• Title/Summary/Keyword: Therapeutic potentials

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Development of Non-Immunosuppressive FK506 Derivatives as Antifungal and Neurotrophic Agents

  • Jung, Jin A;Yoon, Yeo Joon
    • Journal of Microbiology and Biotechnology
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    • v.30 no.1
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    • pp.1-10
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    • 2020
  • FK506, also known as tacrolimus, is a clinically important immunosuppressant drug and has promising therapeutic potentials owing to its antifungal, neuroprotective, and neuroregenerative activities. To generate various FK506 derivatives, the structure of FK506 has been modified by chemical methods or biosynthetic pathway engineering. Herein, we describe the mode of the antifungal action of FK506 and the structure-activity relationship of FK506 derivatives in the context of immunosuppressive and antifungal activities. In addition, we discuss the neurotrophic mechanism of FK506 known to date, along with the neurotrophic FK506 derivatives with significantly reduced immunosuppressive activity. This review suggests the possibility to generate novel FK506 derivatives as antifungal as well as neuroregenerative/neuroprotective agents.

Synthesis of New Benzaminoquinoline Derivatives with Antiproliferative Activity against Melanoma Cell Line (흑색종 세포증식 저해효능의 새로운 Benzaminoquinoline 유도체의 합성)

  • Yoo, Kyung-Ho;Nam, Bong-Soo
    • Journal of the Korean Applied Science and Technology
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    • v.26 no.3
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    • pp.297-305
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    • 2009
  • Melanoma is the most serious type of skin cancer as a malignant tumor of melanocytes. In this work, the syntheses of a novel series of benzaminoquinoline derivatives 1a-c and their antiproliferative activities against A375 human melanoma cell line were described. All the compounds ($IC_{50}=0.78-1.02{\mu}M$) showed superior antiproliferative activities to Sorafenib ($IC_{50}=5.58{\mu}M$) as a reference compound. These results suggested that benzaminoquinoline derivatives have potentials as a therapeutic agent for the treatment for melanoma.

Mitochondria-targeting theranostics

  • Kang, Han Chang
    • Biomaterials Research
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    • v.22 no.4
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    • pp.221-234
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    • 2018
  • Background: Interest in subcellular organelle-targeting theranostics is substantially increasing due to the significance of subcellular organelle-targeting drug delivery for maximizing therapeutic effects and minimizing side effects, as well as the significance of theranostics for delivering therapeutics at the correct locations and doses for diseases throughout diagnosis. Among organelles, mitochondria have received substantial attention due to their significant controlling functions in cells. Main body: With the necessity of subcellular organelle-targeting drug delivery and theranostics, examples of mitochondria-targeting moieties and types of mitochondria-targeting theranostics were introduced. In addition, the current studies of mitochondria-targeting theranostic chemicals, chemical conjugates, and nanosystems were summarized. Conclusion: With the current issues of mitochondria-targeting theranostic chemicals, chemical conjugates, and nanosystems, their potentials and alternatives are discussed.

Synthesis and $BK_{ca}$-channel Opening Activity of Substituted l0-H-Benzo[4-5]furo[3,2-b]indole-carboxylic acids

  • Gormemis, Ahmet-Erkam;Soo, Ha-Tal;Park, Chul-Seung;Kim, Yong-Chul
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.188.2-188.2
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    • 2003
  • Large-conductance $Ca^{2+}$ activated potassium channels $(BK_{ca})$ are widely distributed and play key roles in various cell functions. In nerve cells, B $K_{ca}$ channels shorten the duration of action potentials and block $Ca^{2+}$ entry thereby repolarizing excitable cells after excitation. $(BK_{ca})$ channel opening has been postulated to confer neuroprotection during stroke and has attracted attention as a means for therapeutic intervention in asthma, hypertension, convulsion, and traumatic brain injury. (omitted)

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Convergent Analysis of Old People Eye Movement Training on Change of Cognitive Ability (안구 운동이 노인의 인지능력 변화에 미치는 융합적 분석)

  • Bae, Seahyun;Kim, Kyung-Yoon
    • Journal of the Korea Convergence Society
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    • v.9 no.5
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    • pp.121-127
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    • 2018
  • The objective of the present study was to investigate the effect of eye movement on cognitive ability using Mini-Mental State Examination for Dementia Screening (MMSE-DS) and the amplitude and latency of P300 from event-related potentials after 55 elderly participants were randomly stratified into the saccadic eye movement (SEM) group and the smooth pursuit eye movement (SPEM) group, and performed eye movement for 4 weeks. As a result, P300 amplitude significantly increased and P300 latency significantly shortened in the SEM and SPEM groups. MMSE-DS showed a significant increase in both groups; upon comparing the groups, the SEM group showed a significant difference in orientation and the SPEM group in attention. In conclusion, it is thought that SEM and SPEM can improve and maintain the cognitive ability of the elderly and may be used as therapeutic tools for dementia prevention and mild dementia.

Usefulness of Electrophysiological Tests in Movement Disorders (이상운동 질환에서의 신경생리적 검사법의 유용성)

  • Seo, Man-Wook;Lee, Kwang-Woo
    • Annals of Clinical Neurophysiology
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    • v.1 no.2
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    • pp.126-146
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    • 1999
  • In clinical neurology various different electrophysiological tests are widely used to demonstrate the unsuspected malfunctioning in the nervous system and to monitor over time the clinical status of patients. In addition clinical neurologists and neurosurgeons take advantage of the intraoperative monitorings to increase the quality of neurosurgical operations in the posterior fossa, in the spinal cord, or in visual pathways. In the field of movement disorders, elecrophysiolgical tests provide neurologists with making accurate differential diagnoses with useful therapeutic stratergies as well as with investigating the pathophysiological machanisms. By using the electromyographic tests it could be possible for us to evaluate the types of blephalospasm, the extent of hemifacial spasm, the level of myoclonus, and the prime muscles of torticollis etc. Sometimes the myographic guidance may be critical for choosing the exact injecting site of botulinum toxin. These several decades various electroencephalographic and evoked potential tests has been utilized in the electrophysiological laboratories to understand the basic pathophysiology of myoclonus, spasticity and other central motor dysfunctions. It could be one of the breakthroughs in the area of behavorial neurology that the brain function can be mapped by the spontaneous or evoked electrical activities of nervous system since the movement related potentials (MRPs) had been studies for several decades. Various reflex tests such as masseter reflex, blink reflex, click evoked vestibulocollic reflex, facial reflex, stretch reflex, flexor reflex, H-reflex, H-reflex recovery curve, vestibular inhibition of H-reflex, reciprocal inhibition, recurrent or Renshaw reflex, Ib inhibition, cutaneous reflex have been also used to understand normal or abnormal physiology in movement disorders. Polysomnography, posturography and gait studies are also applied in clinical neurology in association with with movement disorders which are useful in deciding the treatment regimen.

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Association of Therapeutic Response and Change of Mismatch Negativity in Schizophrenia Patients (조현병 환자의 치료 반응에 따른 Mismatch Negativity 변화)

  • Lee, Soyoen;Rhie, Eui Hyeok;Kim, Jong Woo;Kang, Won Sub
    • Korean Journal of Biological Psychiatry
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    • v.24 no.4
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    • pp.188-195
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    • 2017
  • Objectives Schizophrenia is characterized by disturbances in perception and cognition. Attenuated mismatch negativity (MMN) reflects central auditory dysfunction in schizophrenia. The aim of this study is to compare MMN changes before and after treatment in schizophrenia patients and to assess their association with treatment response. Methods Twenty-three schizophrenia patients underwent an oddball paradigm. MMN was calculated by the difference waveforms of the event-related potentials (ERPs) elicited by subtracting standard from deviant stimulus. The clinical symptoms were measured by the Positive and Negative Syndrome Scale (PANSS), the Psychotic Symptom Rating Scale (PSYRATS). Follow-up evaluation was conducted when the PANSS total score decreased by 30% or more (treatment response group) or before discharge (non-response group). Results The treatment response group showed significantly larger MMN amplitude improvement and latency reduction than the non-response group after treatment (Fz ; mean amplitude p = 0.035, FCz ; p = 0.041). The auditory hallucination group showed shorter latency than that of the group without hallucinations. Additionally, auditory hallucination was associated with prolonged MMN latency and shortened after treatment in the auditory hallucination response group (Fz ; p = 0.048). Conclusions These results suggest that the attenuated MMN amplitude reflects the progression of the disease. The increment of MMN amplitude and shortening of latency after treatment may reflect cognitive functional recovery of central auditory sensory processing.

Systematic Review on the Yaksun Study (최근 국내에서 진행된 약선 연구 동향 고찰)

  • Han, Seung Yoon;Kim, Sung Hye;Han, Sang Yun;Han, Yoo Ri;Lee, Han Byul;Kwon, Young Kyu;Chae, Han
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.29 no.4
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    • pp.295-304
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    • 2015
  • The purpose of this study was to systematically review published articles on Yaksun studies and provide understanding on current and future studies with Yaksun and medical treatment with food. We performed systematic review on the Yaksun studies published recent 16 years from 2000 to 2016 using seven Korean database on research articles. We found 90 articles are relevant for the analysis. The articles on Yaksun were significantly increased since 2005. As for the research field, Food Science (39 articles, 31.0%) and Tourism (20 articles, 15.9%) were dominant throughout the years. Researchers from Science of cookery (35 articles, 35.0%) and Food and Nutrition (32 articles, 32.0%) were found to be most frequent. The prime type of research on Yaksun were the We found that the Survey (49 articles, 52.7%) was the most frequent research method and basic research for providing related data (41 articles, 45.6%) was easily found as for the purpose of the article. We found that there were insufficient reports on clinical efficacy of Yaksun, especially with the treatment of diseases. The interest of medical professionals is needed for the better understanding on the medical use of Yaksun and therapeutic diet which has potentials for integrative medicine.

The effects of Korean Red Ginseng-derived components on oligodendrocyte lineage cells: Distinct facilitatory roles of the non-saponin and saponin fractions, and Rb1, in proliferation, differentiation and myelination

  • Lee, Ahreum;Kwon, Oh Wook;Jung, Kwi Ryun;Song, Gyun Jee;Yang, Hyun-Jeong
    • Journal of Ginseng Research
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    • v.46 no.1
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    • pp.104-114
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    • 2022
  • Background: Abnormalities of myelin, which increases the efficiency of action potential conduction, are found in neurological disorders. Korean Red Ginseng (KRG) demonstrates therapeutic efficacy against some of these conditions, however effects on oligodendrocyte (OL)s are not well known. Here, we examined the effects of KRG-derived components on development and protection of OL-lineage cells. Methods: Primary OL precursor cell (OPC) cultures were prepared from neonatal mouse cortex. The protective efficacies of the KRG components were examined against inhibitors of mitochondrial respiratory chain activity. For in vivo function of Rb1 on myelination, after 10 days of oral gavage into adult male mice, forebrains were collected. OPC proliferation were assessed by BrdU incorporation, and differentiation and myelination were examined by qPCR, western blot and immunocytochemistry. Results: The non-saponin promoted OPC proliferation, while the saponin promoted differentiation. Both processes were mediated by AKT and extracellular regulated kinase (ERK) signaling. KRG extract, the saponin and non-saponin protected OPCs against oxidative stress, and both KRG extract and the saponin significantly increased the expression of the antioxidant enzyme. Among 11 major ginsenosides tested, Rb1 significantly increased OL membrane size in vitro. Moreover, Rb1 significantly increased myelin formation in adult mouse brain. Conclusion: All KRG components prevented OPC deaths under oxidative stress. While non-saponin promoted proliferation, saponin fraction increased differentiation and OL membrane size. Furthermore, among all the tested ginsenosides, Rb1 showed the biggest increase in the membrane size and significantly enhanced myelination in vivo. These results imply therapeutic potentials of KRG and Rb1 for myelin-related disorders.

Neurophysiological Evaluation of the Motor System Using Transcranial Magnetic Stimulation (뇌자기자극을 이용한 운동신경계의 신경생리학적 평가)

  • Shin, Hae-Won;Sohn, Young-H.
    • Annals of Clinical Neurophysiology
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    • v.13 no.1
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    • pp.1-12
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    • 2011
  • Transcranial magnetic stimulation (TMS) is a non-invasive tool used to study aspects of human brain physiology, including motor function and the pathophysiology of various brain disorders. A brief electric current passed through a magnetic coil produces a high-intensity magnetic field, which can excite or inhibit the cerebral cortex. Although various brain regions can be evaluated by TMS, most studies have focused on the motor cortex where motor evoked potentials (MEPs) are produced. Single-pulse and paired-pulse TMS can be used to measure the excitability of the motor cortex via various parameters, while repetitive TMS induces cortical plasticity via long-term potentiation or long-term depression-like mechanisms. Therefore, TMS is useful in the evaluation of physiological mechanisms of various neurological diseases, including movement disorders and epilepsy. In addition, it has diagnostic utility in spinal cord diseases, amyotrophic lateral sclerosis and demyelinating diseases. The therapeutic effects of repetitive TMS on stroke, Parkinson disease and focal hand dystonia are limited since the duration and clinical benefits seem to be temporary. New TMS techniques, which may improve clinical utility, are being developed to enhance clinical utilities in various neurological diseases.