• Title/Summary/Keyword: the Drugs

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Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex (새로운 Platinum (II) Complex [Pt (II)(trans-d-dach)(DPPE)] $(NO_3)_2$의 항암효과 및 신독성에 관한 연구)

  • Jung Jee-Chang;Lee Moon-Ho;Chang Sung-Goo;Rho Young-Soo
    • The Korean Journal of Pharmacology
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    • v.31 no.1 s.57
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    • pp.103-114
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    • 1995
  • Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (Ⅱ) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,2-bis(diphenylphosphino) ethane (DPPE) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of [Pt(trans-ddach)(DPPE).$2NO_3(PC)$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC demonstrated acceptable antitumor activity aganist P388, L-1210 lymphocytic leukemia cells and SK=OV3 human ovarian adenocarcinoma cells, and significant. activity as compared with that. cisplatin. The toxicity of PC was found quite less than thar of cisplatin using MTT, $[^3H]$ thymidine uptake and glucose consumption tests in rabbit proximal tubule cells, human kidney cortical cells and human renal cortical tissues. Based on these results, this novel platinum compound represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low toxicity.

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RNAi and miRNA in Viral Infections and Cancers

  • Mollaie, Hamid Reza;Monavari, Seyed Hamid Reza;Arabzadeh, Seyed Ali Mohammad;Shamsi-Shahrabadi, Mahmoud;Fazlalipour, Mehdi;Afshar, Reza Malekpour
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.12
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    • pp.7045-7056
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    • 2013
  • Since the first report of RNA interference (RNAi) less than a decade ago, this type of molecular intervention has been introduced to repress gene expression in vitro and also for in vivo studies in mammals. Understanding the mechanisms of action of synthetic small interfering RNAs (siRNAs) underlies use as therapeutic agents in the areas of cancer and viral infection. Recent studies have also promoted different theories about cell-specific targeting of siRNAs. Design and delivery strategies for successful treatment of human diseases are becomingmore established and relationships between miRNA and RNAi pathways have been revealed as virus-host cell interactions. Although both are well conserved in plants, invertebrates and mammals, there is also variabilityand a more complete understanding of differences will be needed for optimal application. RNA interference (RNAi) is rapid, cheap and selective in complex biological systems and has created new insight sin fields of cancer research, genetic disorders, virology and drug design. Our knowledge about the role of miRNAs and siRNAs pathways in virus-host cell interactions in virus infected cells is incomplete. There are different viral diseases but few antiviral drugs are available. For example, acyclovir for herpes viruses, alpha-interferon for hepatitis C and B viruses and anti-retroviral for HIV are accessible. Also cancer is obviously an important target for siRNA-based therapies, but the main problem in cancer therapy is targeting metastatic cells which spread from the original tumor. There are also other possible reservations and problems that might delay or even hinder siRNA-based therapies for the treatment of certain conditions; however, this remains the most promising approach for a wide range of diseases. Clearly, more studies must be done to allow efficient delivery and better understanding of unwanted side effects of siRNA-based therapies. In this review miRNA and RNAi biology, experimental design, anti-viral and anti-cancer effects are discussed.

Simple, Rapid and Sensitive Portable Molecular Diagnosis of SFTS Virus Using Reverse Transcriptional Loop-Mediated Isothermal Amplification (RT-LAMP)

  • Baek, Yun Hee;Cheon, Hyo-Soon;Park, Su-Jin;Lloren, Khristine Kaith S.;Ahn, Su Jeong;Jeong, Ju Hwan;Choi, Won-Suk;Yu, Min-Ah;Kwon, Hyeok-il;Kwon, Jin-Jung;Kim, Eun-Ha;Kim, Young-il;Antigua, Khristine Joy C.;Kim, Seok-Yong;Jeong, Hye Won;Choi, Young Ki;Song, Min-Suk
    • Journal of Microbiology and Biotechnology
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    • v.28 no.11
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    • pp.1928-1936
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    • 2018
  • Recently, human infections caused by severe fever with thrombocytopenia syndrome virus (SFTSV), which can lead to fatality, have dramatically increased in East Asia. With the unavailability of vaccines or antiviral drugs to prevent and/or treat SFTSV infection, early rapid diagnosis is critical for prevention and control of the disease. Here, we report the development of a simple, rapid and sensitive portable detection method for SFTSV infection applying reverse transcription-loop mediated isothermal amplification (RT-LAMP) combined with one-pot colorimetric visualization and electro-free reaction platform. This method utilizes a pocket warmer to facilitate diagnosis in a resource-limited setting. Specific primers were designed to target the highly-conserved region of L gene of SFTSV. The detection limit of the RT-LAMP assay was approximately $10^0$ viral genome copies from three different SFTSV strains. This assay exhibited comparable sensitivity to qRT-PCR and 10-fold more sensitivity than conventional RT-PCR, with a rapid detection time of 30 to 60 minutes. The RT-LAMP assay using SFTSV clinical specimens has demonstrated a similar detection rate to qRT-PCR and a higher detection rate compared to conventional RT-PCR. Moreover, there was no observed cross-reactive amplification of other human infectious viruses including Japanese Encephalitis Virus (JEV), Dengue, Enterovirus, Zika, Influenza and Middle East Respiratory Syndrome Coronavirus (MERS-CoV). This highly sensitive, electro- and equipment-free rapid colorimetric visualization method is feasible for resource-limited SFTSV field diagnosis.

Preparation and Characterization of Hyaluronic Acid Loaded PLGA Scaffold by Emulsion Freeze-Drying Method (히알루론산을 함유한 PLGA 지지체의 제조 및 특성결정)

  • Ko, Youn-Kyung;Kim, Soon-Hee;Jeong, Jae-Soo;Park, Jung-Soo;Lim, Ji-Ye;Kim, Moon-Suk;Lee, Hae-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.6
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    • pp.505-511
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    • 2007
  • Poly(lactide-co-glycolide)(PLGA) and hyaluronic acid (HA) has been widely used as biocompatible scaffold materials to regenerate tissue. In this present study, we fabricated microporous PLGA and HA loaded PLGA scaffolds by a emusion freeze-drying method. In order to confirm that the release profile of cytokine or water-soluble drugs, we manufactured the granulocyte macrophage colony stimulating factor(GM-CSF) loaded PLGA and HA-PLGA scaffold. All scaffolds were characterized using scanning electron microscope(SEM), mercury porosimeter and wettability measurement. Cell proliferation and viability were assessed by a 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium-bromide (MTT) test. The porosity of HA-PLGA scaffold was greater than 95% with the total pore area of $261\;m^2/g$. The HA-FLGA scaffold exhibited well interconnected pores to allow greater cell adhesion and prolixferation. It was proven by higher cell viability in the HA-PLGA scaffold than PLGA alone. This may be due to the enhanced natural properties and higher water retention capacity of HA.

A Study on Life Changes of Oral Lichen Planus Patients by SRRS (SRRS를 이용한 구강 편평태선 환자의 생활변화에 관한 연구)

  • Ko, Myung-Yun;Park, Su-Hyeon;Ok, Su-Min;Huh, Joon-Young;Ahn, Yong-Woo;Jeong, Sung-Hee
    • Journal of Oral Medicine and Pain
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    • v.37 no.1
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    • pp.9-17
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    • 2012
  • Lichen planus is a chronic inflammatory mucocutaneous disease that affects multiple sites of the body. Often it involves the oral mucosa, but also involve other sites such as skin, genitals, scalp and nails. There is no clear cause of oral lichen planus (OLP), current data suggest that OLP is a T-cell mediated autoimmune disorder which may have an altered self-peptide triggering apoptosis of oral epithelial cells. Usually OLP appears in middle-aged women which tends to be chronic with periods of exacerbation and remission. There are many theories those causes the OLP such as psychological and environmental factors, genetic tendency, drugs and more. 60-70% of lichen planus is accompanied by oral lesions, and more than half of its cases are not able to defined by their skin. In this study, among all the possibility(possible) theories, we tried to evaluate the influence of emotional stress in exacerbating OLP. There were thirty patients with a clinical or histological diagnosis of OLP and other thirty subjects who did not show any signs of systemic disorders include OLP. They were evaluated by using modified Holmes and Rahe's Social Readjustment Rating Scale (SRRS). As a result, a significantly higher level of stress was found in the OLP patients than the control group. Therefore it could be concluded that psychological stressors play an important role in the exacerbating OLP.

The Anticancer Effects and Drug Metabolic Enzyme Change by Intraperitoneal Injection of Agrimonia Pilosa Ledeb (선학초 (짚신나물) 복강주사의 항암효과 탐색 및 약물 대사효소의 변화)

  • Choi, Jung-Won;Jang, Bo-Hyung;Lee, Ju-Ah;Ko, Ho-Yeon;Jung, Hee;Jun, Chan-Yong;Park, Jong-Hyung;Kim, Ji-Hye;Ko, Seong-Gyu;Choi, You-Kyung
    • The Journal of Korean Medicine
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    • v.30 no.4
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    • pp.129-141
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    • 2009
  • Objective: This study was to investigate the anti-tumor effect, safety, safety, mechanism and metabolizing enzyme of Agrimonia pilosa LEDEB (APL) in female C57B/L mouse tumor (in vivo). Method: First, to evaluate the antitumor activity of APL, we divided the mice into four groups: normal, control, APL50 (50mg/kg), and APL100 (100mg/kg). LLC-obtained American Type Culture Collection was used. LLC had been inoculated to induce tumors. To measure the anti-tumor effect of APL, we calibrated tumor size and weight. To analyze the mechanism of anti-tumor in APL, we used western blotting and to observe metabolizing enzyme in APL we used to real-time PCR. Result: APL50 and APL100 significantly inhibited tumor growth from 12 days after medicine injected. APL did not induce caspase-dependent apoptosis in LLC-bearing mouse tumor. In APL100, it decreased 41% and 71% in CYP2D22 and CYP3A11, respectively. Conclusion: These results suggest that APL has some anti-tumor effects in female C57B/L mouse tumor. APL should be used carefully with other drugs related with CYP2D22 and CYP3A11.

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A Comparison of Two Intramuscular Doses of a Xylazine-Diazepam-Ketamine Combination in Dogs (개에서 Xylazine-diazepam-ketamine 병용마취 시 두 가지 근육내 투여 용량 비교)

  • Lee, Jae-Yeon;Seo, Ji-Won;Cho, Jae-Geum;Cho, Ha-Eun;Jeong, Seong-Mok;Kim, Myung-Cheol
    • Journal of Veterinary Clinics
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    • v.29 no.1
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    • pp.12-17
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    • 2012
  • Many drugs are administered intramuscularly to immobilize and anesthetize dogs. There are many established intramuscular (IM) anesthetic combinations for dogs; however, little information is available on the effects of a xylazinediazepam-ketamine (XDK) combination. The purpose of this study was to investigate the anesthetic effects of the XDK combination in dogs. Twelve adult mixed bred dogs were used. All dogs were anesthetized with an IM injection of diazepam (0.5 mg/kg) and xylazine (1.1 mg/kg) with low-dose ketamine (5 mg/kg; group 1) or high-dose ketamine (10 mg/kg; group 2) in one syringe. After administration of the test dose, the animals were positioned in a right lateral recumbency, and analgesia and cardiopulmonary data were collected and recorded. The duration of anesthesia in group 2 was significantly longer than that of group 1 (mean [sd] 68.0 [7.6] v 51.3 [2.7] minutes). Blood pressure increased significantly after XDK administration in both groups, and $S_aO_2$ levels decreased significantly from baseline at 10, 20, and 30 minutes in both groups. XDK administration produced satisfactory sedation and analgesia in all dogs. In conclusion, intramuscular administration of xylazine-diazepam-ketamine combination at a doses of 1.1 mg/kg xylazine, 0.5 mg/kg diazepam, and 5 or 10 mg/kg ketamine appeared to be effective short duration anesthetic protocols in dogs.

Transmission of Multiple Drag-Resistance in Hospital Pseudomonas aeruginosa by Intraspecies Conjugation System (병원녹농균(病院綠膿菌)의 동종균접합(同種菌接合)에 의한 다제내성(多劑耐性)의 전달(傳達))

  • Kim, Chung;Han, Wang-Su;Seo, In-Su
    • The Journal of the Korean Society for Microbiology
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    • v.14 no.1
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    • pp.49-61
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    • 1979
  • Two hundred and ninety-five strains of Peudomonas aeruginosa isolated from clinical sources were tested for drug resistance and demonstration of R plasmids by intraspecies conjugation system. Sixty strains were found highly resistant to two or more of drugs. The rate of resistant strains were 38.9% to kanamycin(km), 33.2% to streptomydn(sm), 22.7% to sulfisomidine(Sa), 14.2% to chloramphenicol(Cp), 13.8% to tetracycline(Tc), 3.0% to carbenicillin(Cb), and to gentamicin(Gm), respectively. But no strains was resistant to nalidixic acid and colistine. They were resistant to per milliliter to more than $400{\mu}g$ per ml. of Tc, $800{\mu}g$ per ml of Cp and of Sm, $6,400{\mu}g$ per ml. of Sa, $200{\mu}g$ per ml. of Cb, $100{\mu}g$ per ml. of Gm, and $25{\mu}g$ per ml. of colistine. Forty-three strains of Pseudomonas aeruginosa could be transferred their resistance to Pseudomonas aeruginosa 2-70, 1005 rifampin resistant FP-auxotrophic mutant. Of sixty multiple resistant strains, forty-three(71.6%) demonstrated R plasmids; nineteen carried resistance to(Tc Cp Sm Sa), six to(Tc Cp Sm), three to(Tc Cp Sa), and Cp, five to(Tc Sm Sa), two to(Tc Sa), (Cp Sm) and Tc, and one to(Cp Sm Sa). Degree of resistance of recipients recieving R plasmids from donors were almost the same level of resistance as the donor in regardless of mating temperature at $25^{\circ}C$ and $37^{\circ}C$. Resistance to Tc, Sm, and Sa were transferred to a very few of recipient cells at five minutes after mating with donor and recipient cells but resistance to Cp were transferred to the majority of recipient cells. The transfer frequency of Tc, Cp, Sm, and Sa resistance from donors to recipients were from $1.0^{-1.4}\;to\;1.0^{-3.5}$ at $25^{\circ}C$ for 18 hours of incubation and were from $1.0^{-1.5}\;to\;1.0^{-3.5}$ at $37^{\circ}C$ for 18 hours of incubation.

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Isolation of an Anticariogenic Compound from Magnoliae Bark (후박피(Magnoliae bark)로부터 항충치활성을 갖는 물질의 분리)

  • Lee, Youn-Soo;Park, Hun-Joo;You, Jae-Sun;Park, Hyung-Hwan;Kwon, Ik-Boo;Lee, Hyeon-Yong
    • Korean Journal of Food Science and Technology
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    • v.30 no.1
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    • pp.230-236
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    • 1998
  • We have screened total 32 herbal drugs to find the highest activity against human cariogenic enzyme, glucosyltransferase (GTase) from the extracts of Magnoliae bark. The extracts were separated into three phases, i. e. water, n-butanol and ethylacetate according to their solvent polarity. Among them, ethylacetate fraction had approximately more than 70% of total activities, and the active principle was further isolated by prep. HPLC following silicagel column chromatography to yield single compound as white powder. The chemical structure of the compound was finally elucidated to be 4,4'-dihydroxy-3,3'-dimethoxylignan from the spectral data of FAB-MS. $^1H-\;and\;^{13}C-NMR$ spectrometries. The compound was also shown to have relatively strong antibacterial activity against ten types of cariogenic oral bacteria and one kind of Actinomyces sp.

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TREATMENT OF IMMATURE TEETH WITH A 3-MIX PASTE: CASE REPORT (항생제를 이용한 미성숙 영구치의 치험례)

  • Kim, So-Jung;Cho, Hae-Sung;Chung, Youn-Joo;Choi, Sung-Chul;Park, Jae-Hong
    • Journal of the korean academy of Pediatric Dentistry
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    • v.38 no.1
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    • pp.44-50
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    • 2011
  • An immature tooth with infected pulp has numerous potential complications. Conventional apexification with calcium hydroxide has several disadvantages, including susceptibility to tooth fracture. This method does not promote continual root development. Pulp revascularization of a necrotic, immature permanent tooth will allow further development of the root and dentinal structure. Disinfection of the root canal system is a prerequisite for pulp revascularization and tissue regeneration. A combination of antibiotic drugs (ciprofloxacin, metronidazole, and minocycline) is effective for disinfection of necrotic pulp, and has been used successfully in regenerative endodontic treatment. These case reports involve the treatment of 3 immature permanent teeth with necrotic pulp using a 3-Mix paste and mineral trioxide aggregate. All cases showed the notable apical maturation with closure of the apex and increased thickness of dentinal walls. This approach suggests a paradigm shift in treating endodontically involved immature permanent teeth from the traditional apexification with calcium hydroxide to the conservative approach by providing a favorable environment for tissue regeneration.