35 research outputs found

    Anti-Hepatitis C Virus Dinorditerpenes from the Roots of <i>Flueggea virosa</i>

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    Along with four known terpenoids (<b>1</b>–<b>4</b>), eight new dinorditerpenes (<b>5</b>–<b>12</b>) were isolated and identified from the roots of <i>Flueggea virosa</i>. The absolute configurations of <b>4</b>–<b>6</b> were determined by the Mosher’s method, and that of <b>5</b> was confirmed by single-crystal X-ray diffraction analysis. Using the hepatitis C virus cell culture infection system, compounds <b>1</b>, <b>3</b>, <b>11</b>, and <b>12</b> exhibited significant anti-HCV activity with EC<sub>50</sub> values of 5.6, 5.0, 7.5, and 6.6 μM, respectively. Compounds <b>11</b> and <b>12</b> were nontoxic toward the tested Huh7.5 cell lines

    Toxicological effects of NCKU-21, a phenanthrene derivative, on cell growth and migration of A549 and CL1-5 human lung adenocarcinoma cells

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    <div><p>Background</p><p>Chemotherapy insensitivity continues to pose significant challenges for treating non-small cell lung cancer (NSCLC). The purposes of this study were to investigate whether 3,6-dimethoxy-1,4,5,8-phenanthrenetetraone (NCKU-21) has potential activity to induce effective toxicological effects in different ethnic NSCLC cell lines, A549 and CL1-5 cells, and to examine its anticancer mechanisms.</p><p>Methods</p><p>Mitochondrial metabolic activity and the cell-cycle distribution were analyzed using an MTT assay and flow cytometry in NCKU-21-treated cells. NCKU-21-induced cell apoptosis was verified by Annexin V-FITC/propidium iodide (PI) double-staining and measurement of caspase-3 activity. Western blotting and wound-healing assays were applied to respectively evaluate regulation of signaling pathways and cell migration by NCKU-21. Molecular interactions between target proteins and NCKU-21 were predicted and performed by molecular docking. A colorimetric screening assay kit was used to evaluate potential regulation of matrix metalloproteinase-9 (MMP-9) activity by NCKU-21.</p><p>Results</p><p>Results indicated that NCKU-21 markedly induced cytotoxic effects that reduced cell viability <i>via</i> cell apoptosis in tested NSCLC cells. Activation of AMP-activated protein kinase (AMPK) and p53 protein expression also increased in both NSCLC cell lines stimulated with NCKU-21. However, repression of PI3K-AKT activation by NCKU-21 was found in CL1-5 cells but not in A549 cells. In addition, increases in phosphatidylserine externalization and caspase-3 activity also confirmed the apoptotic effect of NCKU-21 in both NSCLC cell lines. Moreover, cell migration and translational levels of the gelatinases, MMP-2 and MMP-9, were obviously reduced in both NSCLC cell lines after incubation with NCKU-21. Experimental data obtained from molecular docking suggested that NCKU-21 can bind to the catalytic pocket of MMP-9. However, the <i>in vitro</i> enzyme activity assay indicated that NCKU-21 has the potential to increase MMP-9 activity.</p><p>Conclusions</p><p>Our results suggest that NCKU-21 can effectively reduce cell migration and induce apoptosis in A549 and CL1-5 cells, the toxicological effects of which may be partly modulated through PI3K-AKT inhibition, AMPK activation, an increase in the p53 protein, and gelatinase inhibition.</p></div

    Regulation of growth control-associated proteins by NCKU-21 in A549 and CL1-5 cells.

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    <p>Expressions and activation levels of relative proteins were examined in A549 (A) and CL1-5 (B) cells after treatment with NCKU-21. Total and phosphorylated levels of the tested proteins were examined in cells treated with NCKU-21 for 24 hr and 30 min, respectively. * <i>P</i> < 0.05 and ** <i>P</i> < 0.01, compared to the control group (without NCKU-21 treatment).</p

    Chemical Constituents of the Rhizomes of <i>Bletilla formosana</i> and Their Potential Anti-inflammatory Activity

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    Nine new phenanthrenes (<b>1</b>–<b>9</b>) and a new benzyl glycoside (<b>10</b>) together with 45 known compounds were isolated from the rhizomes of <i>Bletilla formosana</i>. The structures of <b>1</b>–<b>10</b> were elucidated primarily on the basis of their 1D and 2D NMR spectroscopic data. Most of the isolated compounds were evaluated for their anti-inflammatory activities. The results showed that IC<sub>50</sub> values for the inhibition of superoxide anion generation and elastase release ranged from 0.2 to 6.5 μM and 0.3 to 5.7 μM, respectively. Structure–activity relationships of the isolated compounds were also investigated. The inhibitory potencies were determined as phenanthrenes > bibenzyls > biphenanthrenes

    Inhibitory effect of NCKU-21 on cell migration of A549 and CL1-5 cells.

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    <p>Cell migration levels were examined using a wound-healing assay in A549 and CL1-5 cells treated with NCKU-21 for 18 hr. Pictures were acquired from A549 (A) and CL1-5 (C) cells after 0 and 18 hr of NCKU-21 treatment. Statistical results obtained from A549 (B) and CL1-5 (D) cells are presented as histograms. Scale bar: 500 μm. ** <i>P</i> < 0.01, compared to that of the group without NCKU-21 treatment.</p

    Regulation of the metabolic activity and cell-cycle distribution of NCKU-21.

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    <p>Metabolic activity (A and B) and cell-cycle distribution (C and D) of non-small cell lung cancer (NSCLC) cells (A549 and CL1-5) examined at 24 hr after treatment with NCKU-21. NCKU-21 at a concentration of 2 μM was used to analyze the cell-cycle distribution. * <i>P</i> < 0.05 and ** <i>P</i> < 0.01, compared to the control group (without NCKU-21 treatment).</p

    Regulation of cell migration-associated proteins by NCKU-21 in A549 and CL1-5 cells.

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    <p>Protein expressions of matrix metalloproteinase-2 (MMP-2) and MMP-9 were analyzed in A549 (A) and CL1-5 (B) cells treated with NCKU-21 for 24 hr. * <i>P</i> < 0.05 and ** <i>P</i> < 0.01, compared to the control group (without NCKU-21 treatment).</p

    Regulation of phosphatidylserine (PS) externalization and caspase-3 activity by NCKU-21 in A549 and CL1-5 cells.

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    <p>Membrane translocation of PS was determined by staining with Annexin V-FITC/propidium iodide (PI) and then analyzed by flow cytometry in A549 and CL1-5 cells treated with 2 μM of NCKU-21 for 24 hr. Data are displayed as a representative dot plot and statistical histogram in A549 (A and B) and CL1-5 (C and D) cells. Relative caspase-3 activity was measured in A549 (E) and CL1-5 (F) cells treated with 2 μM of NCKU-21 for 24 hr. ** <i>P</i> < 0.01, compared to the control group (without NCKU-21 treatment).</p

    Regulation of human matrix metalloproteinase-9 (MMP-9) activity by NCKU-21.

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    <p>NC (negative control), the group under the original reaction condition without MMP-9 added; PC (positive control), the group under the original reaction condition with no inhibitors or test compounds added; ARP101, PC group treated with 2 μM ARP101; Vehicle, PC group treated with 0.6% DMSO; NCKU-21, PC group treated with 2 μM NCKU-21. ** <i>P</i> < 0.01 compared to the control group.</p
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