• Title/Summary/Keyword: active agent

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JPH203, a selective L-type amino acid transporter 1 inhibitor, induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells

  • Choi, Dae Woo;Kim, Do Kyung;Kanai, Yoshikatsu;Wempe, Michael F.;Endou, Hitoshi;Kim, Jong-Keun
    • The Korean Journal of Physiology and Pharmacology
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    • v.21 no.6
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    • pp.599-607
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    • 2017
  • Most normal cells express L-type amino acid transporter 2 (LAT2). However, L-type amino acid transporter 1 (LAT1) is highly expressed in many tumor cells and presumed to support their increased growth and proliferation. This study examined the effects of JPH203, a selective LAT1 inhibitor, on cell growth and its mechanism for cell death in Saos2 human osteosarcoma cells. FOB human osteoblastic cells and Saos2 cells expressed LAT1 and LAT2 together with their associating protein 4F2 heavy chain, but the expression of LAT2 in the Saos2 cells was especially weak. JPH203 and BCH, a non-selective L-type amino acid transporter inhibitor, potently inhibited L-leucine uptake in Saos2 cells. As expected, the intrinsic ability of JPH203 to inhibit L-leucine uptake was far more efficient than that of BCH in Saos2 cells. Likewise, JPH203 and BCH inhibited Saos2 cell growth with JPH203 being superior to BCH in this regard. Furthermore, JPH203 increased apoptosis rates and formed DNA ladder in Saos2 cells. Moreover, JPH203 activated the mitochondria-dependent apoptotic signaling pathway by upregulating pro-apoptotic factors, such as Bad, Bax, and Bak, and the active form of caspase-9, and downregulating anti-apoptotic factors, such as Bcl-2 and Bcl-xL. These results suggest that the inhibition of LAT1 activity via JPH203, which may act as a potential novel anti-cancer agent, leads to apoptosis mediated by the mitochondria-dependent intrinsic apoptotic signaling pathway by inducing the intracellular depletion of neutral amino acids essential for cell growth in Saos2 human osteosarcoma cells.

Aerosol Deposition and Behavior on Leaves in Cool-temperate Deciduous Forests. Part 2: Characteristics of Fog Water Chemistry and Fog Deposition in Northern Japan

  • Yamaguchi, Takashi;Noguchi, Izumi;Watanabe, Yoko;Katata, Genki;Sato, Haruna;Hara, Hiroshi
    • Asian Journal of Atmospheric Environment
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    • v.7 no.1
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    • pp.8-16
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    • 2013
  • The fog water chemistry and deposition in northern Japan were investigated by fog water and throughfall measurements in 2010. Fog water was sampled weekly by an active-string fog sampler at Lake Mashu from May to November. Throughfall measurements were conducted using rain gauges under three deciduous trees along the somma of the lake from August to October. The mean fog deposition rate (flux) was calculated using throughfall data to estimate the total fog water deposition amount for the entire sampling period. $NH_4{^+}$ and $SO{_4}^{2-}$ were the most abundant cation and anion, respectively, in the fog water samples. A mean pH of 5.08 in the fog water, which is higher than those in rural areas in Japan, was observed. The [$NH_4{^+}$]/[$SO{_4}^{2-}$] equivalent ratio in fog water was larger than 1.0 throughout the study period, indicating that $NH_3$ gas was the primary neutralizing agent for fog water acidity. The mean rate and total amount of fog water deposition were estimated as 0.15 mm $h^{-1}$ and 164 mm, respectively. The amounts of nitrogen and sulfate deposition via fog water deposition were corresponded to those reported values of the annual deposition amounts via rainfall.

Effect of Ginsenoside Re on Depression- and Anxiety-Like Behaviors and Cognition Memory Deficit Induced by Repeated Immobilization in Rats

  • Lee, Bom-Bi;Shim, In-Sop;Lee, Hye-Jung;Hahm, Dae-Hyun
    • Journal of Microbiology and Biotechnology
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    • v.22 no.5
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    • pp.708-720
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    • 2012
  • In this study, we assessed the effects of ginsenoside Re (GRe) administration on repeated immobilization stress-induced behavioral alterations using the forced swimming test (FST), the elevated plus maze (EPM), and the active avoidance conditioning test (AAT). Additionally, we examined the effect of GRe on the central adrenergic system by observing changes in neuronal tyrosine hydroxylase (TH) immunoreactivity and brain-derived neurotrophic factor (BDNF) mRNA expression in the rat brain. Male rats received 10, 20, or 50 mg/kg GRe (i.p.) 30 min before daily exposures to repeated immobilization stress (2 h/day) for 10 days. Activation of the hypothalamic-pituitary-adrenal (HPA) axis in response to repeated immobilization was confirmed by measuring serum levels of corticosterone (CORT) and the expression of corticotrophin-releasing factor (CRF) in the hypothalamus. Repeated immobilization stress increased immobility in the FST and reduced open-arm exploration in the EPM test. It also increased the probability of escape failures in the AAT test, indicating a reduced avoidance response. Daily administration of GRe during the repeated immobilization stress period significantly inhibited the stress-induced behavioral deficits in these behavioral tests. Administration of GRe also significantly blocked the increase in TH expression in the locus coeruleus (LC) and the decrease in BDNF mRNA expression in the hippocampus. Taken together, these findings indicate that administration of GRe prior to immobilization stress significantly improved helpless behaviors and cognitive impairment, possibly through modulating the central noradrenergic system in rats. These findings suggest that GRe may be a useful agent for treating complex symptoms of depression, anxiety, and cognitive impairment.

Patent and Anti-wrinkle Cosmetics

  • Jang Jinah
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.29 no.2 s.43
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    • pp.131-147
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    • 2003
  • In the 21st century, the development of cosmetics is led to pursue the high functionality of cosmetics with excellent effectiveness and safety. As Cosmetic Act took effect in 2000, functional cosmetics is provided in the law. As a result, the research and development of functional cosmetics has continually increased, and the number of patent applications in functional cosmetics has also rapidly increased as a plan for preoccupying in the functional cosmetics age. Now, the cosmetic industry has a great interest in developing anti-wrinkle cosmetics among functional cosmetics, because women's desire for having young resilient skin has increased since Korea entered an aging society thanks to the advanced medical technology. The patent application trends of anti-wrinkle cosmetics at home since 2000 particularly show the rapid increase in the applications in natural plant extracts. It may be because Korean consumers preference of vegetable cosmetics has resulted in the development of raw materials based on the traditional medicine. As for the existing preparation such as Retinoid or Ascorbic acid, the patent application itself will be an essential technical element in the future because patent applications are filed in the field of a preparation of cosmetics for stabilizing ingredients, reducing skin irritability or promoting absorbance, and in the field of cosmetic formulation technology. As there are many studies on the causes of skin wrinkles, it is expected that new raw materials of cosmetics can be developed due to new mechanisms, and that the number of patent applications in new technologies will increase due to a change in the thought of cosmetics accompanied by the integration of cosmetics with biotechnology using Genetic Engineering, including the practical application of the medicine previously used far treating skin diseases to an anti-wrinkle agent and the mass production of active ingredients of cosmetics.

Whitening Effect of Biochanin A (Biochanin A의 미백 효과에 관한 연구)

  • Park, Sung Ha;Kim, A Hyun;Park, Byoung Jun;Kim, Jin Jun
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.39 no.4
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    • pp.289-294
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    • 2013
  • To develop a new whitening agent for cosmetics, we investigated the inhibitory effects of biochanin A on melanogenesis. The biochanoin A is an active component in the extracts of Dalbergia odorifera T. Chen. It reduced melanin contents of B16F1 melanoma cells in a dose-dependent manner and decreased to about 48% at a concentration 10 ${\mu}g/mL$. It also inhibited the expression in microphthalmia associated transcription factor (MITF), Tyrosinase, Tyrosinase related protein 1 (Trp-1), and Tyrosinase related protein 2 (Trp-2) in melanocytes. The results suggested that biochanin A has considerable potential as a cosmetics ingredient with a whitening effect.

Sanguiin H-6 Blocks Endothelial Cell Growth through Inhibition of VEGF Binding to VEGF Receptor

  • Lee Sung-Jin;Lee Hak-Kyo
    • Archives of Pharmacal Research
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    • v.28 no.11
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    • pp.1270-1274
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    • 2005
  • The vascular endothelial growth factor (VEGF) plays a key role in angiogenesis, which is a process where new blood vessels develop from the endothelium of a pre-existing vasculature. VEGF exerts its activity by binding to its receptor tyrosine kinase, KDR/Flk-1, which is expressed on the surface of endothelial cells. A methanol extract and organic solvent (n-hexane, ethyl acetate, n-butanol, aqueous) fractions from Rubus coreanus were examined for their inhibitory effects on VEGF binding to the VEGF receptor. The methanol extract from the crude drug were found to significantly inhibit VEGF binding to the VEGF receptor ($IC_{50}$$\thickapprox$27 $\mu$g/mL). Among the fractions examined, the aqueous fraction from the medicinal plant showed potent inhibitory effects against the binding of KDR/Flk-1-Fc to immobilized $VEGF_{165}$ in a dose­dependent manner ($IC_{50}$$\thickapprox$11 $\mu$g/mL). Sanguiin H-6 was isolated as an active principle from the aqueous fraction, and inhibited the binding of KDR/Flk-1-Fc to immobilized $VEGF_{165}$ in a dose­dependent manner ($IC_{50}$$\thickapprox$0.3 $\mu$g/mL). In addition, sanguiin H-6 efficiently blocked the VEGF­induced HUVEC proliferation in a dose-dependent manner ($IC_{50}$$\thickapprox$7.4 $\mu$g/mL) but had no effect on the growth of HT1080 human fibrosarcoma cells. This suggests that sanguiin H-6 might be a potential anti-angiogenic agent.

Growth Factor Releasing Porous Poly (${\varepsilon}-caprolactone$)-Chitosan Matrices for Enhanced Bone Regenerative Therapy

  • Im, Su-Yeon;Cho, Seon-Hye;Hwang, Jeong-Hyo;Lee, Seung-Jin
    • Archives of Pharmacal Research
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    • v.26 no.1
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    • pp.76-82
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    • 2003
  • Drug releasing porous poly($\varepsilon$-caprolactone) (PCL)-chitosan matrices were fabricated for bone regenerative therapy. Porous matrices made of biodegradable polymers have been playing a crucial role as bone substitutes and as tissue-engineered scaffolds in bone regenerative therapy. The matrices provided mechanical support for the developing tissue and enhanced tissue formation by releasing active agent in controlled manner. Chitosan was employed to enhance hydrophilicity and biocompatibility of the PCL matrices. PDGF-BB was incorporated into PCL-chitosan matrices to induce enhanced bone regeneration efficacy. PCL-chitosan matrices retained a porous structure with a 100-200 $\mu$m pore diameter that was suitable for cellular migration and osteoid ingrowth. $NaHCO_3$ as a porogen was incorporated 5% ratio to polymer weight to form highly porous scaffolds. PDGF-BB was released from PCL-chitosan matrices maintaining therapeutic concentration for 4 week. High osteoblasts attachment level and proliferation was observed from PCL-chitosan matrices. Scanning electron microscopic examination indicated that cultured osteoblasts showed round form and spread pseudopods after 1 day and showed broad cytoplasmic extension after 14 days. PCL-chitosan matrices promoted bone regeneration and PDGF-BB loaded matrices obtained enhanced bone formation in rat calvarial defect. These results suggested that the PDGF-BB releasing PCL-chitosan porous matrices may be potentially used as tissue engineering scaffolds or bone substitutes with high bone regenerative efficacy.

A Study on Curing Reaction of 1-Chlobutadiene-Butadiene Copolymer by Moisture (1-Chlorobutadiene-Butadiene Copolymer의 수가교반응(水架橋反應)에 관한 연구(硏究)(I))

  • Yoo, Chong-Sun;Paik, Nam-Chul
    • Elastomers and Composites
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    • v.22 no.3
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    • pp.195-203
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    • 1987
  • In this study, as one of the developing ways of the functional elastomer, improvement of the functionality of CB-BR was attempted through moisture curing reaction. The curing reaction of CB-BR was determined with an use of 3-aminopropyltriethoxysilane(APS) as a crosslinking agent, also a solution reaction with an active chlorine of CB-BR was elucidated by using a reaction kinetics theory and a study of physical property was made through moisture curing on the compound of 3-aminopropyltriethoxysilane and CB-BR The results of this study obtained are as follows : 1) CB-BR reacted easily with APS in the liquid state and the reaction rate coefficient and activation energy were as follows : 2) Optimum pressure condition of moisture cured elastomer(CB-BR+APS) was 20 minutes at $150^{\circ}C$, and the crosslinked elastomer was close to the theoretical value (q=1) for Flory's equation($\frac{\alpha}{\alpha-1}=q{\nu}RT$)

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Analysis of epidemiological change of hair colored Acer palmatum Leaves extract as hair treatment product (헤어 트리트먼트제로서 단풍잎 추출물 컬러링 모발의 역학적 변화분석)

  • Park, Jang-Soon
    • Journal of Digital Convergence
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    • v.18 no.8
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    • pp.479-484
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    • 2020
  • In the social atmosphere where the importance of appearance is increasing day by day, efforts and desires of modern people are becoming more active and diversified, and the beauty beauty industry is gradually becoming more specialized and specialized due to these effects. Hair damage is inevitable due to the excessive permanent wave or hair coloring of modern people. However, as the hair is damaged, the cuticle peels off and falls off, and the tensile force decreases and the satisfaction after hair styling or perm decreases relatively. Therefore, it is necessary to manage damaged hair, but since artificial synthetic products occupy most of hair treatment agents on the market, it is necessary to develop a hair treatment product containing antioxidants useful for the human body. In this study, the effect of maple leaf extract on the mechanical change of colored hair was analyzed to investigate the potential of maple leaf extract as a hair treatment agent to improve damaged hair and improve hair health. It is considered that this study will be used as basic data for the development of hair beauty products using natural products in the future.

Technology on the Shrinkage Reduction of High Performance Concrete (고성능 콘크리트의 수축 저감 기술)

  • Koh, Kyung-Taek;Ryu, Gum-Sung;Kang, Su-Tae;Park, Jung-Jun;Kim, Sung-Wook;Han, Cheon-Goo
    • Proceedings of the Korea Concrete Institute Conference
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    • 2008.04a
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    • pp.1101-1104
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    • 2008
  • Recently, active researches are conducted on high performance concrete(HPC) exhibiting high strength and high fluidity. These researches are resulting in increased applications on real structures. In order to satisfy the required performances, HPC makes use of large quantities of binder and presents low water-cementitious material ratio. Such mixing is increasing significantly the autogenous shrinkage, which subsequently is likely to favor the potential development of cracks. Therefore, we investigated the effect of used materials and mix proportions on the shrinkage properties of HPC, and of the use of expansive additives and shrinkage reducing agents on the HPC. The autogenous shrinkage of HPC using blast furnace slag are tend to be increased, in some case have the potential development of cracks by only the autogenous shrinkage. Also the using method in combination with expansive additive and shrinkage reducing agent is more effective than the separately using method of that.

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