• Title, Summary, Keyword: conventional drugs

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Evolutionary and Comparative Genomics to Drive Rational Drug Design, with Particular Focus on Neuropeptide Seven-Transmembrane Receptors

  • Furlong, Michael;Seong, Jae Young
    • Biomolecules & Therapeutics
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    • v.25 no.1
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    • pp.57-68
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    • 2017
  • Seven transmembrane receptors (7TMRs), also known as G protein-coupled receptors, are popular targets of drug development, particularly 7TMR systems that are activated by peptide ligands. Although many pharmaceutical drugs have been discovered via conventional bulk analysis techniques the increasing availability of structural and evolutionary data are facilitating change to rational, targeted drug design. This article discusses the appeal of neuropeptide-7TMR systems as drug targets and provides an overview of concepts in the evolution of vertebrate genomes and gene families. Subsequently, methods that use evolutionary concepts and comparative analysis techniques to aid in gene discovery, gene function identification, and novel drug design are provided along with case study examples.

Effect of the Geijibokryunghwan Water Extracts on Stimulus-induced Superoxide Generation and Tyrosyl Phosphorylation in Human Neutrophils

  • Choi, Meung-Hee;Park, Won-Han
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.2
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    • pp.477-481
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    • 2006
  • A clinical report indicates that 'Geijibokryunghwan(GBH) is very effective in treating thrombosis in those patients who have difficulties with more conventional antithrombotic drugs. The isolation and identification of various compounds from this plant and the same genus have been reported by several groups. However, the pharmaceutical effect of the GBH on superoxide generation in human neutrophils has not been studied. In the present report, we investigated the possibility of using herbal medicine as an alternative therapy. In particular, we studied tremor in antiatheroscleosis. In this report, we shows the GBH extract can be used as a potential atherosclerosis preventive agent in human. The effect of GBH on stimulus-induced superoxide generation and phosphorylation of tyrosine residues of protein in human neutrophils was investigated. In a conclusion, GBH suppressed tyrosine phosphorylase in a dose-dependent manner, and may have pharmacoceutical applications. These data suggest that GBH extracts merits investigation as a potential anti-atherosclerogenic agent in humans.

Targeting Multidrug Resistance with Small Molecules for Cancer Therapy

  • Xia, Yan;Lee, Kyeong
    • Biomolecules & Therapeutics
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    • v.18 no.4
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    • pp.375-385
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    • 2010
  • Conventional cancer chemotherapy is seriously limited by tumor cells exhibiting multidrug resistance (MDR), which is caused by changes in the levels or activity of membrane transporters that mediate energy-dependent drug efflux and of proteins that affect drug metabolism and/or drug action. Cancer scientists and oncologists have worked together for some time to understand anticancer drug resistance and develop pharmacological strategies to overcome such resistance. Much focus has been on the reversal of the MDR phenotype by inhibition of ATP-binding cassette (ABC) drug transporters. ABC transporters are a family of transporter proteins that mediate drug resistance and low drug bioavailability by pumping various drugs out of cells at the expense of ATP hydrolysis. Many inhibitors of MDR transporters have been identified, and though some are currently undergoing clinical trials, none are in clinical use. Herein, we briefly review the status of MDR in human cancer, explore the pathways of MDR in chemotherapy, and outline recent advances in the design and development of MDR modulators.

Cell behavior study using microfluidic chip (마이크로 유체 칩을 이용한 세포행태에 관한 연구)

  • Park, Joong-Yull;Lee, Sang-Hoon
    • Proceedings of the KSME Conference
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    • pp.1450-1454
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    • 2008
  • In the conventional biology, the most of cell studies was carried out by culturing cells in the Petri dish and by investigating cellular behavior under the diverse bio-molecule (cell signalling materials, drugs or etc.) conditions. However, in vivo environments, diverse stimulations including chemical, mechanical and topological environments involved in the proliferation, differentiation and migration of cells and it is almost impossible to provide these conditions with traditional method. We have developed the methods to provide the well defined chemical and mechanical stimulations using microfluidic devices and applied these approaches to the study of environmental effect on cells. In this paper, we will introduce our microfluidic chips to provide microenvironment and its applications using several cells.

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Active microneedle actuated by thermopneumatic force (열 공압을 이용한 능동 미세바늘의 제작)

  • An J.Y.;Hwang I.H.;You S.K.;Lee J.H.
    • Proceedings of the Korean Society of Precision Engineering Conference
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    • pp.694-697
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    • 2005
  • This paper presents a novel movable microneedle that becomes active when necessary to use. Conventional researches have been focused on the fabrication of microneedles and the interface with fluidic chip [1,2]. Therefore, we proposed an active microneedle to sample body fluids or deliver drugs in a controlled amount by actuating the needles. This allows us to keep the needles in operation only when necessary so that both the body skin and the needles can be protected from undesirable external disturbance while no operation.

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Considerations for submucosal midazolam administration in combination with oral and inhaled medications for sedation of pediatric dental patients

  • Baek, Kwanwoo
    • Journal of Dental Anesthesia and Pain Medicine
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    • v.15 no.2
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    • pp.47-52
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    • 2015
  • Sedation allows patients to maintain their airway independently and respond appropriately to physical stimulation and verbal command while maintaining a minimum depressed level of consciousness. Drugs commonly used for sedation of pediatric dental patients include a combination of chloral hydrate, hydroxyzine, and nitrous oxide-oxygen. Midazolam is a benzodiazepine and currently one of the most commonly used intravenous sedative agents. It can be easily titrated to provide a wide range of sedation, from conscious sedation to deep sedation, and exhibits a wide safety margin without severe respiratory and circulatory depression. At an appropriate dose, it also decreases patient anxiety and induces amnesia. We found that the submucosal administration of midazolam combined with chloral hydrate provided increased sedative effects and decreased the postoperative vomiting response compared with conventional chloral hydrate administration, with no significant difference in physiological responses. The depth of sedation can be titrated using this technique.

Characteristic Features of Cytotoxic Activity of Flavonoids on Human Cervical Cancer Cells

  • Sak, Katrin
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.19
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    • pp.8007-8018
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    • 2014
  • Cervical cancer is the most common gynecologic malignancy worldwide and development of new therapeutic strategies and anticancer agents is an urgent priority. Plants have remained an important source in the search for novel cytotoxic compounds and several polyphenolic flavonoids possess antitumor properties. In this review article, data about potential anticarcinogenic activity of common natural flavonoids on various human cervical cancer cell lines are compiled and analyzed showing perspectives for the use of these secondary metabolites in the treatment of cervical carcinoma as well as in the development of novel chemotherapeutic drugs. Such anticancer effects of flavonoids seem to differentially depend on the cellular type and origin of cervical carcinoma creating possibilities for specific targeting in the future. Besides the cytotoxic activity per se, several flavonoids can also contribute to the increase in efficacy of conventional therapies rendering tumor cells more sensitive to standard chemotherapeutics and irradiation. Although the current knowledge is still rather scarce and further studies are certainly needed, it is clear that natural flavonoids may have a great potential to benefit cervical cancer patients.

Health Benefits of Moringa oleifera

  • Abdull Razis, Ahmad Faizal;Ibrahim, Muhammad Din;Kntayya, Saie Brindha
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.20
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    • pp.8571-8576
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    • 2014
  • Phytomedicines are believed to have benefits over conventional drugs and are regaining interest in current research. Moringa oleifera is a multi-purpose herbal plant used as human food and an alternative for medicinal purposes worldwide. It has been identified by researchers as a plant with numerous health benefits including nutritional and medicinal advantages. Moringa oleifera contains essential amino acids, carotenoids in leaves, and components with nutraceutical properties, supporting the idea of using this plant as a nutritional supplement or constituent in food preparation. Some nutritional evaluation has been carried out in leaves and stems. An important factor that accounts for the medicinal uses of Moringa oleifera is its very wide range of vital antioxidants, antibiotics and nutrients including vitamins and minerals. Almost all parts from Moringa can be used ad a source for nutrition with other useful values. This mini-review elaborates on details of its health benefits.

A case of Hashimoto's encephalopathy presenting with seizures and psychosis

  • Lee, Min-Joo;Lee, Hae-Sang;Hwang, Jin-Soon;Jung, Da-Eun
    • Clinical and Experimental Pediatrics
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    • v.55 no.3
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    • pp.111-113
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    • 2012
  • Hashimoto's encephalopathy (HE) is a rare, poorly understood, autoimmune disease characterized by symptoms of acute or subacute encephalopathy associated with increased anti-thyroid antibody levels. Here, we report a case of a 14-year-old girl with HE and briefly review the literature. The patient presented with acute mental changes and seizures, but no evidence of infectious encephalitis. In the acute stage, the seizures did not respond to conventional antiepileptic drugs, including valproic acid, phenytoin, and topiramate. The clinical course was complicated by the development of acute psychosis, including bipolar mood, insomnia, agitation, and hallucinations. The diagnosis of HE was supported by positive results for antithyroperoxidase and antithyroglobulin antibodies. Treatment with methylprednisolone was effective; her psychosis improved and the number of seizures decreased. HE is a serious but curable, condition, which might be underdiagnosed if not suspected. Anti-thyroid antibodies must be measured for the diagnosis. HE should be considered in patients with diverse neuropsychiatric manifestations.

The role of lipids in the pathogenesis and treatment of type 2 diabetes and associated co-morbidities

  • Erion, Derek M.;Park, Hyun-Jun;Lee, Hui-Young
    • BMB Reports
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    • v.49 no.3
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    • pp.139-148
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    • 2016
  • In the past decade, the incidence of type 2 diabetes (T2D) has rapidly increased, along with the associated cardiovascular complications. Therefore, understanding the pathophysiology underlying T2D, the associated complications and the impact of therapeutics on the T2D development has critical importance for current and future therapeutics. The prevailing feature of T2D is hyperglycemia due to excessive hepatic glucose production, insulin resistance, and insufficient secretion of insulin by the pancreas. These contribute to increased fatty acid influx into the liver and muscle causing accumulation of lipid metabolites. These lipid metabolites cause dyslipidemia and non-alcoholic fatty liver disease, which ultimately contributes to the increased cardiovascular risk in T2D. Therefore, understanding the mechanisms of hepatic insulin resistance and the specific role of liver lipids is critical in selecting and designing the most effective therapeutics for T2D and the associated co-morbidities, including dyslipidemia and cardiovascular disease. Herein, we review the effects and molecular mechanisms of conventional anti-hyperglycemic and lipid-lowering drugs on glucose and lipid metabolism.