Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
Volume 7, Issue 6
Displaying 1-7 of 7 articles from this issue
Reviews
  • Fanghua Qi, Zhixue Wang, Pingping Cai, Lin Zhao, Jianjun Gao, Norihiro ...
    2013 Volume 7 Issue 6 Pages 212-224
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    Since the significant public health hazard of Hepatitis B virus (HBV) infection and obvious drug resistance and dose-dependent side effects for common antiviral agents (e.g., interferonalpha, lamivudine, and adefovir), continuous development of agents to treat HBV infection is urgently needed. Traditional Chinese medicine (TCM) is an established segment of the health care system in China. Currently, it is widely used for chronic hepatitis B (CHB) in China and many parts of the world. Over a long period of time in clinical practice and in basic research progress, the effectiveness and beneficial contribution of TCM on CHB have been gradually known and confirmed. Based upon our review of related papers and because of our prior knowledge and experience, we have selected some Chinese medicines, including Chinese herbal formulas (e.g., Xiao-Chai-Hu-Tang, Xiao-Yao-San, and LongDan-Xie-Gan-Tang), single herbs (e.g., Phyllanthus niruri, Radix astragali, Polygonum cuspidatum, Rheum palmatum, and Salvia miltiorrhiza) and related active compounds (e.g., wogonin, artesunate, saikosaponin, astragaloside IV, and chrysophanol 8-O-beta-D glucoside) and Chinese medicine preparations (e.g., silymarin, silibinin, kushenin, and cinobufacini), which seem effective and worthy of additional and indepth study in treating CHB, and we have given them a brief review. We conclude that these Chinese herbal medicines exhibit significant anti-HBV activities with improved liver function, and enhanced HBeAg and HBsAg sero-conversion rates as well as HBV DNA clearance rates in HepG2 2.2.15 cells, DHBV models, or patients with CHB. We hope this review will contribute to an understanding of TCM and related active compounds as an effective treatment for CHB and provide useful information for the development of more effective antiviral drugs.
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  • Xiaolei Zhao, Jinxiang Han
    2013 Volume 7 Issue 6 Pages 225-232
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    Traditional Chinese Medicine (TCM) developed based on ancient Chinese philosophy. Its characteristics include abstract theories, fuzzy concepts, subjective diagnostic methods and it lacks clarity, and rigor as well as vindication from modern sciences, which makes development of TCM remain stagnant. Thus, how to free the theory of TCM from heavy philosophy to achieve separation of medicine and philosophy, and to use the contemporary cuttingedge science and technology to transform the theory of TCM and then to achieve its scientific paradigm shift, is a way for TCM to get out of the woods. This article, focusing on the problems existing in the development of the modernization of TCM, introduces the concept, the connotation as well as the important role of Quantum TCM in the modernization of TCM. Additionally, based on the view that the body's electromagnetic radiation can characterize the human "Qi" in TCM, we discuss several experimental technology systems for the diagnosis of Quantum TCM in detail. By analyzing and comparing these technology systems, we come to the conclusion that the biophoton analytical technology (BPAT) is more worthy of further study in building the experimental technology system for the diagnosis of Quantum TCM.
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  • Penghui Yang, Lei Zhang, Yingjie Zhang, Jian Zhang, Wenfang Xu
    2013 Volume 7 Issue 6 Pages 233-242
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    Acetylation and deacetylation of histones are important in regulating gene expression and play a key role in modification of gene transcription. Specific HDACs isoforms can be regarded as a target for cancer therapy avoiding side-effects, HDAC6 with a unique physiological function and structure has become a hot issue recently. The unique isoform HDAC6 is involved in tumorigenesis, development and metastasis through tubulin, HSP90, invasin and ubiquitin-protein. Here we review the structure elements, biological function, and recent selective inhibitors of HDAC6, and study the structure-activity and structureselectivity relationship.
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Brief Report
  • Yong Han, Yaoyao Li, Yan Shen, Jie Li, Wenjun Li, Yuemao Shen
    2013 Volume 7 Issue 6 Pages 243-247
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    A novel pyrrolo[1,4]benzodiazepine antibiotic, designated oxoprothracarcin (3), was isolated from the marine strain Streptomyces sp. M10946 along with three known secondary metabolites, cyclo(D)-Pro-(D)-Val (1), cyclo(D)-Pro(D)-Leu (2), and limazepine A (4). The chemical structures of these substances were elucidated by spectroscopic analyses, including 1D- and 2D-NMR and ESI-MS. Antitumor and antibacterial assays indicated that compounds 1-4 weakly inhibit the growth of MDA-MB-231 and A549 cells. The isolation of compound 3 with a high yield (36 mg/10 L) indicated that this marine S. sp. M10946 may provide new lead compounds for structural modification and drug screening.
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Original Articles
  • Chunling Hu, Xiaozhi Peng, Yinpin Tang, Yanwen Liu
    2013 Volume 7 Issue 6 Pages 248-253
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    We previous identified the antifibrotic active ingredients from Carapax Trionycis as two peptides. Here, we synthesized these two peptides (peptide 1 and peptide 2) by a solid phase method and examined their effects on proliferation and activation of cultured hepatic stellate cells (HSC) which are the main ECM (extracellular matrix)-producing cells in fibrosis progression. We demonstrated that peptide 1 and peptide 2 significantly reduced HSC proliferation and activation in a dose dependent manner. Further, peptide 1 and peptide 2 could interfere with TGF-signaling by down-regulating Smad 3 phosphorylation. Thus, these synthetic peptides of Carapax Trionycis could inhibit proliferation and activation of HSC and might be used as a candidate for treatment of liver fibrosis.
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  • Toru Ichinose, Thommas Mutemi Musyoka, Ken Watanabe, Nobuyuki Kobayash ...
    2013 Volume 7 Issue 6 Pages 254-260
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    Betanodaviruses, members of the family Nodaviridae, are the causal agents of viral nervous necrosis (VNN) in many species of marine farmed fish. In the aquaculture industry, outbreaks of betanodavirus infection result in devastating damage and heavy economic losses. Although an urgent need exists to develop drugs against betanodavirus infection, there have been few reports about antibetanodavirus drugs. In this study, we examined the inhibitory effect of Oligonol, a purified phenolic extract from lychee fruit, on betanodavirus infection in fish cells. Oligonol significantly inhibited replication of betanodavirus (EC50 = 0.9-1.8 μg/mL) as shown by the reduction of the virus-induced cytopathogenic effect (CPE) and the protection of cells in the crystal violet staining assay. The inhibition was dose dependent. A time-of-addition assay indicated that Oligonol's action takes place at an early stage of the viral infection. According to an attachment inhibition assay, it is possible that Oligonol partially inhibits attachment of the virion to the cell. Our data show that Oligonol could serve as an antiviral agent against betanodavirus.
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  • Omar M. E. Abdel-Salam, Enayat A. Omara, Nadia A. Mohammed, Eman R. Yo ...
    2013 Volume 7 Issue 6 Pages 261-271
    Published: December 31, 2013
    Released on J-STAGE: March 17, 2014
    JOURNAL FREE ACCESS
    This study aimed to investigate the effect of cerebrolysin on oxidative stress in the brain and liver during systemic inflammation. Rats were intraperitoneally challenged with a single subseptic dose of lipopolysaccharide (LPS; 300 μg/kg) without or with cerebrolysin at doses of 21.5, 43 or 86 mg/kg. After 4 h, rats were euthanized and the brain and liver tissues were subjected to biochemical and histopathological analyses. Cerebrolysin revealed inhibitory effects on the elevation of lipid peroxidation and nitric oxide induced by LPS. In contrast, the decrease in reduced glutathione level and paraoxonase activity induced by LPS was attenuated by an injection of cerebrolysin in a dose-dependent manner. Moreover, cerebrolysin reduced LPS-induced activation of brain NF-κB and reversed LPS-induced decline of brain butyrylcholinesterase and acetylcholinesterase activities in a dose-dependent manner. Histopathological analyses revealed that neuronal damage and liver necrosis induced by LPS were ameliorated by cerebrolysin dosedependently. Cerebrolysin treatment dose-dependently attenuated LPS-induced expressions in cyclooxygenase 2, inducible nitric oxide synthase, and caspase-3 in the cortex or striatum as well as the liver. These results suggest that cerebrolysin treatment might have beneficial therapeutic effects in cerebral inflammation. Cerebrolysin might also prove of value in liver disease and this possibility requires further exploration.
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