Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
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Volume 8 , Issue 3
Showing 1-6 articles out of 6 articles from the selected issue
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Review
  • Keming Zhang, Peipei Song, Jianjun Gao, Gaohua Li, Xin Zhao, Shaogeng ...
    Volume 8 (2014) Issue 3 Pages 102-109
    Released: July 17, 2014
    JOURNALS FREE ACCESS
    China has 50% of the worldwide hepatocellular carcinoma (HCC) cases, and the HBV-related cases accounts for approximately 85%. Over the past few decades, although a series of standardized management methods for HCC has been implemented in China, most HCC patient in China still suffered from advanced-stage disease, in consequence, reducing the opportunity of curable treatment that can be offered to achieve long-term disease-free survival for HCC patient. Accordingly, strategies including screening and diagnose HCC at an earlier stage are urgently needed in China. In this study, the current status, challenges, and prospects of early detection of HCC in China have been analyzed. The result indicated the need for using multi serum biomarkers for early HCC detection. During the past ten years, the research on the clinical usefulness of novel serum biomarkers of des-γ-carboxy-prothrombin (DCP), Dickkopf-1 (DKK1) and Midkine (MDK) in early HCC detection for Chinese patients found that the novel serum biomarker can complete the measurement of α-fetoprotein (AFP) in the diagnosis process of HCC, particularly for the patient with negative AFP with/or at an early stage. More large-scale, multi-center studies are expected to be performed in China to provide further evidence, and using novel and reliable serum biomarkers to complement AFP as a new trend is expected to be extensively used in clinical practice to facilitate early detection for those patients with HCC in China.
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Brief Report
  • Pengzhan Li, Yanmei Tan, Guyue Liu, Yang Liu, Jianzhen Liu, Yanzhen Yi ...
    Volume 8 (2014) Issue 3 Pages 110-116
    Released: July 17, 2014
    JOURNALS FREE ACCESS
    A new series of 1,5-disubstituted indolin-2,3-diones was synthesized and their inhibition of the growth of a human acute promyelocytic leukemia (HL-60) cell line was evaluated. These compounds had promising inhibition of HL-60 cell growth in vitro. Results indicated that compounds with a benzyl substituent at the N-1 position on the indolin-2,3-dione ring had more potent antiproliferative activity than those with a (4-fluorobenzyl) amino-2-oxoethyl substituent at the N-1 position. Among the compounds synthesized, compound 8l inhibited half of cell growth at a concentration of 0.07 μM and compound 8p did so at a concentration of 0.14 μM. These compounds may serve as lead compounds for further optimization in order to develop novel anticancer agents.
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Original Articles
  • Fangyuan Shi, Zongtao Li, Lingjin Kong, Yuanchao Xie, Tao Zhang, Wenfa ...
    Volume 8 (2014) Issue 3 Pages 117-120
    Released: July 17, 2014
    JOURNALS FREE ACCESS
    As a RNA polymerase inhibitor, 6-fluoro-3-hydroxypyrazine-2-carboxamide commercially named favipiravir has been proved to have potent inhibitory activity against RNA viruses in vitro and in vivo. A four-step synthesis of the compound is described in this article, amidation, nitrification, reduction and fluorination with an overall yield of about 8%. In addition, we reported the crystal structure of the title compound. The molecule is almost planar and the intramolecular O−H•••O hydrogen bond makes a 6-member ring. In the crystal, molecules are packing governed by both hydrogen bonds and stacking interactions.
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  • Chan Hum Park, Dong Young Rhyu, Jeong Sook Noh, Chul Min Park, Takako ...
    Volume 8 (2014) Issue 3 Pages 121-131
    Released: July 17, 2014
    JOURNALS FREE ACCESS
    The Chinese prescription Kangen-karyu, comprised of six crude drugs, has received much attention due to its numerous biological activities. The present study was conducted to examine whether Kangen-karyu has an ameliorative effect on dyslipidemia. The effect of Kangen-karyu was evaluated using 3T3-L1 adipocytes, and also db/db mice as an experimental model for diabetic dyslipidemia. Kangen-karyu significantly inhibited adipocyte differentiation and lipid accumulation. Kangen-karyu also down-regulated the mRNA levels of peroxisome proliferator-activated receptor (PPAR)γ, sterol regulatory element-binding protein (SREBP)-1c, and fatty acid synthase, and the protein levels of aP2 and PPARγ, which indicates that Kangen-karyu inhibited adipogenesis during adipocyte differentiation, and may have potential anti-dyslipidemia effects. In addition, the administration of Kangen-karyu reduced hyperlipidemia in db/db type 2 diabetic mice through a decline in the serum levels of lipids, and an improvement of lipoprotein profiles. The enhanced hepatic triglyceride level of the db/db mice was significantly reduced by Kangen-karyu administration through the down-regulation of SREBP-1 and lipogenic enzymes in the liver. These findings indicate that Kangen-karyu exerts anti-dyslipidemia effects in adipocytes and type 2 diabetic db/db mice.
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Case Report
Commentary
  • Zhigang Wang, Peipei Song, Jufeng Xia, Yoshinori Inagaki, Wei Tang, No ...
    Volume 8 (2014) Issue 3 Pages 134-138
    Released: July 17, 2014
    JOURNALS FREE ACCESS
    Hepatocellular carcinoma (HCC) is the most common type of liver cancer. Hepatic resection has long been considered a main treatment option for HCC, but the high rate of recurrence after hepatic resection remains a problem that impacts the prognosis and survival of patients with HCC. Thus, clarifying the factors for survival and risk factors for tumor recurrence after hepatic resection is crucial. Imaging studies are currently emphasized before selecting a treatment and predicting the prognosis for patients with HCC. Recently, laboratory testing of des-gamma-carboxyprothrombin (DCP), alpha-fetoprotein (AFP), indocyanine green 15 min after administration (ICG-R15), and γ-glutamyl transpeptidase (γ-GTP) has garnered attention as a way to select treatment and predict the prognosis of patients with HCC. γ-GTP in particular has critical clinical significance as an indicator of prognosis. This indicator helps to predict prognosis and it helps with the selection of further treatment, as was revealed by studies based on different subgroups of patients published in the past 5 years. The reason for the association between γ-GTP and early recurrence and poor survival is being investigated. Preoperative laboratory results (DCP, AFP, ICG-R15, and γ-GTP) may warrant attention and need to be fully evaluated before selecting a treatment and predicting prognosis in order to improve the prognosis for patients with HCC.
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