryoung;Park, Joong-Chul;Kim, Jong-Sang
    • Corrosion Science and Technology
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    • 제9권6호
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    • pp.259-264
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    • 2010
  • In continuous hot dip galvanizing process, oxide formation on steel surface has an influence on Zn wetting. High strength automotive steel contains high amount of Si and Mn, where Si-Mn composite oxides such as $Mn_2SiO_4$ or $MnSiO_3$ covers the surface after annealing. Zn wetting depends on how the aluminothermia reaction can reduce the Mn-Si composite oxides and then form inhibition layer such as $Fe_2Al_5$ on the steel surface. The outward diffusion of metallic ions such as $Mn^{2+}$, $Si^{2+}$ in the steel matrix is very important factor for the formation of the surface oxides on the steel surface. The surface state and grain boundaries provide an important role for the diffusion and the surface oxide reactions. Some elements such as P, Sb, and B have a strong affinity for the interface precipitation, and it influence the diffusivity of metallic ions on grain boundaries. B oxide forms very rapildly on the steel surface during the annealing, and this promote complex oxides with $SiO_2$ or MnO. P has inter-reacted with other elements on the grain boundaries and influence the diffusion through on them. Small addition of Sb could suppress the decarburization from steel surface and retards the formation of internal and external selective oxides on the steel surface. Interface control by the trace elements such as Sb could be available to improve the Zn wettability during the hot dip galvanizing.

Agarwood Inhibits Histamine Release from Rat Mast Cells and Reduces Scratching Behavior in Mice -Effect of Agarwood on Histamine Release and Scratching Behavior-

  • Inoue, Eiji;Shimizu, Yasuharu;Masui, Ryo;Tsubonoya, Tomoe;Hayakawa, Tomomi;Sudoh, Keiichi
    • 대한약침학회지
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    • 제19권3호
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    • pp.239-245
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    • 2016
  • Objectives: This study was conducted to clarify the effects of agarwood on histamine release from mast cells in rats and on the scratching behaviors in mice. Methods: Histamine release from rat mast cells induced by compound 48/80 or concanavalin A (Con A) and compound 48/80-induced scratching behavior in mice were examined to investigate the effects of agarwood. The hyaluronidase activity and the 3',5'-cyclic adenosine monophosphate (cAMP) levels in mast cells were examined to investigate the mechanisms for the inhibition of histamine release. The correlation between the inhibitory effects of agarwood on histamine release and the content of its typical ingredients, a 2-(2-phenylethyl)chromone derivatives, was analyzed using thin-layer chromatography. Results: Agarwood showed an inhibitory effect on mast-cell histamine release induced by compound 48/80 or Con A without any effect on hyaluronidase activity; this effect involves an increase in the cAMP levels in mast cells. Oral administration of agarwood showed an inhibitory effect on compound 48/80-induced scratching behavior in mice. The inhibitory effects of agarwood on histamine release were quite different, depending on the area where the agarwood was produced, its quality, and its market price. No correlation was found between the inhibitory effects of agarwood on histamine release and the typical ingredients of agarwood, which are 2-(2-phenylethyl)chromone derivatives. Conclusion: These results show that agarwood inhibits histamine release from mast cells partially through an increase in the cAMP levels in cells. We suggest that some active ingredients of agarwood must be effective on oral intake and that agarwood can be used to treat patients with a number of conditions, including urticaria, atopic dermatitis, and bronchial asthma, in which an increase in histamine release occurs. Differences in the pharmacological effects of this crude drug among markets may provide important information for the quality control of this herbal medicine.

율피추출물의 사람 비만세포주 사이토카인 발현 억제 효과 (Inhibitory Effects of Chestnut Inner Shell Cytokine Production from Human Mast Cell Line)

  • 전동하;장영아;김희영;김수진;김진철;김세현;권대준;한상익;이진태
    • 대한본초학회지
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    • 제28권2호
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    • pp.55-60
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    • 2013
  • Objectives : Atopic dermatitis (AD) is a chronic inflammatory skin disease characterized by eczematous inflammtion of the skin. The chestnut inner shell extracts (CI) has been used as a cosmetic material for a long time in Korea. However, the precise anti-allergy effects of CI have yet to be clearly elucidated. In this study, we attempted to evaluate the effect of CI on mast cell-mediated allergy inflammation. Methods : To find the anti-allergy and inflammatory effect of CI, we investigated the inhibitory effect of CI on the production of inflammatory mediators using by enzyme-linked immunosorbent assay in phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore (A23187) stimulated-human mast cell (HMC-1). Results : In this study, we found that CI did not show cytotoxic effect at up to 10 ug/ml on HMC-1. CI inhibited the production of tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-6 and IL-8 in stimulated HMC-1. Maximal rate of TNF-${\alpha}$, IL-6 and IL-8 inhibition by CI (10 ug/ml) were about 47.6%, 44.1% and 22.5% respectively. In addition, we showed that Fr.3 isolated from n-Butyl alcohol layer of CI attenuated the production of TNF-${\alpha}$, IL-6 and IL-8 in HMC-1. Conclusion : Taken together, the findings of this study provide us with a novel insight action of CI as a potential molecule for use in the treatment of allergic inflammation diseases.

플랜트팜용 3원계 (Zn-Al-Mg) 합금도금 강판의 국부손상에 따른 부식 메커니즘 (Corrosion Mechanism According to Localized Damage of Zn-Al-Mg Alloy Coated Steel Sheet Used in Plant Farm)

  • 박진성;이재원;김성진
    • Corrosion Science and Technology
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    • 제22권2호
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    • pp.123-130
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    • 2023
  • This study aimed to evaluate corrosion resistance of steel coated with GI and Zn-Al-Mg alloy using cyclic corrosion test (CCT) with electrochemical polarization and impedance measurements. Results showed that the Zn-Al-Mg alloy coated steel had a much higher corrosion rate than GI coated steel in early stages of corrosion. With prolonged immersion, however, the corrosion rate of the Zn-Al-Mg alloy coated steel greatly decreased, mainly owing to a significant decrease in the cathodic reduction reaction and an increase in polarization resistance at the surface. This was closely associated with the formation of protective corrosion products including Zn5(OH)8Cl2·H2O and Zn6Al2(OH)16CO3. Moreover, when the steel substrate was locally exposed due to mechanical damage, the kinetics of anodic dissolution from the coating layer and the formation of protective corrosion products on the surface of the Zn-Al-Mg alloy coated steel became much faster compared to the case of GI coated steel. This could provide a longer-lasting corrosion inhibition function for Zn-Al-Mg alloy coated steel used in plant farms.

포도나무 줄기혹병균에 대한 약용식물의 항균활성 및 병발생억제 (In vitro and In vivo Antimicrobial Activities of Medicinal Plants against Crown Gall in Grapevine)

  • 김은수;윤해근
    • 원예과학기술지
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    • 제34권4호
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    • pp.537-548
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    • 2016
  • 항암, 항산화, 항균 활성을 나타내는 9종의 약용식물을 이용하여 포도나무 줄기혹병의 억제효과를 조사하였다. 공시한 식물 중에서 개똥쑥(15mm), 맨드라미의 꽃(27mm)과 잎(13mm), 여주의 미성숙 열매(22mm), 상사화 꽃(7mm), 질경이의 꽃(14mm)과 종자(16mm), 초석잠의 뿌리(13mm), 복숭아 나무의 수지(10mm) 추출물 등이 줄기혹병균(Rhizobium vitis)에 대해 항균활성을 나타내었다. 항균활성의 분획물의 최소억제농도를 확인한 결과 개똥쑥, 맨드라미 잎, 여주 미성숙과 분획물은 각각 50,000배, 질경이 꽃 분획물은 10,000배 희석액이 최소억제농도(MIC)로 확인되었다. 개똥쑥, 맨드라미 꽃과 잎, 여주의 미성숙 열매 추출물의 항균활성물질을 column chromatography와 thin layer chromatography(TLC)를 통하여 분획하였다. 핵산/에틸아세테이트와 메탄올/클로로포름(20:80, v/v)으로 전개한 TLC 분석에서 개똥쑥 추출물에서는 Rf 0.36, 0.69, 0.75, 0.84, 0.94, 맨드라미 꽃 추출물은 Rf 0.96, 0.99, 맨드라미 잎 추출물은 Rf 0.92, 0.97, 여주의 미성숙열매 추출물은 Rf 0.85에서 항균 활성의 분획을 획득하였다. 개똥쑥, 맨드라미 잎, 여주 미성숙 열매 추출물을 물에 희석(500, 1,000, 2,000배)하고 온실에서 R.vitis를 접종한 '거봉' 식물체에 7일 간격으로 관수한 결과, 개똥쑥 희석액은 100%, 맨드라미 잎 추출물(500배 희석액)은 67%, 여주 미성숙 열매 추출물(500배 희석액)은 83.3%의 억제효과를 나타내었다. 이러한 연구 결과는 약용식물 추출물이 포도나무 줄기혹병을 방제할 수 있는 친환경 제제로서의 적용가능성을 제시한 것이라 할 수 있다.

천연물을 이용한 큰느타리 균사배양 및 Angiotensin Converting Enzyme 저해활성 (Mycelial Growth Using the Natural Product and Angiotensin Converting Enzyme Inhibition Activity of Pleurotus eryngii)

  • 강태수;정헌상;이명렬;박희정;조택상;지성택;신명근
    • 한국균학회지
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    • 제31권3호
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    • pp.175-180
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    • 2003
  • 새로운 건강기능성 식품소재를 개발하고자 현미, 가시오가피 및 인진쑥을 기질로 하여 큰느타리버섯 균사의 고체배양 조건을 검토하였으며, 배양산물의 성분분석 및 추출물의 ACE 저해 활성을 조사하였다. 가시오가피와 인진쑥을 현미배지에 첨가시 농도가 증가함에 따라 균사의 생육속도는 감소하였으며, 특히 가시오가피의 첨가가 인진쑥에 비해 큰느타리 균사의 생육에 미치는 영향이 컸다. 배양산물의 성분분석 결과, 수분함량은 $10.9{\sim}12.0%$ 범위이었고, 조단백질, 지질 및 섬유질은 현미배지에서 가장 높았으며, 무기질(칼슘, 칼륨 및 인) 함량은 가시오가피 첨가배지가 가장 높았다. 추출수율은 인진쑥 첨가배지가 4.80%로 가장 높았으며, 추출물의 pH는 현미배지가 pH 6.1로 가장 낮았다. 세가지 시료 추출물의 명도는 $85.8{\sim}87.1$ 범위이었고, 적색도는 현미와 가시오가피 첨가배지가 높았으며, 반면, 황색도는 인진쑥 첨가배지가 가장 높았다. 당 성분을 thin layer chromatography로 분석한 결과, 세가지 시료 모두 2개의 spot가 검출되었고, 이들은 각각 glucose와 maltose로 판단되었다. Angiotensin converting enzyme에 대한 저해율을 측정한 결과, 가시오가피 첨가배지가 시료농도 $0.2{\sim}1.0\;mg/ml$에서 가장 높은 활성을 나타내었다.

산란계 밀집지역의 산란저하성 질병에 관한 연구 (Studies of the egg drop laying diseases from the mass zone layer)

  • 이정원;엄성심;박인규;배정준;정동석;송희종
    • 한국동물위생학회지
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    • 제28권2호
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    • pp.121-146
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    • 2005
  • Newcastle disease (ND), infectious bronchitis (IB), low pathogenic avian Influenza (LPAI) and fowl typhoid (FT) have been known as egg drop laying diseases because of the serious layer damage from mass zone layer. In this study, such egg drop laying diseases were investigated. To access this study, we peformed to evaluate antibody titers in serum and isolated bacteria and virus from organs and feces on May, July and September in 2003. The distribution of ND from January to May, IB and LPAI from October to February of the next year, and FT from March to September were inspected by the question survey in 21 farms. ND revealed to be positive rates of 490 to 474 $(96.7\%)$ in May, 510 to 506 $(99.2\%)$ in July and 510 to 510 $(100\%)$ in September with hemagglutination inhibition (HI) test. The mean antibody titers were 10.2, 9.9 and 10.2, respectively. With regard to IB, 484 out of 490 samples $(98.7\%)$ in May, 508 of 510 $(99.6\%)$ in July and 509 of 510 $(99.8\%)$ in September showed positive results and the mean antibody titers were gradually increased with 8.2, 9.0 and 9.4, respectively. According to HI test of LPAI, the positive results were shown in 442 of 480 $(92.1\%)$, 394 of 494 $(79.8\%)$ and 402 of 483 $(83.2\%)$ in May, July and September, respectively The mean antibody titers were decreased with 4.6, 4.3 and 4.0. The distribution of LPAI also elicited the positive rates of 480 to 475 $(99.0\%)$ in May, 494 to 485$(98.2\%)$ in July, 483 to 472 $(97.7\%)$ in September as determined by ELISA and the mean S/P ratio were 2.319, 2.557 and 2.380, respectively. Compared ELISA results with HI test of LPAI the positive results were 480 to 422 $(92.1\%),\;475(99.0\%),\;494\;to\;394 (79.8\%),\;485 (98.2\%)\;and\;483\;to\;402(83.2\%),\;472(97.7\%)$. Therefore, the positive rate determined by ELISA was higher than that of HI test with 6.9, 18.4 and $14.5\%$, respectively. When performed RT-PCR for ND using organ and feces samples, the pathotypes were detected $5(15.6\%)\;in\;May,\; 2(5.3\%) in\;July,\;2(7.1\%)$ in September but there is no samples showing positive band for LPAI. In attempt to isolate Salmonella gallinarum, bacteria were obtained from 4 cases (12.5%) in May, 9 (23.6%) in July, 5 (17.8%) in September. Thus the highest rate for isolation revealed to be shown in July When evaluated the antimicrobial susceptibility to 18 isolated strains of 5. gallinarum, bacteria were sensitive to trimethoprim/sulfamethox$(61.1\%),\;kanamycin\;(55.5\%),\;ampicillin\;(55.5\%)$ and amoxacillin/clavulanic acid $(55.5\%)$, cephalothin $(50.0\%)$, but resistant to penicillin $(88.9\%)$, streptomycin $(88.9\%)$, erythromycin $(83_4\%)$ and tetracycline $(61.1\%)$. According to HI test of ND and LPAI using captured 164 wild Korean tree sparrows (Passer nontanus), the positive rates were $47.6\%\;and\;57.3\%$, and the mean HI titers were 5.32 and 4.02, respectively. 71 $(43.2\%)\;and\;58(35.3\%)$ in captured sparrows also showed more than 4 titers for HI test to ND and LPAI, respectively However, the attempt for isolation of viruses failed in all samples.

Chlorhexidine 처리가 상아질 접착제의 미세인장결합강도에 미치는 영향 (EFFECT OF CHLORHEXIDINE ON MICROTENSILE BOND STRENGTH OF DENTIN BONDING SYSTEMS)

  • 오은화;최경규;김종률;박상진
    • Restorative Dentistry and Endodontics
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    • 제33권2호
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    • pp.148-161
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    • 2008
  • 본 연구는 상아질 혼성층의 교원섬유를 가수분해하는 효소인 MMPs (Matrix metalloproteinses)의 억제제로 알려진 chlorhexidine (CHX)을 적용 후 결합강도를 측정하였으며, 이를 각각 열순환 처리 후 결합강도를 측정하였다. 또한 주사전자현미경으로 접착계면에서의 파괴 양상을 비교 분석하였다. 우식이 없는 발거한 32개의 제3대구치의 교합면 상아질을 노출시키고 GI그룹에서는 dentin conditioner를 처리 후 2% chlorhexidine을 적용시키고, 산부식 접착제 그룹에서는 인산 산부식을 시행하고 2% chlorhexidine을 적용 후 3단계 산부식형 상아질 접착제 (Scotchbond Multipurpose, SM), 2단계 산부식형 상아질 접착제 (Single Bond, SB)를 도포하고, 자가부식 접착제 그룹에서는 2% chlorhexidine 적용 후 자가부식 상아질 접착제 (Clearfil Tri-S, TS)를 도포한다. 이후 복합 레진 (Z-250)과 GI (Fuji-II LC)를 충전한 시편을 $1\;mm^2$의 단면을 갖는 beam으로 제작하여 열순환 하지 않거나, 10,000회 열순환 ($5\;{\sim}\;55^{\circ}C$)하였다. Universal testing machine (EZ-test; Shimadzu, Japan)에서 cross head speed 1 mm/min로 인장력을 가하여, 미세인장결합강도를 측정하였다. 실험 결과는 유의수준 0.05 level에서 two-way ANOVA를 이용하여 통계분석하였다. 그 후 파절된 시편의 파괴 양상을 현미경 (SEM)으로 관찰하여 다음과 같은 결론을 얻었다; 1. 2% CHX을 적용한 모든 실험군에서 상아질과의 미세인장결합강도가 증가하였고, 열순환은 상아질과의 미세인장결합강도를 감소시켰다 (P > 0.05). 2. CHX 적용 후 열순환 한 군은 CHX을 적용하지 않고 열순환한 군에 비하여 상아질과의 미세인장결합강도가 높았으며, 특히 GI와 TS군에서 유의한 차이를 나타내었다 (P < 0.05). 3. 파괴 양상 분석 결과, 혼성층에서의 접착성 파괴를 보이며, CHX을 적용하면 혼성층 기저부에서 상부로 파괴 부위가 옮겨가는 양상을 나타내었다. 이상의 연구 결과를 토대로, MMPs 억제제인 2% CHX은 글래스 아이오노머 시멘트와 상아질 접착제의 초기 미세인장결합강도에는 영향을 미치지 않으며, CHX 적용이 접착내구성을 유지하는데 도움이 되었다.