• Applied Biological Chemistry
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• v.35 no.2
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• pp.76-81
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• 1992

The technicals of KC-7079, isoprothiolane, perfluidone and tricyclazole were granulated with a mixture of inorganic carrier and oil-soluble binder, that is, stearly alcohol or ethyl cellulose. The concentration of the released active ingredient from the granules was analyzed at several days intervals after immersion of these granules in water at $25^{\circ}C$. At the content of stearyl alcohol less than $80g\;kg^{-1}$, the granule kneaded with stearyl alcohol mixture and water disintegrated in water. But the granule kneaded with methanol disintegrated in water at the content of stearyl alcohol less than $30g\;kg^{-1}$. The less the KC-7079-stearyl alcohol granule disintegrated, the slower the release rate of KC-7079 was. No matter how was increased the stearyl alcohol content, the release rate of KC-7079 granule which did not disintegrate was not significantly changed. The sustained releasing effect of the granules was little in the other three pesticides of which the water solubility was higher than of KC-7079(21 ppm). The granule made of ethyl cellulose did not disintegrate even at $5g\;kg^{-1}$ of ethyl cellulose. With the increase of ethyl cellulose content and the decrease of active ingredient in the granules, the sustaining effect of the granules on releasing acitive ingredient was increased. The lower the water solubility of pesticide was, the release rate tended to be sustained except perfluidone.

• Archives of Pharmacal Research
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• v.25 no.3
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• pp.349-356
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• 2002

The present study was performed to examine the effect of fangchinoline, a bis- benzylisoquinoline alkaloid, which exhibits the characteristics of a $Ca^{2+}$ channel blocker, on cyanide-induced neurotoxicity using cultured rat cerebellar granule neurons. NaCN produced a concentration-dependent reduction of cell viability, which was blocked by MK-801, an N-methyl-D-aspartate (NMDA) receptor antagonist, verapamil, L-type$Ca^{2+}$channel blocker, and L-NAME, a nitric oxide synthase inhibitor. Pretreatment with fangchinoline over a concentration range of 0.1 to 10 $\mu$M significantly decreased the NaCN-induced neuronal cell death, glutamate release into medium, and elevation of $[Ca^{2+}]_i$ and oxidants generation. These results suggest that fangchinoline may mitigate the harmful effects of cyanide-induced neuronal cell death by interfering with $[Ca^{2+}]_i$influx, due to its function as a $Ca^{2+}$ channel blocker, and then by inhibiting glutamate release and oxidants generation.

• Polymer(Korea)
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• v.34 no.3
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• pp.269-273
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• 2010

The primary objective of this work is to find the optimal condition for the granule tablet formulation of alfuzosin-HCl that aims to achieve a sustained drug release. (Hydroxypropyl)methyl cellulose (HPMC) is one of the most widely used polymer as a drug formulation and therefore has been utilized in this study as an excipient. Alfuzosin-HCl granule tablet was developed using the various viscosities of HPMC and the effects of viscosity on drug release was investigated. Fourier transform-infrared (FTIR) and X-ray diffraction (XRD) were employed to investigate the chemical structure and crystallization of alfuzosin-HCl in the formulation. We prepared the granule tablet by a direct compression method and studied the release profile in the stimulated intestinal fluid (pH 6.8). As the viscosity of HPMC increased the release of alfuzosin-HCl decreased, demonstrating that controlled release of alfuzosin-HCl can be achieved by varying the viscosity of HPMC.

• 한국전자현미경학회:학술대회논문집
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• 2004.11a
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• pp.40-42
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• 2004

• Journal of Korean Society of Environmental Engineers
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• v.36 no.11
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• pp.781-790
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• 2014

Contaminants such as organic matters, nutrients and toxic chemicals in rivers and lakes with a weak flow rate are first removed from the water and accumulated in the sediments. Subsequently, they are released into the water column again, posing direct/indirect adverse effects on the water quality and aquatic ecosystems. In particular, phosphorus is known to accelerate the eutrophication phenomenon when it is released into the water column via physical disturbance and biological/chemical actions as one of important materials that determine the primary production of aquatic ecosystems and an element that is stored mainly in the sediments in the process of material circulation in the body of water. In this study, the effect on reducing phosphorus release in sediments was analyzed by applying different capping materials to lake water, where the effect of aquatic microorganisms is taken into account, and to distilled water, where the effect of microorganisms is excluded. The experimental results showed that capping with chemical materials such as Fe-gypsum and $SiO_2$-gypsum further reduced the phosphorus release by at least 40% compared to the control case. Composite materials like granule gypsum+Sand showed over 50% phosphorus release reduction effect. Therefore, it is determined that capping with chemical materials such as granule-gypsum and eco-friendly materials such as sand is effective in reducing phosphorus release. The changes in phosphorus properties in the sediments before and after capping treatment showed that gypsum input helped to change the phosphorus that is present in lake sediments into apatite-P, a stable form that makes phosphorus release difficult. Based on the above results, it is expected that the application of capping technology will contribute to improving the efficiency of reducing phosphorus release that occurs in river and lake sediments.

• The Korean Journal of Pesticide Science
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• v.9 no.3
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• pp.243-249
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• 2005

The chemical and toxicological studies were conducted with acetamiprid 2% granules including different controlling agents for development of controlled-release acetamiprid 2% granule. The fundamental formulation recipe of acetamiprid 2% granule was prepared by the insoluble matrix using polyethylene wax. Starch, cellulose and mineral (calcium carbonate) were used as controlling agents. As a result of studies, release rate of active ingredient from granules into water static condition at $25^{\circ}C$ was increased by addition of starch and cellulose, but was decreased by addition of calcium carbonate. We could select calcium carbonate as controlling agent and make three granules which there were difference in release profiles of active ingredient according to contents of polyethylene wax. 24 hours-release rates of acetamiprid from three granules into water static condition at $25^{\circ}C$ were respectively 75, 50 and 25% when contents of wax were 2, 10 and 20%. The granule which 24 hours-release rate was 25% showed lower acute toxicity against mice and rats.

• Journal of Korean Society of Environmental Engineers
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• v.28 no.4
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• pp.438-446
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• 2006

A lab-scale batch test was conducted to develop capping materials to reduce the sediment phosphorus in the stagnant water zone of Gyeongancheon in Paldang Lake. The mean grain size(Mz) of sediment in the investigated area was 7.7 ${\phi}$, which is very fine, and the contents of organic carbon($C_{org}$) was 2.4%, which is very high. For the phosphorous release experiment to select the optimal capping material, sand layer, powder-gypsum($CaSO_4{\cdot}2H_2O$), granule-gypsum, complex layer(gypsum+sand) and the control were compared and evaluated in the 150 L reactor for 45 days. In case of the capping with the sand, it was found that the phosphorous from the sediment could be reduced by around 50%. However, it was found that this caused the reduction of the dissolved oxygen in the water column(by less than 3 mg/L) due to the resuspension of sediment and the organic matter decomposition that comes from the generation of $CH_4$ gas in the 1 cm of the sand layer. Therefore, it is likely that the sand layer has to be thickener in case of the sand capping. Powder-gypsum and granule-Gypsum reduced phosphorous release by more than 80%. However, the concentration of ${SO_4}^{2-}$ in the water column increased, making it difficult to apply it to the drinking water protection zone. We developed Fe-Gypsum and $SiO_2$-gypsum materials to reduce the solubility of ${SO_4}^{2-}$. Powder-Gypsum creates the interception film that does not have any aperture on the sediment layer when it is combined with the water. However phosphorous release caused by the generation of $CH_4$ gas may happen at a time when the gypsum layer has the crack. Capping through the complex layer(granule-Gypsum+sand(1 cm)) found to be suitable for the drinking water protection zone because it was effective to prevent phosphorus release. Moreover, this leads to the lower solubility from the concentration of ${SO_4}^{2-}$ into the water column than the powder-Gypsum and granule-Gypsum. The addition of gypsum($CaSO_4{\cdot}2H_2O$) into the sediment can reduce the progress of methanogensis because fast early diagenesis and sufficient supply of ${SO_4}^{2-}$ to the sediment, stimulate the SRB(sulfate reducing bacteria) highly.

• Journal of Applied Biological Chemistry
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• v.63 no.2
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• pp.131-136
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• 2020

When blood vessels are damaged, a fast hemostatic response should occur to minimize blood loss and maintain normal circulation. Platelet activation and aggregation are essential in this process. However, excessive platelet aggregation or abnormal platelet aggregation may be the cause of cardiovascular diseases such as thrombosis, stroke, and atherosclerosis. Therefore, finding a substance capable of regulating platelet activation and suppressing agglutination reaction is important for the prevention and treatment of cardiovascular diseases. 6,7-Dimethoxy-2H-chromen-2-one (Scoparone), found primarily in the roots of Artemisia or Scopolia plants, has been reported to have a pharmacological effect on immunosuppression and vasodilation, but studies of platelet aggregation and its mechanisms are still insufficient. This study confirmed the effect of scoparone on collagen-induced human platelet aggregation, TXA₂ production, and major regulation of intracellular granule secretion (ATP and serotonin release). In addition, the effect of scoparone on the phosphorylation of the phosphoproteins PI3K/Akt and mitogen-activated protein kinases (MAPK) involved in signal transduction in platelet aggregation was studied. As a result, scoparone significantly inhibited the phosphorylation of PI3K/Akt and MAPK, which significantly inhibited platelet aggregation through TXA₂ production and intracellular granule secretion (ATP and serotonin release). Therefore, we suggest that scoparone is an antiplatelet substance that regulates the phosphorylation of phosphoproteins such as PI3K/Akt and MAPK and is of value as a preventive and therapeutic agent for platelet-derived cardiovascular disease.

• Animal cells and systems
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• v.12 no.4
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• pp.211-217
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• 2008

Bax, a pro-apoptotic member of Bcl-2 family proteins, plays a central role in the mitochondria-dependent apoptosis. Apoptotic signals induce the translocation of Bax from cytosol into the mitochondria, which triggers the release of apoptogenic molecules such as cytochrome C and apoptosis-inducing factor, AIF. Bax-inhibiting peptide(BIP) is a cell permeable peptide comprised of five amino acids designed from the Bax-interaction domain of Ku70. Because BIP inhibits Bax translocation and Bax-mediated release of cytochrome C, BIP suppresses Bax-dependent apoptosis. In this study, we observed that BIP inhibited staurosporine-induced neuronal death in cultured cerebral cortex and cerebellar granule cells, but BIP failed to rescue granule cells from trophic signal deprivation-induced neuronal death, although both staurosporine-induced and trophic signal deprivation-induced neuronal death are dependent on Bax. These findings suggest that the mechanisms of the Bax activation may differ depending on the type of cell death induction, and thus BIP exhibits selective suppression of a subtype of Bax-dependent neuronal death.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.391-395
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• 1995

Several lines of evidence indicate that physiological activity of N-methyl-D-aspartate (NMDA) receptor was blocked by physiological concentration of $Mg^{2+}$ (1.2 mM). However, the activity of NMDA receptor may not be blocked totally with this concentration of $Mg^{2+}$ under elevated membrane potential by kainate. Here, we described the effect of $Mg^{2+}$ on NMDA receptor and how much of NMDA receptor functions could be activated by kainate. Effects of NMDA receptor antagonist on kainate-induced elevation of intracellualr $Ca^{2+}$ levels $([Ca^{2+}]_i)$ and extracellular glutamate level were examined in cultured rat cerebellar granule neurons. kainate-induced elevation of $([Ca^{2+}]_i)$ was not affected by physiological concentration of $Mg^{2+}$. Kainate-induced NMDA-induced elevation was blocked by the same concentration of $MG^{2+}$Kainate-induced elevation of [$([Ca^{2+}]_i)$ was decreased by 32% in the presence of NMDA antagonists, MK-801 and CPP (3-[2-carboxypiperazine-4-yl]propyl-1-phosphonic acid), in $Mg^{2+}$ free buffer. Kainate receptor-activated gluamate release was also decreased (30%) by MK-801 or CPP. These resuts show that certain extent of elevations of intracellular $Ca^{2+}$ and extracellular glutamate by kainate is due to coativation of NMDA receptors.