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Yang, Sungjae,Kim, Yong,Jeong, Deok,Kim, Jun Ho,Kim, Sunggyu,Son, Young-Jin,Yoo, Byong Chul,Jeong, Eun Jeong,Kim, Tae Woong,Han Lee, In-Sook,Cho, Jae Youl The Korean Society of Applied Pharmacology 2016 Biomolecules & Therapeutics(구 응용약물학회지) Vol.24 No.6
(E)-3-Phenyl-1-(2-pyrrolyl)-2-propenone (PPP) is a pyrrole derivative of chalcone, in which the B-ring of chalcone linked to ${\beta}$-carbon is replaced by pyrrole group. While pyrrole has been studied for possible Src inhibition activity, chalcone, especially the substituents on the B-ring, has shown pharmaceutical, anti-inflammatory, and anti-oxidant properties via inhibition of NF-${\kappa}B$ activity. Our study is aimed to investigate whether this novel synthetic compound retains or enhances the pharmaceutically beneficial activities from the both structures. For this purpose, inflammatory responses of lipopolysaccharide (LPS)-treated RAW264.7 cells were analyzed. Nitric oxide (NO) production, inducible NO synthase (iNOS) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$) mRNA expression, and the intracellular inflammatory signaling cascade were measured. Interestingly, PPP strongly inhibited NO release in a dose-dependent manner. To further investigate this anti-inflammatory activity, we identified molecular pathways by immunoblot analyses of nuclear fractions and whole cell lysates prepared from LPS-stimulated RAW264.7 cells with or without PPP pretreatment. The nuclear levels of p50, c-Jun, and c-Fos were significantly inhibited when cells were exposed to PPP. Moreover, according to the luciferase reporter gene assay after cotransfection with either TRIF or MyD88 in HEK293 cells, NF-${\kappa}B$-mediated luciferase activity dose-dependently diminished. Additionally, it was confirmed that PPP dampens the upstream signaling cascade of NF-${\kappa}B$ and AP-1 activation. Thus, PPP inhibited Syk, Src, and TAK1 activities induced by LPS or induced by overexpression of these genes. Therefore, our results suggest that PPP displays anti-inflammatory activity via inhibition of Syk, Src, and TAK1 activity, which may be developed as a novel anti-inflammatory drug.
Yang, Sungjae,Kim, Byeongwoo,Kim, Hanbeen,Moon, Joonbeom,Yoo, Daekyum,Baek, Youl-Chang,Lee, Seyoung,Seo, Jakyeom Asian Australasian Association of Animal Productio 2020 Animal Bioscience Vol.33 No.2
Objective: This study was realized to evaluate the nutritional value of rice grains as a replacement for corn grains in the diet of growing Hanwoo steers. Methods: Two experimental diets were prepared: i) Corn total mixed ration (TMR) consisting of 20% corn grains and ii) Rice TMR consisting of 20% rice grains, in a dry matter (DM) basis. These treatments were used for in vitro rumen fermentation and in vivo growth trials. In the rumen fermentation experiment, the in vitro DM digestibility (IVDMD), in vitro crude protein digestibility (IVCPD), in vitro neutral detergent fiber digestibility, pH, ammonia nitrogen, and volatile fatty acids (VFA) were estimated at 48 h, and the gas production was measured at 3, 6, 12, 24, and 48 h. Twenty four growing Hanwoo steers (9 months old; body weight [BW]: 259±13 kg) were randomly divided into two treatment groups and the BW, dry matter intake (DMI), average daily gain (ADG), and feed conversion ratio (FCR) were measured. Results: The in vitro experiment showed that the IVDMD, IVCPD, and VFA production of the Rice TMR were higher than those of the Corn TMR (p<0.05). The growth trial showed no differences (p>0.05) in the final BW, ADG, DMI, and FCR between the two TMRs. Conclusion: The use of rice grains instead of corn grains did not exhibit any negative effects on the rumen fermentation or growth performance, thereby rice grains with a DM of less than 20% could be used as a starch source in the diet of growing steers.
Yang, Woo Seok,Ko, Jaeyoung,Kim, Eunji,Kim, Ji Hye,Park, Jae Gwang,Sung, Nak Yoon,Kim, Han Gyung,Yang, Sungjae,Rho, Ho Sik,Hong, Yong Deog,Shin, Song Seok,Cho, Jae Youl Hindawi Publishing Corporation 2014 Mediators of inflammation Vol.2014 No.-
<P>21-O-Angeloyltheasapogenol E3 (ATS-E3) is a triterpenoid saponin recently isolated from the seeds of the tea tree <I>Camellia sinensis</I> (L.) O. Kuntze. ATS-E3 has several beneficial properties including anti-inflammatory, antidiabetic, antiatherosclerotic, and anticancer effects. Unlike other phenolic compounds isolated from tea plants, there are no studies reporting the pharmacological action of ATS-E3. In this study, we therefore aimed to explore the cellular and molecular inhibitory activities of ATS-E3 in macrophage-mediated inflammatory responses. ATS-E3 remarkably diminished cellular responses of macrophages such as FITC-dextran-induced phagocytic uptake, sodium nitroprusside- (SNP-) induced radical generation, and LPS-induced nitric oxide (NO) production. Analysis of its molecular activity showed that this compound significantly suppressed the expression of inducible NO synthase (iNOS), nuclear translocation of nuclear factor- (NF-) <I>κ</I>B subunits (p50 and p65), phosphorylation of inhibitor of <I>κ</I>B kinase (IKK), and the enzyme activity of AKT1. Taken together, the novel triterpenoid saponin compound ATS-E3 contributes to the beneficial effects of tea plants by exerting anti-inflammatory and antioxidative activities in an AKT/IKK/NF-<I>κ</I>B-dependent manner.</P>
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>
Isoprenyl carboxyl methyltransferase inhibitors: a brief review including recent patents
Yang, Woo Seok,Yeo, Seung-Gu,Yang, Sungjae,Kim, Kyung-Hee,Yoo, Byong Chul,Cho, Jae Youl Springer Vienna 2017 Amino acids Vol.49 No.9
<P>Among the enzymes involved in the post-translational modification of Ras, isoprenyl carboxyl methyltransferase (ICMT) has been explored by a number of researchers as a significant enzyme controlling the activation of Ras. Indeed, inhibition of ICMT exhibited promising anti-cancer activity against various cancer cell lines. This paper reviews patents and research articles published between 2009 and 2016 that reported inhibitors of ICMT as potential chemotherapeutic agents targeting Ras-induced growth factor signaling. Since ICMT inhibitors can modulate Ras signaling pathway, it might be possible to develop a new class of anti-cancer drugs targeting Ras-related cancers. Researchers have discovered indole-based small-molecular ICMT inhibitors through high-throughput screening. Researchers at Duke University identified a prototypical inhibitor, cysmethynil. At Singapore University, Ramanujulu and his colleagues patented more potent compounds by optimizing cysmethynil. In addition, Rodriguez and Stevenson at Universidad Complutense De Madrid and Cancer Therapeutics CRC PTY Ltd., respectively, have developed inhibitors based on formulas other than the indole base. However, further optimization of chemicals targeted to functional groups is needed to improve the characteristics of ICMT inhibitors related to their application as drugs, such as solubility, effectiveness, and safety, to facilitate clinical use.</P>
( Sungjae Yang ),( Yong Kim ),( Deok Jeong ),( Jun Ho Kim ),( Sunggyu Kim ),( Young-jin Son ),( Byong Chul Yoo ),( Eun Jeong Jeong ),( Tae Woong Kim ),( In-sook Han Lee ),( Jae Youl Cho ) 한국응용약물학회 2016 Biomolecules & Therapeutics(구 응용약물학회지) Vol.24 No.6
(E)-3-Phenyl-1-(2-pyrrolyl)-2-propenone (PPP) is a pyrrole derivative of chalcone, in which the B-ring of chalcone linked to bcarbon is replaced by pyrrole group. While pyrrole has been studied for possible Src inhibition activity, chalcone, especially the substituents on the B-ring, has shown pharmaceutical, anti-inflammatory, and anti-oxidant properties via inhibition of NF-kB activity. Our study is aimed to investigate whether this novel synthetic compound retains or enhances the pharmaceutically beneficial activities from the both structures. For this purpose, inflammatory responses of lipopolysaccharide (LPS)-treated RAW264.7 cells were analyzed. Nitric oxide (NO) production, inducible NO synthase (iNOS) and tumor necrosis factor-a (TNF-a) mRNA expression, and the intracellular inflammatory signaling cascade were measured. Interestingly, PPP strongly inhibited NO release in a dose-dependent manner. To further investigate this anti-inflammatory activity, we identified molecular pathways by immunoblot analyses of nuclear fractions and whole cell lysates prepared from LPS-stimulated RAW264.7 cells with or without PPP pretreatment. The nuclear levels of p50, c-Jun, and c-Fos were significantly inhibited when cells were exposed to PPP. Moreover, according to the luciferase reporter gene assay after cotransfection with either TRIF or MyD88 in HEK293 cells, NF-kB-mediated luciferase activity dose-dependently diminished. Additionally, it was confirmed that PPP dampens the upstream signaling cascade of NF-kB and AP-1 activation. Thus, PPP inhibited Syk, Src, and TAK1 activities induced by LPS or induced by overexpression of these genes. Therefore, our results suggest that PPP displays anti-inflammatory activity via inhibition of Syk, Src, and TAK1 activity, which may be developed as a novel anti-inflammatory drug.
저전력 CMOS 디지털 회로 설계에서 경로 균등화에 의한 글리치 감소 기법
양재석(Jaeseok Yang),김성재(Sungjae Kim),김주호(Juho Kim),황선영(Sun-Young Hwang) 한국정보과학회 1999 정보과학회논문지 : 시스템 및 이론 Vol.26 No.10
본 논문은 CMOS 디지털 회로에서의 전력 소모의 주원인인 신호의 천이중에서 회로의 동작에 직접적인 영향을 미치지 않는 불필요한 신호의 천이인 글리치를 줄이기 위한 효율적인 알고리즘을 제시한다. 제안된 알고리즘은 회로의 지연 증가 없이 게이트 사이징과 버퍼 삽입에 의해 경로 균등(peth balancing)을 이룸으로써 글리치를 감소시킨다. 경로 균등화를 위하여 먼저 게이트 사이징을 통해 글리치의 감소와 동시에, 게이트 크기의 최적화를 통해 회로 전체의 캐패시턴스까지 줄일 수 있으며, 게이트 사이징 만으로 경로 균등화가 이루어지지 않을 경우 버퍼 삽입으로 경로 균등화를 이루게 된다. 버퍼 자체에 의한 전력 소모 증가보다 글리치 감소에 의한 전력 감소가 큰 버퍼를 선택하여 삽입한다. 이때 버퍼 삽입에 의한 전력 감소는 다른 버퍼의 삽입 상태에 따라 크게 달라질 수 있어 ILP (Integer Linear Program)를 이용하여 적은 버퍼 삽입으로 전력 감소를 최대화 할 수 있는 저전력 설계 시스템을 구현하였다. 제안된 알고리즘은 LGSynth91 벤치마크 회로에 대한 테스트 결과 회로의 지연 증가 없이 평균적으로 30.4%의 전력 감소를 얻을 수 있었다. This paper presents an efficient algorithm for reducing glitches caused by spurious transitions in CMOS logic circuits. The proposed algorithm reduces glitches by achieving path balancing through gate sizing and buffer insertion. The gate sizing technique reduces not only glitches but also effective capacitance in the circuit. In the proposed algorithm, the buffers are inserted between the gates where power reduction achieved by glitch reduction is larger than the additional power consumed by the inserted buffers. To determine the location of buffer insertion, ILP (Integer Linear Program) has been employed in the proposed system. The proposed algorithm has been tested on LGSynth91 benchmark circuits. Experimental results show an average of 30.4% power reduction.