• 제목/요약/키워드: Preclinical research

검색결과 230건 처리시간 0.029초

Characterization of Preclinical in Vitro and in Vivo Pharmacokinetic Properties of KPLA-012, a Benzopyranyl 1,2,3-Triazole Compound, with Anti-Angiogenetic and Anti-Tumor Progressive Effects

  • Nam, So Jeong;Lee, Taeho;Choi, Min-Koo;Song, Im-Sook
    • Mass Spectrometry Letters
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    • 제9권2호
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    • pp.61-65
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    • 2018
  • KPLA-012, a benzopyranyl 1,2,3-triazole compound, is considered a potent $HIF-1{\alpha}$ inhibitor based on the chemical library screening, and is known to exhibit anti-angiogenetic and anti-tumor progressive effects. The aim of this study was to investigate the pharmacokinetic properties of KPLA-012 in ICR mice and to investigate in vitro characteristics including the intestinal absorption, distribution, metabolism, and excretion of KPLA-012. The oral bioavailability of KPLA-012 was 33.3% in mice. The pharmacokinetics of KPLA-012 changed in a metabolism-dependent manner, which was evident by the low recovery of parent KPLA-012 from urine and feces and metabolic instability in the liver microsomes. However, KPLA-012 exhibited moderate permeability in Caco-2 cells ($3.1{\times}10^{-6}cm/s$) and the metabolic stability increased in humans compared to that in mice (% remaining after 1 h; 47.4% in humans vs 14.8% in mice). Overall, the results suggest that KPLA-012 might have more effective pharmacokinetic properties in humans than in mice although further studies on its metabolism are necessary.

Changes in Blood Constituents of Rabbits Subjected to Transportation under Hot, Humid Tropical Conditions

  • Nakyinsige, K.;Sazili, A.Q.;Aghwan, Z.A.;Zulkifli, I.;Goh, Y.M.;Fatimah, A.B.
    • Asian-Australasian Journal of Animal Sciences
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    • 제26권6호
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    • pp.874-878
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    • 2013
  • Unlike Europe (particularly, Italy and Spain), where a number of studies have been conducted on the stressful effects of transport on rabbit welfare, few studies have been conducted on transportation of rabbits under hot, humid tropical conditions experienced in countries like Malaysia. We studied the effects of transportation in hot humid tropical conditions of Malaysia on physiometabolic changes in New Zealand white rabbits. Eighty experimental animals were divided into two groups of 40 bucks each and transported for either 3 or 1 h. Transportation caused a significant upsurge of aspartate aminotransferase, alanine aminotransferase and creatine kinase activities (p<0.001) though did not significantly affect lactate dehydrogenase (LDH) activity (p = 0.0706). Both transportation periods caused elevation in plasma glucose levels, lactic acidosis and dehydration as evidenced through elevated packed cell volume and plasma protein concentration. It was concluded that regardless of the duration, transport of rabbits under hot humid tropical conditions, resulted in heat distress since the rabbits showed hyperglycemia, hypercalcemia, lactacidemia, lymphocytopenia, dehydration and increase in blood enzyme activities.

Potential of some traditionally used edible plants for prevention and cure of diabesity associated comorbidities

  • Kumar, Vikas;Thakur, Ajit Kumar;Verma, Suruchi;Yadav, Vaishali;Chatterjee, Shyam Sunder
    • 셀메드
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    • 제5권2호
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    • pp.8.1-8.22
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    • 2015
  • Medicinal uses of edible and other plants for prevention and cure of obesity and overweight associated metabolic and mental health problems have since long been known to scholars and practitioners of Ayurvedic and other traditionally known system of medicine. Modernized versions of numerous edible plant derived formulations mentioned in ancient Ayurvedic texts are at present some of the most popular, or best selling, herbal remedies in India and numerous other countries suffering from double burden of diseases caused by malnutrition and obesity. Preclinical and clinical information now available on edible plants and their bioactive constituents justify traditionally known medicinal uses of products derived from them for prevention and cure of obesity associated type-2 diabetes, psychopathologies and other health problems. Such information now available on a few edible Ayurvedic plants and their formulations and suggesting that their stress response regulating effects are involved in their broad spectrums of bioactivity profiles are summarized in this communication. Implications of recent physiological and pharmacological observations made with numerous phytochemicals isolated from edible plants for better understanding of traditionally known medicinal uses of herbal remedies are also pointed out.

임상실습 전 동료멘토링 학습을 적용한 OSCE 프로그램이 간호학생의 핵심기본간호술 수행자신감과 비판적 사고성향에 미치는 효과 (The effects of Peer Mentoring Learnings-based Preclinical OSCE program on Self-Confidence on Core Basic Nursing Skills and Critical Thinking Disposition for Nursing Student)

  • 윤매옥;주연숙
    • 디지털융복합연구
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    • 제15권7호
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    • pp.285-295
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    • 2017
  • 본 연구는 임상실습 전 동료멘토링 학습을 적용한 OSCE프로그램(객관적 구조화 임상시험)을 실시하여 간호학생의 핵심기본간호술 자신감 및 비판적 사고성향에 미치는 효과를 파악하고자 수행하였다. 연구설계는 비동등성 대조군 전후실험설계의 실험연구로 연구대상은 J도 소재 일개 4년제 대학 간호학과 2학년 학생 68명이었으며 연구기간은 2016년 2월부터 2017년 2월까지였다. 연구결과 임상실습 전 동료 멘토링 학습을 적용한 OSCE프로그램(객관적 구조화 임상시험)이 핵심 기본간호술 수행자신감과 비판적 사고성향을 대조군에 비해 실험군이 유의하게 증가시켰고, 중재 후 핵심기본간호술 자신감과 비판적 사고성향 간에 긍정적 상관관계가 있는 것으로 나타났다. 따라서 임상실습 전 동료멘토링 학습을 적용한 OSCE프로그램이 간호학생의 핵심기본간호술 자신감과 비판적 사고성향을 향상시키는데 효과적이었으므로 이를 토대로 동료멘토링 학습을 적용한 OSCE프로그램의 효과를 비교분석하는 연구를 제언한다.

Intracranial anaplastic oligodendroglioma concurrent with hydrocephalus and syringomyelia in a Boston terrier dog

  • Park, Chul;Kang, Byeong-Teck;Yoo, Jong-Hyun;Kim, Ha-Jung;Jung, Dong-In;Lim, Chae-Young;Kim, Jae-Hoon;Woo, Eung-Je;Kang, Sang-Chul;Park, Hee-Myung
    • 대한수의학회지
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    • 제48권1호
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    • pp.93-98
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    • 2008
  • A 6-year-old female Boston terrier dog was presented with seizure episode, forelimb paraparesis, excessive panting, and ataxia. On physical and neurological examination, episcleral vessel engorgement, delayed postural reaction, delayed pupillary light reflex (both direct and consensual), and crossed forelimb were noted. Serum biochemical profiles were not remarkable other than mildly elevated hepatic enzymes. On cerebrospinal fluid analysis, elevated protein concentration was observed. In magnetic resonance imaging scans, the left frontal brain lesion with ring enhancement strongly suggested the presence of intracranial tumor. Concurrently, secondary hydrocephalus and syringomyelia were also observed. The dog was euthanized at 4 months after initial presentation because of aggravated neurological signs. This case was definitely diagnosed as an intracranial anaplastic oligodendroglioma based on postmortem histopathologic examination.

게르마늄 복합물인 STB-HO-BM에 대한 유전독성에 관한 연구 (Genotoxicity Studies of STB-HO-BM, a Germanium Complex)

  • 송시환;정연권;홍동호
    • Toxicological Research
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    • 제22권2호
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    • pp.145-151
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    • 2006
  • We have investigated the genotoxicity of STB-HO-BM using in vitro and in vivo system such as Ames reverse mutation test, chromosomal aberration test and micronucleus test. in Ames reverse mutation test, STB-HO-BM treatment at the dose range up to 5,000 ug/plate did not induce mutagenicity in Salmonella typhimurium TA98, TA100, TA102, TA1535, TA 1537 and in Escherichia coli WP2 uvrA with and without metabolic activation. Any significant aberration wasn't observed in chinese hamster lung (CHL) fibroblast cells treated with STB-HO-BM at the concentration of 12.5, 2.5, 5 mg/ml both in the absense and presence of metabolic activation system. In mouse micrnucleus test, no significant increase in the occurrence of micronucleated polychromatic erythrocytes was observed in ICR male mice orally administered with STB-HO-BM at the doses of 0.5, 1.0, 2.0 g/kg. These results indicate that STB-HO-BM has no mutagenic potential under the condition in this study.

돼지의 과립막세포 종양 (Granulosa cell tumor in a sow)

  • 김형석;강상철;정지열;김현섭;김대용;김재훈
    • 대한수의학회지
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    • 제48권3호
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    • pp.323-326
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    • 2008
  • A two-year-old mixed breed sow was requested to the Veterinary Pathology Laboratory of Cheju National University with a clinical signs of severe abdominal pain and sudden death. Grossly, there was severe hemorrhage in abdominal cavity. Most of internal parenchymas and subcutaneous muscle showed severe pale discoloration. Both ovaries were enlarged with oval to round protruding multilobular masses and dark red in color. And they were firm and contained multiple small cysts in their cut surface. Histopathologically, numerous neoplastic granulosa cells had spherical-to-oval, hyperchromatic nuclei and scant eosinophilic cytoplasms were distributed with follicular pattern in ovarian masses. And the typical Call-Exner bodies, distinctive microcavityies, were observed in the center of small neoplastic follicles. Based on the gross and histopathologic findings, this case was diagnosed as granulosa cell tumor. In our best knowledge, this is believed to be the first report of granulosa cell tumor in a sow in Korea.

Development of Drugs and Technology for Radiation Theragnosis

  • Jeong, Hwan-Jeong;Lee, Byung Chul;Ahn, Byeong-Cheol;Kang, Keon Wook
    • Nuclear Engineering and Technology
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    • 제48권3호
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    • pp.597-607
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    • 2016
  • Personalized medicine is tailored medical treatment that targets the individual characteristics of each patient. Theragnosis, combining diagnosis and therapy, plays an important role in selecting appropriate patients. Noninvasive in vivo imaging can trace small molecules, antibodies, peptides, nanoparticles, and cells in the body. Recently, imaging methods have been able to reveal molecular events in cells and tissues. Molecular imaging is useful not only for clinical studies but also for developing new drugs and new treatment modalities. Preclinical and early clinical molecular imaging shows biodistribution, pharmacokinetics, mechanisms of action, and efficacy. When therapeutic materials are labeled using radioisotopes, nuclear imaging with positron emission tomography or gamma camera can be used to treat diseases and monitor therapy simultaneously. Such nuclear medicine technology is defined as radiation theragnosis. We review the current development of drugs and technology for radiation theragnosis using peptides, albumin, nanoparticles, and cells.

Oncogene-Driven Metabolic Alterations in Cancer

  • Min, Hye-Young;Lee, Ho-Young
    • Biomolecules & Therapeutics
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    • 제26권1호
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    • pp.45-56
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    • 2018
  • Cancer is the leading cause of human deaths worldwide. Understanding the biology underlying the evolution of cancer is important for reducing the economic and social burden of cancer. In addition to genetic aberrations, recent studies demonstrate metabolic rewiring, such as aerobic glycolysis, glutamine dependency, accumulation of intermediates of glycolysis, and upregulation of lipid and amino acid synthesis, in several types of cancer to support their high demands on nutrients for building blocks and energy production. Moreover, oncogenic mutations are known to be associated with metabolic reprogramming in cancer, and these overall changes collectively influence tumor-microenvironment interactions and cancer progression. Accordingly, several agents targeting metabolic alterations in cancer have been extensively evaluated in preclinical and clinical settings. Additionally, metabolic reprogramming is considered a novel target to control cancers harboring un-targetable oncogenic alterations such as KRAS. Focusing on lung cancer, here, we highlight recent findings regarding metabolic rewiring in cancer, its association with oncogenic alterations, and therapeutic strategies to control deregulated metabolism in cancer.

Avian malaria associated with Plasmodium spp. infection in a penguin in Jeju Island

  • Ko, Kyeong-Nam;Kang, Sang-Chul;Jung, Ji-Youl;Bae, Jong-Hee;Kim, Jae-Hoon
    • 대한수의학회지
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    • 제48권2호
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    • pp.197-201
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    • 2008
  • Plasmodium spp. in domestic and wild birds are microscopic, intracellular parasitic protozoa within the blood cells and tissues cause avian malaria. A 17-month-old Magellan penguin (Spheniscus magellanicus) with a clinical signs of anorexia, depression, and respiratory distress for 3 days was submitted to the Pathology Department of Veterinary Medicine, Cheju National University in October 2005. It was born and reared in the Jeju Island. Grossly, the liver was enlarged, pale and friable. The spleen was also enlarged with dark red coloration and friable. Histopathologically, the lesions in the liver were characterized by multifocal infiltration of macrophages and lymphocytes especially in perivascular regions. The schizonts of Plasmodium spp. contained up to 30 merozoites were found in numerous infiltrated mononuclear cells. Similarly, histiocytic cells were proliferated in red pulp of spleen and the schizonts were found in these cells. Numerous dark brown pigments were widely distributed in the liver and spleen. The result of the nested polymerase chain reaction clarified the causative agent of this case was Plasmodium spp.. This is the first report for the outbreak of avian malaria caused by Plasmodium spp. in a penguin that was born and reared in Jeju Island in Korea.