• 제목/요약/키워드: Bradykinin

검색결과 77건 처리시간 0.026초

부신수질 크로마핀(Chromaffin) 세포를 이용한 승마 추출무의 카테콜라민 분비 저해작용 (The Effects of Cimicifuga Racemosa Extracts on the Inhibition of Catecholamine Secretion in Bovine Chromaffin Cells)

  • 우경철;서병선
    • 생약학회지
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    • 제34권4호통권135호
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    • pp.318-323
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    • 2003
  • Extracts of Black cohosh (Cimicifugae rhizoma) have been used for the treatment of climacteric complaints for decades. A significant number of woman entering menopause exhibit the following symptoms: getting hot flushes, night sweats, irritability, depression, and anxiety, A reduction of the frequency of hot flushes equivalents and hints on the antidepressant activity of Cimcifuga extracts. In the present work, we have screened several 80% ethanol extracts from medicinal plants and found that the extracts from Cimicifugae Rhizoma(Black cohosh:승마) have inhibitory effect on catecholamine secretion in bovine chromaffin cell. Since this extract inhibited 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP)-induced catecholamine secretion, but did not inhibit KCl, bradykinin, and veratridine-evoked case, this inhibitory effect is mediated by nicotinic acetylcholine receptors with noncompetitive manner.

SHR에 있어 Enalapril의 ACE억제효과에 대한 Ginkgo biloba Extract(EGb 761)의 영향 (Effects of Ginkgo biloba Extract (EGb 761) on the Enalapril-induced ACE Inhibition in SHRs)

  • 이영미;염윤기;신완균;손의동;안형수
    • 약학회지
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    • 제45권1호
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    • pp.93-100
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    • 2001
  • Drug inetraction between of enalapril-induced angiotensin converting enzym) inhibitory effect and Ginkgo biloba Ext.-induced antioxidant action was evaluated in spontaneously hypertensive rats. Combination treatment of enalapril (20 mg/kg/day p.o.) and Ginkgo biloba Ext. (60 mg/kg/day, p.o.) for 6 weeks in drinking water to SHRs resulted the inhibition of ACE activity in lung tissue, angiotensin I-induced pressure response and plasma angiotensin II concentration as similar to enalapril alone treatment. But these effects were sustained after 1 week withdrawal of enalapril and Ginkgo biloba Ext. co-administeration. Also, coadministered group did not increase the concentration of bradykinin in lung tissue, which were different from enalapril alone treated group. Co-administration of enalapril and Ginkgo biloba Ext. inhibited the hemolysis induced by UV B type, even Ginkgo biloba Ext. alone treated group did not. These results suggested that Ginkgo biloba Ext. sustained ACE inhibitory effect and reduced the inhibitory effect of bradykinin inactivation induced by enalapril, meanwhile, enalapril increased the antioxidant effect of Ginkgo biloba Ext.

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Theoretical Study on Hydrophobicity of Amino Acids by the Solvation Free Energy Density Model

  • Kim, Jun-Hyoung;Nam, Ky-Youb;Cho, Kwang-Hwi;Choi, Seung-Hoon;Noh, Jae-Sung;No, Kyoung-Tai
    • Bulletin of the Korean Chemical Society
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    • 제24권12호
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    • pp.1742-1750
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    • 2003
  • In order to characterize the hydrophobic parameters of N-acetyl amino acid amides in 1-octanol/water, a theoretical calculation was carried out using a solvation free energy density model. The hydrophobicity parameters of the molecules are obtained with the consideration of the solvation free energy over the solvent volume surrounding the solute, using a grid model. Our method can account for the solvent accessible surface area of the molecules according to conformational variations. Through a comparison of the hydrophobicity of our calculation and that of other experimental/theoretical works, the solvation free energy density model is proven to be a useful tool for the evaluation of the hydrophobicity of amino acids and peptides. In order to evaluate the solvation free energy density model as a method of calculating the activity of drugs using the hydrophobicity of its building blocks, the contracture of Bradykinin potentiating pentapeptide was also predicted from the hydrophobicity of each residue. The solvation free energy density model can be used to employ descriptors for the prediction of peptide activities in drug discovery, as well as to calculate the hydrophobicity of amino acids.

간문맥 고혈압 고양이에서 비-간 교감신경성 반사의 변동에 대한 연구 (Studies of Alterations in Spleno-Hepatic Reflex in Portal Hypertensive Cats)

  • 송환규;임병용;김치대;홍기환
    • 대한약리학회지
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    • 제23권1호
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    • pp.15-23
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    • 1987
  • 만성 간문맥 고혈압에 동반하는 내장 충혈에 대한 발생 기전을 규명하기 위하여 고양이의 간문맥을 결찰하고 그 경과에 따라 비 -간 교감 신경성 반사 흥분의 변동과 동시에 순환 역동학적 변동을 관찰하였다. 1. 대조 고양이 (Sham 수술군)에서 비동맥을 통하여 capsaicin, bradykinin 및 vasopressin을 주사 하였을 매에는 전신 동맥압의 반사 흥분뿐만 아니라 비정맥압의 상승을 초래하였다. 그러나 심박동수는 변화가 없었다. 동시에 비장(비-비 반사) 및 간장 (비 -간 반사)에서 교감 신경의 만사 흥분을 일으켰다. 2. Capsaicin을 간 표면에 도포하였을 때는 간 신경 흥분 (간-간 반사)과 등시에 승압 반사를 유발시켰다. 3. 문맥 결찰 후에는 비정맥압은 시간 경과에 따라 증가 하였고 이에 동반하여 전신 동맥압은 감소하였다. 그러나 승압반사 항진은 제2일에 현저하게 야기되었고 그후 대조치로 회복되었다. 비-비 또는 비-간 교감 신경 반사 흥분은 제8일에 현저히 감약되었다. 4. 이상의 성적을 종합하면 비장 및 간장에 분포하는 교감 신경 반사 흥분은 동일한 중추 지배에 의하여 조절되고, 간문맥 결찰 후 내장 반사 흥분의 감소는 내장 충혈의 발생과 밀접한 관련이 있을 것으로 사료되었다.

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Neurotensin Induces Catecholamine Secretion and Calcium Rise by B2 Bradykinin Receptor Activation in PC12 Cells

  • Park, Tae-Ju;Kim, Kyong-Tai
    • 한국생물물리학회:학술대회논문집
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    • 한국생물물리학회 1998년도 학술발표회
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    • pp.32-32
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    • 1998
  • The effect of neurotensin (NT) was investigated in rat pheochromocytoma (PC12) cells. When PC12 cells were treated with micromolar concentrations of NT, [$^3$H]norepinephrine ([$^3$H]NE) secretion and elevation of cytosolic Ca$\^$2+/ concentration ([Ca$\^$2+/]i) were evoked in a concentration-dependent manner with an EC$\sub$50/ of 50 ${\mu}$M.(omitted)

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택사의 Alisol성분들이 몇가지 Agonist에 의한 적출장관 수축에 미치는 영향 (Effect of Alisols Isolated from Alisma orientale Jazep. Against Several Agonists in Isolated Rat Ileum)

  • 윤혜숙;정성현;김영숙
    • 생약학회지
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    • 제12권4호
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    • pp.200-202
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    • 1981
  • Alisol B(II) and alisol B monoacetate (III) isolated from the rhizome of Alisma orientale Jazepczuk (Alismataceae) showed antagonistic effects against the contractions induced by angiotensin and bradykinin in rat ileum. However, they seem to be nonspecific antagonism.

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Isolation of Angiotensin I Converting Enzyme (ACE) Inhibitor from fermented oyster, Crassostrea gigas

  • Park, Ji-Young;Je, Jae-Young;Park, Pyo-Jam;Kim, Se-Kwon
    • 한국어업기술학회:학술대회논문집
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    • 한국어업기술학회 2002년도 추계 수산관련학회 공동학술대회발표요지집
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    • pp.193-194
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    • 2002
  • Angiotensin I converting enzyme (ACE) inhibitor was purified from Crassostrea gigas. The ACE belongs to the class of metalloprotease. This enzyme plays an important physiological role in regulating blood pressure of the rennin-angiotensin system by converting from angiotensin I to octapeptide angiotensin II, a potent vasoconstrictor and by inactivating bradykinin, which has depressor action. (omitted)

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Chlorpromazine Inhibits Store-operated Calcium Entry and Subsequent Norepinephrine Secretion in PC12 Cells

  • Park, Se-Young;Kim, Yong-Hyun;Lee, Yong-Kyu;Kim, Kyong-Tai
    • 한국생물물리학회:학술대회논문집
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    • 한국생물물리학회 1999년도 학술발표회 진행표 및 논문초록
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    • pp.67-67
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    • 1999
  • The effect of chlorpromazine on the store-operated Ca$\^$2+/ entry subsequently activated via the phospholipase C signaling pathway was investigated in PC12 cells. Chlorpromazine caused a rapid decline of the bradykinin-induced Ca$\^$2+/ increase to basal level without attenuating the peak level.(omitted)

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Screening of Natural Products for Endothelial and Renal Nitric Oxide Production

  • Kim, Hyeyoung;Han, Sang-Won
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1997년도 춘계학술대회
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    • pp.90-90
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    • 1997
  • Natural products, which have been used for the treatment of hypertension, diuresis and nephritis in traditional oriental medicine, were selected for the screening of nitric oxide (NO) production in endothelial cells and kidney tissues in vitro as well as in vivo by measuring the conversion of [$\^$14/C]-L-arginine to [$\^$14/C]-L-citrulline, a coproduct of the enzyme reaction with NO. Confluent monolayer of endothelial cells were used for the screening of 16 natural products. Among the natural products, Zizyphus jujuba and Codonopsis pilosula stimulated endothelial NO synthase activity. Thus, both confluent monolayer of endothelial cells and kidney homogenates (glomeruli, cortical tubules, meudllae) were treated with Zizyphus jujuba and Codonopsis pilosula (final concentration 10 $\mu\textrm{g}$/$m\ell$) and NO releases were compared with those by receptor - dependent agonists, bradykinin and ADP and receptor - independent calcium ionophore A23187 in vitro. In rat experiment, NO releases in glomeruli, cortical tubules and medullae and plasma renin activity were assessed after intraperitoneal injection of Zizyphus jujuba and Codonopsis pilosula (10 mg/kg/day for 4 days). As a result, both Zizyphus jujuba and Codonopsis pilosula significantly increased NO releases in cultured endothelial cells, kidney tissues in vitro as well as in vivo. Stimulation of NO releases by Zizyphus jujuba and Codonopsis pilosula was similar to those by receptor - dependent agonists, bradykinin and ADP and receptor - independent calcium ionophore A23187 in cultured endothelial cells. However, plasma renin activity was not influenced by these two natural products. In conclusion, stimulatory effects of Zizyphus jujuba and Codonopsis pilosula on NO release in kidney may contribute their hypotensive effects and antinephritic action possibly by increasing renal blood flow.

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Regulation of Adenosine-activated GIRK Channels by Gq-coupled Receptors in Mouse Atrial Myocytes

  • Cho, Ha-Na
    • The Korean Journal of Physiology and Pharmacology
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    • 제14권3호
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    • pp.145-150
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    • 2010
  • Adenosine (Ado) is an important mediator of the endogenous defense against ischemia-induced injury in the heart. The action of Ado is mediated by activation of G protein-gated inwardly rectifying $K^+$ (GIRK) channels. In turn, GIRK channels are inhibited by reducing phosphatidylinositol 4,5-bisphosphate ($PIP_2$) through Gq protein-coupled receptors (GqPCRs). We previously found that GIRK channels activated by acetylcholine, a muscarinic M2 acetylcholine receptor agonist, are inhibited by GqPCRs in a receptor-specific manner. However, it is not known whether GIRK channels activated by Ado signaling are also regulated by GqPCRs. Presently, this was investigated in mouse atrial myocytes using the patch clamp technique. GIRK channels were activated by $100\;{\mu}M$ Ado. When Ado was repetitively applied at intervals of 5~6 min, the amplitude of second Ado-activated GIRK currents ($I_{K(Ado)}$) was $88.3{\pm}3.7%$ of the first $I_{K(Ado)}$ in the control. Pretreatment of atrial myocytes with phenylephrine, endothelin-1, or bradykinin prior to a second application of Ado reduced the amplitude of the second $I_{K(Ado)}$ to $25.5{\pm}11.6%$, $30.5{\pm}5.6%$, and $96.0{\pm}2.7%$, respectively. The potency of $I_{K(Ado)}$ inhibition by GqPCRs was different with that observed in acetylcholine-activated GIRK currents ($I_{K(ACh)}$) (endothelin-1>phenylephrine>bradykinin). $I_{K(Ado)}$ was almost completely inhibited by $500\;{\mu}M$ of the $PIP_2$ scavenger neomycin, suggesting low $PIP_2$ affinity of $I_{K(Ado)}$. Taken together, these results suggest that the crosstalk between GqPCRs and the Ado-induced signaling pathway is receptor-specific. The differential change in $PIP_2$ affinity of GIRK channels activated by Ado and ACh may underlie, at least in part, their differential responses to GqPCR agonists.