• 약학회지
• /
• 제41권3호
• /
• pp.345-351
• /
• 1997

The purpose of this investigation was to determine the inhibition of $Na^+,\;K^+$-ATPase, cyclicAMP phophodiesterase and platelet activation by secondary metabolites isolated from mar ine organisms. The secondary metabolites were isolated and identified as six diterpenoids(1 : astrogorgin, 2 : ophirin, 3 : calicophirin B, 4, 5 and 6 : cladiellin) from the dichloromethane extract of Muricellajsp., four ceramides(1,2,3, and 4) from Acabaria undulata and three antharaquinones(1,2 : crysophanol, and 3 : physcion) from Urechis unicintus. The results demonstrated that diterpenoids(2,3, and 4) showed the inhibition of cyclicAMP phosphodiesterase, and ceramides(1,3, and 4) showed the inhibition of cyclicAMP phosphodiesterase and thrombin(0.1 units/ml)-induced aggregation of washed rabbit platelet, and anthrapuinones((1,2, and 3) showed the inhibition of $Na^+,\;K^+$-ATPase. Among the anthraquionones, 1,2-dimethoxy-3-methyl-8-hydroxy-anthraquinone(1) showed the inhibition of collagen(1.0 ${\mu}g$/ml)-induced aggregation in a concenration-dependent manner with IC50 value of 42.8 ${\mu}g$M.

• Genomics & Informatics
• /
• 제5권2호
• /
• pp.77-82
• /
• 2007

Serotonin (5-HT), the endogenous nonselective 5-HT receptor agonist, activates the inositol-1,4,5-triphosphate/calcium $(InsP3/Ca^{2+})$ signaling pathway and exerts both stimulatory and inhibitory actions on cAMP production and neuromodulin secretion in rat hypothalamic neurons. Specific mRNA transcripts for 5-HT1A, 5-HT2C and 5-HT4 were identified in rat hypothalamic neurons. These experiments were supported by combined techniques such as cAMP and a $Ca^{2+}$ assays in order to elucidate the associated receptors and signaling pathways. The cAMP production and neuromodulin release were profoundly inhibited during the activation of the Gi-coupled 5-HT1A receptor. Treatment with a selective agonist to activate the Gq-coupled 5-HT2C receptor stimulated InsP3 production and caused $Ca^{2+}$ release from the sarcoplasmic reticulum. Selective activation of the Gs-coupled 5-HT4 receptor also stimulated cAMP production, and caused an increase in neuromodulin secretion. These findings demonstrate the ability of 5-HT receptor subtypes expressed in neurons to induce neuromodulin production. This leads to the activation of single or multiple G-proteins which regulate the $InsP3/Ca^{2+}/PLC-{\gamma}$ and adenyl cyclase / cAMP signaling pathways.

• 대한의생명과학회지
• /
• 제20권3호
• /
• pp.129-138
• /
• 2014

In this study, we investigated the effect of water extract from rice bran (RB) on ADP ($20{\mu}M$)-stimulated platelet aggregation. RB dose-dependently inhibited ADP-induced platelet aggregation, and its $IC_{50}$ value was $224.0{\mu}g/mL$, which was increased by adenylate cyclase inhibitor SQ22536 and cAMP-dependent protein kinase (A-kinase) inhibitor Rp-8-Br-cAMPS. RB elevated the phosphorylation of VASP ($Ser^{157}$) which was also inhibited by SQ22536 and Rp-8-Br-cAMPS. It is thought that RB-elevated cAMP contributed to the phosphorylation of VASP ($Ser^{157}$) to inhibit ADP-induced platelet aggregation. Therefore, we demonstrate that RB has an antiplatelet effect via cAMP-dependent phosphorylation of VASP ($Ser^{157}$), and RB may have preventive or therapeutic potential for platelet aggregation-mediated diseases, such as thrombosis, myocardial infarction, atherosclerosis, and ischemic cerebrovascular disease.

• Archives of Pharmacal Research
• /
• 제12권3호
• /
• pp.207-213
• /
• 1989

This study was performed to investigate the mechanism of in vitro cytotosic actions of polyacetylenes which are panaxydol, panaxynol and panaxytriol isolated from Panax ginseng C. A. Meyer. DNA synthesis of L1210 cells was significantly inhibited with dose dependent pattern when L1210 cells were treated for 1 hour with over 5 .mu.g/ml of polyacetylenes. Panaxydol which had the most potent cytotoxicity among three polyacetylenes showed also the strongest inhibitory effect on DNA synthesis. Intracellular cyclic AMP levels of L1210 cells treated with 2.5 $\mu$g/ml of panaxydol or panaxytriol were significantly elevated on the incubation duration. The elevation of cyclic AMP levels by panaxytriol was higher than that by panaxydol, but no significant increase in cyclic AMP by panaxynol was observed. All three polyacetylenes had no effect on glycolysis of L1210 cells. Electron microscopic observations revealed that polyacetylenes caused damage to plasma membranes of L1210 cells in proportion to their cytotoxicities at each $ED_{50}$ value (panaxydol > panaxynol> panaxytriol). These results suggest that cytotoxicities of polyacetylenes against L1210 cells might be mediated by elevated cyclic AMP level, even though the relationship among their cytotoxicities, inhibitory effect on DNA synthesis and ability to elevation of cyclic AMP level are not fully agreed, and might be also related to membrane damage.

• Asian-Australasian Journal of Animal Sciences
• /
• 제13권7호
• /
• pp.901-905
• /
• 2000

An experiment was conducted to investigate the effect of caffeine, cAMP and cattle seminal plasma on preservation of semen at ultra low temperature ($-196{^{\circ}C}$). Each semen sample was divided into four parts equal in volume and sperm concentration; three were treated with caffeine, or cAMP, or cattle seminal plasma (CSP) and the fourth was kept as control. Sperm motility, abnormal spermatozoa, live-dead count and acrosomal damage were studied at different stages of freeze preservation viz.; just after dilution, at $5{^{\circ}C}$, at glycerolisation, before freezing, just after freezing, 24 hours of storage, and one week of storage. Sperm motility (58.39, 61.33, 52.00 and 50.39 per cent), non-eosinophilic spermatozoa (72.55, 69.98, 63.31 and 67.64 per cent), abnormal spermatozoa (5.71, 4.98, 8.04 and 5.66 per cent) and acrosomal damage (13.28, 13.33, 14.80 and 14.65 per cent) were observed in cAMP, caffeine, cattle seminal plasma and control, respectively, at every stage of freeze preservation. From this study it could be concluded that freezability of buffalo semen can be improved through the addition of caffeine followed by cAMP and cattle seminal plasma.

• Journal of Microbiology
• /
• 제34권4호
• /
• pp.374-378
• /
• 1996

In the aquatic fungus Allomyces macrogynus the effects of $Ca^{2+}$ and cAMP on the intracellular signal transduction of zoospore germination were studied using in vitro protein phosphorylation assay system. An endogenously phosphorylated protein (p50) having molecular weight of 50 kDa on SDS-PAGE was found in soluble fractions of both zoospore and mycelium. In zoospore extract, the endogenous phosphorylation of p50 was weak without any effectors, but was enhanced by $Ca^{2+}$ and even more by cAMP. Phosphorylation of the same protein in mycelial extract was high only in the absence of cAMP. Irrespective of the presence of $Ca^{2+}$ and cAMP, its phosphorylation was antagonistically suppressed in assay of combined zoospore and mycelial extracts. These results suggest that p50 is interconvertible in phosphorylation/dephosphorylation as a novel protein involved in germination of A. macrogynus. The antagonistic effect of cAMP to the phosphorylation of p50s from different developmental stages may be important in the regulation of cellular differentiation.

• 한국산학기술학회논문지
• /
• 제6권2호
• /
• pp.110-115
• /
• 2005

표면 경화가 요구되는 소재에 코발트계 합금 분말을 용사 소모재로 하고 플라즈마 트랜스퍼드 아크(PTA) 용사 공정을 이용하여 표면 개질부를 제조하였다. 표면 개질부는 다른 용사 변수는 일정하게 유지한 상태에서 용사 전류만을 변화하여 제조하였다. 용사 전류를 80에서 140 amp까지 20 amp씩 증가하면서 개질층을 제조하였다. 두께가 일정한 모재에 전류를 변화하여 표면 개질층을 제조하는 경우 용사후 모재에서 발생하는 냉각 효과가 다르게 되고 이는 개질층의 폭과 두께 등의 기하학적 형상과 미세 조직, 그리고 미세경도 등의 특성에 영향을 미치는 것으로 나타났다. 용사 전류를 120amp로 사용한 경우 미세조직이 조밀하고 미세경도 값이 가장 높은 값을 나타내는 개질층을 얻을 수 있었다. 전류를 증가함에 따라 개질층의 폭은 증가하지만 높이는 큰 변화가 없는 것으로 나타났다.

• 무역학회지
• /
• 제43권6호
• /
• pp.93-112
• /
• 2018

최근 항만구역내의 대기오염원 감축을 위해 미국을 비롯한 중국 등 세계 각국의 노력이 다양하게 이뤄지고 있다. 항만에 기항하는 선박이 많아질수록 물동량과 선박에서 배출되는 대기오염물질 역시 증가되고 있기 때문에 항만공사와 선사 및 터미널운영사의 사회적책임이 중요해 지고 있다. 육상전력공급시설(AMP)은 선박의 디젤발전기를 대체하여 육상 전력을 선박에 공급함으로서 발전기에서 배출되는 대기오염물질을 감소시키는 공해방지대책이다. 본 연구는 광양항의 효율적인 육상전력공급설비 운영방안 도출을 위해 정박 시 AMP요금과 Bunk Fuel 요금을 비교하였다.

• 공업화학
• /
• 제9권1호
• /
• pp.107-114
• /
• 1998

40, 50, 60, 70, $80^{\circ}C$에서 20wt%와 30wt%의 AMP 수용액에 대한 $CO_2$의 용해도를 실험을 통해서 구하였다. Kent-Eisenberg 모델을 변형하여 주어진 온도범위에서 30wt% AMP 수용액에 대한 실험값의 회귀분석을 통해 평형상수값과 상관관계식을 구하였으며, 계산된 평형상수값과 모델을 통해서 20wt% AMP 수용액에 대한 $CO_2$의 용해도를 예측한 결과는 실험값과 잘 일치함을 보였다. 본 연구에서 구한 평형상수의 상관관계식을 이용하여 문헌에 제시된 조건에서의 용해도를 예측한 값과 대단히 엄밀한 모델로 알려진 Deshmukh-Mather의 모델에 의한 예측값을 비교했을 때, 두 값은 거의 일치하였다. 그러므로, 제시한 상관관계식과 변형된 Kent-Eisenberg모델은 AMP수용액에 대한 $CO_2$의 흡수평형을 정확하게 나타낸다고 볼 수 있다. 액상의 각 물질의 농도를 평형모델을 이용하여 계산하였으며, AMP의 우수한 흡수능은 steric hindrance 효과에 의한 불안정한 carbamate의 형성에서 기인함을 확인하였다. AMP에 대한 $CO_2$의 용해도 자료로부터, Gibbs-Helmholtz 식을 이용하여 ${\Delta}Hs$의 값을 구하였다.

• The Korean Journal of Physiology and Pharmacology
• /
• 제20권1호
• /
• pp.9-14
• /
• 2016

Adenosine 3',5'-cyclic monophosphate (cAMP) participates in the regulation of numerous cellular functions, including the $Na^+-K^+$-ATPase (sodium pump). Ouabain, used in the treatment of several heart diseases, is known to increase cAMP levels but its effects on the atrium are not understood. The aim of the present study was to examine the effect of ouabain on the regulation of atrial cAMP production and its roles in atrial endothelin-1 (ET-1) secretion in isolated perfused beating rabbit atria. Our results showed that ouabain ($3.0{\mu}mol/L$) significantly increased atrial dynamics and cAMP levels during recovery period. The ouabain-increased atrial dynamics was blocked by KB-R7943 ($3.0{\mu}mol/L$), an inhibitor for reverse mode of $Na^+-Ca^{2+}$ exchangers (NCX), but did not by L-type $Ca^{2+}$ channel blocker nifedipine ($1.0{\mu}mol/L$) or protein kinase A (PKA) selective inhibitor H-89 ($3.0{\mu}mol/L$). Ouabain also enhanced atrial intracellular cAMP production in response to forskolin and theophyline ($100.0{\mu}mol/L$), an inhibitor of phosphodiesterase, potentiated the ouabain-induced increase in cAMP. Ouabain and 8-Bromo-cAMP ($0.5{\mu}mol/L$) markedly increased atrial ET-1 secretion, which was blocked by H-89 and by PD98059 ($30{\mu}mol/L$), an inhibitor of extracellular-signal-regulated kinase (ERK) without changing ouabain-induced atrial dynamics. Our results demonstrated that ouabain increases atrial cAMP levels and promotes atrial ET-1 secretion via the mitogen-activated protein kinase (MAPK)/ERK signaling pathway. These findings may explain the development of cardiac hypertrophy in response to digitalis-like compounds.