• 제목/요약/키워드: 6-Propyl

검색결과 218건 처리시간 0.027초

HY251, a Novel Decahydrocyclopenta[a]indene Analog, Induces Apoptosis via tBid-Mediated Intrinsic Pathway in Human Ovarian Cancer PA-1 Cells

  • Suh, Hyewon;Choi, Ko-Woon;Kim, Myung Sic;Kim, Jeong Hyeon;Noh, Sun Young;Sung, Moon-Hee;Lee, Chul-Hoon
    • Journal of Microbiology and Biotechnology
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    • 제22권11호
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    • pp.1591-1595
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    • 2012
  • We previously isolated a novel compound, HY251, with the molecular structure of 3-propyl-2-vinyl-1,2,3,3a,3b,6,7,7a,8,8a-decahydrocyclopenta[a]indene-3,3a,7a,8a-tetraol from the roots of Aralia continentalis. The current study was designed to evaluate the detailed molecular mechanisms underlying the apoptotic induction by HY251 in human ovarian cancer PA-1 cells. TUNEL assay and Western blot analyses revealed an appreciable apoptotic induction in PA-1 cells treated with $60{\mu}M$ of HY251 for 24 h. This apoptotic induction was associated with caspase-8-dependent Bid cleavage, which in turn resulted in the formation of pro-apoptotic truncated Bid (tBid), and activation of caspase-9 and -3, as well as the cleavage of poly(ADP-ribose) polymerase (PARP). Moreover, we found that this death event was also associated with the significant up-regulation and activation of the p53 tumor-suppressor protein through phosphorylation at Ser15. Therefore, we suggest that HY251 may be a potent cancer chemotherapeutic candidate for the treatment of ovarian cancer.

Effects of 3,5,3'-triiodo-L-thyronine ($T^3$) on Growth of GR-transgenic Coho Salmon, Oncorhynchus Kitsutch

  • Kang, Duk-Young;Robert H. Devlin
    • 한국수정란이식학회:학술대회논문집
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    • 한국수정란이식학회 2002년도 국제심포지엄
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    • pp.101-101
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    • 2002
  • GH-transgenic coho salmon (Oncorhynchus kitsutch) juveniles in tGH*T$_3$and tGH*PTU were fed with the diets containing 1 ug/g fish of 3,5,3'-triiodo-L-thyronine (T$_3$) and 30 ug/g fish of 6-n-propyl-2- thiouracil (PTU), respectively, to assess the effect of these drugs on the change of physiological activity, growth and survival rate in comparison with normal transgenic (tGH*C) and nontransgenic coho salmon (Wild) for 90 days. Although the daily food intakes of all transgenic (tGH)-groups were higher than Wild, the amount was reduced by exogenous PTU supply. The fred efficiencies of tGH-groups were lower than Wild, but the efficiency was reduced both by T$_3$and PTU. The survival rate of tGH-group was significantly higher than that of Wild, but there was no significant difference among tGH-groups. Although the growth of tGH-coho salmon was faster than Wild. the growth rate of transgenic salmon was increased by exogenous T$_3$, but was reduced by PTU Plasma TT$_4$levels of tGH-groups was approximately 2-fold higher relative to Wild, but there were no difference of plasma TT$_4$levels among tGH-groups. plasma TT$_3$level or tGH-coho salmon was increased by exogenous T$_3$administration, but was reduced by exogenous PTU. In addition, although plasma GH levels of all tGH-groups were higher than that of Wild, the GH level in plasma of transgenic coho salmon was increased by exogenous T$_3$and reduced by exogenous PTU. In the meantime, the transgenic fishes also displayed head, jaw and opercular abnormalities typical of the offsets of this gene construct in coho salmon, indicating that some imbalance in growth processes has been induced. However, the abnormalities of transgenic coho salmon was reduced following exogenous PTU administration.

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토양중 Light Hydrocarbon의 용매추출에 미치는 계면활성제의 영향 (Effect of Surfactant on Solvent Extraction for Light Hydrocarbon from Soils)

  • Hwang, Keon-Joong;Atalay, Asmare
    • 한국환경보건학회지
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    • 제24권2호
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    • pp.74-79
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    • 1998
  • 본 실험은 light hydrocarbon에 오염된 토양을 용매 추출할 때 계면활성제의 영향을 평가하고자 6가지의 계면활성제 (Witbreak DPG-482, Witbreak DRA-22, Witcomul 4016, Witcolate SL-1, Adsee 799, Triton X-100)와 2가지 용매(물, 메타놀)를 대상으로 실험하였다. Light hydrocarbon으로는 benzene, toluene, ethyl bnzene, o-xylene, m-xylene, p-xylene, n-propyl benzene, 1,2,4-trimethyl benzene, 그리고 n-butyl benzene등 9가지를 대상으로 하였다. 계면활성제중 Adsee-799과 Witbreadk DRA-22가 토양중 light hydrocarbon의 물추출 효율을 다소 증가시키는 것으로 나타나고 있으며, 나머지 계면활성제는 효과가 없었다. 또한 물중의 계면활성제의 농도가 0.5%이하에서는 효과가 없는 것으로 나타나고 있으며, 계면활성제의 농도가 4%일때 평균 10.8%의 추출증가 효과가 있었다. 메타놀을 추출용매로 사용할 때에는 Witbread DPG-782와 Witbreak DRA-22가 약 10%의 추출증가 효과를 나타내고 있었다.

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폴리(스티렌-이소부틸렌-스티렌) 삼중블록 공중합체의 합성, 분석 및 혈액적합성 (Synthesis, Characterization and Haemocompatibility of Poly(styrene-b-isobutylene-b-styrene) Triblock Copolymers)

  • 렌핑;우이보;구원일;리슈신;마오징;샤오페이;리강
    • 폴리머
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    • 제35권1호
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    • pp.40-46
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    • 2011
  • The synthesis of well-defined poly(styrene-b-isobutylene-b-styrene) (SIBS) triblock copolymers was accomplished by cationic sequential block copolymerization of isobutylene (IB) with styrene (St) using 1,4-di(2-chloro-2-propyl) benzene (DCC) /$TiCl_4$/2,6-di-tert-butylpyridine(DtBP) as an initiating system in methyl chloride ($CH_3Cl$)/methylcyclohexane(MeChx) (50/50 v/v) solvent mixture at $-80^{\circ}C$. The triblock copolymers exhibited excellent thermoplastic and elastomeric characteristics. Tensile strengths and Shore hardness increased with increasing polystyrene (PS) content, while elongation at break decreased. The blood-compatibility of SIBS was assessed by SEM observation of the platelet adhesion, blood clotting time and haemolysis ratio. The haemolysis ratios were below 5% which met the medical materials standard. The platelet adhesion test further indicated that SIBS block copolymers had a good blood compatibility.

Development of a Quantitative Analytical Method for Determining the Concentration of Human Urinary Paraben by LC-MS/MS

  • Lee, Seung-Youl;Son, Eunjung;Kang, Jin-Young;Lee, Hee-Seok;Shin, Min-Ki;Nam, Hye-Seon;Kim, Sang-Yub;Jang, Young-Mi;Rhee, Gyu-Seek
    • Bulletin of the Korean Chemical Society
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    • 제34권4호
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    • pp.1131-1136
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    • 2013
  • Parabens, the esters of p-hydroxybenzoic acid, have been widely used as antimicrobial preservatives in cosmetic products, drugs, and processed foods and beverages. However, some parabens have been shown to have weak estrogenic effects through in vivo and in vitro studies. Because such widespread use has raised concerns about the potential human health risks associated with exposure to parabens, we developed a simultaneous analytical method to quantify 4 parabens (methyl, ethyl, propyl, and butyl) in human urine, by using solid-phase extraction and high-performance liquid chromatography coupled with triple quadrupole mass spectrometry. This method showed good specificity, linearity ($R^2$ > 0.999), accuracy (92.2-112.4%), precision (0.9-9.6%, CV), and recovery (95.7-102.0%). The LOQs for the 4 parabens were 1.0, 0.5, 0.2, and 0.5 ng/mL, respectively. This method could be used for quick and accurate analysis of a large number of human samples in epidemiological studies to assess the prevalence of human exposure to parabens.

누룩에 따른 약주의 품질 평가 (The Quality of Yakju be brewed from many kind of Nuruk)

  • 이미경;이성우;배상면
    • 동아시아식생활학회지
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    • 제1권1호
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    • pp.99-111
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    • 1991
  • In each nuruk using today, effect of pH on glucoamylase activity and viable cell count of yeast and bacteria was measured. Common components during fermentation, alcohol, acetaldehyde and acetone, amino acid composition, and total sugars and mineral content were determined in yakju(korean wine) brewed from different ingredients and by different methods. Results are summarized as follows ; 1. The lower the pH, the lower the glucoamylase activity in JK, BK, JK-S BK-S and JN. But the higher the glucoamylase activity ratio in Koji and KN. 2. Yeast and bacteria cell count could not determined in nuruk inoculated of seed. In JK, BK and JN, yeast cell count was 50${\times}$104∼80${\times}$104, bacteria cell count was 5${\times}$106∼24${\times}$106. 3. In yakju during fermentation, pH was higher in RU, total acidity content was higher in ST-N, ST-K, RU and ST-RUPO and alcohol content was lower in RUPO and ST-RUPO. 4. Ethanol and acetaldehyde content were highest in dukyunju. Trace amount of acetone was determined only in ST-K, RUPO and ST-RUPO . n-Propyl alcohol content was higher in ST-K, ST-RUPO and ST-N, iso-butyl alcohol content was higher in L-RUPO, Dukyunju and Songyupju and iso-amyl alcohol content was higher in Songyupju, RU, L-RUPO and Dukyunju. 5. In amino acids composition of each yakju, Pro, Ala and Val content was higher than other amino acids. Total amino acids content was the highest in Dukyunju and second highest in ST-N, NH3 was higher in ST-N, Dukyunju, RUPO than other samples. 6. Total sugars content was the highest in ST-N and second highest in RU. 7. P, K and Mg content were higher in Dukyunju and ST-N than in other samples. In Dukyunju, Ca and P ratio was 0.075 because of low Ca content and high P content.

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KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure

  • Lee, Jeong Hyun;Seo, Ho Won;Ryu, Jae Yong;Lim, Chae Jo;Yi, Kyu Yang;Oh, Kwang-Seok;Lee, Byung Ho
    • Biomolecules & Therapeutics
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    • 제28권5호
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    • pp.482-489
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    • 2020
  • G protein-coupled receptor kinase 5 (GRK5) has been considered as a potential target for the treatment of heart failure as it has been reported to be an important regulator of pathological cardiac hypertrophy. To discover novel scaffolds that selectively inhibit GRK5, we have identified a novel small molecule inhibitor of GRK5, KR-39038 [7-((3-((4-((3-aminopropyl)amino)butyl)amino)propyl)amino)-2-(2-chlorophenyl)-6-fluoroquinazolin-4(3H)-one]. KR-39038 exhibited potent inhibitory activity (IC50 value=0.02 µM) against GRK5 and significantly inhibited angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes. In the pressure overload-induced cardiac hypertrophy mouse model, the daily oral administration of KR-39038 (30 mg/kg) for 14 days showed a 43% reduction in the left ventricular weight. Besides, KR-39038 treatment (10 and 30 mg/kg/day, p.o.) showed significant preservation of cardiac function and attenuation of myocardial remodeling in a rat model of chronic heart failure following coronary artery ligation. These results suggest that potent GRK5 inhibitor could effectively attenuate both cardiac hypertrophy and dysfunction in experimental heart failure, and KR-39038 may be useful as an effective GRK5 inhibitor for pharmaceutical applications.

DCFH-DA를 이용한 항산화제의 세포내 oxidative stress 억제 효과에 관한 연구 (The anti-oxidative stress effect of antioxidants in the cell using DCFH-DA)

  • 유영근;신미희;최종완
    • 대한화장품학회지
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    • 제28권1호
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    • pp.42-57
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    • 2002
  • 본 연구는 널리 알려져 있는 항산화제들의 세포 수준에서의 anti-oxidative stress 효과 및 그 기작을 알아보기 위한 연구이다. 연구에 사용한 항산화제로는 지용성인 retinol, $\alpha$-tocopherol, propyl gallate(PG) 및 butylated hydroxy toluene(BHT)과 수용성인 ascorbic acid, $\alpha$-glucosyl rutin 및 green tea extract를 사용하였으며 이들 항산화제들의 시간별 세포 생존율을 NR assay 로 측정한 후 적정 농도에서 DCFH-DA(2', 7'-dichlorofluorescin-diacetate) 를 이용하여 항산화제들의 anti-oxidative stress 억제 효과를 시간별로 측정하였다. 또한 이들 항산화제의 항산화 기작을 알아보기 위하여 NBT(Nitro-blue-tetrazolium) 및 DPPH(Diphenyl-picry-hydrazl)도 병행하여 실시하였다. Anti-oxidative stress 실험에서 지용성 항산화제들은 전반적으로 수용성 항산화제에 비하여 세포에 대한 독성이 상대적으로 강하여 retinol 의 경우에는 0.01%에서 oxidative stress 억제 효과를 관할할 수 있었으며 1 시간경과 후 측정시 53.1%의 억제 효과를 보여 주었다. PG 의 경우에는 0.1%에서 2 시간 경과 후 측정시 50%의 oxidative stress 억제 효과를 보여주었다. 수용성 항산화제인 green tea extract 및 $\alpha$-glucosyl rutin의 경우에는 1%에서 1시간 경과 후 측정시 각 각 51.6% 및 69.7%의 oxidative stress 억제 효과를 관찰할 수 있었다. 또한 시료처리 후 자외선 조사시 oxidative stress 억제 효과의 경우 수용성 항산화제인 ascorbic acid, $\alpha$-glucosyl rutin 및 green tea extract 와 지용성 항산화제 중에서는 $\delta$-tocopherol 에서만 oxidative stress 억제 효과가 관찰되었으나 자외선을 조사 하지 않았을 때 보다 약 20%-40%까지 억제 효과가 감소되었다. 그리고 PG 및 retinol 의 경우에는 자외선 조사시 독성이 증가하여 oxidative stress 억제 효과를 측정할 수 없었다. NBT실험에서 $\alpha$-glucosyl rutin, $\alpha$-tocopherol 및 PG 1%에서 70%이상의 superoxide anion 생성 억제 효과를 보였으며 DPPH 실험에서는 ascorbic acid 와 PG 1%에서 98%의 hydroxyl radical 생성 억제 효과를 보여 주었다. 본 실험을 통하여 BHT 를 제외하고 전반적으로 세포 수준에서의 oxidative stress 에 대한 억제 효과를 확인해 볼 수 있었으며 특히 수용성 항산화제들에서 두드러진 효과를 보여 주었다.

Influence of Alkali and Silane Treatment on the Physico-Mechanical Properties of Grewia serrulata Fibres

  • JAIN, Bhupesh;MALLYA, Ravindra;NAYAK, Suhas Yeshwant;HECKADKA, Srinivas Shenoy;PRABHU, Shrinivasa;MAHESHA, G.T.;SANCHETI, Gaurav
    • Journal of the Korean Wood Science and Technology
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    • 제50권5호
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    • pp.325-337
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    • 2022
  • Grewia serrulata fibres were chemically treated with 3%, 6%, and 9% NaOH for the duration of 4 h. Additionally, the NaOH-treated fibres were also treated with 3 - (trimethoxysilyl) propyl methacrylate (silane). Properties such as density and tensile strength of the treated fibres were compared against the untreated fibres. The highest density was obtained in the case of 9% NaOH + silane treated fibres, which was 26.47% higher than untreated fibres, implying effective removal of hemicellulose. Likewise, the highest tensile strength was also obtained in the case of 9% NaOH + silane treated fibres. The increment observed in the tensile strength of the natural fibres was related to the removal of impurities, hemicellulose, and stress-raisers as well as deposition over the fibre surface that smoothed it. These observations were further validated by estimating changes in chemical constituents due to chemical treatment along with characterization techniques such as scanning electron microscopy and thermogravimetric analysis.

새로운 5,6-dihydro-2-trifluoromethyl-1,4-oxathiincarboxanilide 유도체의 항균활성에 미치는 치환-phenylcarbamoyl group의 영향 (Influence of substituted phenylcarbamoyl group on the fungicidal activites of a new 5,6-dihydro-2-trifluoromethyl-1,4-oxathiincarboxanilide derivatives)

  • 성낙도;유성재;남기달;장기혁;한호규
    • 농약과학회지
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    • 제2권3호
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    • pp.64-69
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    • 1998
  • 기질(S) 화합물로 30종의 5,6-dihydro-2-trifluoromethyl-1,4-oxathiin carboxanilide 유도체들을 합성하고 벼 잎집무늬 마름병균(Rhizoctonia solani)과 밀 붉은 녹병균(Puccinia recondita)에 대한 항균활성(in vivo) 값($pI_{50}$)을 측정하였다. (S)는 잘록병균보다 밀 붉은녹병균에 대하여 보다 큰 항균활성을 나타내었으며 두 종의 균에 대하여 3-methoxy, 11, 3-iso-propyloxy, 13 및 3-iso-propyl 치환체, 25가 제일 큰 활성을 보였다. 그리고 치환(X)-phenylcarbamoyl group의 변화에 따른 물리-화학 파라미터와 항균활성($pI_{50}$)으로부터 구조-활성관계(SAR)를 검토 한 결과, 벼 잎집무늬 마름병균에 대하여는 공명효과에 따른 전자밀게(R<0)의 소수성이 큰(${\pi}>0$) m-alkyl 치환기(X)가, 그리고 밀 붉은녹병균에 대하여는 분자 분극율(Sp.Pol.)과 분자의 음하전(ABSQ<0)을 위시하여 HOMO에너지(e.v.)가 클수록(HOMO<0) 높은 항균활성을 나타내었다. 또한, 전하-조절 반응에 의한 수용체-(S)간의 상호작용과 높은 활성발현 조건들이 검토되었다.

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