• Title/Summary/Keyword: Calcium compound

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Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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Inhibitory effects of Cortex Mori on Compound 48/80-induced Anaphylactic Shock and Cutaneous Reaction

  • Jun, Byoung-Deuk;Chai, Ok-Hee;Park, Myoung-Hee-;Lee, Hern-Ku-;Lee, Moo-Sam-
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.243-243
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    • 1994
  • Although active systemic anaphylaxis and passive cutaneous anaphylaxis have been empolyed to study anaphylactic hypersensitivity, it is difficult and time-consuming to induce these reactions in experimental animals. In recent, Jun et al have found a simple method to induced anaphylactic hypersensitivity such as anaphylactic shock(AS) and cutaneous reaction(CR) using compound48/80. Cortex mori (Morus alba L.), the root bark of mulberry tree has been used as an antiphlogistic, diuretic, and expectorant in herbal medicine. The purpose of this study was to determine whether the methanol extract of Cortex mori could inhibit the compound 48/80-induced AS and CR. To induce AS, various doses of compound 48/80 (5, 7.5, 10, 15$\mu\textrm{g}$/gm B.W.) were injected intraperitoneally (i.p.) into ICR mice. The animals were pretreated by three injection(i.p.) of Cortex mori before compound 48/80 administration. Peripheral blood was collected from the right ventricle to estimate the level of serum histamine at 15 minutes after the injctin(i.p.) of various concentration of compound48/80. Mortility rate, mean death time and mesenteric mast cell degranulation rate were evaluated over a 72 hour period. To estimate the effect of Cortex mori on compound 48/80-induced cutaneous reaction, various doses of compound 48/80 with or without Cortex mori were injected intradermally(i.d.) into the shaved flank of Sprague-Dawley rats, and the blue cutaneous patchs induced by Evans'blue injection at the compound 48/80 alone and Cortex mori plus compound 48/80 injection sites were observed. As a Parameter of these reactions, the levels of histamine in the supernatant, calcium uptake and intracellular CAMP of RPMC were measured. supernatant, 1)compound 48/80-induced mortility rate, mean death time, mesenteric mast cell degranulation rate, and serum histamine level in ICR mice were significantly inhibited by pretreatment of Cortex mori, 2) cutaneous reaction inducd by compound48/80 was well developed in Sprague-Dawley rat, but Cortex mori inhibited the compound 48/80-induced blue patch formation remarkably, 3) the compound 48/80-induced degranulation, histamine release and calcium uptake of RPMC pretreated with Cortex mori were significantly inhibited, compared to those of control without Cortex mori pretreatment, and 4)the level of cAMP of RPMC was reduced bythe increased concentration of compound 48/80, pretreatment of Cortex mori not only inhibited the compound 48/80-induced reduction of CAMP but also significantly increased the level of cAMP naturally, from the above results, it is suggested that Cortex mori has an some substances with an ability to inhibits the compound 48/80-induced AS,CR, and mast cell activation.

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SBR/Organoclay Nanocomposites for the Application on Tire Tread Compounds

  • Kim, Wook-Soo;Lee, Dong-Hyun;Kim, Il-Jin;Son, Min-Jin;Kim, Won-Ho;Cho, Seong-Gyu
    • Macromolecular Research
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    • v.17 no.10
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    • pp.776-784
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    • 2009
  • N,N-dimethyldodecylamine (tertiary amine)-modified MMT (DDA-MMT) was prepared as an organically modified layered silicate (OLS), after which styrene-butadiene rubber (SBR) nanocomposites reinforced with the OLS were manufactured via the latex method. The layer distance of the OLS and the morphology of the nanocomposites were characterized by X-ray diffraction (XRD) and transmission electron microscopy (TEM). By increasing the amount of N,N-dimethyldodecylamine (DDA) up to 2.5 g, the maximum values of torque, tensile strength and wear resistance of the SBR nanocomposites were increased due to the increased dispersion of the silicate layers in the rubber matrix and the increased crosslinking of the SBR nanocomposites by DDA itself. When SBR nanocomposites were manufactured by using the ternary filler system (carbon black/silica/OLS) to improve their dynamic properties as a tire tread compound, the tan $\delta$(at $0^{\circ}C$ and $60^{\circ}C$) property of the compounds was improved by using metal stearates instead of stearic acid. The mechanical properties and wear resistance were increased by direct substitution of calcium stearate for stearic acid because the filler-rubber interaction was increased by the strong ionic effect between the calcium cation and silicates with anionic surface. However, as the amount of calcium stearate was further increased above 0.5 phr, the mechanical properties and wear resistance were degraded due to the lubrication effect of the excessive amount of calcium stearate. Consequently, the SBR/organoclay nanocomposites that used carbon black, silica, and organoclay as their ternary filler system showed excellent dynamic properties, mechanical properties and wear resistance as a tire tread compound for passenger cars when 0.5 phr of calcium stearate was substituted for the conventionally used stearic acid.

Inhibitory Effect of Spirodela Polyrhiza on the Mast Cell-Mediated Immediate Hypersensitivity

  • Kim Young Hee;Ko Woo Shin
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.3
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    • pp.919-923
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    • 2004
  • Spirodela polyrhiza(L.) Schleid (Lemnaceae) have been used as a traditional drug in treating urticaria and itching. However, the exact role of Spirodela polyrhiza in allergic reaction has not been clarified yet. Type 1 hypersensitivity (immediate hypersensitivity), popularly known as allergy, is a major clinical problem in humans. It has been found that the histamine release from mast cells is an essential step in the pathological process of immediate hypersensitivity. In the present study, the effect of aqueous extract of Spirodela polyrhiza (AESP) on immediate hypersensitivity was investigated. AESP inhibited the antigen-induced passive cutaneous anaphylaxis (PCA). AESP in vitro exhibited a dose-dependent inhibition of degranulation in RPMC stimulated by compound 48/80. AESP also suppressed the morphological changes and the increase of intracellular free calcium level induced by compound 48/80. These results suggest that inhibitory effect of AESP on immediate hypersensitivity may be mediated through the decrease of intracellular free calcium levels, and AESP importantly contributes to the treatment of anaphylaxis and may be useful for other allergic disease.

Utilization of Industrial Wastes as Fertilizer (산업폐기물(産業廢棄物)의 비료화(肥料化))

  • Shin, Jae-Sung;Han, Ki-Hak
    • Applied Biological Chemistry
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    • v.27
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    • pp.68-79
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    • 1984
  • An increased population and rapidly expanding industrial development have led to enormous amounts of various domestic and industrial wastes. The proper disposal of ever-increasing wastes is a growing global problem. Land treatment is one of the rational approaches that are environmentally safe and economically practical. It has long been practised in many sites. Recycling of industrial wastes on agricultural land can provide better possible means for maintaining environmental quality and utilizing waste-resources. Even though industrial wastes are beneficial as soil amendment and fertilizer, they have some limitation on land application because of wide variability as well as physicochemical problem in their composition. A direct application of solid and liquid wastes on land is being practised in Korea and some experimental results are presented. The direct application of fermentation waste on rice resulted in a 6 percent yield increase. Another organic residue from glutamic acid fermentation is widely used not only as a direct application as a liquid fertilizer but also for a raw material of organic compound fertilizer. These wastes are much promising as sources of plant nutrients, since they have large amounts of nutrients, especially nitrogen with few toxic metals. On the other hand, fertilizers developed from inorganic industrial wastes include calcium silicate, calcium sulfate and ammonium sulfate. The calcium silicate fertilizer simply produced from slag, by-product of iron and steel manufacturing plant is one of the most successful example of the conversion of wastes to fertilizer and slag production capacity totals to over three million MT/year. About 200,000 MT of calcium silicate fertilizer is currently applied in the paddy rice every year. Calcium sulfate, a waste from the wet phosphoric acid process is to some extent used as a filler of compound fertilizers but quite large quantites are directly applied for the reclamation of tidal flat.

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Effects of Extracellular Calcium and Starvation on Biochemical Indices of the Rat Hepatocytes

  • Kim, Ki-Sung
    • Toxicological Research
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    • v.11 no.2
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    • pp.199-203
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    • 1995
  • The focus of this study was to investigate that cellular parameters and glucose uptake might be altered by extracellular calcium and starvation. Addition of 1 mM $Ca^{++}$ to hepatocytes (equalling to the free calcium concentration of blood) significantly increased intracellular $Na^+$ and decreased $Na^+$ & LDH leakage. This pertains to the hepatocytes of control rats as well as those of rats fasted for 24 and 48. hr. These effects might be come from the membrane-stabilizing effects of calcium. But calcium had no effects on cell volumes, superoxide-formation and glucose uptake. Actually hepatocytes of starved rats showed changes in several cellular parameters. Starvation increased LDH leakage, glucose uptake and the total concentration of $Na^+$ and $Na^+$ whereas it markedly decreased cell volumes. Since total tonicity remained unchanged, intracellular $Na^+$ and $Na^+$ could contribute to a higher share of total osmolarity in starvation. Starvation increased the cytoplasmic pH because $R-NH^{3+}$ions and their corresponding counterions disappeared. This increase may be related to suppress the protonization of amino groups in proteins. Starvation decreased hepatic glycogen, a major compound that affects cytosolic volume of hepatocytes. The data indicate that starvation increases the glucose transport activity. The possible molecular basis will be discussed.

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Buffering Effects of Calcium Salts in Kimchi: Lowering Acidity, Elevating Lactic Acid Bacterial Population and Dextransucrase Activity

  • Seo, Eun-Chae;Moon, Jin-Seok;Jung, Jee-Yun;Kim, Ji-Sun;Eom, Hyun-Ju;Kim, So-Young;Yoon, Hyang-Sik;Han, Nam-Soo
    • Journal of Microbiology and Biotechnology
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    • v.19 no.12
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    • pp.1644-1649
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    • 2009
  • This study investigates the buffering effects of calcium salts in kimchi on the total acidity, microbial population, and dextransucrase activity. Calcium chloride or calcium carbonate was added to dongchimi-kimchi, a watery radish kimchi, and the effects on various biochemical attributes were analyzed. The addition of 0.1% calcium chloride produced a milder decrease in the pH after 24 days of incubation, which allowed the lactic acid bacteria to survive longer than in the control. In particular, the heterofermentative Leuconostoc genus population was 10-fold higher than that in the control. When sucrose and maltose were also added along with the calcium salts, the dextransucrase activity in the kimchi was elevated and a higher concentration of isomaltooligosaccharides was synthesized when compared with the control. Calcium chloride was determined as a better activator compound of dextransucrase than calcium carbonate, probably because of its higher solubility. Therefore, the results of this study confirm the ability of the proposed approach to modulate the kimchi fermentation process and possibly enhance the quality of kimchi based on the addition of dietary calcium salts.

Inhibitory Effects of Several Korean Traditional Herbs on Anaphylactic Reaction and Mast Cell Activation (아나필락시스 반응과 비만세포 활성화에 대한 한국전통약제의 억제효과)

  • Chai, Ok-Hee
    • Applied Microscopy
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    • v.40 no.4
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    • pp.201-209
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    • 2010
  • Korean traditional herbs, especially Anemarrhena asphodeloides (A. asphodeloides), Salvia miltiorrhiza (S. miltiorrhiza), and Terminalia chebula (T. chebula) have been known to have the immunomodulatory, anti-tumor, and anti-inflammatory effects. However, direct cellular mechanism underlying the mast cell-mediated anaphylaxis-like reaction has poorly been understood. In the present study, the effects of the methanol extracts of A. asphodeloides (MEAA), S. miltiorrhiza (MESM), and T. chebula (METC) on anaphylactic reaction were investigated. Using in vitro and in vivo experiments, the influences of MEAA, MESM, and METC on the compound 48/80-induced anaphylaxis-like reaction and mast cell activation, and IgEmediated PCA were examined. Results are below; 1) MEAA, MESM, and METC significantly inhibited systemic anaphylaxis-like reaction, ear swelling response, and IgE-mediated PCA. 2) the compound 48/80-induced mast cell degranulation, histamine release of rat peritoneal mast cells (RPMC) were significantly inhibited by the pretreatment with MEAA, MESM, and METC, and 3) the compound 48/80-induced calcium influx in RPMC was significantly inhibited by the pretreatment with MEAA, MESM, and METC. These results suggest that MEAA, MESM, and METC may be an activity to inhibit the compound 48/80-induced or anti-DNP IgE-mediated anaphylactic reactions by blocking histamine release and calcium uptake into RPMC. MEAA, MESM, and METC potentially may serve as an effective therapeutic tool for allergic diseases.

Mechanism of Inhibitory Action of Anaphylaxis by Aqueous Extract of Poncirus trifoliata (즉시형(卽時型) 알레르기 반응(反應)에 있어서 물추출액(抽出液)의 억제작용기전(抑制作用機轉))

  • Hwang, Gwang-Ho;Lee, Eon-Jeong;Song, Bong-Keun;Kim, Hyeong-Kyun
    • The Journal of Korean Medicine
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    • v.18 no.1
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    • pp.316-325
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    • 1997
  • The dried unripe fruit of Poncirus trifoliata L. is widely used to treat urticaria, itch and indigestion in folk medicine. And recently it was reported the component of the fruit was found to exhibit an inhibitory effect on histamine release from mast cells. So to evaluate the effect of aqueous extract of Poncirus trifoliata L.(PTFE) on compound 48/80-induced histamine release, the study was carried out in rat peritoneal mast cell. PTFE $(10^{-3}{\sim}1mg/ml)$ inhibits the histamine release induced by compound 48/80 $(5{\mu}g/ml)$ in rat peritoneal mast cells. To clarify the mechanism of these inhibition, we investigated the effect of PTFE on cAMP and intracellular calcium content. The increase in cAMP content, when PTFE was added, was transient. At concentration of 1mg/ml, the cAMP content of mast cells was significantly increased at a rate of 53 times of basal cells at 10sec. PTFE inhibits histamine release by augmenting the cAMP content in mast cells. Moreover, PTFE inhibits intracellular calcium release induced by compound 48/80. This result suggests that PTFE may be useful for the prevention and treatment of allergy-related disease.

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