http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Nitric oxide synthase inhibitors: a review of patents from 2011 to the present
Yang, Yanyan,Yu, Tao,Lian, Yu-ji,Ma, Rujun,Yang, Sungjae,Cho, Jae Youl Informa UK, Ltd. 2015 Expert opinion on therapeutic patents Vol.25 No.1
<P><B><I>Introduction:</I></B> Nitric oxide synthases (NOSs) are a family of enzymes that play an essential role in synthesizing nitric oxide (NO) by oxidizing <SMALL>L</SMALL>-arginine. As previously reported, NO is a significant mediator in cellular signaling pathways. It serves as a crucial regulator in insulin secretion, vascular tone, peristalsis, angiogenesis, neural development and inflammation. Due to its important role, the inhibition of these vital enzymes provides, as tools, the opportunity to gain an insight into potential therapeutic applications targeting NOSs.</P><P><B><I>Areas covered:</I></B> This paper reviews the patent literature between 2011 and mid-2014 that specified inhibitors of NOS family members as the significant targets. Google and Baidu search engines were used to find relevant patents and clinical information using NOSs or NOS inhibitor as search terms.</P><P><B><I>Expert opinion:</I></B> Considerable recent progress has been made in the development of NOS inhibitors with pharmacodynamic and pharmacokinetic properties, and such development is likely to continue. The patented compounds attenuated mostly embodying evidence from <I>in vitro</I> and <I>in vivo</I> trials that demonstrate good potential for future clinical human trials and industrial applications. Furthermore, new techniques such as X-ray ligand crystallographic study and structure-activity relationship were popularly utilized, which give new insights for developing novel, safe, efficient and selective NOS inhibitors.</P>
Yanyan Tang,Yiding Hu,Yi Li,Haorong Wu,Liangwei Chen,Lan Yu 한양대학교 세라믹연구소 2021 Journal of Ceramic Processing Research Vol.22 No.5
A series of layered CuCr1-xMgxO2 (0 ≤ x ≤ 0.08) polycrystalline ceramics were prepared. The effects of substituting Mg2+cations for Cr3+ cations on the grain composition, grain size, grain quantity, and electrical conductivity were investigated. When x = 0–0.04, the distinct layered structure grain grew rapidly with the increase of magnesium in the composition, andthe average grain size increased from 2.5 μm (x = 0) to 15 μm (x = 0.04) due to the decrease of activation energy. Furthermore,the bulk density and lattice constant also reached the maximum and minimum values of 4.367 g/cm3 and 17.083 respectivelyat x = 0.04. When x = 0.05–0.08, the average grain size slightly decreased due to the grown-up second-phase MgCr2O4hindering of grain growth. The results showed that the average size of the second-phase MgCr2O4 had reached 1.3 μm whenx = 0.04. In general, the larger the grain size of polycrystalline ceramics, the more defects in the grain boundaries, and thebetter its electrical conductivity. Therefore, the solid-phase reaction, which can obtain larger grain size and more grainboundary defects, was chosen here to prepare CuCr1-xMgxO2 polycrystalline ceramics, so as to obtain a highly conductiveCuCr1-xMgxO2 ceramic material. The minimum resistivity of the obtained CuCr0.6Mg0.4O2 polycrystalline ceramic is only 0.091Ω·cm, which is of great significance for the development of transparent conductive oxides.
Yanyan Yang,Yue Qi,Wenli Zhai,Jianing Tan,Suyang Feng,Jie Zhang,Mengxiao Shen,Liuding Wang,Xiaoyang Yu,Xiaoshu Qu 대한금속·재료학회 2020 ELECTRONIC MATERIALS LETTERS Vol.16 No.5
Tungsten oxide (WO3) has received attention as an electrochromic material because of its excellent properties. However,the long switch time and low coloration efficiency of WO3film limit its use. Herein, a nanocomposite film containingPreyssler-type polyoxometalate (POM) K12.5Na1.5[NaP5W30O110]·15H2O (P5W30) and WO3nanoparticles has been fabricatedby layer-by-layer (LbL) self-assembly methods and characterized by UV-Vis spectra, scanning electron microscopy, X-rayphotoelectron spectroscopy and electrochemical workstation. Compared to the pure WO3film, the [P5W30/WO3]20 filmhas better electrochromic properties. Then, the electrochromic properties of [P5W30/WO3]20 film were studied in differentelectrolyte. The results indicated that the composite film show high coloration efficiency (191.62 cm2C−1), fast switch time(2.58 s, 1.48 s), good CV stability (500 th) in 0.5 M LiClO4/PC electrolyte, and successfully assembled of an electrochromicdevice. These advantages can make the nanocomposite film become a promising candidate for potential application inelectrochromic devices.
Molecular mechanism of protopanaxadiol saponin fraction-mediated anti-inflammatory actions
Yanyan Yang,이종성,이만휘,Tao Yu,백광수,성낙윤,김용,윤기정,Ji Hye Kim,Yi-Seong Kwak,Sungyoul Hong,김종훈,조재열 고려인삼학회 2015 Journal of Ginseng Research Vol.39 No.1
Background: Korean Red Ginseng (KRG) is a representative traditional herbal medicine with manydifferent pharmacological properties including anticancer, anti-atherosclerosis, anti-diabetes, and antiinflammatoryactivities. Only a few studies have explored the molecular mechanism of KRG-mediatedanti-inflammatory activity. Methods: We investigated the anti-inflammatory mechanisms of the protopanaxadiol saponin fraction(PPD-SF) of KRG using in vitro and in vivo inflammatory models. Results: PPD-SF dose-dependently diminished the release of inflammatory mediators [nitric oxide (NO),tumor necrosis factor-a, and prostaglandin E2], and downregulated the mRNA expression of their correspondinggenes (inducible NO synthase, tumor necrosis factor-a, and cyclooxygenase-2), withoutaltering cell viability. The PPD-SF-mediated suppression of these events appeared to be regulated by ablockade of p38, c-Jun N-terminal kinase (JNK), and TANK (TRAF family member-associated NF-kappa-Bactivator)-binding kinase 1 (TBK1), which are linked to the activation of activating transcription factor 2(ATF2) and interferon regulatory transcription factor 3 (IRF3). Moreover, this fraction also amelioratedHCl/ethanol/-induced gastritis via suppression of phospho-JNK2 levels. Conclusion: These results strongly suggest that the anti-inflammatory action of PPD-SF could be mediatedby a reduction in the activation of p38-, JNK2-, and TANK-binding-kinase-1-linked pathways andtheir corresponding transcription factors (ATF2 and IRF3).
Molecular mechanism of protopanaxadiol saponin fraction-mediated anti-inflammatory actions
Yanyan Yang,Jongsung Lee,Man Hee Rhee,Tao Yu,Kwang-Soo Baek,Nak Yoon Sung,Yong Kim,Keejung Yoon,Ji Hye Kim,Yi-Seong Kwak,Sungyoul Hong,Jong-Hoon Kim,Jae Youl Cho 고려인삼학회 2015 Journal of Ginseng Research Vol.39 No.3
Background: Korean Red Ginseng (KRG) is a representative traditional herbal medicine with many different pharmacological properties including anticancer, anti-atherosclerosis, anti-diabetes, and anti-inflammatory activities. Only a few studies have explored the molecular mechanism of KRG-mediated anti-inflammatory activity. Methods: We investigated the anti-inflammatory mechanisms of the protopanaxadiol saponin fraction (PPD-SF) of KRG using in vitro and in vivo inflammatory models. Results: PPD-SF dose-dependently diminished the release of inflammatory mediators [nitric oxide (NO), tumor necrosis factor-α, and prostaglandin E₂], and downregulated the mRNA expression of their corresponding genes (inducible NO synthase, tumor necrosis factor-α, and cyclooxygenase-2), without altering cell viability. The PPD-SF-mediated suppression of these events appeared to be regulated by a blockade of p38, c-Jun N-terminal kinase (JNK), and TANK (TRAF family member-associated NF-kappa-B activator)-binding kinase 1 (TBK1), which are linked to the activation of activating transcription factor 2 (ATF2) and interferon regulatory transcription factor 3 (IRF3). Moreover, this fraction also ameliorated HCl/ethanol/-induced gastritis via suppression of phospho-JNK2 levels. Conclusion: These results strongly suggest that the anti-inflammatory action of PPD-SF could be mediated by a reduction in the activation of p38-, JNK2-, and TANK-binding-kinase-1-linked pathways and their corresponding transcription factors (ATF2 and IRF3).
Yu, Tao,Yang, Yanyan,Kwak, Yi-Seong,Song, Gwan Gyu,Kim, Mi-Yeon,Rhee, Man Hee,Cho, Jae Youl The Korean Society of Ginseng 2017 Journal of Ginseng Research Vol.41 No.2
Background: Ginsenoside Rc (G-Rc) is one of the major protopanaxadiol-type saponins isolated from Panax ginseng, a well-known medicinal herb with many beneficial properties including anticancer, anti-inflammatory, antiobesity, and antidiabetic effects. In this study, we investigated the effects of G-Rc on inflammatory responses in vitro and examined the mechanisms of these effects. Methods: The in vitro inflammation system used lipopolysaccharide-treated macrophages, tumor necrosis $factor-{\alpha}/interferon-{\gamma}-treated$ synovial cells, and HEK293 cells transfected with various inducers of inflammation. Results: G-Rc significantly inhibited the expression of macrophage-derived cytokines, such as tumor necrosis $factor-{\alpha}$ and $interleukin-1{\beta}$. G-Rc also markedly suppressed the activation of TANK-binding kinase $1/I{\kappa}B$ kinase ${\varepsilon}/interferon$ regulatory factor-3 and p38/ATF-2 signaling in activated RAW264.7 macrophages, human synovial cells, and HEK293 cells. Conclusion: G-Rc exerts its anti-inflammatory actions by suppressing TANK-binding kinase $1/I{\kappa}B$ kinase ${\varepsilon}/interferon$ regulatory factor-3 and p38/ATF-2 signaling.
Tao Yu,모상현,김상범,Yanyan Yang,김은지,이연월,조종관,김경희,유병철,조재열,유화승 한국식품영양과학회 2013 Journal of medicinal food Vol.16 No.1
HangAmDan-B (HAD-B) is a powdered mixture of eight ethnopharmacologically characterized folk medicines that is prescribed for solid masses and cancers in Korea. In view of the finding that macrophage-mediated inflammation is a pathophysiologically important phenomenon, we investigated whether HAD-B modulates inflammatory responses and explored the associated molecular mechanisms. The immunomodulatory activity of HAD-B in toll-like receptor-activated macrophages induced by lipopolysaccharide (LPS) was assessed by measuring nitric oxide (NO) and prostaglandin E2 (PGE2) levels. To identify the specific transcription factors (such as nuclear factor [NF]–κB and signaling enzymes) targeted by HAD-B, biochemical approaches, including kinase assays and immunoblot analysis, were additionally employed. HAD-B suppressed the production of PGE2 and NO in LPS-activated macrophages in a dose-dependent manner. Furthermore, the extract ameliorated HCl/EtOH-induced gastritis symptoms. Moreover, HAD-B significantly inhibited LPS-induced mRNA expression of inducible NO synthase and cyclooxygenase (COX)-2. Interestingly, marked inhibition of NF-κB and activating transcription factor was observed in the presence of HAD-B. Data from direct kinase assays and immunoblot analysis showed that HAD-B suppresses activation of the upstream signaling cascade involving spleen tyrosine kinase, Src, p38, c-Jun N-terminal kinase, and transforming growth factor β–activated kinase 1. Finally, kaempferol, but not quercetin or resveratrol was identified as a bioactive compound in HAD-B. Therefore, our results suggest that HAD-B possesses anti-inflammatory activity that contributes to its anticancer property.
Tao Yu,Yanyan Yang,곽이성,송관규,김미연,이만휘,조재열 고려인삼학회 2017 Journal of Ginseng Research Vol.41 No.2
Background: Ginsenoside Rc (G-Rc) is one of the major protopanaxadiol-type saponins isolated from Panax ginseng, a well-known medicinal herb with many beneficial properties including anticancer, antiinflammatory, antiobesity, and antidiabetic effects. In this study, we investigated the effects of G-Rc on inflammatory responses in vitro and examined the mechanisms of these effects. Methods: The in vitro inflammation system used lipopolysaccharide-treated macrophages, tumor necrosis factor-a/interferon-g-treated synovial cells, and HEK293 cells transfected with various inducers of inflammation. Results: G-Rc significantly inhibited the expression of macrophage-derived cytokines, such as tumor necrosis factor-a and interleukin-1b. G-Rc also markedly suppressed the activation of TANK-binding kinase 1/IkB kinase ε/interferon regulatory factor-3 and p38/ATF-2 signaling in activated RAW264.7 macrophages, human synovial cells, and HEK293 cells. Conclusion: G-Rc exerts its anti-inflammatory actions by suppressing TANK-binding kinase 1/IkB kinase ε/interferon regulatory factor-3 and p38/ATF-2 signaling.