• Title/Summary/Keyword: 억제작용

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윤활 오일에서 재가 생기지 않는 산화방지제, 구리 반응 억제제와 부식 방지제의 이용에 관한 고찰

  • 강석춘
    • Tribology and Lubricants
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    • v.6 no.2
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    • pp.1-15
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    • 1990
  • 본 해설에서는 윤활 오일에서 구리 반응 억제제와 철의 부식 억제제에 관한 내용을 검토한 것으로 자동산화 화정의 초기 생성과 연쇄적인 전파, 확산 및 종료 그리고 1차 및 2차 산화 억제제에 관해서 서술한 것이다. 구리 반응 억제제와 부식 억제 성질 및 작용이 고려되고 첨가제로써의 응용에 관해 조사하였다.

Agonist-Antagonist Effects of Buprenorphine on Action Potentials of Frog Sciatic Nerve Fibers (개구리 좌골신경에 대한 Buprenorphine의 작용 양상)

  • Lee, Jong-Hwa;Frank, George B.
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.23-30
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    • 1989
  • Buprenorphine, one of the mixed agonist-antagonist opioid drugs was used to inverstigate the opioid receptor on frog sciatic nerve A fibers. Action potentials were recorded for 4 hrs by a sucrose gap apparatus which were separated by four rubber membranes. To examine the one of the mechanism of action of buprenorphine, meperidine or naloxone was added after or before the treatment of buprenorphine. The results of this experiment were as follows: 1. Buprenorphine suppressed significantly the compound action potentials of frog sciatic nerve, and the maximal effects were shown both at $10^{-4}\;M$ and at $10^{-8}\;M$. 2. The dose-response relationship of buprenorphine on the depressant effect in frog sciatic nerve was biphasic and inverted U-shaped. 3. Buprenorphine blocked the effect of Meperidine $(10^{-3}\;M)$ on this preparation. 4. The depressant effcct of Buprenorphine on frog sciatic nerve was blocked by $10^{-8}\;M$ naloxone. From the above results, buprenorphine acts as one of agoinist-antagonistic effect on frog sciatic nerve, and the opioid receptor on this preparation is located on or near the intracellular opening of the sodium channels, which are sensitive to naloxone.

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항이뇨작용기전 검색(Naproxen을 중심으로)

  • 이한구;유강준;임동윤;고석태
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.285-285
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    • 1994
  • Naproxen을 개의 정맥내 투여하였을때 뇨량의 감소와 더불어 삼투질제거율(Cosm), 뇨중 $Na^{+}$$K^{+}$의 배설율( $E_{Na}$ , $E_{k}$ )의 감소와 신세뇨관에서의 $Na^{+}$$K^{+}$의 재흡수율( $R_{Na}$ , $R_{k}$ )과 K/Na비의 증대를 나타내었으며 신혈류량(RPF)이 감소하였다. 한쪽 신동맥내에 naproxen을 투여하였을때 투여신(실험신)에서의 이뇨작용과 대조신에서의 항이뇨작용을 나타내었다. 경동맥에 naproxen을 투여하였을때도 뚜렷한 항이뇨작용을 나타내었다. 이와같은 두경우에서의 항이뇨 작용시의 신기능변화는 정맥내 naproxen의 경우와 같은 양상을 나타내었다. 경동맥내의 naproxen의 항이뇨작용은 신신경 제거에 의하여 영향을 받지 않았으나 정맥내로의 arachidonic acid나 indomethacin의 전처리에 의하여서는 나타나지 않았다. 경동맥내의 naproxen은 정맥내의 spironolactone의 이뇨작용을, 정맥내의 spironolactone은 경동맥내의 naproxen의 항이뇨작용을 억제하였다. 이상의 결과로 보아 naproxen은 중추성 항이뇨작용과 $Na^{+}$저류를 나타내며 이는 prostaglasdin의 합성억제와 aldosterone양 작용에 의하는 것으로 사료된다.

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Anti-melanogenesis Effect of Phenolic Compounds Isolated from Gastrodia elata (천마(Gastrodia elate) 추출물로부터 분리된 페놀성 물질의 멜라닌 생성 억제작용)

  • 김경태;김진국;박선희;이정하;이수희;김기호;박수남
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.1
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    • pp.33-38
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    • 2004
  • Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

Effects of Calcium Antagonists on Superoxide Generation, NADPH Oxidase Activity and Phagocytic Activity in Activated Neutrophils (칼슘 길항제가 활성화된 호중구에서의 $O_{\overline{2}}$의 생성, NADPH oxidase활성도 및 탐식작용에 미치는 영향)

  • Lee, Chung-Soo;Han, Eun-Sook;Lee, Kwang-Soo
    • The Korean Journal of Pharmacology
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    • v.23 no.1
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    • pp.33-44
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    • 1987
  • NADPH oxidase dependent superoxide generation and phagocytosis in neutrophils stimulated with opsonized zymosan or heat aggregated IgG were coincided with the process of calcium uptake. The responses in activated neutrophils were enhanced with increasing concentrations of extracellular calcium and these effects were significantly inhibited by calcium chelators, EGTA and EDTA. The superoxide generation in activated neutrophils was reduced by dantrolene and chlorpromazine. Calcium antagonists, bepredil, diltiazem, verapamil, nifedipine and nimodipine effectively inhibited the calcium uptake, superoxide generation and phagocytosis in activated neutrophils, and NADPH oxidase activity was also inhibited. The results suggest that calcium antagonists may inhibit the superoxide generation and phagocytosis in activted neurtophils by the inhibition of calcium influx and by the action on intracellular redistribution of calcium and NADPH oxidase system.

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Antioxidative Activiry and Anticlastogeniciry of Cassia tora L. seeds Extract and its Major Component, $Nor-rubrofusarin-6-{\beta}-D-glucoside$ (결명자 추출물과 노르-루브로푸사린의 산화적 스트레스억제효과 및 항염색체손상과 효과)

  • 김수희;최재수;허문영
    • Journal of Food Hygiene and Safety
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    • v.13 no.4
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    • pp.394-399
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    • 1998
  • 결명자의 주용성분인 노르-루브로푸사린의 함량이 높은 추출물을 얻기 위하여 결명자분말을 0~100%의 에탄올수용액으로 추출하여 고농도의 노르-루브로푸사린을 함유하는 결명자 추출물을 제조하였다. 결명자추출물과 주요 함유성분인 노르-루브로푸사린은 항산화활성과 프리라디칼소거 작용을 나타내었으며, H2O2 유도 세포독성에 대해서도 억제적으로 작용하여 cyto-protective effect를 나타내었다. 또한 DNA crosslinking agent 인 mitomycin C 유도 소핵생성에도 결명자 70% 에탄올추출물과 노르-루브로파사린이 매우 높은 억제활성을 나타내었다. 따라서 결명자 추출물과 노르-루브로푸사린은 산소라디칼들에 의한 산화적 손상 및 DNA 손상 등에 억제적으로 작용하는 기전을 활용하여 항산화성 스트레스를 통한 항노화 , 암예방제로서의 응용가능성이 높은 물질로 판단되었다.

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Analysis of Available Component in Artemisiae Herba (약쑥의 유용성분 정량분석)

  • Ryu Su-Noh;Kang Sam Sik
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.49 no.spc1
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    • pp.169-175
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    • 2004
  • 동의보감에 수재되어 있는 약쑥은 식용뿐만이 아니고 한방에서는 출혈 및 지혈약으로 자궁출혈, 임신중의 출혈, 코피지혈 등에 효과가 크다고 알려져 왔다. 또한 부인병과 건위, 설사치료와 항암활성, HeLa cell에 대한 억제작용도 보고되어 있다. MeOH엑스가 HCl-EtOH유발법, $1\%$ 암모니아 수용액 유발법, HCl-aspirin 유발법등에 의하여 유발된 위 손상에 대하여 강한 억제 작용을 나타내고 있는데 이는 flavonoid의 일종인 eupatilin으로 확인된 바 있다. 이 물질이 5-lipoxygenase inhibitor ($ID_{50}=14{\times}16^{-6}M$) 작용과 prosta glandin synthase의 활성을 약간 억제한다고 보고되었다. 약쑥의 eupatilin과 jaceosidin을 분리하여 그 화학구조를 구명하였다. 이를 지표물질로 하여 HPLC 분석조건과 HPLC용 검체의 조제, 표준검량선을 작성하였다. 강화사자발쑥 100 g의 잎에는 eupatilin은 240 mg, jaceosidin은 10 mg함유되어 있고 싸주아리쑥에는 eupatilin은 330 mg, jaceosidin은 123 mg 함유되어 있음이 확인되었다.

Effect of Soluble EPCR on the Anti-Inflammatory Effects by Activated Protein C (수용성 EPCR에 의한 활성화된 단백질 C의 항염증 작용에 관한 연구)

  • Bae, Jong-Sup;Park, Moon-Ki;Park, Sang-Wook
    • Korean Chemical Engineering Research
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    • v.47 no.4
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    • pp.501-505
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    • 2009
  • In this study, we evaluated the effect of soluble EPCR(Soluble Endothelial Protein C Receptor, sEPCR) on the anti-inflammatory activities by activated protein C(APC) in endothelium. We demonstrated that sEPCR inhibited the barrier protective activity, the inhibition of neutrophils adhesion toward endothelial cells and the inhibition of transendothelial migration by APC in endothelial cells. Interestingly, sEPCR also blocked the mechanism by which APC inhibited the expression of cell adhesion molecules(CAM) by TNF-alpha in endothelial cells. These results suggested that the anti-inflammatory activities of APC was inhibited by sEPCR which blocked the binding motifs of Gla domain of APC to membrane bound EPCR. This finding will provide the important evidence in the development of new medicine for the treatment of severe sepsis and inflammatory diseases and good clue for understanding unknown mechanisms by which APC showed the anti-inflammatory activities in endothelium.

Inhibitory Action of Maillard Reaction Products Derived from Glucose Amino Acids on the Formation of N-nitrosamine (Glucose-아미노산계 Maillard 반응생성물의 니트로사민 생성억제작용)

  • 이동호;이태기;여생규;염동민;김선봉;박영호
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.23 no.1
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    • pp.137-142
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    • 1994
  • The present paper was carried out to investigate the inhibition of carcinogenic N-nitrosodimethylamine(NDMA) formation by Maillard reactiion products and nondialyzable melanoidins, obtiane dfrom the glucoseamino acids(Lys, Gly, Arg, His) model systems under different pH conditions(pH 1.2, 4.2 and 6.0). Maillard raction products and nondialyzable melanoidins, produced from the 4 model systems, had a inhibitory action of N-nitrosodimethylamine formation. The inhibitiondegree by the nondialyzable mealanoidins. at pH 1.2 was similar to that at pH 4.2 and that by ascorbic acid at pH 1.2 . Inhibitory action of N-nitrosodimehylamine formation by the reduced Maillard reaction products and nondialyzable melanoidins were lower than that of original samples. Accordingly, it is assumed that the inhibition of N-nitrosodimehtylamine formation of Maillard reaction products is due to their reducing powers.

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Inhibitory Effects of ${\gamma}$-Aminobutyric Acid on the Contractility of Isolated Rat Vas Deferens (흰쥐의 적출 정관 수축성에 대한 ${\gamma}$-Aminobutyric Acid의 억제작용)

  • Ahn, Ki-Young;Kwon, Oh-Cheol;Ha, Jeoung-Hee;Lee, Kwang-Youn;Kim, Won-Joon
    • Journal of Yeungnam Medical Science
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    • v.9 no.2
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    • pp.382-395
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    • 1992
  • GABA is an inhibitory neurotransmitter in central nervous system and produce sedative, antianxiety and muscle reaxing effects via $GABA_A$ receptor or $GABA_B$ receptor. Recently it is known that GABA is widely distributed throughout peripheral organs and may playa physiological role in certain organ. The vas deferens is innervated by species-difference. These study, therefore, was performed to investigate the mode and the mechanism of action of GABA on the norepiniphrine-, ATP- and electric stimulation-induced contraction of vas deferens of rat. Sprague-Dawley rats were sacrificed by cervical dislocation. The smooth muscle strips were isolated from the prostastic portion and were mounted in the isolated muscle bath. PSS in the bath was aerated with 95/5%-$O_2/CO_2$ at $33^{\circ}C$. Muscle tensions were measured by isometric tension transducer and were recorded by biological recording system. 1. GABA, muscimol, a $GAB_A$ agonist, and baclofen, a $GABA_B$ agonist inhibited the electric field stimulation(EFS, 0.2Hz, 1mSec, 80 V, monophasic square wave)-induced contraction with a rank order of potency of GABA greater than baclofen greater than muscimol. 2. The inhibitory effect of GABA was antagonized by delta aminovaleric acid(DAVA), a $GABA_B$ antagonist, but not by bicuculline, a $GABA_A$ mtagonist. 3. The inhibitory effect of baclofen was antagonized by DAVA, but the effect of muscimol was not antagonized by bicuculline. 4. Exogenous norepinephrine(NE) and ATP contracted muscle strip concentration dependently, but the effect of acetylcholine was negligible : and GABA did not affect the NE-and ATP-induced contractions. 5. GABA, baclofen and muscimol did not affect basal tone, and GABA did not affect the NE-and ATP-induced contractionsm 6. EFS-induced contraction was including 2 distinctable components. The first phasic component was inhibited by beta gamma-methylene ATP(mATP), a desensitizing agent of APT receptor and the second tonic component was reduced by pretreatment of reserpine(3 mg/Kg, IP). 7. GABA inhibited the EFS-induced contraction of reserpinized strips, but not the mATP-treated strips. These results suggest that in the prostatic portion of the rat vas deferens, adrenergic and purinergic neurotransmissions are exist, and GABA inhibits the release of ATP via presynaptic $GABA_B$ receptor on the excitatory neurons.

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