• Title/Summary/Keyword: Free release

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Study on the Effect of Gamigehyuldeung-tang on Gultamate Receptor, free Radical and Brain Damage in Rats (가미계혈등탕이 Glutamate receptor와 Free radical 및 뇌손상 보호에 미치는 영향)

  • An Jong suk;Kim Dong Hee;Kim Yun Sik;Lee Young Gu;Park Jong Ho;Namgung Uk;Seol In Chan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.17 no.3
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    • pp.728-737
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    • 2003
  • This study was investigated to prove the effect of GMGHT on the gultamate receptor, free radical and brain damage in rats sujected to Brain Ischemia The results were as follows; 1, GMGHT showed significant inhibitory effect of GMGHT on LDH release induced by NMDA, AMPA, and kinate. 2. GMGHT showed significant inhibitory effect of GMGHT on LDH release induced by BSO and Fe/sup 2+/. 3. GMGHT decreased coma duration time in a infatal dose of KCN and showed 30% of survival rate in a fatal dose. 4. GMGHT decreased ischemic area and edema incited by the MCA blood flow block. 5. GMGHT showed improvement of forelimb and hindlimb test after MCA occulusion in neurological exemination. 6. GMGHT showed no significant change after MCA occulusion in pathological observation as normal group. These results indicate that GMGHT can be used in the brain damage sujected to Brain Ischemia. Further study will be needed about the functional mechanism and etc.

Cytotoxicity, Stability and Antitumor Activity of 5-Fluorouracil Prodrugs Entrapped in Liposomes (리포좀에 봉입한 5-플루오로우라실 프로드럭의 세포독성, 안정성 및 항암효과)

  • Lee, Gye-Won;Ji, Ung-Gil
    • YAKHAK HOEJI
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    • v.40 no.5
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    • pp.522-531
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    • 1996
  • 5-fluorouracil(5-FU) derivatives synthesized with four N-acyloxycarbonyl group such as 1-(N-t-butyloxycarbonyl)glycyloxymethyl-5-FU(BGFU), 1-(N-t-butyloxycarbonyl)leucyloxymethy l-5-FU(BLFU), 1-(N-t-carbobenzyloxymethyl)glycyoxymethyl-5-FU(CGFU) and 1-(N-t-carbobenzyloxymethyl)leucyloxymethyl-5-FU(CLFU) were entrapped into liposomes with different lipid compositions. The entrapment efficiency and release rate of drugs from each liposomes were evaluated. The particle size of liposomes, cytotoxicity and stability of drug-entrapped in liposomes were evaluated. The entrapment efficiency in 5-FU derivatives liposomes was dependent on the lipophilicity of N-acyloxymethyl derivatives. The drug entrapment efficiency also increased on the content of lipid increased up to 200mcmol of lipid per milliliter of liposomal solution. However, inclusion of additives such as cholesterol, dicetylphosphate and stearylamine decreased the entrapment efficiency. The mean particle size and size distribution were varied with lipid compositions and lipophilicity of prodrugs. The release rates of drugs from liposomes were not affected by additives, but those of BGFU and CGFU entrapped in liposomes with cholesterol decreased. Cytotoxicity of BLFU and CLFU entrapped in liposomes decreased by 3~5 fold compared with those of free two prodrugs. Liposome-entrapped 5-FU prodrugs were more stable either at pH 7.4 or in human plasma. Especially, 5-FU prodrugs entrapped in liposome with dipalmitoylphosphatidylcholine(DMPC) was the most stable in human plasma. Compared with free BLFU, BLFU entrapped in DMPC liposome showed a superior antitumor activity at all doses used. In contrast, CLFU entapped in liposomes were more toxic than free prodrug.

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Analysis of Dynamic Crack Propagation using MLS Difference Method (MLS 차분법을 이용한 동적균열전파 해석)

  • Yoon, Young-Cheol;Kim, Kyeong-Hwan;Lee, Sang-Ho
    • Journal of the Computational Structural Engineering Institute of Korea
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    • v.27 no.1
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    • pp.17-26
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    • 2014
  • This paper presents a dynamic crack propagation algorithm based on the Moving Least Squares(MLS) difference method. The derivative approximation for the MLS difference method is derived by Taylor expansion and moving least squares procedure. The method can analyze dynamic crack problems using only node model, which is completely free from the constraint of grid or mesh structure. The dynamic equilibrium equation is integrated by the Newmark method. When a crack propagates, the MLS difference method does not need the reconstruction of mode model at every time step, instead, partial revision of nodal arrangement near the new crack tip is carried out. A crack is modeled by the visibility criterion and dynamic energy release rate is evaluated to decide the onset of crack growth together with the corresponding growth angle. Mode I and mixed mode crack propagation problems are numerically simulated and the accuracy and stability of the proposed algorithm are successfully verified through the comparison with the analytical solutions and the Element-Free Galerkin method results.

Characteristics of $Ca^{2+}$ Stores in Rabbit Cerebral Artery Myocytes

  • Kim, Sung-Joon;Kim, Jin-Kyung;So, In-Suk;Suh, Suk-Hyo;Lee, Sang-Jin;Kim, Ki-Whan
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.3
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    • pp.313-322
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    • 1998
  • In a myocyte freshly isolated from rabbit cerebral artery, the characteristics of $Ca^{2+}$ release by histamine or caffeine were studied by microspectrofluorimetry using a $Ca^{2+}-binding$ fluorescent dye, fura-2. Histamine (5 ${\mu}M$) or caffeine (10 mM) induced a phasic rise of cytoplasmic free $Ca^{2+}$ concentration $([Ca^{2+}]_C)$ which could occur repetitively with extracellular $Ca^{2+}$ but only once or twice in $Ca^{2+}-free$ bathing solution. Also, the treatment with inhibitor of sarcoplasmic reticulum $Ca^{2+}-ATPase$ suppressed the rise of $[Ca^{2+}]_C$ by histamine or caffeine. In $Ca^{2+}-free$ bathing solution, short application of caffeine in advance markedly attenuated the effect of histamine, and vice versa. In normal $Ca^{2+}-containing$ solution with ryanodine (2 ${\mu}M$), the caffeine-induced rise of $[Ca^{2+}]_C$ occurred only once and in this condition, the response to histamine was also suppressed. On the other hand, in the presence of ryanodine, histamine could induce repetitive rise of $[Ca^{2+}]_C$ while the amplitude of peak rise became stepwisely decreased and eventually disappeared. These results suggest that two different $Ca^{2+}-release$ mechanisms (caffeine-sensitive and histamine-sensitive) are present in rabbit cerebral artery myocyte and the corresponding pools overlap each other functionally. Increase of $[Ca^{2+}]_C$ by histamine seems to partially activate ryanodine receptors present in caffeine-sensitive pool.

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The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies (이트라코나졸 마이크로스폰지의 약물 전달 시스템: 제조, 특성 및 방출 연구)

  • Cho, Young-Ho;Lee, Jong-Hwa;Kim, Hak-Hyung;Lee, Gye-Won
    • KSBB Journal
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    • v.26 no.3
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    • pp.217-222
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    • 2011
  • Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of $Eudragit^{(R)}$ E100 and polyvinyl alcohol(PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing micro sized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from microsponges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.

A Polymeric Antibacterial Agent with Sustained Anti-bacterial Activity: Cellulose Xanthate-metal-neomycin Complexes

  • Kim, In-Ho;Jung, Yun-Jin;Kim, Young-Mi
    • Journal of Pharmaceutical Investigation
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    • v.36 no.6
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    • pp.371-375
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    • 2006
  • Neomycin coupled to a polymer matrix via a metal linker was prepared and evaluated for prolonging antibacterial activity. Microcrystallized cellulose was chemically modified to cellulose xanthate(MCX) to afford metal binding sites. MCX was treated with Cu(II), Fe(III) or Zn(II) followed by reaction with neomycin (Ne). The release of Ne from MCX-Zn(II)-Ne was investigated and its activity duration was measured by ditch plate method. The amount of metal bound to MCX was 0.36 mmol/g matrix, 0.26 mmol/g matrix and 0.56 mmol/g matrix for Cu(II), Zn(II) and Fe(III), respectively. Ne bound to MCX-metal chelates was 0.006 mmol, 0.07 mmol and 0.01 mmol per g MCX for Cu(II), Zn(II) and Fe(III), respectively. The Ne release from MCX-Zn(II)-Ne was sustained even after seven washes, whereas Ne from MC/Zn(II)/Ne mixture was almost completely released in two washes. Antibacterial activity was prolonged with MCX-Zn(II)-Ne and MCX-Fe(III)-Ne, but not with MCX-Cu(II)-Ne when compared with that of free Ne. Taken together, these results suggest that neomycin coupled to MCX via a proper metal linker has a potential as a polymeric antibacterial agent with sustained activity.

Effects of Zinc on Spontaneous Miniature GABA Release in Rat Hippocampal CA3 Pyramidal Neurons

  • Choi, Byung-Ju;Jang, Il-Sung
    • The Korean Journal of Physiology and Pharmacology
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    • v.10 no.2
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    • pp.59-64
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    • 2006
  • The effects of $Zn^{2+}$ on spontaneous glutamate and GABA release were tested in mechanically dissociated rat CA3 pyramidal neurons which retained functional presynaptic nerve terminals. The spontaneous miniature excitatory and inhibitory postsynaptic currents (mEPSCs and mIPSCs, respectively) were pharmacologically isolated and recorded using whole-cell patch clamp technique under voltage-clamp conditions. $Zn^{2+}$ at a lower concentration $(30{\mu}M)$ increased GABAergic mIPSC frequency without affecting mIPSC amplitude, but it decreased both mIPSC frequency and amplitude at higher concentrations $({\ge}300{\mu}M)$. In contrast, $Zn^{2+}$ (3 to $100{\mu}M$) did not affect glutamatergic mEPSCs, although it slightly decreased both mIPSC frequency and amplitude at $300{\mu}M$ concentration. Facilitatory effect of $Zn^{2+}$ on GABAergic mIPSC frequency was occluded either in $Ca^{2+}$-free external solution or in the presence of $100{\mu}M$ 4-aminopyridine, a non-selective $K^{+}$ channel blocker. The results suggest that $Zn^{2+}$ at lower concentrations depolarizes GABAergic nerve terminals by blocking $K^{+}$ channels and increases the probability of spontaneous GABA release. This $Zn^{2+}$-mediated modulation of spontaneous GABAergic transmission is likely to play an important role in the regulation of neuronal excitability within the hippocampal CA3 area.

Direct release of embryonic sporophytes from adult Nereocystis luetkeana (Laminariales, Ochrophyta) in a high latitude estuary

  • Ulaski, Brian P.;Konar, Brenda
    • ALGAE
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    • v.36 no.2
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    • pp.147-154
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    • 2021
  • Kelp life history pathways alternate between macroscopic sporophytes that produce spores and microscopic gametophytes that produce gametes. Occasionally, an alternative pathway is seen. This study examined the circumstances by which the high latitude estuarine bull kelp, Nereocystis luetkeana, foregoes the "free-living microscopic stages by releasing embryonic sporophytes directly from sori. Sori were collected from adult N. luetkeana sporophytes from eight locations within Kachemak Bay, Alaska in 2018 and 2020 to examine spatial and temporal development of embryonic sporophytes on sori. Distinctions were made between sori collected from first-generation and overwintered adults to assess the influence of parental age on embryonic sporophyte release. Further distinctions were made between sori collected from attached and drifting individuals to assess the influence of the status of parental attachment to substrate on embryonic sporophyte release. Inspection of propagules released from sori after 48-h incubations indicated that embryonic sporophytes were occasionally released alongside viable spores. Though embryonic sporophytes were released from sori as early as spring, it was not evident that they were bound by seasonal or spatial limits. The percent of propagules that were embryonic sporophytes ranged from 0% to 100% but were not significantly different between first-generation and overwintered adults, nor were they different between attached and drifting individuals. Nevertheless, the characteristic of directly releasing embryonic sporophytes from adult sporophytes might have ecological advantages for N. luetkeana.

The study of free formaldehyde remained in resin finished fabrics (수지가공시 중에 잔존한 유리 Formaldehyde에 관한 연구)

  • Song Wha Soon;Cho Seung Sik;Kim Sung Reon
    • Journal of the Korean Society of Clothing and Textiles
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    • v.2 no.1
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    • pp.125-131
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    • 1978
  • This study was intended to clarify (1) the release of free formaldehyde (2) transfer of free formaldehyde to the contacted fabrics during storing, and (3) the removal effect of free formaldehyde by washing from resin finished fabrics. The results of this study were as follow; 1. The decrease rate of free formaldehyde content in fabrics was higher during storing in open air, poly bag, and glass tube in descending order and the content of free formaldehyde in fabrics was decreased in glyoxal resin finished but, increased in Melamine M-3 resin finished when the fabrics was stored in polybag and in glass tube. 2. Increased amount of formaldehyde transfer to contacted fabrics was noted with Melamine M-3 resin finished than that of glyoxal resin finished. Increased amount of formaldehyde transfer as well as more free formaldehyde were noted in cotton fabrics than in polyester/ cotton blend. 3. The effect of removing free formaldehyde from the fabrics was better in case of solid alkaline soap, synthetic alkaline powdered detergents, neutral detergents in descending order. The romoval of free formaldehyde was marked after the 1st washing and almost no increase in free formaldehyde was found after three times of washing. 4. After first washing, the content of formaldehyde in Melamine M-3 resin finished fabrics increased more rapidly than that of glyoxal resin finished fabrics in condition of closed storing.

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Effect of $Na^+$ Removal on the Action of Ethanol in Cat Ileal Longitudinal Muscle (장관 평활근에서 Na-free용액이 Ethanol의 효과에 미치는 영향)

  • Suh, Duk-Jun;Kim, So-Sun;Woo, Jae-Suk;Kim, Young-Keun
    • The Korean Journal of Physiology
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    • v.20 no.1
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    • pp.125-133
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    • 1986
  • The effect of ethanol on the contraction of intestinal smooth muscle in Na-free solution was studied using cat ileal longitudinal muscle strips. Ethanol $(0.5{\pm}4%)$ inhibited both the spontaneous mechanical activity and base-line tension in normal physiological salt solution. However, in Na-free solution it induced a reversible contraction. The excitatory effect by ethanol in Na-free solution was increased with increasing the concentrations of ethanol and the time incubated in Na-free solution. The excitatory response by ethanol was reduced by increasing the concentrations of Na in incubated medium . Ethanol-induced contractile response was not affected by $Ca^{2+}$ removal in bathing medium. In Na-free solution, the contraction by ethanol was inhibited by Las. but was not affected by verapamil. The contraction induced by Na removal in solution was inhibited by the pretreatment of ethanol. These results suggest that ethanol may induce the contraction by increasing the release of superficially membrane-bound $Ca^{2+}$ and/or intracellular $Ca^{2+}$ in Na-free physiological salt solution.

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