• Title/Summary/Keyword: therapeutic potential

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The Synthesis of Novel Cyclobutyl Nucleoside as Potential Antiviral Agents

  • Wi, Hyung-Hwa;Kook, Min-Cheol;Choi, Bo-Gil
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.237.3-238
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    • 2003
  • Carbonucleosides has extensively been studied as a promising anti-viral agents having chemical and metabolical stability. As yet there are no rules relating the structures of carbocyclic nucleosides to their therapeutic activity. although trends among certain kinds of structure have been tentatively put forward. In our research program for discovery of anti-viral drugs, the novel cyclobutyl nucleosides can be expected to be potential antiviral drugs as analogues of cyclobut-A, anti-HBV agent. (omitted)

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Application of genome engineering for treatment of retinal diseases

  • Jo, Dong Hyun;Kim, Jeong Hun
    • BMB Reports
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    • v.51 no.7
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    • pp.315-316
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    • 2018
  • Genome engineering with clustered regularly interspaced short palindromic repeats (CRISPR) system can be used as a tool to correct pathological mutations or modulate gene expression levels associated with pathogenesis of human diseases. Owing to well-established local administration methods including intravitreal and subretinal injection, it is relatively easy to administer therapeutic genome engineering machinery to ocular tissues for treating retinal diseases. In this context, we have investigated the potential of in vivo genome engineering as a therapeutic approach in the form of ribonucleoprotein or CRISPR packaged in viral vectors. Major issues in therapeutic application of genome engineering include specificity and efficacy according to types of CRISPR system. In addition to previous platforms based on ribonucleoprotein and CRISPR-associated protein 9 derived from Campylobacter jejuni, we evaluated the therapeutic effects of a CRISPR RNA-guided endonuclease derived from Lachnospiraceae bacterium ND2006 (LbCpf1) in regulating pathological angiogenesis in an animal model of wet-type age-related macular degeneration. LbCpf1 targeting Vegfa or Hif1a effectively disrupted the expression of genes in ocular tissues, resulting in suppression of choroidal neovascularization. It was also notable that there were no significant off-target effects in vivo.

Effects and Mechanisms of Taurine as a Therapeutic Agent

  • Schaffer, Stephen;Kim, Ha Won
    • Biomolecules & Therapeutics
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    • v.26 no.3
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    • pp.225-241
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    • 2018
  • Taurine is an abundant, ${\beta}-amino$ acid with diverse cytoprotective activity. In some species, taurine is an essential nutrient but in man it is considered a semi-essential nutrient, although cells lacking taurine show major pathology. These findings have spurred interest in the potential use of taurine as a therapeutic agent. The discovery that taurine is an effective therapy against congestive heart failure led to the study of taurine as a therapeutic agent against other disease conditions. Today, taurine has been approved for the treatment of congestive heart failure in Japan and shows promise in the treatment of several other diseases. The present review summarizes studies supporting a role of taurine in the treatment of diseases of muscle, the central nervous system, and the cardiovascular system. In addition, taurine is extremely effective in the treatment of the mitochondrial disease, mitochondrial encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and offers a new approach for the treatment of metabolic diseases, such as diabetes, and inflammatory diseases, such as arthritis. The review also addresses the functions of taurine (regulation of antioxidation, energy metabolism, gene expression, ER stress, neuromodulation, quality control and calcium homeostasis) underlying these therapeutic actions.

A potential anticacner therapeutic strategy using light-emitting diode (자궁경부암세포 치료를 위한 발광다이오드의 응용)

  • Park, Chul Woo;Park, Kitae;Choi, Hojong;Choe, Se-woon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2017.05a
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    • pp.712-713
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    • 2017
  • Clinically applicable light emitting diode (LED) has been widely investigated because of relatively low heat generation, low cytotoxicity, and non-invasiveness compared to other therapeutic methods. Therefore, we investigated the therapeutic effects of several wavelengths of light emitting diode against human cervical cancer cells and analyzed the individual inhibitory effect for the cancer cell proliferation. In the experiment, prepared HeLa cells were exposed by red, green and blue light-emitting diode for 10 minutes each. Relatively short-wavelength light-emitting diode (blue) showed stronger therapeutic effects than relatively long-wavelength light-emitting diodes.

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Evaluation of Muscle Fatigue Recovery Effect and Meridian Potential Change using Magnetic Acupuncture System (자화침 시스템을 이용한 경락전위 유발효과 및 근피로 회복 평가)

  • Kim, Soo-Byeong;Park, Sun-Woo;Ahn, Soon-Jae;Lee, Na-Ra;Lee, Seung-Wook;Min, Se-Eun;Kim, Young-Ho;Lee, Yong-Heum
    • Korean Journal of Acupuncture
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    • v.29 no.1
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    • pp.83-92
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    • 2012
  • Objectives : The purpose of this research was to develop the magnetic acupuncture system which used solenoid coil for magnetizing acupuncture needle. The system could generate the meridian electric potential (MEP) similar to the potential by manual acupuncture. Thus, we tried to confirm the therapeutic effect that is caused by the MEP generation. Methods : To confirm the MEP, we stimulated the magnetic acupuncture with at 2Hz, $92.7{\pm}2mT$, PEMFs (Pulsed Electro-Magnetic Fields) at ST37 and measured the evoked potential between ST36 and ST41. Also, we conducted a fatigue recovery test using isokinetic exercise in order to identify the therapeutic effect on musculoskeletal disorders. We chose LR9 as a stimulation point. To observe the state of fatigue, we measured the EMG and analyzed median frequency and peak torque for 20minutes. Results : We observed that MEP which incurred from magnetic acupuncture was higher than he reported MEP induced by manual acupuncture. Moreover, its modes were divided into two types by the direction of magnetic flux. When generating magnetic flux in the direction of acupoint, the positive peak voltage of the MEP was generated. In contrast, negative peak voltage of the MEP was generated whenever meganetic flux generated in the outward direction. As a result of fatigue recovery, the median frequency (MF) of the magnetic acupuncture group were recovered faster than that of the non-stimulation group. However, the peak torques of both groups were not restored until after 20 minutes. Conclusions : We confirmed that the magnetic acupuncture system can lead to the MEP similar to manual acupuncture. Moreover, the MEP had a therapeutic effect on the musculoskeletal disorders.

Ginsenosides from Korean Red Ginseng ameliorate lung inflammatory responses: inhibition of the MAPKs/NF-κB/c-Fos pathways

  • Lee, Ju Hee;Min, Dong Suk;Lee, Chan Woo;Song, Kwang Ho;Kim, Yeong Shik;Kim, Hyun Pyo
    • Journal of Ginseng Research
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    • v.42 no.4
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    • pp.476-484
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    • 2018
  • Background: Korean Red Ginseng (steamed and dried white ginseng, Panax ginseng Meyer) is well known for enhancing vital energy and immune capacity and for inhibiting cancer cell growth. Some clinical studies also demonstrated a therapeutic potential of ginseng extract for treating lung inflammatory disorders. This study was conducted to establish the therapeutic potential of ginseng saponins on the lung inflammatory response. Methods: From Korean Red Ginseng, 11 ginsenosides (Rb1, Rb2, Rb3, Rc, Rd, Re, Rf, Rg1, Rg2, Rg3, and Rh2) were isolated. Their inhibitory potential and action mechanism were evaluated using a mouse model of lung inflammation, acute lung injury induced by intranasal lipopolysaccharide administration. Their anti-inflammatory activities were also examined in lung epithelial cell line (A549) and alveolar macrophage (MH-S). Results: All ginsenosides orally administered at 20 mg/kg showed 11.5-51.6% reduction of total cell numbers in bronchoalveolar lavage fluid (BALF). Among the ginsenosides, Rc, Re, Rg1, and Rh2 exhibited significant inhibitory action by reducing total cell numbers in the BALF by 34.1-51.6% (n = 5). Particularly, Re showed strong and comparable inhibitory potency with that of dexamethasone, as judged by the number of infiltrated cells and histological observations. Re treatment clearly inhibited the activation of mitogen-activated protein kinases, nuclear factor-${\kappa}B$, and the c-Fos component in the lung tissue (n = 3). Conclusion: Certain ginsenosides inhibit lung inflammatory responses by interrupting these signaling molecules and they are potential therapeutics for inflammatory lung diseases.

Synthesis of Heterocyclic Substituted Pyridine Analogs as Potential Therapeutics for Neurodegenerative Diseases

  • Park, Haeil;Peter A. Crooks
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1999.04a
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    • pp.1-4
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    • 1999
  • The potential therapeutic benefit of nicotinic ligands in a variety of neurodegenerative pathologies involving the CNS has energized research efforts to develop nicotinic acetylcholine receptor (nAChR) subtype-selective ligands. In particular, there has been a concerted effort to develop nicotinic compounds with selectivity for CNS nAChRs as potential pharmacological tools in the management of these disorders. The characterization of other novel nicotinic ligands such as epibatidine. showing a marked increase in potency at nAChRs, has provided additional support for the development of potent, selective ligands at individual nAChR subtypes. We have developed and studied a number of nicotinic compounds to identify potential candidates exhibiting such selectivity. In the present study, we report the synthesis and biological evaluations of some azabicyclic and azatricyclic nicotine analogs to decipher the relationship among steric requirements of the nicotine's pyrrolidine ring system, binding affinity and subtype-selectivity.

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Fyn Kinase: A Potential Therapeutic Target in Acute Kidney Injury

  • Uddin, Md Jamal;Dorotea, Debra;Pak, Eun Seon;Ha, Hunjoo
    • Biomolecules & Therapeutics
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    • v.28 no.3
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    • pp.213-221
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    • 2020
  • Acute kidney injury (AKI) is a common disease with a complex pathophysiology which significantly contributes to the development of chronic kidney disease and end stage kidney failure. Preventing AKI can consequently reduce mortality, morbidity, and healthcare burden. However, there are no effective drugs in use for either prevention or treatment of AKI. Developing therapeutic agents with pleiotropic effects covering multiple pathophysiological pathways are likely to be more effective in attenuating AKI. Fyn, a non-receptor tyrosine kinase, has been acknowledged to integrate multiple injurious stimuli in the kidney. Limited studies have shown increased Fyn transcription level and activation under experimental AKI. Activated Fyn kinase propagates various downstream signaling pathways associated to the progression of AKI, such as oxidative stress, inflammation, endoplasmic reticulum stress, as well as autophagy dysfunction. The versatility of Fyn kinase in mediating various pathophysiological pathways suggests that its inhibition can be a potential strategy in attenuating AKI.

Topical Application of S1P2 Antagonist JTE-013 Attenuates 2,4-Dinitrochlorobenzene-Induced Atopic Dermatitis in Mice

  • Kang, Jisoo;Lee, Ju-Hyun;Im, Dong-Soon
    • Biomolecules & Therapeutics
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    • v.28 no.6
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    • pp.537-541
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    • 2020
  • Sphingosine-1-phosphate (S1P) and its receptors have been implicated in atopic dermatitis. S1P2 was found to function as a proallergic receptor, while its antagonist JTE-013 was found to suppress allergic asthma in mice. Topical application of JTE-013 has not been investigated in an in vivo model of atopic dermatitis. Therefore, the therapeutic potential of JTE-013 topical application was evaluated by the use of a 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mouse model. DNCB-induced inflammation and mast cell accumulation in skin tissues were significantly suppressed by topical JTE-013 treatment in BALB/c mice. DNCB-induced increase of lymph nodes sizes and elevated inflammatory cytokines (IL-4, IL-13, IL-17, and IFN-γ) in lymph nodes were also significantly reduced by the JTE-013 treatment. Elevated serum levels of IgE were significantly suppressed by the topical treatment of JTE-013. In summary, the topical treatment of JTE-013 S1P2 antagonist suppressed DNCB-induced atopic dermatitis symptoms and immune responses. These results suggested JTE-013 as a potential therapeutic agent for atopic dermatitis.

Atorvastatin: In-Vivo Synergy with Metronidazole as Anti-Blastocystis Therapy

  • Basyoni, Maha M.A.;Fouad, Shawky A.;Amer, Marwa F.;Amer, Ahmed Fathy;Ismail, Dalia Ibrahim
    • Parasites, Hosts and Diseases
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    • v.56 no.2
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    • pp.105-112
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    • 2018
  • Blastocystis is an enteric Straminopile in tropical, subtropical and developing countries. Metronidazole has been a chemotheraputic for blastocystosis. Failures in its regimens were reported and necessitate new studies searching for alternative therapeutic agents. Aim of current study is to investigate potential effects of Atorvastatin (AVA) compared to the conventional chemotherapeutic MTZ in experimentally Blastocystis-infected mice. Anti-Blastocystis efficacy of AVA was evaluated parasitologically, histopathologically and by transmission electron microscopy using MTZ (10 mg/kg) as a control. Therapeutic efficacy of AVA were apparently dose-dependent. Regimens of AVA (20 and 40 mg/kg) proved effective against Blastocystis infections with highreduction in Blastocystis shedding (93.4-97.9%) compared to MTZ (79.3%). The highest reductions (98.1% and 99.4%)were recorded in groups of combination treatments AVA 20-40 mg/kg and MTZ 10 mg/kg. Blastocystis was nearly eradicated by the 20th day post infection. Genotype analysis revealed that genotype I was most susceptible, genotype III was less. Histopathologic and ultrastructural studies revealed apoptotic changes in Blastocystis and significant improvement of intestinal histopathological changes more remarkable in combinational therapy groups. Thus, the present study offers AVA as a potential candidate for Blastocystis therapy combined with MTZ.