Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
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Volume 8 , Issue 5
Showing 1-7 articles out of 7 articles from the selected issue
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Reviews
  • Wei Zhang, Tianqiang Song
    Volume 8 (2014) Issue 5 Pages 194-200
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    Colorectal cancer liver metastases (CRLM) are common and found in almost 50% of patients with colorectal cancer. Surgical resection has proved to be the most effective therapy for metastatic colorectal cancer isolated to the liver and has yielded long term survival. However, recurrence frequently occurs within the remaining liver as well as at extra-hepatic sites. The role of adjuvant therapy has been investigated in many studies but has still been controversial until now. This review examines the incorporation of adjuvant systemic chemotherapy, regional chemotherapy with hepatic arterial infusion and molecular targeted therapy following liver resection for patients with CRLM, and summarized the advantage and adverse effects for these treatments. Finally, we propose the prospective of future adjuvant treatments to further improve prognosis.
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  • Dongliang Wang, Wenwen Ru, Yunpeng Xu, Jianling Zhang, Xianxian He, Gu ...
    Volume 8 (2014) Issue 5 Pages 201-207
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    In China, Colla corii asini is a health-care food and traditional Chinese medicine widely used in life-nourishing and clinical hematic antanemic therapy for more than 2,000 years. In this paper we compiled the chemical constituents isolated and detected from Colla corii asini including amino acids, proteins/gelatins, polysaccharides, volatile substances, inorganic substances, etc. Meanwhile we investigated the biological activities of Colla corii asini, which have been reported over the past few decades, including, hematologic diseases inhibitory activities, anti-aging activity, antitumor activity, immunomodulatory activity, bone repair activity, anti-inflammatory activity, antifatigue activity, etc. However, few reports on the relationships between the chemical constituents and bioactivities have been found, further studies of Colla corii asini are still necessary to facilitate research and development in the future.
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Brief Reports
  • Heng Xue, Qingyan Xu, Chunhua Lu, Yuemao Shen
    Volume 8 (2014) Issue 5 Pages 208-211
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    Isotryptoquivaline F (1) was isolated from Aspergillus sp. CM9a, an endophytic fungus of Cephalotaxus mannii. The structure was elucidated by extensively 1D and 2D NMR and HR ESI MS spectroscopy. It has good TNF-α antagonistic effect, and can be used for anti-inflammatory drugs or other bioactive leading drugs.
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  • Takuya Nakatsubo, Saori Nishitani, Yuko Kikuchi, Satoshi Iida, Kana Ya ...
    Volume 8 (2014) Issue 5 Pages 212-217
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    In eukaryotes, the Mediator complex is an essential transcriptional cofactor of RNA polymerase II (Pol II). In humans, it contains up to 30 subunits and consists of four modules: head, middle, tail, and CDK/Cyclin. One of the subunits, MED15, is located in the tail module, and was initially identified as Gal11 in budding yeast, where it plays an essential role in the transcriptional regulation of galactose metabolism with the potent transcriptional activator Gal4. For this reason, we investigated the function of the human MED15 subunit (hMED15) in transcriptional activation. First, we measured the effect of hMED15 knockdown on cell growth in HeLa cells. The growth rate was greatly reduced. By immunostaining, we observed the colocalization of hMED15 with the general transcription factors TFIIE and TFIIH in the nucleus. We measured the effects of siRNA-mediated knockdown of hMED15 on transcriptional activation using two different transcriptional activators, VP16 and SREBP1a. Treatment with siRNAs reduced transcriptional activation, and this reduction could be rescued by overexpression of HA/Flag-tagged, wild-type hMED15. To investigate hMED15 localization, we treated human MCF-7 cells with the MDM2 inhibitor Nutlin-3, thus inducing p21 transcription. We found that hMED15 localized to both the p53 binding site and the p21 promoter region, along with TFIIE and TFIIH. These results indicate that hMED15 promotes transcriptional activation.
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Original Articles
  • Haizhen Li, Chao Li, Tao Shen, Lijuan Zhao, Dongmei Ren
    Volume 8 (2014) Issue 5 Pages 218-224
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    Eriodictyol is a flavanone well-known for its antioxidative activity. Due to a chiral carbon atom in position C-2, eriodictyol always exist in racemic form. In order to study the a Chiral Amylose-C column as chiral stationary phase. Online coupling HPLC-circular dichroism (CD) method was used for the determination of elution order and the absolute configurations of the two eluates. The protective effects of racemic and enantiomeric eriodictyol against H2O2-induced cytotoxicity with EA.hy926 cells were tested. The results showed that the two enantiomers of eriodictyol and the corresponding racemate were equipotent, suggesting that the configuration of the C-2 chiral center does not influence the cytoprotective activity against H2O2-induced oxidative stress in EA.hy926 cells.
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Commentary
  • Xiaoyang Li, Wenfang Xu
    Volume 8 (2014) Issue 5 Pages 225-228
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    Histone deacetylases (HDACs) have attracted a great deal of interest as anticancer drug targets, and many HDAC inhibitors (HDACIs) have displayed clinical efficacy in treating specific tumors. However, all of these agents have significant toxicity, including fatigue, nausea, vomiting, thrombocytopenia, and neutropenia. Thus, increased effort is being directed toward developing selective HDACIs that are tolerated better and cause fewer adverse reactions. This article focuses mainly on the N-hydroxycinnamamide-based HDAC 1/3 dual inhibitors, and this article outlines the anticancer potential of these inhibitors. Since selective HDAC1/3 inhibitors may cause fewer adverse reactions than selective pan-HDACIs and selective Class Ι inhibitors in clinical settings, further study of their mechanism of anticancer activity and optimization of their structure is warranted.
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  • Jianjun Gao, Lin Yin
    Volume 8 (2014) Issue 5 Pages 229-231
    Released: November 08, 2014
    JOURNALS FREE ACCESS
    The Ebola outbreak in West Africa this year is causing global panic. The high mortality of this disease is largely due to lack of effective preventive vaccines or therapeutic drugs. Realizing the gravity and urgency in controlling the epidemic, governments and drug companies across the world have taken many strong measures to speed up the process of drug development. Several representative candidate drugs that demonstrate potent anti-Ebola activity in preclinical studies have been pushed forward to higher research stages to obtain an earlier official license. It is expected that proven preventive or therapeutic regimens could be established in the near future.
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