• Title/Summary/Keyword: dual mode of action

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Antimicrobial Peptides (AMPs) with Dual Mechanisms: Membrane Disruption and Apoptosis

  • Lee, Juneyoung;Lee, Dong Gun
    • Journal of Microbiology and Biotechnology
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    • v.25 no.6
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    • pp.759-764
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    • 2015
  • Antimicrobial peptides (AMPs) are one of the critical components in host innate immune responses to imbalanced and invading microbial pathogens. Although the antimicrobial activity and mechanism of action have been thoroughly investigated for decades, the exact biological properties of AMPs are still elusive. Most AMPs generally exert the antimicrobial effect by targeting the microbial membrane, such as barrel stave, toroidal, and carpet mechanisms. Thus, the mode of action in model membranes and the discrimination of AMPs to discrepant lipid compositions between mammalian cells and microbial pathogens (cell selectivity) have been studied intensively. However, the latest reports suggest that not only AMPs recently isolated but also well-known membrane-disruptive AMPs play a role in intracellular killing, such as apoptosis induction. In this mini-review, we will review some representative AMPs and their antimicrobial mechanisms and provide new insights into the dual mechanism of AMPs.

Studies on Diuretic Action of Bumetanide (Bumetanide의 이뇨작용에 관한 연구)

  • 고석태;김일용
    • YAKHAK HOEJI
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    • v.29 no.3
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    • pp.130-143
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    • 1985
  • Bumetanide, when given intravenously in dogs, induced a potent diuresis with an increased amounts of sodium and potassium excreted in urine due to inhibition of reabsorbing them in renal tubule. Furthermore, clearances of osmolar substance and para-aminohippuric acid were increased, but clearace of free water diminished without any change of creatinine clearance. Bumetanide, administered directly into a renal artery, elicited diuresis only in the infused(experimental) kidney by the same mode of action as in the intravenous cases in renal function of the dog. Renal effects of intravenous bumetanide after pretreatment with the small dose of indomethacin (5.0mg/kg) revealed reduction only in clearance of paraaminohippuric acid. However the much dose of indomethacin (5.0mg/kg+5.0mg/kg/hr) or arachidonic acid showed a significant inhibition in the change rates of all renal function by bumetanide. Morover, pretreatment of probenecid also made a marked reduction in renal effects induced by bumetanide. From the above results, it is thought that bumetanide causes diuretic action due to dual mechanism inhibiting reabsorption of electrolytes in loop of Henle and increasing blood flow in kindney, that are provoked through the mediation of prostaglandins.

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A study on the Nonlinear Normal Mode Vibration Using Adelphic Integral

  • Huinam Rhee;Kim, Jeong-Soo
    • Journal of Mechanical Science and Technology
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    • v.17 no.12
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    • pp.1922-1927
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    • 2003
  • Nonlinear normal mode (NNM) vibration, in a nonlinear dual mass Hamiltonian system, which has 6$\^$th/ order homogeneous polynomial as a nonlinear term, is studied in this paper. The existence, bifurcation, and the orbital stability of periodic motions are to be studied in the phase space. In order to find the analytic expression of the invariant curves in the Poincare Map, which is a mapping of a phase trajectory onto 2 dimensional surface in 4 dimensional phase space, Whittaker's Adelphic Integral, instead of the direct integration of the equations of motion or the Birkhoff-Gustavson (B-G) canonical transformation, is derived for small value of energy. It is revealed that the integral of motion by Adelphic Integral is essentially consistent with the one obtained from the B-G transformation method. The resulting expression of the invariant curves can be used for analyzing the behavior of NNM vibration in the Poincare Map.

Sorption and Diffusion of Carbon Dioxide in Polystyrene Membrane (폴리스티렌 막에서 $CO_2$의 수착과 확산)

  • Kim, You-Whan;Cho, Du-Hyun;Bae, Seong-Youl;Kumaawa, Hidehiro
    • Membrane Journal
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    • v.3 no.2
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    • pp.79-82
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    • 1993
  • The sorption equilibria and permeabilities for $CO_2$ in a homogeneous membrane of polystyrene with the glass transition temperature of $95^{\circ}C$ were measured at a temperature of $60^{\circ}C$ and gas pressures up to 1.6 MPa and 2.5 MPa, respectively. The sorption isotherm had the form af dual-mode sorption model at low gas pressures, but became linear at pressures above 1.3 MPa. The linear portion of the isotherm extrapolated to the origin. The pressure dependence of the rnean permeability coefficient deviated upward from the dualsrhode mobility model prediction. It was found that the glass transition was brought out by the plasticization action of sotbed $CO_2$ at a gas pressure of 1.3 MPa from the sorption isotherm. And this result was consistent with an increase in the mean permeability coefficient with applied gas pressure.

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Dynamic analysis of a magneto-electro-elastic material with a semi-infinite mode-III crack under point impact loads

  • Feng, Wenjie;Liu, Jinxi
    • Structural Engineering and Mechanics
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    • v.27 no.5
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    • pp.609-623
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    • 2007
  • The problem of a semi-infinite magneto-electro-elastically impermeable mode-III crack in a magneto-electro-elastic material is considered under the action of impact loads. For the case when a pair of concentrated anti-plane shear impacts, electric displacement and magnetic induction impacts are exerted symmetrically on the upper and lower surfaces of the crack, the magneto-electro-elastic field ahead of the crack tip is determined in explicit form. The dynamic intensity factors and dynamic energy density factor are obtained. The method adopted is to reduce the mixed initial-boundary value problem, by using the Laplace and Fourier transforms, into three simultaneous dual integral equations, one of which is converted into an Abel's integral equation and the others into a singular integral equation with Cauchy kernel. Based on the obtained fundamental solutions of point impact loads, the solutions of two kinds of different loading cases are evaluated by integration. For some particular cases, the present results reduce to the previous results.

Identification of Proapoptopic, Anti-Inflammatory, Anti-Proliferative, Anti-Invasive and Anti-Angiogenic Targets of Essential Oils in Cardamom by Dual Reverse Virtual Screening and Binding Pose Analysis

  • Bhattacharjee, Biplab;Chatterjee, Jhinuk
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.6
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    • pp.3735-3742
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    • 2013
  • Background: Cardamom (Elettaria cardamom), also known as "Queen of Spices", has been traditionally used as a culinary ingredient due to its pleasant aroma and taste. In addition to this role, studies on cardamom have demonstrated cancer chemopreventive potential in in vitro and in vivo systems. Nevertheless, the precise poly-pharmacological nature of naturally occurring chemo-preventive compounds in cardamom has still not been fully demystified. Methods:In this study, an effort has been made to identify the proapoptopic, anti-inflammatory, anti-proliferative, anti-invasive and anti-angiogenic targets of Cardamom's bioactive principles (eucalyptol, alpha-pinene, beta-pinene, d-limonene and geraniol) by employing a dual reverse virtual screening protocol. Experimentally proven target information of the bioactive principles was annotated from bioassay databases and compared with the virtually screened set of targets to evaluate the reliability of the computational identification. To study the molecular interaction pattern of the anti-tumor action, molecular docking simulation was performed with Auto Dock Pyrx. Interaction studies of binding pose of eucalyptol with Caspase 3 were conducted to obtain an insight into the interacting amino acids and their inter-molecular bondings. Results:A prioritized list of target proteins associated with multiple forms of cancer and ranked by their Fit Score (Pharm Mapper) and descending 3D score (Reverse Screen 3D) were obtained from the two independent inverse screening platforms. Molecular docking studies exploring the bioactive principle targeted action revealed that H- bonds and electrostatic interactions forms the chief contributing factor in inter-molecular interactions associated with anti-tumor activity. Eucalyptol binds to the Caspase 3 with a specific framework that is well-suited for nucleophilic attacks by polar residues inside the Caspase 3 catalytic site. Conclusion:This study revealed vital information about the poly-pharmacological anti-tumor mode-of-action of essential oils in cardamom. In addition, a probabilistic set of anti-tumor targets for cardamom was generated, which can be further confirmed by in vivo and in vitro experiments.

Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?

  • Chang, Eun Jung;Choi, Eun Ji;Kim, Kyung Hoon
    • The Korean Journal of Pain
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    • v.29 no.3
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    • pp.153-157
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    • 2016
  • Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the ${\mu}$-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys. The most common adverse reactions are nausea, dizziness, vomiting, and somnolence. Constipation is more common in use of the ER formulation. Precautions against concomitant use of central nervous system depressants, including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol, or use of tapentadol within 14 days of the cessation of monoamine oxidase inhibitors, are advised. The safety and efficacy have not been established for use during pregnancy, labor, and delivery, or for nursing mothers, pediatric patients less than 18 years of age, and cases of severe renal impairment and severe hepatic impairment. The major concerns for tapentadol are abuse, addiction, seeking behavior, withdrawal, and physical dependence. The presumed problem for use of tapentadol is to control the ratio of MOR agonist and NRI. In conclusion, tapentadol produces both nociceptive and neuropathic pain relief, but with worries about abuse and dependence.

A Study on the Nonlinear Normal Mode Vibration Using Adelphic Integral (Adelphic Integral을 이용한 비선형 정규모드 진동 해석)

  • Huinam Rhee;Joo, Jae-Man;Pak, Chol-Hui
    • Proceedings of the Korean Society for Noise and Vibration Engineering Conference
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    • 2001.11b
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    • pp.799-804
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    • 2001
  • Nonlinear normal mode (NNM) vibration, in a nonlinear dual mass Hamiltonian system, which has 6th order homogeneous polynomial as a nonlinear term, is studied in this paper. The existence, bifurcation, and the orbital stability of periodic motions are to be studied in the phase space. In order to find the analytic expression of the invariant curves in the Poincare Map, which is a mapping of a phase trajectory onto 2 dimensional surface in 4 dimensional phase space, Whittaker's Adelphic Integral, instead of the direct integration of the equations of motion or the Birkhotf-Gustavson (B-G) canonical transformation, is derived for small value of energy. It is revealed that the integral of motion by Adelphic Integral is essentially consistent with the one obtained from the B-G transformation method. The resulting expression of the invariant curves can be used for analyzing the behavior of NNM vibration in the Poincare Map.

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Synthesis of Hybrid Bivalent Ligand Quinolone Derivatives (혼성 Bivalent Ligand 퀴놀론 유도체의 합성)

  • Lee, Sang-Pil;Im, Chae-Uk;Kim, Dong-Soon;Yim, Chul-Bu
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.664-672
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    • 1994
  • Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in viかo antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds $25{\sim}42$ with hydrogen in the presence of 10% Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.

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Postharvest biological control of garlic blue mold rot caused by Pantoea agglomereans and its mode of action

  • Kwon, Mi-Kyung;Kim, Yong-Ki;Shim, Hong-Sik;Park, Kyung-Suk;Kim, Choong-Hoe
    • Proceedings of the Korean Society of Plant Pathology Conference
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    • 2003.10a
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    • pp.104.1-104
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    • 2003
  • To screen for potential biocontrol agents against postharvest disease of garlics caused by Penicillium hirsutum, a total of 933 isolates (432 fungi and 501 bacteria) were isolated from the rhizoshere or rhizoplane of garlics. Among them, Pantoea agglomerans isolate 59-4 (Pa 59-4) was selected for a potential biocontrol agent by in vivo wounded garlic bulb assay, When the spore suspension (10$\^$5/ spores/$m\ell$) of Penicillium hirsutum was co-inoculated with spore or cell suspension of each fungal or bacterial isolate on wounded garlics, the isolate highly suppressed disease development. Soaking garlic bulbs in the suspension of Pa 59-4 significantly reduced garlic decay from p. hirsutum. However, Pa 59-4 did not inhibit the mycelial growth of P. hirsutum in dual-culture with P. hirsutum on Tryptic soy agar. In order to elucidate mode of action of Pa 59-4 nutrient competition between Pa 59-4 and P. hirsutum was investigated using tissue culture plates with cylinder inserts containing defusing membrane reported by Janisiewicz et al. The results showed that Pa 59-4 effectively suppressed spore germination and mycelial growth of blue mold in the low concentration (0.5%) of garlic juice, but did not suppress those of blue mold in the higher concentration (5%) of garlic juice. This result suggests that the mechanism in biocontrol of garlic blue mold by Pa 59-4 may involve in nutrient competition with P. hirsutum on garlic bulbs.

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