Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
Volume 10 , Issue 6
Showing 1-10 articles out of 10 articles from the selected issue
Reviews
  • Qin-ge Ding,, Jie Zang, Shuai Gao, Qianwen Gao, Wenwen Duan, Xiaoyang ...
    2016 Volume 10 Issue 6 Pages 276-284
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: December 18, 2016
    JOURNALS FREE ACCESS

    Nitric oxide (NO) plays important roles in cardiovascular regulation, nerve transmission delivery and immune responses. In the last semicenturry, it has been proved that though low concentration of NO is tumor-promoting, high concentration of NO could exhibit multiple antitumor effects, which led to the research and development of kinds of NO donors and NO donor hybrid compounds as antitumor agents. Herein, the recent development of NO donor hybrid compounds is briefly reviewed.

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  • Mehmet Emin Önger, Burcu Delibaş, Aysın Pınar Türkmen, Erkan Erener, B ...
    2016 Volume 10 Issue 6 Pages 285-291
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: October 17, 2016
    JOURNALS FREE ACCESS

    Nerve injuries result in functional loss in the innervated organ or body parts, and recovery is difficult unless surgical treatment has been done. Different surgical treatments have been suggested for nerve repair. Tissue engineering related to growth factors has arisen as an alternative approach for triggering and improving nerve regeneration. Therefore, the aim of this review is to provide a comprehensive analysis related to growth factors as tools for optimizing the regeneration process. Studies and reviews on the use of growth factors for nerve regeneration were compiled over the course of the review. According to literature review, it may be concluded that growth factors from different sources present promising treatment related to nerve regeneration involved in neuronal differentiation, greater myelination and axonal growth and proliferation of specific cells for nerve repair.

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  • Raja A.H Kuchay
    2016 Volume 10 Issue 6 Pages 292-299
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: October 17, 2016
    JOURNALS FREE ACCESS

    Administration of chemotherapy often leads to gastrointestinal mucositis (GIM). GIM manifests as nausea, abdominal pain and diarrhoea in recipients of chemotherapy. GIM is a major complication occurring in approximately 80% of patients receiving 5-flurouracil treatment. These side-effects may become so severe that significant dose reductions are required, ultimately affecting treatment efficacy and patient survival. Complementary and alternative medicine (CAM) is a growing area of public interest. This review will provide an overview of current knowledge of complementary medicinal therapies for chemotherapy induced GIM. An understanding of this evolving literature is useful in discussing these therapies with patients who are considering using them.

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Original Articles
  • Yuko Wada, Yukie Takaoka, Mitsuru Nozawa, Miho Goto, Ken-ichi Shimokaw ...
    2016 Volume 10 Issue 6 Pages 300-306
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: October 04, 2016
    JOURNALS FREE ACCESS

    We measured the pH, water-vapor permeability, adhesive force, peeling-force, elongation rate, support flexibility, and peeling time of medicinal and over-the-counter (OTC) tape preparations containing felbinac. When measuring the pH of each preparation, Felnabion (pH 4.5) was weakly acidic, and EMEC and Tokuon (pH 7.0) were neutral. When measuring the water-vapor permeability of each preparation, that of a generic product, EMEC (380 g/m2/24h), was twice as high as that of a brand-name product, Seltouch (189 g/m2/24 h). The adhesive force was measured using the ball tack test. The adhesive forces of OTC drugs, Salomethyl, Homepass, and Tokuhon (1.04 g), were higher than that of Seltouch (0.06 g). Concerning peeling-force measurement, the peeling-forces of a generic product, Falzy (4.15 N), and an OTC drug, Omuneed (4.89 N), were higher than that of Seltouch (0.91 N). The elongation rates of a generic product, Sumilu (319%), and OTC drugs, Nabolin (298%) and Homepass (299%), were higher than that of Seltouch (251%), but that of Tokuhon (72%) was lower. The support flexibilities of EMEC (150 degrees) and Tokuhon (131 degrees) were higher than that of Seltouch (96 degrees). In addition, the peeling time of Seltouch was 120 min or more, whereas those of EMEC and Nabolin were 1.4 and 0.2 min, respectively. These results suggest that the differences in pharmaceutical properties, such as the pH, water-vapor permeability, adhesive force, peeling-force, elongation rate, support flexibility, and peeling time, among the preparations markedly influence patients' subjective comfortableness. The results of this study facilitated individuals’ comfortableness-matched drug selection.

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  • Akihiro Matsumoto, Satoshi Murao, Michiko Matsumoto, Chie Watanabe, Ma ...
    2016 Volume 10 Issue 6 Pages 307-313
    Published: 2016
    Released: January 15, 2017
    JOURNALS FREE ACCESS

    The feasibility of fabricating Janus particles based on phase separation between a hard fat and a biocompatible polymer was investigated. The solvent evaporation method used involved preparing an oil-in-water (o/w) emulsion with a mixture of poly (lactic-co-glycolic) acid (PLGA), hard fat, and an organic solvent as the oil phase and a polyvinyl alcohol aqueous solution as the water phase. The Janus particles were formed when the solvent was evaporated to obtain certain concentrations of PLGA and hard fat in the oil phase, at which phase separation was estimated to occur based on the phase diagram analysis. The hard fat hemisphere was proven to be the oil phase using a lipophilic dye Oil Red O. When the solvent evaporation process was performed maintaining a specific volume during the emulsification process; Janus particles were formed within 1.5 h. However, the formed Janus particles were destroyed by stirring for over 6 h. In contrast, a few Janus particles were formed when enough water to dissolve the oil phase solvent was added to the emulsion immediately after the emulsification process. The optimized volume of the solvent evaporation medium dominantly formed Janus particles and maintained the conformation for over 6 h with stirring. These results indicate that the formation and stability of Janus particles depend on the rate of solvent evaporation. Therefore, optimization of the solvent evaporation rate is critical to obtaining stable PLGA and hard fat Janus particles.

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  • Pham Thi Be Tu, Binh Cao Quan Nguyen, Shinkichi Tawata, Cheong-Yong Yu ...
    2016 Volume 10 Issue 6 Pages 314-322
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: October 17, 2016
    JOURNALS FREE ACCESS

    We previously demonstrated that the oncogenic kinase PAK4, which both melanomas and normal melanocytes express at a very high level, is essential for their melanogenesis. In the present study, using the highly sensitive "Macaroni-Western" (IP-ATP-Glo) kinase assay, we investigated the melanogenic potential of another oncogenic kinase PAK1, which melanoma (B16F10) cells express only at a very minute level. After transfecting melanoma cells with PAK1-shRNA for silencing PAK1 gene, melanin content, tyrosinase activity, and kinase activity of PAK1 were compared between the wild-type and transfectants. We found that (i) PAK1 is significantly activated by melanogenic hormones such as IBMX (3-isobutyl-1-methyl xanthine) and α-MSH (melanocyte-stimulating hormone), (ii) silencing the endogenous PAK1 gene in melanoma cells through PAK1-specific shRNA reduces both melanin content and tyrosinase activity in the presence of both serum and melanogenic hormones to the basal level, (iii) the exogenously added wild-type PAK1 in the melanoma cells boosts the α-MSH-inducible melanin level by several folds without affecting the basal, and (iv) α-MSH/IBMX-induced melanogenesis hardly takes place in the absence of either serum or PAK1, clearly indicating that PAK1 is essential mainly for serum- and α-MSH/IBMX-dependent melanogenesis, but not the basal, in melanoma cells. The outcome of this study might provide the first scientific basis for explaining why a wide variety of herbal PAK1-blockers such as CAPE (caffeic acid phenethyl ester), curcumin and shikonin in cosmetics are useful for skin-whitening.

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  • Hao Hu, Jinhui Dai, Minjie Chen, Lanting Chen, Lingli Jiang, Ran Lin, ...
    2016 Volume 10 Issue 6 Pages 323-328
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: November 27, 2016
    JOURNALS FREE ACCESS

    The aim of this study was to evaluate primitively whether the extent and component of astigmatism influences regression in degree of spherical (DS) and the best corrected visual acuity (BCVA) of children with hyperopia of +5.00 diopters (D) or greater. Children were screened from the outpatient refraction database in the Wenling No. 1 People's Hospital in Zhejiang province and in Eye & ENT Hospital of Fudan University between June 2005 and December 2015. Eligible eyes were divided into three groups according to the extent of astigmatism: group of astigmatism ≤ −2 D of cylinder, group without astigmatism or with astigmatism ≥ −0.5 D of cylinder, and the group with astigmatism ≥ −0.75 D and ≤ −1.75 D of cylinder. For the component of astigmatism, eyes with astigmatism as ≤ −0.75 D of cylinder were divided into 3 groups: with the rule (WTR), against the rule (ATR) and the group with the oblique. Differences in the changes of BCVA and refractive error (RE) during follow-up terms were compared within and among groups. Differences in the mean DS or BCVA were not statistically significant between groups according to the extent of the astigmatism at the last visit (p = 0.2396 and p = 0.2131, respectively). As for the component of astigmatism, the group with oblique astigmatism had more severe hyperopia than the group of WTR (p < 0.0001) and mean BCVA in the group of ATR were better than that of the other two groups (p < 0.0001) at the first visit. However, the among-group changes were not significant at the end of the observation (p > 0.1). The regression of DS and improvement of the BCVA in children with hyperopia of +5.00D or greater may be irrespective of the component and the extent of astigmatism.

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  • Zhiliang Hu, Yongfeng Yang, Jian cheng, Cong Cheng, Yun Chi, Hongxia W ...
    2016 Volume 10 Issue 6 Pages 329-333
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: October 11, 2016
    JOURNALS FREE ACCESS

    Cryptococcal meningitis (CM) is a common opportunistic infection with a high mortality rate in human immunodeficiency virus (HIV)-infected patients. It is unclear whether mannitol could be used to manage neurological symptoms in HIV-associated CM. Here, we retrospectively analyzed the clinical data of 33 patients with HIV-associated symptomatic CM at our hospital where mannitol was used to relieve neurologic symptoms. With the empirical mannitol therapy, patients had a median of 2 episodes (range, 1-6 episodes) of headaches the day at the starting of anti-cryptococcal therapy. The median score of pain intensity assessed by numerical rating scales was 7-point (range, 4-8 points). After the administration of mannitol, the score of pain intensity was reduced to 3-point or less. Three weeks after anti-cryptococcal therapy, 75.8% (25/33) of the patients did not report headaches. During the initial 3 weeks of anti-cryptococcal therapy, 13 patients had a total of 42 episodes of seizures. 97.6% (41/42) of the episodes of seizures were controlled after the administration of mannitol. Overall, 87.9% (29/33) of the patients survived more than 10 weeks without the need of therapeutic cerebrospinal fluid drainage. Mannitol was used for median of 26 days (range, 1-85 days) in these 29 patients. One patient had permanent vision loss. This study indicates that mannitol may possibly relieve neurologic symptoms in HIV-associated CM. It is worth re-revaluating the role of mannitol administration as a symptom control strategy in mild cases of HIV-associated CM.

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Case Report
  • Yesim Coskun, Ipek Akman, Canan Yildirim, Mustafa Kemal Demir
    2016 Volume 10 Issue 6 Pages 334-337
    Published: 2016
    Released: January 15, 2017
    [Advance publication] Released: December 18, 2016
    JOURNALS FREE ACCESS

    Neonatal meningoencephalitis is a severe condition for the developing brain of a newborn. Radiologic findings of necrosis and liquefaction due to hemorrhagic meningoencephalitis may be confused with brain abcess. In this article, we report a neonate having liquefaction necrosis due to hemorrhagic meningoencephalitis mimicing intracranial abscess due to Proteus mirabilis. We would like to describe the clinical course and evolution of brain imaging and emphasize the importance of the serial MR imaging (MRI).

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