• Title/Summary/Keyword: multi-drug

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Investigation of Herb-Drug Interactions between Korean Red Ginseng Extract and five CYP Substrates by LC-MS/MS

  • Jo, Jung Jae;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • 제8권4호
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    • pp.98-104
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    • 2017
  • Ginseng (Panax ginseng Meyer) is a well-known health functional food used as a traditional herbal drug in Asian countries owing to its diverse pharmacological effects. Herb-drug interactions may cause unexpected side effects of co-administered drugs by the alteration of pharmacokinetics through effects on cytochrome P450 activity. In this study, we investigated the herb-drug interactions between Korean red ginseng extract (KRG) and five CYP-specific probes in mice. The pharmacokinetics of KRG extract induced-drug interactions were studied by cassette dosing of five CYP substrates for CYP1A, 2B, 2C, 2D, and 3A and the LC-MS/MS analysis of the blood concentration of metabolites of each of the five probes. The linearity, precision, and accuracy of the quantification method of the five metabolites were successfully confirmed. The plasma concentrations of five metabolites after co-administration of different doses of the KRG extract (0, 0.5, 1, and 2 g/kg) were quantified by LC-MS/MS and dose-dependent pharmacokinetic parameters were determined. The pharmacokinetic parameters of the five metabolites were not significantly altered by the dose of the KRG extract. In conclusion, the single co-administration of KRG extract up to 2 g/kg in vivo did not cause any significant herb-drug interactions linked to the modulation of CYP activity.

In silico Study on the Interaction between P-glycoprotein and Its Inhibitors at the Drug Binding Pocket

  • Kim, Namseok;Shin, Jae-Min;No, Kyoung Tai
    • Bulletin of the Korean Chemical Society
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    • 제35권8호
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    • pp.2317-2325
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    • 2014
  • P-glycoprotein (P-gp) is a member of the ATP-Binding Cassette transporter superfamily and mediates transmembrane efflux of many drugs. Since it is involved in multi-drug resistance activity in various cancer cells, the development of P-gp inhibitor is one of the major concerns in anticancer therapy. Human P-gp protein has at least two "functional" drug binding sites that are called "H" site and "R" site, hence it has multi-binding-specificities. Though the amino acid residues that constitute in drug binding pockets have been proposed by previous experimental evidences, the shapes and the binding poses are not revealed clearly yet. In this study, human P-gp structure was built by homology modeling with available crystal structure of mouse P-gp as a template and docking simulations were performed with inhibitors such as verapamil, hoechst33342, and rhodamine123 to construct the interaction between human P-gp and its inhibitors. The docking simulations were performed 500 times for each inhibitor, and then the interaction frequency of the amino acids at the binding poses was analyzed. With the analysis results, we proposed highly contributing residues that constitute binding pockets of the human P-gp for the inhibitors. Using the highly contributing residues, we proposed the locations and the shapes of verapamil binding site and "R" site, and suggested the possible position of "H" site.

고분자 블렌딩을 이용하여 제조된 독사조신 다중층 펠렛의 약물방출제어 (Controlled Release of Doxazosin in Multi-layered Pellet Using Polymer Blending)

  • 윤주용;박상욱;이수영;김문석;이봉;강길선;이해방
    • 폴리머
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    • 제32권4호
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    • pp.322-327
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    • 2008
  • 본 연구에서 제조한 다중층 펠렛은 수팽윤성 고분자를 포함하는 시드층, 모델 약물인 독사조신을 함유한 약물층, 약물의 방출을 제어하는 다공성막 그리고 지질층으로 구성되어 있으며, 유동층 코팅 방법을 이용하여 제조하였다. 펠렛을 구성하는 각각의 층에 다양한 특성을 가지는 고분자들의 블렌딩에 따른 독사조신의 약물방출 거동을 확인하기 위하여 히드록시프로필메틸셀룰로오스(HPMC)와 에틸셀룰로오스(EC)의 양을 달리하여 약물층을 제조하였고, 셀룰로오스 아세테이트(CA)와 $Eudragit^{(R)}$ RS의 비율을 달리하여 다공성막을 제조하였다. 그리고 지질층에 의한 방출 거동을 확인하고자 피마자유의 두께를 다르게 하여 펠렛을 제조한 결과, 대략 $1500{\mu}m$의 균일한 크기를 가지는 구형의 펠렛을 얻었다. 수용액에서 용출시험을 통하여 시간에 따른 약물방출량을 확인한 결과, 약물층에 첨가된 고분자 중, EC의 비율과 다공성막에서 CA의 비율이 증가하고, 피마자유층의 두께가 두꺼워지면 약물의 방출이 감소함을 알 수 있었다. 그리고 약물방출을 제어하는데 가장 큰 역할을 하는 다공성막의 다공형성거동 역시 SEM을 통해 확인하였다.

Renal protective effects of zingerone in a mouse model of sepsis

  • Lee, Bong-Seon;Lee, Changhun;Yang, Sumin;Ku, Sae-Kwang;Bae, Jong-Sup
    • BMB Reports
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    • 제52권4호
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    • pp.271-276
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    • 2019
  • Zingerone (ZGR), a phenolic alkanone isolated from ginger, has been reported to possess pharmacological activities such as anti-inflammatory and anti-apoptotic effects. This study was initiated to determine whether ZGR could modulate renal functional damage in a mouse model of sepsis and to elucidate the underlying mechanisms. The potential of ZGR treatment to reduce renal damage induced by cecal ligation and puncture (CLP) surgery in mice was measured by assessment of serum creatinine, blood urea nitrogen (BUN), lipid peroxidation, total glutathione, glutathione peroxidase activity, catalase activity, and superoxide dismutase activity. Treatment with ZGR resulted in elevated plasma levels of BUN and creatinine, and of protein in urine in mice with CLP-induced renal damage. Moreover, ZGR inhibited nuclear $factor-{\kappa}B$ activation and reduced the induction of nitric oxide synthase and excessive production of nitric acid. ZGR treatment also reduced the plasma levels of interleukin-6 and tumor necrosis $factor-{\alpha}$, reduced lethality due to CLP-induced sepsis, increased lipid peroxidation, and markedly enhanced the antioxidant defense system by restoring the levels of superoxide dismutase, glutathione peroxidase, and catalase in kidney tissues. Our study showed renal suppressive effects of zingerone in a mouse model of sepsis, suggesting that ZGR protects mice against sepsis-triggered renal injury.

인삼농축액에서 GC를 이용한 잔류농약 동시다성분 분석법의 개발 (Development of Simultaneous Analysis for the Multi-residual Pesticides in the Ginseng Extract using Gas Chromatography)

  • 신영민;이선화;손영욱;정지윤;정성욱;박흥재;김성훈;원영준;이창희;김우성;홍무기;채갑용
    • 한국환경과학회지
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    • 제15권1호
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    • pp.85-94
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    • 2006
  • The simultaneous analysis of multi-residual pesticides was developed using a gas chromatography (GC) method. In this study, a simple and reliable methodology was improved to detect 154 kinds of pesticides in sinseng extract sample by using a liquid-liquid extraction procedure, open column chromagraphy and chromatographic analysis by CC electron capture detector (ECD) and GC nitrogen-phosphorus detector (NPD). The 154 kinds of pesticides were classified in 4 groups according to the chemical structure. The extraction of pesticides was experimented with $70\%$ acetone and dichloromethane/petroleum ether in order, and cleaned up via open column chromatography $(3\times30cm)$ packed with florisil $(30g,\;130^{\circ}C,\;12hrs)$. The final extract was concentrated in a rotator evaporator at $40^{\circ}C$ until dryness. Then the residue was redissolved to 2ml with acetone, and analyzed by GC-ECD and GC-NPD. The applied concentration of pesticides was over $1\~10{\mu}g/ml$. The recovery tests were ranged from $70.7\%$ to $115.2\%$ with standard deviations between 0.3 and $5.7\%$ of the standard spiked to the ginseng extract sample (Group $I\~IV$). The limit of detection (LOD) ranged from 0.001 to $0.099{\mu}g/ml$ (Group $I\~IV$). The 9 kinds of pesticides were not detected. The developed method was applied satisfactory to the determination of the 154 kinds of pesticides in the ginseng extract with good reproducibility and accuracy.

Comparative Study on Antioxidant Activity and Multi-drug Resistance Reversing Activity in Korean Colored Soybean Cultivars

  • Boo, Hee-Ock;Lee, Jong-Ill;Koshio, Kaihei;Song, Won-Seob;Chon, Sang-Uk
    • 한국자원식물학회지
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    • 제24권3호
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    • pp.319-323
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    • 2011
  • The purpose of this study is to analyze antioxidant activity and multidrug resistance reversing activity in several Korean colored soybean (Glycine max Merr.) cultivars. Antioxidant activity of methanol extracts from colored soybean cultivars was evaluated by TBARS (thiobarbituric acid reactive substances), DPPH (1, 1-diphenyl-2-picrylhydrazyl) and ABTS (2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) methods. By means of TBARS, cultivar "Jeonnam #1" showed the highest activity until 7 days, and followed by "Black #1", "Jinyul" and "Black #3", showing lower activity than that of BHT (butylated hydroxytoluene). Methanol extracts of all cultivars proved that DPPH radical scavenging activity is dose-dependent. Methanol extract from cultivar "Jeonnam #1" showed highest DPPH radical scavenging activity, and followed by cultivars "Black #1". MDR (multi-drug resistance reversing) activity, however, showed the highest effect in "Black #3" and the lowest "Black #1" cultivar. These results suggest that seed colors of soybean may play an important role in antioxidant activity and MDR activity.

수입산 담수관상어 및 양식 해산어의 장내세균에서 나타나는 내성균 위험성 비교 (Comparative risks of resistant microorganisms in the intestinal track of imported freshwater ornamental fish and cultured marine fish)

  • 윤소혜;전려진;김영진;진지웅;정현도
    • 한국어병학회지
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    • 제25권2호
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    • pp.77-84
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    • 2012
  • Various antibiotics, that could induce the appearance of resistant microorganisms, have been used for treatment or prevention of bacterial diseases in marine and ornamental fish. We determined and characterized the level of antibiotic-resistant bacteria and proportion of multi-drug resistant bacteria in intestinal microflora of both marine fish cultured in Korea and imported ornamental freshwater fish. For this the bacterial species and resistance to antibiotics were investigated in intestine of rock bream Oplegnathus fasciatus cultured in Korea and pearl gourami Trichogaster leeri imported from Singapore to characterise. Although the bacterial species were different, proportions of resistant bacteria to single antibiotics or multi-drug were higher in intestinal microflora of pearl gourami Trichogaster leeri imported from Singapore than in rock bream Oplegnathus fasciatus cultured in Korea. These results indicate that various antibiotics have been being used before trading without measures in the market of asian ornamental fishes, providing high risks for the emergence of multi-drug resistant bacteria.

A Study on the Health Management of Polypharmacy Use in the Elderly

  • Choi, Keum-Bong
    • International journal of advanced smart convergence
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    • 제10권4호
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    • pp.206-214
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    • 2021
  • The purpose of this study is to identify the level of polypharmacy use, drug knowledge, and drug misuse behavior in the elderly, and to understand the correlation between them and their effect on drug misuse behavior. The study design was a descriptive survey study, and the participants of the study were 215 elderly people from the local community center. The research tool used drug knowledge, drug misuse behavior, and the data collection period was from February 8 to 19, 2021. The data analysis were descriptive statistics, t-test, one-way ANOVA, Pearson's correlation coefficient, and regression analysis. As a result of the study, a significant correlation variable for the drug knowledge of the elderly showed a significant correlation with prescription and non-prescription, r=.145 (p<0.05), and r=.-. 136, which showed a negative significant correlation (p<0.05). As for the significant correlation variable in the drug misuse behavior of the elderly, when prescription and non-prescription were combined, there was a significant correlation with r=.256 (p<0.01), and when not using drugs, r=.-.225 was negative. showed a significant correlation (p<0.01). In terms of the effect on drug misuse behavior, chronic disease =.145, prescription and non-prescription use = .233, which had a positive effect, and non-prescription = -.328, indicating a negative and significant effect. The provision of education on the safe use of drugs by the elderly should first be provided in the community. In addition, we need systematic education and social support for the transmission of correct knowledge on multi-drug use by the elderly and for health management.

Analysis of Dibenzocyclooctadiene Lignans in Omija Wine and Cheong by Liquid Chromatography-Tandem Mass Spectrometry

  • Seo, Hyung-Ju;Ji, Seung-Bae;Kim, Sin-Eun;Lee, Gyung-Min;Moon, Seong-Hun;Jang, Dae-Sik;Liu, Kwang-Hyeon
    • Mass Spectrometry Letters
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    • 제11권2호
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    • pp.30-35
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    • 2020
  • Schisandra chinensis is a traditional herbal medicine that is widely spread in Korea, Japan, and China. The fruits of S. chinensis Bailon, known as omija in Korea, have traditionally been used for the treatment of coughs, fatigues, and insomnia. Up to now, there have been several reports for the identification of major lignan compounds and their quantitation in S. chinensis extracts. To the best of our knowledge, however, there is no report on the analysis of lignans in omija wine and omija cheong (sugared omija or omija sugar syrup). In the present study, seven dibenzocyclooctadiene lignans (gomisin A, gomisin B, gomisin C, gomisin N, schisandrin, deoxyschisandrin, and wuweizisu C) in omija wine and omija cheong were analyzed and quantitated using liquid chromatography-tandem mass spectrometry. Among seven lignans, pharmacologically active gomisin A, schisandrin, and deoxyschisandrin, which are major components in fruits of S. chinensis, were the most abundant lignans in omija wine and cheong. The content of lignan in omija wine was in the order: schisandrin > gomisin A > deoxyschisandrin > gomisin N > gomisin B > gomisin C > wuweizisu C. The concentration of deoxyschisandrin and gomisin N in omija wine was approximately 2.0- and 6.0-fold higher than for omija cheong. Additionally, this study provided a systematic identification of lignans in omija wine and cheong and indicated that the omija wine and cheong might be of value for their dietary application.