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Kim, Byung Hak,Roh, Eunmiri,Lee, Hwa Young,Lee, In-Jeong,Ahn, Byeongwoo,Jung, Sang-Hun,Lee, Heesoon,Han, Sang-Bae,Kim, Youngsoo American Society for Pharmacology and Experimental 2008 Molecular pharmacology Vol.73 No.4
<P>Benzoxathiole derivatives have been used in the treatment of acne and have shown cytostatic, antipsoriatic, and antibacterial properties. However, little is known about the molecular basis for these pharmacological properties, although nuclear factor (NF)-kappaB activation is closely linked to inflammation and cell proliferation. Here, we demonstrate that the novel small-molecule benzoxathiole 6,6-dimethyl-2-(phenylimino)-6,7-dihydro-5H-benzo-[1,3]oxathiol-4-one (BOT-64) inhibits NF-kappaB activation with an IC(50) value of 1 muM by blocking inhibitory kappaB(IkappaB) kinase beta (IKKbeta), and suppresses NF-kappaB-regulated expression of inflammatory genes in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. BOT-64 inhibits IKKbeta-mediated IkappaBalpha phosphorylation in LPS-activated macrophages, resulting in sequential prevention of downstream events, including proteolytic degradation of IkappaBalpha, DNA binding ability, and transcriptional activity of NF-kappaB. BOT-64 inhibits LPS-inducible IKKbeta activity in the cells and catalytic activity of highly purified IKKbeta. Moreover, the effect of BOT-64 on cell-free IKKbeta was abolished by substitution of Ser-177 and Ser-181 residues in the activation loop of IKKbeta to glutamic acid residues, indicating a direct interaction site of benzoxathiole. BOT-64 attenuates NF-kappaB-regulated expression of inflammatory genes such as inducible nitric-oxide synthase, cyclooxygenase-2, tumor necrosis factor-alpha, interleukin (IL)-1beta, and IL-6 in LPS-activated or expression vector IKKbeta-transfected macrophages. Furthermore, BOT-64 dose-dependently increases the survival rates of endotoxin LPS-shocked mice.</P>
Kim, Byung-Wook,More, Sandeep Vasant,Yun, Yo-Sep,Ko, Hyun-Myung,Kwak, Jae-Hwan,Lee, Heesoon,Suk, Kyoungho,Kim, In-Su,Choi, Dong-Kug Springer Science and Business Media LLC 2016 Acta pharmacologica Sinica. Vol.37 No.3
<P>Aim: To investigate the anti-neuroinflammatory activity of a novel synthetic compound, 7-methylchroman-2-carboxylic acid N-(2-trifluoromethyl) phenylamide (MCAP) against LPS-induced microglial activation in vitro. Methods: Primary mouse microglia and BV2 microglia cells were exposed to LPS (50 or 100 ng/mL). The expression of iNOS and COX-2, proinflammatory cytokines, NF-kappa B and p38 MAPK signaling molecules were analyzed by RT-PCR, Western blot and ELISA. The morphological changes of microglia and nuclear translocation of NF-kappa B were visualized using phase contrast and fluorescence microscopy, respectively. Results: Pretreatment with MCAP (0.1, 1, 10 mu mol/L) dose-dependently inhibited LPS-induced expression of iNOS and COX-2 in BV2 microglia cells. Similar results were obtained in primary microglia pretreated with MCAP (0.1, 0.5 mu mol/L). MCAP dose-dependently abated LPS-induced release of TNF-alpha, IL-6 and IL-1 beta, and mitigated LPS-induced activation of NF-kappa B by reducing the phosphorylation of I kappa B alpha in BV2 microglia cells. Moreover, MCAP attenuated LPS-induced phosphorylation of p38 MAPK, whereas SB203580, a p38 MAPK inhibitor, significantly potentiated MCAP-caused inhibition on the expression of MEF-2 (a transcription factor downstream of p38 MAPK). Conclusion: MCAP exerts anti-inflammatory effects in murine microglia in vitro by inhibiting the p38 MAPK and NF-kappa B signaling pathways and proinflammatory responses. MCAP may be developed as a novel agent for treating diseases involving activated microglial cells.</P>
Hak Kim, Byung,Lee, Kum-Ho,Chung, Eun Yong,Chang, Yoon Sook,Lee, Heesoon,Lee, Chong-Kil,Min, Kyung Rak,Kim, Youngsoo Elsevier 2006 european journal of pharmacology Vol.543 No.1
<P><B>Abstract</B></P><P>6-Hydroxy-7-methoxychroman-2-carboxylic acid (3-nitrophenyl)amide (CP-1158) is a synthetic chroman carboxamide with trolox-like chemical structure. In the present study, CP-1158 was found to inhibit interleukin (IL)-6 production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. The CP-1158 attenuated LPS-induced synthesis of IL-6 transcript but also inhibited LPS-induced IL-6 promoter activity. Further, CP-1158 attenuated LPS-induced syntheses of tumor necrosis factor (TNF)-α, IL-1β, interferon-inducible protein (IP)-10 and macrophage inflammatory protein (MIP)-1β transcripts. Nuclear factor (NF)-κB has been evidenced to play a major mechanism in LPS-induced expression of IL-6 or other inflammatory cytokines. CP-1158 prevented LPS-induced nuclear translocation of NF-κB complex and subsequently inhibited DNA binding activity of NF-κB complex as well as NF-κB transcriptional activity in macrophages RAW 264.7. However, CP-1158 did not affect LPS-induced phosphorylation and degradation of inhibitory κB (IκB). In another experiment, CP-1158 inhibited IL-6 promoter activity elicited by expression vectors encoding NF-κB p50 or p65 subunit. Taken together, CP-1158 inhibited LPS-induced expression of inflammatory cytokines including IL-6, targeting NF-κB activating pathway downstream IκB degradation, and thus could provide an anti-inflammatory potential of chroman carboxamide.</P>
김희순 ( Heesoon Kim ) 한국도시지리학회 2016 한국도시지리학회지 Vol.19 No.3
This paper studied the formation and development of Havana as an operation tool for Spanish Imperial. During the colonial period, the establishment of centralized authoritarian system of Spanish monarch has been Havana`s development motivity. This motivity influenced Havana`s urban system, economy, and society and it made difference between Havana and other Spanish colonial cities. Spanish monarch had established the viceroyalty system as means of reinforcement of royal power and consolidation of centralized ruling structure in the Spanish Imperial and appointed Havana as a hub spot. Spanish monarch had managed her centralized colonial economy by the regulation of trade through the flota system. As a center point of flota system, Havana had been attacked by the Caribbean pirates and it made Havana a fortified city. English occupation of Havana during 1762~1763 provided a momentum of Spanish monarch`s Bourbon reform. By Bourbon reform, Spanish monarch intended to tighten the control of America colony and advance new source of wealth in America, and it propelled Havana`s economic and urban development. In the end of the 18th century, Havana got an impetus of the development of the sugar industry by the Haitian Revolution. The origin of urban development of Havana stems from the outside of the city. Thus, it was the centralized colonial system of Spanish Imperial and it made Havana a noticeable city.
메틸크로만-2-카르복실산 N-(이치환)페닐아마이드 유도체의 NF-κB 저해 구조-활성 상관 관계
김태정(Tae-Jeong Kim),곽재환(Jae-Hwan Kwak),김영수(Youngsoo Kim),정재경(Jae-Kyung Jung),이희순(Heesoon Lee) 대한약학회 2011 약학회지 Vol.55 No.2
During the search for a novel compound that can inhibit NF-κB activation, 6-hydroxy-7-methoxychroman-2- carboxylic acid phenyl amide (KL-1156) was identified as a good inhibitor of NF-κB activation. In the present study, we describe the synthesis of methylchroman-2-carboxylic acid N-(disubstituted)phenylamide derivatives (1 and 2 serieses). In addition, their inhibitory effects of NF-κB are compared with activity of KL-1156 and SAR (structure activity relationship) are explored.
Heesoon Park,Kyeong Hee Lee,Ha Kyung Oh,Choong Woo Kim,Hyo-jung Kang,Sung-Hee Choi,Hyunman Shin 한국토양비료학회 2020 한국토양비료학회지 Vol.53 No.3
Jujube is a deciduous broad-leaved tree belonging to the buckthorn family(Rhamnaceae) and is widelycultivated in Southeast Asia and Southeast Europe, including Korea and China and mainly consumedmedicinal herbs or dried jujube. In recent years, consumption of fresh fruits has increased, and organicorchard has also increased. The purpose of this study was to investigate soil chemical changes and growthcharacteristics of jujube when replacing the total amount of nitrogen fertilizer with organic matter in rainshelter house. In March 2017, after soil testing, bark, animal compost, rice bran, oil cake and chemicalfertilizers (NPK) were treated based on nitrogen content. After treatment of organic materials, by March 2020,the pH increased and organic matter, phosphoric acid and cation content in soil increased. After harvest ofjujube, the yield of compost treatment was the highest and the NPK treatment was the lowest. The length,hardness and weight of fruit were greater in the NPK treatment, but the diameter and sugar content were notsignificantly different from the organic material treatments except rice bran. Therefore, when the cultivationof the jujube, nitrogen fertilizer was totally replaced with organic material, there was the effect of improvingsoil chemistry, such as an increase in the organic content of the jujube orchard and an increase in the yield ofjujube but no clear effect on fruit quality.