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This research explored the synergistic effects and the mechanism of parthenolide (PTL) and vorinostat (suberoylanilide hydroxamic acid, SAHA) on the proliferation of A549 non-small cell lung cancer cells. The combination effect of PTL and SAHA was detected by cell counting kit-8 (CCK-8) and colony formation assays. Scratch test was performed to detect cell migration. Annexin V-fluorescein isothiocyanate isomer/propidium iodide (FITC/PI) flow cytometry and Western blot analyses were used to determine cell apoptosis and its mechanism. The results showed that combination of PTL and SAHA inhibited the proliferation and migration of A549 with a synergistic effect compared to the single-drug groups. The combination of PTL and SAHA had synergistic effect to induce cell apoptosis by regulating p53 and c-myc pathways, and affected the expression levels of poly ADP-ribose polymerase (PARP), cysteinyl aspartate specific proteinase (caspase)-9, and caspase-3. Taken together, this study shows that combination of PTL and SAHA has synergistic effect, induces cell apoptosis and inhibits A549 proliferation, which is likely to be a novel strategy for the treatment of non-small cell lung cancer.
RESUMO
This research investigated the effect of parthenolide on the proliferation and migration of human breast cancer cells and explored the molecular mechanism of that effect. Surface plasmon resonance and fluorescence resonance energy transfer melting were used to detect the binding and stabilizing ability of PTL and G-quadruplex. MTT assays were used to determine the effect of PTL on the proliferation of MCF-7 breast cancer cells. A wound healing assay was performed to detect the migration of MCF-7. The results indicate that PTL shows good binding and stabilizing activities with c-myc G-quadruplex with a KD = 13.1 μmol·L-1. PTL inhibited the proliferation of MCF-7 cells with an IC50 of 21.3 μmol·L-1 (24 h), 14.5 μmol·L-1 (48 h) and 9.1 μmol·L-1 (72 h). PTL inhibited MCF-7 breast cancer cell proliferation and migration and down-regulated the transcription and expression level of c-myc by targeting G-quadruplex.
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Objective::Camptosorus sibiricus is a kind of herbal medicine and famous folk medicine. However, the bioactivities or pharmacological effects of the C. sibiricus remain to be unclear. Therefore, it is necessary to make a systematic study on chemical constituents from C. sibiricus, so as to further study its potential medicinal value, and provide certain chemical basis and foundation for the comprehensive development and the search for pharmacological activity. Method::Various column chromatographic technologies, (silica gel, Sephadex LH-20 and ODS column chromatography) as well as HPLC were adopted to separate chemical constituents of C. sibiricus extract. The structure of the purified compounds was elucidated by nuclear magnetic resonance (NMR) and high-resolution electrospray ionization-mass spectrometry (HR-ESI-MS). Result::Totally 10 compounds have been isolated from water extract of C. sibiricus. By spectroscopic methods, they were elucidated as 7-dien-3-on-9-O-β-D-glucoside (1), bridelionoside F (2), (3R, 5S, 6S, 7E, 9S)-megastigm, an-7-ene-3, 5, 6, 9-tetrol 9-O-β-D-glucopyranoside (3), (6S, 7E, 9R)-roseoside (4), (3S, 5S, 6R, 9R)-3-hydroxy-5, 6-epoxy-β-ionol-9-O-β-glucopyranoside (5), 6, 9-dihydroxy-4, 7-megastigmadien-3-one (6), (3R, 6R, 7E, 9R)-3, 9-dihydroxy-4, elaphoside A (7), ptelatoside-A (8), n-butyl-a-β-D-fructofuranoside (9), dibutylphthalate(10)based on physical and chemical properties. Conclusion::All compounds were obtained from C. sibiricus for the first time. The discovery of these compounds further enriched the chemical constituents of C. sibiricus, and provided experimental and scientific basis for the comprehensive development and utilization of C. sibiricus.
RESUMO
Previous studies have demonstrated that the Chinese medicine paeoniflorin, derived from the Ranunculaceae plant peony, peony, purple peony root, was able to have anti-inflammatory, anti-ulcer, anti-hypersusceptibility and anti-oxidation activity. In order to elucidate the pesticide effect and the mechanisms by which paeoniflorin exerts its effect of anti-inflammation and immunoregulation on oxazolone-induced colitic mice, disease activity index (DAI) and histological grading of colitis (HGC) were evaluated in animal model. Moreover, the expressions of HBD-2, IL-6 and IL-10 of mice with experimental colitis were observed with immunohistochemistry and RT-PCR in this study. Results showed that DAI and HGC of oxazolone control group was significantly higher than that of normal control group, and that paeoniflorin groups and 5-ASA group, compared with oxazolone control group, could alleviate the symptoms and histological damages of colitic mice (P < 0.05, P < 0.01). The expression of HBD-2 and IL-6 cytokine on the colon of colitic mice was higher than that of normal control, paeoniflorin and 5-ASA groups (P < 0.05, P < 0.01), but the expression of IL-10 is lower than that of normal control, paeoniflorin and 5-ASA groups (P < 0.05, P < 0.01). The positive correlations were demonstrated between the expression of (HBD-2 and IL-6) and DAI (Pearson r = 0.728, Pearson r = 0.758, P < 0.01, respectively), (HBD-2 and IL-6) and HGC (Pearson r = 0.819, Pearson r = 0.825, P < 0.01, respectively), whereas, the negative correlations were demonstrated between the expression of IL-10 and DAI (Pearson r = -0.789, P < 0.01), IL-10 and HGC (Pearson r = -0.725, P < 0.01). It can be concluded that to some extent paeoniflorin effectively alleviate the symptoms of oxazolone-induced colitis through regulating the expression of HBD-2, IL-6 and IL-10.