• Title/Summary/Keyword: Drug efficacy

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A Potential Efficacy of Rebamipide as Anti-gastric Cancer Drug (위암치료제로서 rebamipide의 잠재적 효능)

  • Min, Do Sik
    • Journal of Life Science
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    • v.26 no.10
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    • pp.1214-1217
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    • 2016
  • Rebamipide is a mucosal-protective antiulcer drug, but its mechanism of action in gastric cancer remains elusive. CagA, a major virulence factor of Helicobacter pylori (H. pylori), is associated with the risk of gastric cancer. CagA protein is injected into gastric epithelial cells and deregulates a variety of cellular signaling molecules. CagA from H. pylori induces phospholipase D1 (PLD1) expression through NFκB activation in gastric epithelial cells, followed by invasion and proliferation of gastric epithelial cancer cells. Infection with cagA-positive H. pylori and expression of CagA enhances the binding of NFκB to the PLD1 promoter. Rebamipide abolishes H. pylori cagA-induced PLD1 expression via inhibition of binding of NFκB to the PLD1 promoter and also inhibits PLD activity. Moreover, rebamipide abolishes H. pylori CagA-induced β-catenin and the expression of a target cancer stem cell (CSC) marker gene via upregulation of miRNA-320a and -4496, followed by attenuation of self-renewal capacity of H. pylori CagA-infected gastric CSCs. In addition, rebamipide increases the chemosensitivity of CagA-expressed gastric CSCs and suppresses gastric carcinogenesis. Thus, it is speculated that rebamipide might show a potent efficacy as chemotherapeutic drug against gastric cancer cells. In this review, we summarizes recent results regarding the novel insights for the efficacy of rebamipide in gastric cancer cells.

Chemotherapeutic Efficacy of Trimethoprim-Sulfamethoxaxole ($Bactrim^{\circledR}$) in Experimental Murine Toxoplasmosis (Trimethoprim-sulfamethoxazole이 톡소플라스마 감염 마우스의 혈액상에 미치는 영향)

  • 조성원;용태순
    • Parasites, Hosts and Diseases
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    • v.25 no.2
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    • pp.199-208
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    • 1987
  • The chemotherapeutic efficacy of trimethoprim-sulfamethoxazole ($Bactrim^{\circledR}$) in mice experimentally infected with Toxoplasma gcndii was evaluated. The average survival days and survival rate of mice infected intraperitoneally with $1{\times}10^5$ trophozoites and treated with $Bactrim^{\circledR}$ were compared with those of untreated group. The hematologic findings of blood samples of experimental mice were observed for comparison of side elects between $Bactrim^{\circledR}$ and pyrimethamine ($Daraprim^{\circledR}$), the latter of which has been one of the favorable drugs for the treatment of toxoplasmosis. The results are summarized as follows: 1. $Bactrim^{\circledR}$ showed a strong evidence of potent anti-Toxoplasma activity. The survival rate of mice administered with 24 mg of $Bactrim^{\circledR}$ per mouse per day for 7 days, was 83.3%, and the rate was increased to 100% in mice administered with two-fold concentrated dose of the drug. 2. The average numbers of white blood cells (W.B.C.) in the mouse groups treated with $Bactrim^{\circledR}$ or $Daraprim^{\circledR}$ were more increased than those only infected with T. gondii. The mice treated with $Daraprim^{\circledR}$ however, showed remarkably decreased numbers of W.B.C. as compared with those treated with $Bactrim^{\circledR}$ . 3. The average numbers of red blood cells (R.B.C.) and platelets both in the drug-treated and untreated T. gondii-infected mice were decreased as compared with normal mice. The numbers of R. B. C. in $Daraprim^{\circledR}-treated$ mice, however, were more decreased than in $Bactrim^{\circledR}-treated$ mice. 4. The average levels of hemoglobin both in the drug.treated and untreated T. gondii-infected mice were decreased, compared with normal mice. But there was no difference in the levels of hemoglobin between $Bactrim^{\circledR}$ and $Daraprim^{\circledR}-treated$ groups. In conclusion, trimethoprim.sulfamethoxasole ($Bactrim^{\circledR}$) was proven to be effective and safe for the treatment of murine toxoplasmosis. The efficacy was comparable with pyrimethamine ($Daraprim^{\circledR}$), but bone marrow depression was less severe with $Bactrim^{\circledR}$ treatment.

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The Study on Association of Calcium Channel SNPs with Adverse Drug Reaction of Calcium Channel Blocker in Korean

  • Chung, Myeon-Woo;Bang, Sy-Rie;Jin, Sun-Kyung;Woo, Sun-Wook;Lee, Yoon-Jung;Kim, Young-Sik;Lee, Jong-Keuk;Lee, Sung-Ho;Roh, Jae-Sook;Chung, Hye-Joo
    • Biomolecules & Therapeutics
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    • v.15 no.3
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    • pp.156-161
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    • 2007
  • Rapid advances in pharmacogenomic research have provided important information to improve drug selection, to maximize drug efficacy, and to minimize drug adverse reaction. The SNPs that are the most abundant type of genetic variants have been proven as valid biomarkers to give information on the prediction of pharmacokinetic/pharmacodynamic properties of drugs based on genotype. In order to elucidate a correlation between SNPs of calcium channel encoding gene and adverse reactions of calcium channel blockers, we investigated SNPs in CACNA1C gene known as a binding site of calcium channel blocker. 96 patients with hypertension who had taken or are taking an antihypertensive drug, 1,4-dihydropyridine (DHP) were included for analysis. These patients were composed of 47 patients with adverse drug reactions (ADR) such as edema from calcium channel blockers and 49 patients without ADR as a control group. The exons encoding the drug binding sites were amplified by PCR using specific primers, and SNPs were analyzed by direct sequencing. We found that there was no SNP in the exons encoding DHP binding site, but four novel SNPs in the exon-intron junction region. However, four novel SNPs were not associated with the ADR of calcium channel blockers. In conclusion, this study showed that ADR from calcium channel blockers may not be caused by SNPs of the binding sites of calcium channel blockers in CACNA1C gene.

The Comparative Study on Post-Marketing Surveillance System for Pharmaceuticals (의약품의 시판후 조사제도 비교연구)

  • Kim, In-Beom;Kim, Hong-Jin;Sohn, Uy-Dong
    • YAKHAK HOEJI
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    • v.50 no.3
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    • pp.145-153
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    • 2006
  • The adverse events which do not appear in the approval process tend to occur more frequently at the early stage of the use. Therefore new drugs, drugs with different active substances or routes of administration, or drugs with explicitly different efficacy added are particularly chosen for re-examination, and go through a study, which is conducted on 600 to 3,000 subjects over 4 to 6 years. Since the re-examination system was implemented in January 1995, 880 drug products have been designated as the subject of re-examination and among them 194 drugs have been completed their re-examination as of until March 2005. Post Marketing Surveillance to insure drug safety should be correlated with re-examination of new drug, re-evaluation of drug, and adverse event monitoring system. And the first labeling change should reflect all information collected for a defined period of time after the marketing authorization is granted. Furthermore centralized management through spontaneous reporting system of adverse event for whole period of time would be the most desirable type of system.

Fabrication and Characterization of Flurbiprofen loaded Chitosan Beads for Periodontal Regeneration (치주조직 재생용 플루르비프로펜 함유 키토산 비드의 제조 및 용출특성)

  • Rhee, Su-Jin;Park, Yoon-Jeong;Lee, Seung-Jin;Chung, Chong-Pyoung
    • Journal of Pharmaceutical Investigation
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    • v.27 no.1
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    • pp.71-77
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    • 1997
  • With the aim of improving periodontal regeneration efficacy, as a biodegradable local drug delivery device, drug releasing chitosan beads were prepared. Chitosan beads were prepared through the formation of intermolecular or intramolecular ionic interaction bewteen chitosan and sodium tripolyphosphate and were loaded with flurbiprofen. The mean diameter of the beads was $250\;{\mu}m$. Drug loading efficiency was improved by regulating the pH of tripolyphosphate solution. The drug release kinetics mainly depended upon the hydrophobic properties of the flurbiprofen, that is, the release of flurbiprofen showed initial burst with rapid release for the first day followed by a levelling off of the release rate. However, the release rate could be controlled by the formulation factor including the pH, concentration of the tripolyphosphate solution, gelation time, drug contents. From these results, flurbiprofen loaded chitosan beads were anticipated as biodegradable local drug delivery devices for periodontal regeneneration.

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Analysis of Factors Affecting Medication Compliance of Outpatients (의료기관 외래 이용자의 복약순응 관련 요인분석)

  • Lee, Eui-Kyung;Park, Jeong-Young
    • Quality Improvement in Health Care
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    • v.9 no.2
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    • pp.164-175
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    • 2002
  • Background : The purpose of this study was to investigate the current status of medication compliance of outpatients and to analyze the factors contributing to medication non-compliance Methods : Telephone survey was conducted to the 1,000 outpatients who visited medical institutions during the period from January 2002 to April 2002. Subjects were randomly selected from the telephone directories of the nation, and the socio-demographic characteristics of the respondents such as age, gender and region were matched based on those of outpatients in 2001. Results : The results of survey revealed that those who complied with doctors' regimen in the right way accounted for 82.4%. The compliance increased with the strong belief in the medication, less unwanted side effects and inconvenience, more severity of disease, and lower perceived health status. Compliance rate was also higher in the patients group who experienced the drug education by the pharmacists than those who did not. Conclusion : In order to improve drug compliance, drug information on efficacy, adverse reaction, drug interactions, and basic disease information are to be provided to the patients. Drug education needs to be focused not only on providing knowledge of drugs and diseases but also changing attitude on drug use of the patients.

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Dual Drug-Loaded Liposomes for Synergistic Efficacy in MCF-7 Breast Cancer Cells and Cancer Stem Cells

  • Park, Hee-Bin;Kim, Yun-Ji;Lee, Seong-Min;Park, James S.;Kim, Keun-Sik
    • Biomedical Science Letters
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    • v.25 no.2
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    • pp.159-169
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    • 2019
  • Breast cancer stem cells (BCSCs) in breast cancer cells have self-renewal ability and differentiation potential. They are also resistant to drugs after chemotherapy. To overcome this resistance, we designed negatively charged 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG)-based liposomes for drug delivery. These liposomes have enhanced the therapeutic effects of a range of antitumor therapies by increasing the cellular uptake and improving drug delivery to targets sites. In this study, we investigated whether DMPG-POPC liposomes, including the neutral lipid 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholin (POPC), can specifically bind to MCF-7 breast cancer cells and increase cellular uptake compared with that by CHOL-POPC liposomes. We also estimated the cytotoxicity of DMPG-POPC liposomes encapsulated with both metformin (Met) and sodium salicylate (Sod) against breast cancer cells and BCSCs compared with that of the free drugs. Our results demonstrated that these dual drug-encapsulated liposomes significantly enhanced the cytotoxic and anti-colony formation abilities compared with individual drug-encapsulated liposomes or free drugs in BCSCs. Overall, our results suggest that DMPG-POPC liposomes containing two drugs (Met + Sod) show promise for synergistic anti-cancer therapy of breast cancer by increasing drug delivery efficiency into breast cancer cells and BCSCs.

Drug distribution management system based on IoT

  • Liu, Zeliang;Zhang, Chunmei;Peng, Hui;Xu, Qin;Gao, Yubao
    • KSII Transactions on Internet and Information Systems (TIIS)
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    • v.16 no.2
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    • pp.424-444
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    • 2022
  • In hospitals and pharmacies, the distribution of medicines is an important part. Any mistakes, misses, fake medicines and expired medicines can cause medical accidents. With the widespread application of the Internet of Things technology (IoT), traditional drug distribution methods need to be upgraded. This article proposes a drug distribution management scheme based on the Internet of Things technology. In the production of drugs, a flexible RFID tag was printed on the packaging box, which stored a series of information such as drug name, dosage, raw materials, efficacy, production date, expiration date, and manufacturer. The use of a drug distribution management system combined with RFID readers can identify drug information and effectively prevent the occurrence of erroneous, missed, counterfeit, and expired drugs. It can also improve management efficiency, reduce management costs, and control management risks. Through the circuit design and software system development, the test results show that this solution is effective and feasible, the proposed method can achieve the expected results.

A Study on the Prediction of Drug Efficacy by Using Molecular Structure (분자구조 유사도를 활용한 약물 효능 예측 알고리즘 연구)

  • Jeong, Hwayoung;Song, Changhyeon;Cho, Hyeyoun;Key, Jaehong
    • Journal of Biomedical Engineering Research
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    • v.43 no.4
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    • pp.230-240
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    • 2022
  • Drug regeneration technology is an efficient strategy than the existing new drug development process, which requires large costs and time by using drugs that have already been proven safe. In this study, we recognize the importance of the new drug regeneration aspect of new drug development and research in predicting functional similarities through the basic molecular structure that forms drugs. We test four string-based algorithms by using SMILES data and searching for their similarities. And by using the ATC codes, pair them with functional similarities, which we compare and validate to select the optimal model. We confirmed that the higher the molecular structure similarity, the higher the ATC code matching rate. We suggest the possibility of additional potency of random drugs, which can be predicted through data that give information on drugs with high molecular similarities. This model has the advantage of being a great combination with additional data, so we look forward to using this model in future research.

Reduced Addamycin Cytotoxicity in RIF-1 Multicell Spheroid Due to an Acidic Microenvironment

  • Um, Kyung-Il;Cheston, Sally B.;Suntharalingam, Mohan;Rhee, Juong-G.
    • Environmental Mutagens and Carcinogens
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    • v.17 no.1
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    • pp.7-11
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    • 1997
  • Variations in adriamycin uptake and cytotoxicity were studied in tumor cells that were grown in different growth states and microenvironments. RIF-1 tumor cells were maintained in an RPMI 1640 medium, and grown in either a monolayer or multicell spheroids. For exponentially growing cells, adriamycin cytotoxicity increased with increased dosage up to 2.5 $\mu$g/ml, and this cytotoxicity was reduced when the cells were grown in a plateau phase or in an acidic microenvironment (pH 6.6). This reduced cytotoxicity was correlated with the uptake of the drug. For multicell spheroids, the cytotoxicity of the drug was reduced dramatically, and this reduction was also correlated with a reduced uptake of the drug and an acidic pH inside of the spheroids. When the drug cytotoxicity was evaluated at different locations within the spheroids, the cells in the inner regions were least affected by the drug, suggesting that both an acidic microenvironment and noncycling plateau phase cells are contributing factors in decreasing the efficacy of the drug in an organized tissue, such as multicell spheroids.

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