Zhengyi Yang

Chinese Academy of Sciences, Peping, Beijing, China

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Publications (5)16.19 Total impact

  • Lei Ma · Zhengyi Yang · Chenjing Li · Zhiyuan Zhu · Xu Shen · Lihong Hu
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    ABSTRACT: According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A- and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC(50) = 0.27 μM).
    No preview · Article · Oct 2011 · Journal of Enzyme Inhibition and Medicinal Chemistry
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    Lirui Wang · Xu Wang · Jing Chen · Zhengyi Yang · Liang Yu · Lihong Hu · Xu Shen
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    ABSTRACT: Over-activation of TGFβ signaling pathway and uncontrolled cell proliferation of hepatic stellate cells (HSCs) play pivotal roles in liver fibrogenesis, while the protein serine/threonine phosphatase PP2Cα was reported to negatively regulate TGFβ signaling pathway and cell cycle. Our study aimed to investigate the role of PP2Cα in liver fibrogenesis. The effects of PP2Cα activation on liver fibrosis were investigated in human HSCs and primary rat HSCs in vitro using western blotting, real-time PCR, nuclear translocation, cell viability and cell cycle analyses. The antifibrogenic effects in carbon tetrachloride (CCl(4))- and bile duct ligation (BDL)-induced mice in vivo were assessed using biochemical, histological and immunohistochemical analyses. The results demonstrated that activation of PP2Cα by overexpression or the new discovered small molecular activator NPLC0393 terminated TGFβ-Smad3 and TGFβ-p38 signaling pathways, induced cell cycle arrest in HSCs and decreased α-smooth muscle actin (α-SMA) expression, collagen deposition and hepatic hydroxyproline (HYP) level in CCl(4)- and BDL-induced mice. Our findings suggested that PP2Cα activation might be an attractive new strategy for treating liver fibrosis while the small molecular activator NPLC0393 might represent a lead compound for antifibrogenic drug development. Moreover, our study might provide the first evidence for the role of PP2C family members in the fibrotic disease.
    Full-text · Article · Dec 2010 · PLoS ONE
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    ABSTRACT: J. Neurochem. (2010) 114, 374–385. Alzheimer’s disease (AD) characterizes a progressive neurodegenerative disorder of the brain, while AD patients are afflicted with irreversible loss of neurons and further the intellectual abilities including memory and reasoning. One of the typical hallmarks of AD is the deposition of senile plaque that is contributed mainly by amyloid-β (Aβ), whose production is initiated by beta-site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1). Inhibition of BACE1 is thereby regarded as an attractive strategy for anti-AD drug discovery. Here, we reported that the natural product 2,2′,4′-trihydroxychalcone (TDC) from Glycyrrhiza glabra functioned as a specific non-competitive inhibitor against BACE1 enzyme, and potently repressed β-cleavage of APP and production of Aβ in human embryo kidney cells-APPswe cells. Moreover, the amelioration ability of this compound against the in vivo memory impairment was further evaluated by APP-PS1 double transgenic mice model. It is discovered that treatment of 9 mg/kg/day of TDC could obviously decrease Aβ production and Aβ plaque formation, while efficiently improve the memory impairment based on Morris water maze test. Our findings thus demonstrated that the natural product TDC as a new BACE1 inhibitor could ameliorate memory impairment in mice, and is expected to be potentially used as a lead compound for further anti-AD reagent development.
    Full-text · Article · Jul 2010 · Journal of Neurochemistry
  • Zhengyi Yang · Qiuqun Chen · Lihong Hu
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    ABSTRACT: Triterpene saponins 1-8 were isolated from the aerial parts of Gynostemma pubescens. Among them, compounds 1-4, 8 possess carboxylic groups at both C-21 and C-29, 5 contains a carboxylic group at C-21 and an aldehyde function at C-29, whereas 6 and 7 contain carboxylic groups at C-21 and hydroxymethylene groups at C-29. Their structural elucidation was accomplished by extensive spectroscopic methods including application of 1D (1H, (13)C, (13)C DEPT) and 2D NMR experiments (HMQC, HMBC, HSQC), HRESIMS analysis, as well as by chemical degradation.
    No preview · Article · Aug 2007 · Phytochemistry
  • Feng Yin · Yinan Zhang · Zhengyi Yang · Qiuqun Cheng · Lihong Hu
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    ABSTRACT: Six new dammarane glycosides (1-6) and four known compounds, rutin, kaempferol, quercetin, and linalool 3-O-beta-D-glucopyranoside, were isolated from an ethanol extract of the aerial parts of Gynostemma cardiospermum. The structures of 1-6 were elucidated by 1D and 2D NMR spectroscopic interpretation as well as by chemical degradation. Triterpene aglycons containing carbonyl groups at both C-21 and C-28, as found in compounds 1-5, are being reported in the family Cucurbitaceae for the first time.
    No preview · Article · Nov 2006 · Journal of Natural Products

Publication Stats

60 Citations
16.19 Total Impact Points


  • 2006-2011
    • Chinese Academy of Sciences
      • • Research Center for Modernization of Traditional Chinese Medicine
      • • State Key Laboratory of Drug Research
      Peping, Beijing, China