• Title/Summary/Keyword: 약물 표적

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신규 항암제 DA-125의 급성 및 특수독성 연구

  • 하광원;김부영;박정식;안병옥
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.37-37
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    • 1993
  • 1) 급성독성시험: 랫드와 마우스 공히 투여후 5~6일에 농도의존적의 강한 독성이 발현 되었으며 표적장기로는 소화기계, 임파계, 조혈기계 등으로 나타났다. 랫드에서의 반수 치사량은 암수 각각 771.9(505.6~1178.4)mg/kg과 479.8(302.7~760.4)mg/kg이었으며 마우스에서는 암수 각각 527.4(393.7~701.1)mg/kg과 463.0(308.8~694.2)mg/kg 이었다. 2) 유전독성: S. typhimurium을 이용한 복귀돌연변이시험, CHL세포를 이용한 염색체이상 시험, 마우스에서의 소핵시험결과 DA-125는 돌연변이 유발능을 갖는 것으로 나타났다. 3) 국소자극성: 혈관주위주사에 의한 피부자극성 시험결과 DA-125는 adriamycin의 3배 용량에서 궤양, 괴사등 유사한 병변이 유발되었으나, 병변회복은 adriamycin에 비해 빠른 것으로 나타났다. 또한 토끼에서의 안점막자극시험 결과에서 DA-125는 실제적으로 자극이 없는 것으로 나타났다.

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Prognostic Analysis of Drug-Eluting Balloon Catheter and Drug-Eluting Stent for In-Stent Restenosis of Drug-Eluting Stent (스텐트 재협착 병변에서 약물코팅 풍선카테터과 약물용출 스텐트의 예후 분석)

  • Lee, Doo Hwan;Song, Jong Nam;Park, Sin eui;Choi, Nam Gil;Han, Jae Bok;Kim, In Soo
    • Journal of the Korean Society of Radiology
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    • v.13 no.3
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    • pp.381-389
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    • 2019
  • Although the development of Drug-eluting stent (DES) improved the ISR significantly more than the Bare metal stent (BMS), the coronary stent restenosis (ISR) treatment still has a high recurrence rate. This study is compared the efficacy of DEB with that of DES implantation in patients with ISR. Among 4,316 patients who underwent coronary stent implantation at the Chonnam National University Hospital between November 2012 and December 2016, 187 patients developed ISR on follow-up coronary angiography ($66.3{\pm}11.0years$, 123 males) were enrolled and divided into two groups according to revascularization method as group I (DEB group; n=127) and group II (DES group; n=60). Primary end point was defined as major adverse cardiac events (MACEs), composite of cardiac death (CD), myocardial infaction (MI), target lesion revascularization (TLR) and stent thrombosis (ST) during two-year follow-up between the two groups. There were no differences in the baseline characteristics and angiographic findings except that prevalence of device length was shorter ($21.1{\pm}5.3$ vs. $25.3{\pm}9.6 mm$, p<0.002) in group I.Two-year MACE were not different in the two groups (8.7%vs.10.0%, p=0.789). The incidences of cardiac death (0%vs.0%, p=1.000), MI (1.6%vs.6.7%, p=0.085), TLR(8.7% vs. 10.0%, p=0.789) and ST (0% vs. 0%, p=1000). DEB demonstrated comparable risk reduction for MACEs compared with DES in patients with ISR during two-year follow-up. DEB might be good alternative for the treatment of ISR in patients with ISR.

Drug Delivery Study on Chitosan Nanoparticles Using Iron Oxide (II, III) and Valine (Iron Oxide(II, III)와 Valine을 이용한 키토산 나노입자의 약물전달 연구)

  • Jang, So-Hyeon;Kang, Ik-Joong
    • Korean Chemical Engineering Research
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    • v.59 no.4
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    • pp.514-520
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    • 2021
  • A drug delivery system (DDS) based on nanoparticles has been used as a mediator to improve the efficacy of a drug by controlling the amount of drug released and delivering it to a target place. Chitosan, which is non-toxic and biodegradable, has good biocompatibility and excellent adsorption, so it can be used as a drug delivery vehicle. Valine, the essential amino acids, helps muscle growth and tissue recovery, and along with other amino acids. It lowers blood sugar levels and increases growth hormone production. In this study, Valine was adsorbed on magnetic chitosan which is capable of drug absorption, and Fe3O4-Valine CNPs was prepared through cross-linking with TPP (Tripolyphosphate). And then absorption and release trends of valine were investigated with the Fe3O4-Valine CNPs. Fe3O4, which has relatively high stability, is used to make the drug carrier magnetic so that the drug can be delivered to a target place. At optimal conditions, the absorption and release tendency of Fe3O4-Valine CNP was confirmed by analyzing by UV-Vis through the Ninhydrin test which is the color reaction of amino acids and by measuring the size of the particles, it was confirmed that it is suitable as a drug carrier.

Comparison of Efficacy of Overlapped Versus Long Eluting Stent in Acute Myocardial Infarction Patients with Diffuse Long Lesion (미만성 긴 병변이 있는 급성심근경색환자에서 긴 단일 용출 스텐트 시술과 중첩 스텐트 시술의 효과 비교)

  • Kim, Won Hyo;Kim, In Soo;Kong, Chang gi;Han, Jae Bok
    • Journal of the Korean Society of Radiology
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    • v.14 no.3
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    • pp.319-336
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    • 2020
  • The purpose of this study was to compare the outcomes of two interventional methods, overlapping drug-eluting stents (DES) and long DES, for long-term clinical outcomes in patients with acute myocardial infarction (AMI). A total of 438 patients with AMI (65.9±11.0 years, 306 males) from June 2008 to March 2019 who had diffuse long coronary artery lesion, more than 30mm were divided into two groups; group I (overlapped DES group; n=140) and group II (long DES group; n=298). We compared the incidences of major adverse cardiac events [MACEs; cardiac death, myocardial infaction (MI), target lesion revascularization (TLR) and stent thrombosis (ST)] during 12 months between the two groups. Everolimus-eluting stent was more commonly used in group II than in group I (28.1% vs. 51.8% p<0.001). Mean lesion diameter was slightly longer in group II (3.1±0.3mm vs. 3.2±0.3mm, p=0.042), and prevalence of ACC/AHA lesion type C was higher in group I (41.7% vs. 25.4%, p<0.001). Incidences of MACEs during 12 months were higher in group I than group II (18.5% vs. 14.4%, p=0.034). The rates of cardiac death (2.1% vs. 4.4%, p=0.667), MI (5.0% vs. 2.7%, p=0.260) and stent thrombosis rate (0.7% vs. 1.7%, p=0.669) were similar between the two groups. However, TLR rate was higher in group I (10.7% vs. 5.6%, p=0.041). In multivariate logistic regression analysis, presence of diabetes mellitus [Hazard ratio (HR) 2.383, 95% confidence interval (CI) 1.332-4.260, p=0.003] and use of paclitaxel-eluting stent (HR) 2.367, 95% CI 1.371-4.086, p=0.002) were independent predictors of 12-month MACEs, without significant differences in prevalence between the two groups. In AMI patients with diffuse long lesion, TLR rate was higher in the overlapped DES group during 12-month follow-up. Presence of diabetes and use of paclitaxel-eluting stent were independent predictors of MACEs.

PET-Based Molecular Nuclear Neuro-Imaging

  • Kim, Jong-Ho
    • The Korean Journal of Nuclear Medicine
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    • v.38 no.2
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    • pp.161-170
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    • 2004
  • Molecular Nuclear Neuro-Imaging in "CNS" drug discovery and development tan be divided into four categories that are clearly inter-related.(1) Neuroreceptor mapping to examine the involvement of specific neurotransmitter system in CNS diseases, drug occupancy characteristics and perhaps examine mechanisms of action;(2) Structural and spectroscopic imaging to examine morphological changes and their consequences;(3) Metabolic mapping to provide evidence of central activity and "CNS fingerprinting" the neuroanatomy of drug effects;(4) Functional mapping to examing disease-drug interactions. In addition, targeted delivery of therapeutic agents could be achieved by modifying stem cells to release specific drugs at the site of transplantation('stem cell pharmacology'). Future exploitation of stem cell biology, including enhanced release of therapeutic factors through genetic stem cell engineering, might thus constitute promising pharmaceutical approaches to treating diseases of the nervous system. With continued improvements in instrumentation, identification of better imaging probes by innovative chemistry, molecular nuclear neuro-imaging promise to play increasingly important roles in disease diagnosis and therapy.

Application of sickle red blood cells for targeted cancer therapy (항암치료를 위한 겸형적혈구의 응용)

  • Choe, Se-woon
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • 2016.05a
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    • pp.715-717
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    • 2016
  • Conventional drug carriers such as liposomes, nanoparticles, polymer micelles, polymeric conjugate and lipid microemulsion for cancer chemotherapy shield normal tissues from toxic drugs to treat cancer cells in tumors. However, inaccurate tumor targeting uncontrolled drug release from the carriers and unwanted accumulation in healthy sites can limit treatment efficacy with current conventional drug carriers with insufficient concentrations of drugs in the tumors and unexpected side effects as a result. In this research, we examined the use of sickle red blood cells as a new drug carrier with novel tumor targeting and controlled release properties. Sickle red blood cells show natural tumor preferential accumulation without any manipulation and controlled drug release is possible using a hemolysis method with photosensitizers.

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Chitosan Derivatives for Target of Specific Tissue in the Body (생체 내 특정 조직의 표적을 위한 키토산 유도체)

  • Jang, Mi-Kyeong;Nah, Jae-Woon
    • Applied Chemistry for Engineering
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    • v.21 no.6
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    • pp.593-602
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    • 2010
  • Chitosan as a natural polymer has superior physicochemical properties such as biocompatibility, biodegradability and nontoxicity, but application of chitosan for therapy of cancer and gene related-disease has been limited by poor solubility in aqueous solution. Therefore, low molecular weight water-soluble chitosan (LMWSC) with high reactivity and strong positive charge can be applied as a delivery system having function to carry in the specific tissue the bioactive material like poor solubility drug, or therapeutic gene and developed as a therapeutic system having good therapeutic efficiency. The most important factor for therapy of various diseases is to reveal the antigen or receptor expressed in specific lesion tissue and the antibody and ligand which can bind with antigen is to introduce at the biomaterials for enhancement the therapeutic efficiency. The studies for cationic synthetic polymer as drug or gene delivery have been actively performed, but it has many problems such as toxicity in the body, therapeutic efficiency. From this point of view, this article demonstrated the introduction of functional groups to target the specific tissue and therapeutic strategy using the modification of LMWSC with free-amine group. The development of these delivery system will provide a positive vision for cancer therapy.

Systemic Analysis of Antibacterial and Pharmacological Functions of Anisi Stellati Fructus (대회향의 시스템 약리학적 분석과 항균작용)

  • Han, Jeong A;Choo, Ji Eun;Shon, Jee Won;Kim, Youn Sook;Suh, Su Yeon;An, Won Gun
    • Journal of Life Science
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    • v.29 no.2
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    • pp.181-190
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    • 2019
  • The purpose of this study was to acquire the active compounds of Anisi stellati fructus (ASF) and to analyze the genes and diseases it targets, focusing on its antibacterial effects using a system pharmacological analysis approach. Active compounds of ASF were obtained through the Traditional Chinese Medicine Systems Pharmacology (TCMSP) Database and Analysis Platform. This contains the pharmacokinetic properties of active compounds and related drug-target-disease networks, which is a breakthrough in silico approach possible at the network level. Gene information of targets was gathered from the UnitProt Database, and gene ontology analysis was performed using the David 6.8 Gene Functional Classification Tool. A total of 201 target genes were collected, which corresponded to the nine screened active compounds, and 47 genes were found to act on biological processes related to antimicrobial activity. The representative active compounds involved in antibacterial action were luteolin, kaempferol, and quercetin. Among their targets, Chemokine ligand2, Interleukin-10, Interleukin-6, and Tumor Necrosis Factor were associated with more than three antimicrobial biological processes. This study has provided accurate evidence while saving time and effort to select future laboratory research materials. The data obtained has provided important data for infection prevention and treatment strategies.

The Effect of Low-Frequency Repetitive Transcranial Magnetic Stimulation on Treatment-Resistant Tourette's Syndrome among Children and Adolescents : An Open-Label Study (치료저항성 뚜렛장애를 가진 소아청소년에서 저빈도 반복적 경두개자기자극술의 효과 : 오픈 라벨 연구)

  • Lee, Young-Ji;Chae, Jin Hyuk;Seo, Wan Seok
    • Journal of the Korean society of biological therapies in psychiatry
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    • v.24 no.3
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    • pp.239-246
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    • 2018
  • 목 적 : 본 연구의 목적은 치료저항성 뚜렛장애를 가진 소아 청소년들에 대해서 보조운동영역을 표적으로 한 저빈도 반복적 경두개자기자극술의 효과를 평가하는 것이다. 방 법 : 이 연구는 미국정신의학회 진단기준 및 통계편람, 제 4판을 기준으로 뚜렛장애로 진단받은 10명의 소아 청소년(평균연령 $12.56{\pm}1.04$세)을 대상으로 하였다. 모든 참가자들은 1년 이상 지속적으로 충분한 용량의 약물치료를 받았음에도 불구하고 한국판 예일 틱 증상 평가척도(YGTSS) 20점 이상, 임상인상척도(CGI-TS) 4점 이상을 받았다. 참가자들은 보조운동영역을 표적으로 1 Hz 반복적 경두개자기자극 치료를 매일 20분간 받았으며, 총 20회 치료를 받았다. YGTSS, CGI-TS 및 이상반응 체크리스트는 연구 시작 전과 연구 시작 후 4, 8, 12주에 시행되었다. 결 과 : 틱 증상은 연구 12주차까지 호전된 상태로 지속되었으며, YGTSS와 CGI-TS가 통계적으로 유의하게 감소하였다. 특히 음성 틱 점수의 감소가 운동 틱 점수의 변화보다 전체 YGTSS 점수의 감소에 큰 역할을 한 것으로 나타났다. 그리고 전체 10명의 참가자 중 9명이 심각한 부작용 없이 연구를 끝까지 완료하였다. 결 론 : 본 연구는 보조운동영역을 표적으로 한 저빈도 반복적 경두개자기자극술이 치료 저항성 뚜렛장애를 가진 소아 청소년들에게 효과적이고 안전한 치료도구가 될 수 있음을 시사한다. 이러한 반복적 경두개자기자극술의 치료효과를 확정하기 위해서는 보다 많은 환자를 대상으로 한 잘 통제된 연구가 필요할 것이다.

RELATIONSHIP BETWEEN CHANGES IN EVENT-RELATED POTENTIALS AND CHANGES IN CONTINUOUS PERFORMANCE TEST UNDER THE INFLUENCE OF METHYLPHENIDATE IN ATTENTION-DEFICIT/HYPERACTIVITY DISORDER (주의력 결핍 ${\cdot}$ 과잉행동장애 아동에서 Methylphenidate에 의한 사건관련전위와 연속과제수행 변화사이의 상관성)

  • Choi, Young;Lee, Mu-Suk;Lee, Mi-Suk
    • Journal of the Korean Academy of Child and Adolescent Psychiatry
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    • v.8 no.2
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    • pp.273-286
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    • 1997
  • Objective:This study was designed to evaluate effects of methylphenidate(MPH) on event-related potentials(ERP) and continuous performance test(CPT) in attention-deficit hyperactivity disorder (ADHD) and to see the correlation between changes in ERP and changes in performance. Method:ERP and CPT were used to examine the acute effects of MPH(0.5mg/kg) in eleven ADHD boys(89-103 months old). Results:1) After MPH administration, P3 latency to nontarget stimuli at Fz was significantly decreased (p<0.01) and P2 amplitudes to target stimuli at Pz and at Oz and P3 amplitude to target stimuli at Cz were significantly increased(p<0.05). 2) Commission error and omission error in the CPT-X and commission error in the CPT-AX were decreased(p<0.01), and hits and perceptual sensitivity(d') in the CPT-X and d′ in the CPT-AX were increased(p<0.01). 3) The change of P3 latency to nontarget stimuli at Fz and the change of d′ in the CPT-X were negatively correlated(p<0.05), and the change of P2 amplitude to target stimuli at Pz and d′ in the CPT-AX were positively correlated(p<0.05). Conclusion:MPH improves change orienting reaction, the delivery of task relevant information, accuracy and perceptual sensitivity in ADHD. And the increase of ability to discriminate targets from non-targets reflects reduced evaluation time in large memory component task and enhanced change orienting reaction in simple task.

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