• Title/Summary/Keyword: Basic Drugs

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Enhancing Activity of Anticancer Drugs in Multidrug Resistant Tumors by Modulating P-Glycoprotein through Dietary Nutraceuticals

  • Khan, Muhammad;Maryam, Amara;Mehmood, Tahir;Zhang, Yaofang;Ma, Tonghui
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.16
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    • pp.6831-6839
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    • 2015
  • Multidrug resistance is a principal mechanism by which tumors become resistant to structurally and functionally unrelated anticancer drugs. Resistance to chemotherapy has been correlated with overexpression of p-glycoprotein (p-gp), a member of the ATP-binding cassette (ABC) superfamily of membrane transporters. P-gp mediates resistance to a broad-spectrum of anticancer drugs including doxorubicin, taxol, and vinca alkaloids by actively expelling the drugs from cells. Use of specific inhibitors/blocker of p-gp in combination with clinically important anticancer drugs has emerged as a new paradigm for overcoming multidrug resistance. The aim of this paper is to review p-gp regulation by dietary nutraceuticals and to correlate this dietary nutraceutical induced-modulation of p-gp with activity of anticancer drugs.

Fluorophotometric Determination of Basic Drugs with Lumogallion, Superchrome Garnet Y and Their Alkyl Derivatives (루모갈리온, 슈퍼크롬 가넷 와이 및 그 알킬 유도체에 의한 염기성 의약품의 형광정량)

  • 송만영;김동오;이은엽;안문규
    • YAKHAK HOEJI
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    • v.37 no.3
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    • pp.209-215
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    • 1993
  • Basic drugs could be extracted as ion-paired complexes with Lumogallion, Superchrome Garnet Y and their alkyl derivatives from aqueous acid solution, and then determined fluoro-metrically after addition of aluminum ion. The analysis was carried out as follows; To a 1 ml portion of basic drugs (10$^{-9}$~2$\times$0$^{-8}$mole/ml), 1ml of 0.01w/v% fluorescent reagent solution, and 10ml of dichloroethane are added. The mixture is stirred for 1 minute. After standing for a few minutes, the dichloroethane layer is transfered to 1 ml of 0.1w/v% Al(NO$_{3}$)$_{3}$ ethanol solution. After mixing, and standing for 30 minutes at room temperature, the fluorescence intensity is measured with each maximum excitation and emission wavelength. The reagent blank is run through the whole procedure. From the degree of enhancement of fluorescence intensity, hexyl and dodecyl lumogallion and Superchrome Garnet Y were judged to be the useful one of fluorescent reagent for basic drugs analysis.

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Role of Endogenous Transport Systems for the Transport of Basic and Acidic Drugs at Blood-Brain Barrier (염기성 및 산성 약물의 혈액-뇌관문 투과에 관여하는 내인적 수송계)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.23 no.1
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    • pp.1-9
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    • 1993
  • The endothelial cell of brain capillary called the blood-brain barrier (BBB) has carrier-mediated transport systems for nutrients and drugs. The mechanism of the BBB transport of basic and acidic drugs has been reviewed and examined for endogenous transport systems in BBB in WKY and SHRSP. Acidic drugs such as salicylic acid and basic drugs such as eperisone are taken up in a carrier mediated manner through the BBB via the monocarboxylic acid and amine transport systems. The specific dysfunction for the choline transport at the BBB in SHRSP would affect the function of the brain endothelial cell and brain parenchymal cell. The utilization of the endogenous transport systems of monocarboxylic acid and amine could be promising strategy for the effective drug delivery to the brain.

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Advancements in Antiviral Drug Development: Comprehensive Insights into Design Strategies and Mechanisms Targeting Key Viral Proteins

  • Wang Hangyu;Li Panpan;Shen Jie;Wang Hongyan;Wei Linmiao;Han Kangning;Shi Yichen;Wang Shuai;Wang Cheng
    • Journal of Microbiology and Biotechnology
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    • v.34 no.7
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    • pp.1376-1384
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    • 2024
  • Viral infectious diseases have always been a threat to human survival and quality of life, impeding the stability and progress of human society. As such, researchers have persistently focused on developing highly efficient, low-toxicity antiviral drugs, whether for acute or chronic infectious diseases. This article presents a comprehensive review of the design concepts behind virus-targeted drugs, examined through the lens of antiviral drug mechanisms. The intention is to provide a reference for the development of new, virus-targeted antiviral drugs and guide their clinical usage.

Determination of Basic Drugs with Ion-Selective Membrane Electrodes Using Ion-Exchanger (이온교환체 이온선택성 전극을 이용한 염기성의약품 정량)

  • 이지연;정문모;허문회;김은정;안문규
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.289-293
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    • 1999
  • Many poly (vinyl chloride : PVC) membrane electrodes were investigated for the determination of basic drugs, chlorpromazine, amitriptyline, nortriptyline, etc. These electrodes are based on the use of the ion-association complexes of the basic drugs with eriochrome cyanine R, chromoxane cyanine, chrome azurol S and picric acid as ion-exchange sites in a plasticized PVC matrix. All ion-exchangers except picrate complex were not proper for use, because those complexes in plasticized membrane were excluded into aqueous working solution. These drug electrodes show excellent Nernstian responses in the concentration ranges $10^{-2}~10^{-6}$ mol $dm^{-3}$. Their selectivity with respect to each other, as well as their work-able pH range have been investigated. The major advantages of the proposed methods are their simplicity and speed.

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Ebb-and-Flow of Macroautophagy and Chaperone-Mediated Autophagy in Raji Cells Induced by Starvation and Arsenic Trioxide

  • Li, Cai-Li;Wei, Hu-Lai;Chen, Jing;Wang, Bei;Xie, Bei;Fan, Lin-Lan;Li, Lin-Jing
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.14
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    • pp.5715-5719
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    • 2014
  • Autophagy is crucial in the maintenance of homeostasis and regenerated energy of mammalian cells. Macroautophagy and chaperone-mediated autophagy(CMA) are the two best-identified pathways. Recent research has found that in normal cells, decline of macroautophagy is appropriately parallel with activation of CMA. However, whether it is also true in cancer cells has been poorly studied. Here we focused on cross-talk and conversion between macroautophagy and CMA in cultured Burkitt lymphoma Raji cells when facing serum deprivation and exposure to a toxic compound, arsenic trioxide. The results showed that both macroautophagy and CMA were activated sequentially instead of simultaneously in starvation-induced Raji cells, and macroautophagy was quickly activated and peaked during the first hours of nutrition deprivation, and then gradually decreased to near baseline. With nutrient deprivation persisted, CMA progressively increased along with the decline of macroautophagy. On the other hand, in arsenic trioxide-treated Raji cells, macroautophagy activity was also significantly increased, but CMA activity was not rapidly enhanced until macroautophagy was inhibited by 3-methyladenine, an inhibitor. Together, we conclude that cancer cells exhibit differential responses to diverse stressor-induced damage by autophagy. The sequential switch of the first-aider macroautophagy to the homeostasis-stabilizer CMA, whether active or passive, might be conducive to the adaption of cancer cells to miscellaneous intracellular or extracellular stressors. These findings must be helpful to understand the characteristics, compensatory mechanisms and answer modes of different autophagic pathways in cancer cells, which might be very important and promising to the development of potential targeting interventions for cancer therapies via regulation of autophagic pathways.

Problems of Legal Permissible Limit in Metal Level of Herbal Drugs Using Current Korea (현행 한국의 한약재 중금속기준개정 필요성 고찰)

  • Lee Sun-Dong;Park Kyung-Sik
    • Journal of Society of Preventive Korean Medicine
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    • v.5 no.1
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    • pp.31-40
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    • 2001
  • Legal permissible limit of herbal drugs metal level in Korea is define 'less 30.0ppm in total(except mineral drugs)' including Pb Hg Cd As Cr Ni etc. This limit has a lot of problems in several factors, that is, not divide hazard and essential elements, not consider high and low toxic effect in each metal, not calculate dose-response relationship and average health behavior in Korean etc. As a that result, It has strong limits and weakness in the basic toxicology and Oriental medicine. To improve and correct these factors, We need to several new approach as like below. It must be radical study following problems in short and middle-long period in the future, toxic metal and essential element must be divide to basic toxicology and also be diverse toxic effect. But mineral drugs that included a amount of severe toxic metals is being used as active prescription drug until now. If toxic, safety and side-effect of metals will be considered, mineral drugs must prohibit instantly or use at least after examined toxic effect. But one of the most important things about herbal drugs contamination, all people and department (government, farmer and trader, oriental medicine doctors and association) will be participate cooperative and collection for preventive or the least contamination in herbal drugs.

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A study on the degree of need of the knowledge of pathophysiology, clinical microbiology and mechanisms and effects of drugs in clinical nurses (기초간호자연과학의 병태생리학, 병원미생물, 약물의 기전과 효과 내용별 필요도에 대한 연구)

  • Choe, Myoung-Ae;Byun, Young-Soon;Seo, Young-Sook;Hwang, Ae-Ran;Kim, Hee-Seung;Hong, Hae-Sook;Park, Mi-Jung;Choi, S-Mi;Lee, Kyung-Sook;Seo, Wha-Sook;Shin, Gi-Soo
    • Journal of Korean Biological Nursing Science
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    • v.2 no.1
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    • pp.1-19
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    • 2000
  • The purpose of this study was to define the content of the requisite knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs needed for clinical knowledge for nursing practice. Contents of knowlege on pathological physiology, clinical microbiology, and mechanisms and effects of drugs were constructed from syllabus of basic nursing subjects in 4 colleges of nursing, and textbooks. The degree of need of 72 items was measured with a 4 point scale. The subjects of this study were college-graduated 136 nurses from seven university hospital in Seoul and three in Chonnam Province, Kyungbook Province, and Inchon. They have been working at internal medicine ward, surgical ward, intensive care unit, obstetrics and gynecology ward, pediatrics ward, opthalmology ward, ear, nose, and throat ward, emergency room, rehabilitation ward, cancer ward, and hospice ward. The results were as follows : 1. The highest scored items of the knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs necessary for nursing practice were side effects of drugs, anticoagulants, mechanisms of drugs, antihypertensive drugs, tolerance and addiction of drugs, interactions among drugs, hospital infection in the order of importance. The lowest scored item was structure of microorganisms. 2. The highest order of need according to unit was repair in tissue injury unit, definition etiology classification of inflammation in inflammation unit, transplantation and immunologic response in alterations in immunity unit, thrombus and thrombosis in disorders of cardiovascular function unit, gene disorders in genetic disorders unit, hospital infection in infection unit, virus in microorganisms unit, side reactions of drugs in introduction unit, anticonvulsants in drugs for central nervous system unit, local anesthesia in anesthesia unit, anticoagulants in drugs for cardiovascular system unit, anti-inflammatory drugs in antibiotics unit, anti-ulcer drugs in drugs for digestive system unit, and bronchodilators in drugs for respiratory system unit. 3. The common content of the knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs needed for all clinical areas in nursing were side effects of drugs, anticoagulants, interactions among drugs, and hospital infection. However, the degree of need of each pathological physiology, clinical microbiology, clinical microbiology, and mechanisms and effects of drugs was different depending on clinical areas. 4. Significant differences in the knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs necessary for nursing practice such as tissue changes due to injurious stimuli, degenerative changes of tissue, alterations in metabolism of carbohydrates, ischemia, hyperemia and congestion, hospital infection, structure of microorganism, classification of microorganism, bacteria, virus, antidepressants, antipsychotic drugs, antiemetic drugs, antiparkinsonism drugs, antianxiety drugs, antibiotics, tuberculostatics, antiviral drugs, antifungal drugs, parasiticides, antiulcer drugs, antidiarrheais, and anti constipation drugs were shown according to the work area. 5. Significant differences in the knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs necessary for nursing practice such as transplantation and immunologic response, alterations in the metabolism of uric acid, structure of microorganism, classification of microorganism, immunosuppressants, drugs for congestive heart failure were demonstrated according to the duration of work. Based on these findings, all the 72 items constructed by Korean Academic Society of Basic Nursing science should be included as contents of the knowledge of pathophysiology, clinical microbiology, and mechanisms and effects of drugs.

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Screening of Biological Activity of Crude Drugs Using Brine Shrimp Bioassay (Brine Shrimp Bioassay를 이용한 수종생약의 생리 활성 검색)

  • Lee, Ji-Sook;Kim, Jin-Woong
    • Korean Journal of Pharmacognosy
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    • v.21 no.1
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    • pp.100-102
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    • 1990
  • Brine shrimp bioassay has been frequently utilized as a basic screening method for detecting a broad range of bioactive compounds from natural products. Each methanol, chloroform, and water extract of thirty-eight crude drugs were screened in the brine shrimp bioassay, and a number of crude drugs exhibited toxicity against brine shrimp nauplii.

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Drug Delivery into the Blood-Brain Barrier by Endogenous Substances-A Role of Amine and Monocarboxylic Acid Carrier Systems for the Drug Transport- (내인성물질의 수송계를 이용한 혈액-뇌관문에의 약물송달V-약물의 혈액-뇌관문 투과성에 대한 염기성 아민 및 모노카르본산 수송계의 역할-)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.20 no.4
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    • pp.223-228
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    • 1990
  • The contribution of endogenous transport systems to the blood-brain barrier (BBB) transport of basic and acidic drugs was studied by using a carotid injection technique in rats and an isolated bovine cerebrovascular disease state were compared between the normotensive rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) which have been well established as an animal model with pathogenic similarities to humans. Basic drugs such as eperisone, thiamine and scopolamine inhibited, in a concentration dependent manner the in vivo uptake of $[{^3}H]choline$ through BBB, whereas amino acids and acidic drugs such as salicylic acid and valproic acid did not inhibit the uptake. The uptake of $[^3H]choline$ by B-CAP increased with time and showed a remarkable temperature dependency. The uptake of $[^3H]choline$ by B-CAP showed the very similar inhibitory effects as observed in the in vivo brain uptake, and was competitively inhibited by a basic drug, eperisone. The in vivo BBB uptakes of $[^3H]acetic$ acid and $[^{14}C]salicylic$ acid were dependent on pH of the injectate and the concentration of drugs. Several acidic drugs such such as salicylic acid, benzoic acid and valproic acid inhibited the in vivo uptake of $[^3H]acetic$ acid, whereas amino acid, choline and a basic drug such as eperisone did not inhibit the uptake. The uptake of acetic acid by B-CAP was competitively inhibited by salicylic acid. The permeability surface area product (PS) through BBB for $[^3H]choline$ in SHRSP was significantly lower than that in WKY. The concentration of choline in the brain dialysate in SHRSP was about half of that in WKY, while no significant difference was observed in the plasma concentration of choline between SHRSP and WKY. No significant difference was observed in the transport of monocarboxylic acids, glucose and neutral amino acid through BBB between SHRSP and WKY. From these results, it was concluded that BBB transport system of choline contributes to the transport of basic drugs through BBB, that acidic drugs can be transported via a moncarboxylic acid BBB transport system and that the specific dysfuntion of the BBB choline transport in SHRSP was ascribed to the reduction of the maximum velocity of choline concentration in the brain interstitial fluids.

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