Jun Du

Publications (5)17.45 Total impact

• Article: 2a, a novel curcumin analogue, sensitizes cisplatin-resistant A549 cells to cisplatin by inhibiting thioredoxin reductase concomitant oxidative stress damage.

  Binhua Zhou, Jianing Huang, Yinglin Zuo, Baojian Li, Qiang Guo, Baicheng Cui, Weiyan Shao, Jun Du, Xianzhang Bu
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  ABSTRACT: (1E,4Z,6E)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(5-methylfuran-2-yl)hepta-1,4,6-trien-3-one (2a), a novel curcumin analogue, was previously synthesized in our laboratory as a potential thioredoxin reductase (TrxR) inhibitor with excellent growth inhibitory effects on several TrxR over-expressed cancer cells. In this study, our further studies show that 2a is able to inhibit the growth of cisplatin-resistant A549 (A549/CDDP) cells much more effectively in a dose-dependent manner than that of A549 cells in antiproliferative activity experiments. Moreover, 2a-pretreated A549/CDDP cells are sensitive to cisplatin treatment, which is accompanied by the inhibition of TrxR activity in A549/CDDP cells. As a consequence of targeting TrxR, 2a in turn remarkably up-regulates intracellular reactive oxygen species level, depletes glutathione (GSH), and reduces the GSH/GSSG ratio, suggesting that the intracellular redox balance is shifted to a more oxidative state. Consequently, concomitant with the cell growth inhibition of 2a, apoptosis is induced by 2a probably through increased oxidative stress in A549/CDDP cells. In conclusion, these observations demonstrated that TrxR inhibitors would be promising drugs to achieve a successful combinatory or single cancer chemotherapy.
  European journal of pharmacology 03/2013; · 2.59 Impact Factor
• Article: Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFα-induced nuclear factor-κB activation inhibition.

  Yinglin Zuo, Yi Yu, Shuni Wang, Weiyan Shao, Binhua Zhou, Li Lin, Zhuoyu Luo, Ruogu Huang, Jun Du, Xianzhang Bu
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  ABSTRACT: A series of biaryl-based chalcones were designed as a combination of the natural chalcone and biphenyl moieties, and synthesized by two step chemistry involving Knoevenagel reaction and microwave assistant Suzuki coupling. Sulforhodamine B (SRB) assay was performed to evaluate the cell viability inhibitory abilities of these compounds against five cancer cell lines (A549, CNE2, SW480, MCF-7, and HepG2) from different tissues. Their Nuclear Factor-κB (NF-κB) nuclear translocation inhibitory activities were further investigated by High Content Analysis (HCA) based assay. Most of the compounds showed moderate to strong anticancer and NF-κB nuclear translocation inhibition activities and potent compounds were found.
  European journal of medicinal chemistry 02/2012; 50:393-404. · 3.27 Impact Factor
• Article: Synthesis of Multi‐Functionalized Chromeno[2,3‐c]pyrrol‐9(2H)‐ones: Investigation and Application of Baker–Venkataraman Rearrangement Involved Reactions Catalyzed by 4‐(Dimethylamino)pyridine

  Yanjun Yu, Yun Hu, Weiyan Shao, Jianing Huang, Yinglin Zuo, Yingpeng Huo, Linkun An, Jun Du, Xianzhang Bu
  Annalen der Chemie und Pharmacie 06/2011; 2011(24):4551 - 4563. · 3.10 Impact Factor
• Article: New fluorescent trans-dihydrofluoren-3-ones from aldol-Robinson annulation-regioselective addition involved one-pot reaction.

  Yingpeng Huo, Xu Qiu, Weiyan Shao, Jianing Huang, Yanjun Yu, Yinglin Zuo, Linkun An, Jun Du, Xianzhang Bu
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  ABSTRACT: An unexpected discovery of new trans-4-acetyl-1,9-dimethyl-4,4a-dihydro-3H-fluoren-3-ones from one pot reactions of benzaldehydes and acetylacetone is described. The synthetic mechanism and stereochemistry were discussed. These new derivatives exhibit good fluorescent properties in solutions.
  Organic & Biomolecular Chemistry 11/2010; 8(22):5048-52. · 3.70 Impact Factor
• Article: Synthesis and Identification of New 4-Arylidene Curcumin Analogues as Potential Anticancer Agents Targeting Nuclear Factor-κB Signaling Pathway.

  Xu Qiu, Yuhong Du, Bin Lou, Yinglin Zuo, Weiyan Shao, Yingpeng Huo, Jianing Huang, Yanjun Yu, Binhua Zhou, Jun Du, Haian Fu, Xianzhang Bu
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  ABSTRACT: A series of curcumin analogues including new 4-arylidene curcumin analogues (4-arylidene-1,7-bisarylhepta-1,6-diene-3,5-diones) were synthesized. Cell growth inhibition assays revealed that most 4-arylidene curcumin analogues can effectively decrease the growth of a panel of lung cancer cells at submicromolar and low micromolar concentrations. High content analysis technology coupled with biochemical studies showed that this new class of 4-arylidene curcumin analogues exhibits significantly improved NF-κB inhibition activity over the parent compound curcumin, at least in part by inhibiting IκB phosphorylation and degradation via IKK blockage; selected 4-arylidene curcumin analogues also reduced the tumorigenic potential of cancer cells in a clonogenic assay.
  Journal of Medicinal Chemistry 11/2010; · 4.80 Impact Factor