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DNA Topoisomerase Inhibitory Activity of Constituents from the Flowers of Inula japonica
( Donggen Piao ),( Taein Kim ),( Hai Yan Zhang ),( Hyun Gyu Choi ),( Chong Soon Lee ),( Hyuk Jae Choi ),( Hyeun Wook Chang ),( Mi Hee Woo ),( Jong Keun Son ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Fourteen compounds were isolated from the flowers of Inula japonica THUNB, (Asteraceae), including two new compounds, (1S, 2S, 4S, 5S, 8S, 10R)-2-acetoxy-4,3-dihydroxy-pseudoguai-7(11)-en-12,8-olide (1) and (1S, 2S, 4S, 5S, 8S, 10R)-2,4,13-trihydroxy-pseudoguai-7(qq)-en-12,8-olide (2), and twelve known compounds, budlein B (3), 6 β-hydroquercetin (9), (-)syrigaresinol (10), quercetagetin 3,4`-dimethyl ether (11), luteolin (12), bri-tanin G (13) and inuchinenolide C (14). Structures of 1 and 2 were determined based on one and two dimen-sional (1D)- and (2D)-NMR data and Mosher`s esterification method. Compounds 9 and 12 showed inhibitory activities toward DNA topoisomerase I with IC<sub>50</sub> values of 55.7 and 37.0μm, resoectively, compared to camp-tothecin (CPT) with an IC<sub>50</sub> of 24.5μm. Compounds 7-9 and 11-14 exhibited more potent inhibitory activity against topoisomerases II with IC<sub>50</sub>values of 6.9, 3.8, 3.0, 6.9, 10.0, 14.7 and 13.8μm, respectively, than that of etoposide (VP-16) with an IC<sub>50</sub> of 26.9μm. Compounds 4-7 and 10-14 exhibited weak cytotoxicities to the selected cancer cell lines.
( Yue Lu ),( Donggen Piao ),( Haiyan Zhang ),( Xian Li ),( Guang Hsuan Chao ),( Soon Jin Park ),( Young Chae Chang ),( Cheorl Ho Kim ),( Makoto Murakami ),( Seung Hyun Jung ),( Jung Hye Choi ),( Yong 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
The aim of this study was to investigate the effect of saucerneol F (SF) on the productions of the pro-inflammatory cytokines, TNF-α and IL-6, in IgE/Ag-induced mouse bone marrow-derived mast cells (BMMCs). SF dose-dependently suppressed the transcriptions of these pro-inflammatory cytokines. To identify the molecular mechanisms responsible for these suppressions, we examined the effect of SF on three important transcription factors; activator protein-1 (AP-1), nuclear factor-κB (NF-κB), and STAT5. It was found that SF inhibited the nuclear translocation of the p65 subunit of NF-κB to the nucleus and its DNA-binding ability. SF also attenuated mitogen-activated protein kinase (MAPK)-mediated AP-1 activation and STAT5 activation. Biochemical analysis of FcεRI-mediated signaling pathways demonstrated that SF inhibited the phosphorylation of Fyn and multiple downstream signaling processes, including Syk, Gab2, and the Akt/IKK/IκB and MAPK pathways. Taken together, our results suggest that SF inhibits the production of pro-inflammatory cytokines by suppressing Fyn kinase-dependent signaling events.Crown Copyright ⓒ2013 Published by Elsevier Ltd. All rights reserved.
( Ying Li ),( Donggen Piao ),( Haiyan Zhang ),( Mi Hee Woo ),( Je Hyun Lee ),( Dong Cheul Moon ),( Seung Ho Lee ),( Hyeun Wook Chang ),( Jong Keun Son ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
Cynanchum auriculatum and Cynanchum wilfordii are widely used as folk medicine in Eastern Asia. However, the indeterminacy in the authentic original plant material has resulted in the same appellative name being given to the two plants, and they are commonly misused. Therefore, it is necessary to establish an analytical method for discrimination as well as quality control of the two species. This study was to develop HPLC-UV methods for quality assessment of C. auriculatum and C. wilfordii anddiscrimination between the two species. Two HPLC methods to analyze eight marker compounds were established and validated. The first method analyzed seven marker compounds simultaneously on a reversed-phase column, while the second method analyzed a single marker compound, conduritol F, which exists only in C. wilfordii, on a Si-column. Thirty-nine batches of C. auriculatum and nineteen batches of C. wilfordii that were collected from different geographical regions of South Korea were analyzed by these methods. The constructed data matrix was subjected to principal components analysis and hierarchical cluster analysis in order to classify the samples. The established methods offer a potential strategy for authentication and differentiation of the two species.
Britanin Suppresses IgE/Ag-Induced Mast Cell Activation by Inhibiting the Syk Pathway
( Yue Lu1 ),( Xian Li ),( Young Na Park ),( Okyun Kwon ),( Donggen Piao ),( Young Chae Chang ),( Cheorl Ho Kim ),( Eunkyung Lee ),( Jong Keun Son ),( Hyeun Wook Chang ) 한국응용약물학회 2014 Biomolecules & Therapeutics(구 응용약물학회지) Vol.22 No.3
The aim of this study was to determine whether britanin, isolated from the flowers of Inula japonica (Inulae Flos), modulates the generation of allergic inflammatory mediators in activated mast cells. To understand the biological activity of britanin, the authors investigated its effects on the generation of prostaglandin D2 (PGD2), leukotriene C4 (LTC4), and degranulation in IgE/Ag-induced bone marrow-derived mast cells (BMMCs). Britanin dose dependently inhibited degranulation and the generations of PGD2 and LTC4 in BMMCs. Biochemical analyses of IgE/Ag-mediated signaling pathways demonstrated that britanin suppressed the phosphorylation of Syk kinase and multiple downstream signaling processes, including phospholipase Cγ1 (PLCγ1)-mediated calcium influx, the activation of mitogen-activated protein kinases (MAPKs; extracellular signal-regulated kinase 1/2, c Jun NH2-terminal kinase and p38), and the nuclear factor-κB (NF-κB) pathway. Taken together, the findings of this study suggest britanin suppresses degranulation and eicosanoid generation by inhibiting the Syk-dependent pathway and britanin might be useful for the treatment of allergic inflammatory diseases.