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Flavonoids activating adenosine monophosphate-activated protein kinase
Yong, Yeonjoong,Shin, Soon Young,Jung, Yearam,Jung, Hyeryoung,Ahn, Seunghyun,Chong, Youhoon,Lim, Yoongho The Korean Society for Applied Biological Chemistr 2015 Applied Biological Chemistry (Appl Biol Chem) Vol.58 No.1
Eighteen flavonoids were tested as adenosine monophosphate-activated protein kinase (AMPK) activators. The AMPK activation induced by kaempferide was 1.75 times better than the value obtained at 100 % AMPK phosphorylation. Western blotting analysis of kaempferide demonstrated that it increased the phosphorylation of AMPK in vitro. In silico docking results carried out to elucidate the binding mode between kaempferide and AMPK showed the docking pose of kaempferide in the binding site of AMPK was similar to that of the substrate contained in the crystallographic structure of AMPK. Flavonoids, including kaempferide, are promising potential AMPK activators.
Yong, Yeonjoong,Shin, Soon Young,Jung, Hyeryoung,Ahn, Seunghyun,Lee, Young Han,Koh, Dongsoo,Lim, Yoongho The Korean Society for Applied Biological Chemistr 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.6
Hydroxychalcones act as autophagy inducers and methoxy chalcones induce apoptosis. Additionally, benzoflavones inhibit the hepatitis C virus. Based on these findings, a chalcone derivative, 2-hydroxy-4-methoxy-2',3'-benzochalcone, was prepared. It showed antimitotic activity through its inhibitory effect on tubulin polymerization. Its molecular binding mode with tubulin was elucidated using in silico docking and nuclear magnetic resonance spectroscopy. In addition, the three-dimensional structure of 2-hydroxy-4-methoxy-2',3'-benzochalcone was determined by X-ray crystallography.
Conversion of Flavonoids and Their Conformation by NMR and DFT
Yong, Yeonjoong,Shin, Soon Young,Hwang, Doseok,Ahn, Seunghyun,Koh, Dongsoo,Lim, Yoongho The Korean Society for Applied Biological Chemistr 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.5
Wide range of various biological activities of chalcones motivated the syntheses of three chalcone derivatives. The conversion to flavanones was confirmed by $^1H$-nuclear magnetic resonance (NMR) spectral data. The reason for the aforesaid conversion was elucidated based on the potential energy values of the derivatives, calculated using the density functional theory based on the Hatree-Fock method with B3LYP functional and the $6-31G^*$ basis set. The rate constants of the derivatives were obtained from the NMR data, and the relevant transition states were considered to explain the relationship between the rate constants and the potential energy differences. These findings can help us predict the molecular stabilities of flavonoids, including chalcones and flavanones, using density functional theory calculations.
Lee, Mi So,Yong, Yeonjoong,Lee, Jong Min,Koh, Dongsoo,Shin, Soon Young,Lee, Young Han The Korean Society for Applied Biological Chemistr 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.1
A novel methoxyflavonol derivative, 2-hydroxy-3-(2-methoxyphenyl)-1H-benzo[f]chromen-1-one (designated DK98) was synthesized and its antitumor activity was evaluated in human HCT116 colon cancer cells. DK98 inhibited clonogenicity of HCT116 cells and induced apoptosis through a caspase-mediated pathway, suggesting that DK98 may have potential as a drug candidate for the treatment of human colon cancer.
Kim, Tae Woo,Yong, Yeonjoong,Shin, Soon Young,Jung, Hyeryoung,Park, Kwan Ha,Lee, Young Han,Lim, Yoongho,Jung, Kang-Yeoun Elsevier 2015 Bioorganic chemistry Vol.59 No.-
<P><B>Abstract</B></P> <P>Rapid and efficient synthesis of a phenyl-1<I>H</I>-1,2,3-triazole library enabled cost-effective biological testing of a range of novel non-steroidal anti-inflammatory drugs with potential for improved drug efficacy and toxicity profiles. Anti-inflammatory activities of the phenyl-1<I>H</I>-1,2,3-triazole analogs synthesized in this report were assessed using the xylene-induced ear edema model in mice. At least four analogs, <B>2a</B>, <B>2b</B>, <B>2c</B>, and <B>4a</B>, showed more potent effects than the reference anti-inflammatory drug diclofenac at the same dose of 25mg/kg. To explore relationships between the structural properties of phenyl-1<I>H</I>-1,2,3-triazole analogs and their anti-inflammatory activities in xylene-induced ear edema, comparative molecular field analysis was performed, and pharmacophores showing good anti-inflammatory activities were identified based on an analysis of contour maps obtained from comparative molecular field analysis. The anti-inflammatory effect on the molecular level was tested by the expression of tumor necrosis factor-alpha induced COX-2 using Western blots. Because the addition of the analog <B>2c</B> caused the expression change of TNF-α induced COX-2, the molecular binding mode between <B>2c</B> and COX-2 was elucidated using <I>in silico</I> docking.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Twenty-four phenyl-1<I>H</I>-1,2,3-triazole analogs were synthesized. </LI> <LI> <I>In vivo</I> xylene-induced ear edema model in mice was used. </LI> <LI> At least four analogs showed more potent effects than diclofenac. </LI> <LI> <I>In vitro</I> anti-inflammatory effect was tested using COX-2 Western blots<I>.</I> </LI> <LI> <I>In silico</I> docking study between an analog and COX-2 was performed. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Shin, Soon Young,Yong, Yeonjoong,Hong, Dae Sun,Lee, Da Hyun,Lee, Da Young,Lee, Young Han 한국응용생명화학회 2015 Applied Biological Chemistry (Appl Biol Chem) Vol.58 No.1
The extract of Eriodictyon californicum has been widely used as an essential emollient, and as an anti-inflammatory, antibacterial, and antifungal agent. In this study, antitumor effects of E. californicum were evaluated against HCT116 human colon cancer cells. Treatment with the ethyl acetate extract of E. californicum (EEC) inhibited the short-term viability and long-term clonogenicity of HCT116 cells. We identified several flavonoids, including rosmarinic acid and luteolin, from the EEC by using high-performance liquid chromatography and nuclear magnetic resonance. Luteolin inhibited clonogenicity, activated caspase-7, and induced apoptosis of HCT116 cells. These findings suggest that EEC contains bioactive flavonoids that exhibit antitumor activities.
Shin, Soon Young,Yong, Yeonjoong,Lee, Jongmin,Ahn, Seunghyun,Jung, Kang-Yeoun,Koh, Dongsoo,Lee, Young Han,Lim, Yoongho The Korean Society for Applied Biological Chemistr 2014 Applied Biological Chemistry (Appl Biol Chem) Vol.57 No.4
Flavonoids have always been studied in the context of therapies of human diseases. Among them, chalcone, an open-chain flavonoid, has been used as a key precursor for synthetic lead compounds due to its diverse innate biological activity. Additionally, benzoflavone is known to induce xenobiotic-metabolizing enzyme activity, as well as have potent chemopreventive activity. Therefore, the combined structure of these two compounds should be useful for the discovery of new and/or increased biological activity. In this study, a chalcone derivative, 2'-hydroxy-2,4,6-trimethoxy-5',6'-naphthochalcone (HMNC-74), was synthesized, and its anticancer activity was tested in the HCT116 human colon cancer cell line. An in silico docking study showed that HMNC-74 binds to tubulin. HMNC-74 exhibited the inhibition of clonogenicity of HCT116 cells and cell cycle arrest at the G2/M phase, followed by induction of apoptosis through, at least in part, p53-dependent caspase-7 activation. The results of this study show that HMNC-74 may be an effective chemotherapeutic agent.
Lee, Jeong-Ho,Lee, Kicheol,Lee, Da Hyun,Shin, Soon Young,Yong, Yeonjoong,Lee, Young Han 한국응용생명화학회 2015 Applied Biological Chemistry (Appl Biol Chem) Vol.58 No.4
The invasive potential of malignant tumor cells is critical for their metastasis. This study was undertaken to evaluate the anti-invasive activity of ${\beta}$-myrcene, a natural compound found in the essential oil from Pinus koraiensis cones (EOPC), in metastatic MDA-MB-231 human breast cancer cells. Among four major constituents that included ${\alpha}$-pinene, ${\beta}$-myrcene, 3-carene, and d-limonene, ${\beta}$-myrcene showed the most potent inhibition of tumor necrosis factor-${\alpha}$ ($TNF{\alpha}$)-induced nuclear factor ${\kappa}B$ (NF-${\kappa}B$) activity. Pretreatment with ${\beta}$-myrcene suppressed $TNF{\alpha}$-induced phosphorylation of inhibitor of ${\kappa}B$ kinase and NF-${\kappa}B$ as well as matrix metalloproteinase-9 (MMP-9) gene expression in a dose-dependent fashion. Furthermore, ${\beta}$-myrcene inhibited $TNF{\alpha}$-induced invasion of MDA-MB-231 cells as determined by three-dimensional spheroid invasion assays. These findings suggest that EOPC may promote anti-metastatic activity in breast cancer cells through its downregulation of NF-${\kappa}B$-mediated MMP-9 expression.
A Peptide Produced by Pseudomonas tolaasi, Tolaasin Binds to Metal Ions
Geunhyeong Jo,Doseok Hwang,Yoonkyung Woo,Younggiu Lee,Yeonjoong Yong,강경래,Jiye Hyun,Young-Kee Kim,Dong-Woon Kim,Yoongho Lim 한국응용생명화학회 2011 Applied Biological Chemistry (Appl Biol Chem) Vol.54 No.4
Brown blotch disease in mushrooms is caused by Pseudomonas tolaasin, which produces a peptide toxin, tolaasin I, and zinc ion inhibits the channel formed by tolaasin I. NMR experiments revealed that zinc, sodium, and calcium ions can bind to tolaasin I and their binding position on tolaasin I is the lactone ring.