• Bulletin of the Korean Chemical Society
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• 제1권4호
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• pp.126-131
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• 1980

Seventeen new $N^{6}$-aminoalkyl derivatives of 5'-adenylic acid and adenosine 5'-triphosphate (Compound I-XVII) were synthesized from 6-chloropurine ribonucleoside by reaction with appropriate diamines. This paper discusses the procedure of synthesis and the identification of the derivatives by ultraviolet spectra, high voltage electrophoresis, paper chromatography, elemental analyses, and other chemical methods.

• 대한수의학회지
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• 제27권2호
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• pp.201-206
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• 1987

This study was carried out to investigate the action of ATP, which has been known as the neurotransmitter of noncholinergic- and nonadrenergic-nerve, on the motility of immature pig uterine smooth muscle. The results were summarized as follows; 1. The contraction and the contractile responses caused by ATP were increased in a dose-dependent manner between the concentration of ATP $10^{-6}M$ and $10^{-3}M$. The maximal contractile effect was appeared at the concentration of ATP $10^{-3}M$ and it was 70.2% of 100mM K contraction. 2. The contractile responses induced by ATP ($10^{-4}M$) were not blocked by the pretreatment with cholinergic receptor blocker, atropine ($10^{-6}M$). 3. The contractile responses induced by ATP ($10^{-4}M$) were not blocked by pretreatment with ${\alpha}$-adrenergic receptor blocker, phentolamine ($10^{-6}M$) and ${\beta}$-adrenergic receptor blocker, propranolol ($10^{-6}M$). 4. The contractile response induced by ATP ($10^{-4}M$) was not blocked by the pretreatment with $H_1-receptor$ blocker, pyrilamine ($10^{-6}M$) and $H_2-receptor$ blocker, cimetidine ($10^{-6}M$).

• 한국가축번식학회지
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• 제20권4호
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• pp.395-412
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• 1997

포유동물의 난자는 제 2 감수분열 중기에서 배란되어 수정된다. 일반적으로 포유동물에서의 수정은 inositol triphosphate (IP3) 또는 cyclic adenosine diphosphoribose (cADPr)에 의해 조절되어지는 세포질내 칼슘변화에 의해 일어난다. 난활성이 일어나면 세포질내 고농도의 MPF (maturation promotion factor)는 감소하고, 전핵이 형성되고, cytoskeleton이 재구성되고, 단백질합성이 조절되어진다. 이러한 모든 과정이 정상적으로 일어난 후 수정란은 종특이한 발달경로로 배발달을 시작한다. 본 논문에서는 돼지난자의 인위적인 난활성 유도방법에 대해서 설명하고자 한다. 신호전달(signal transduction) 경로에 의한 하나의 기전이 돼지난자에서 확인되었는데, 이 경로의 자극은 난활성으로 이루어진다. 또한 전기자극에 의한 난활성방법에 의해 12일까지 정상배 발달이 이루어진다고 보고되고 있다. 향후 연구에서는 정자가 어떠한 기전에 의해서 배발달을 시작하게 하는지를 밝혀내야 한다고 본다.

• 전기화학회지
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• 제15권4호
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• pp.249-255
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• 2012

크레아티닌 센서의 생체시료 측정 시 가장 심각한 방해 작용을 발생하는 물질인 크레아틴을 효과적으로 제거하기 위하여 creatine kinase와 adenosine triphosphate를 사용한 두 번째 효소층을 도입하여 크레아틴에 대한 방해작용을 현저히 감소시켰다. 또한 평면형 소형 크레아티닌 센서를 개발하기 위해 탄소전극 표면에 Pt black(Pt-B)을 도입하여 표면적을 증가시킴으로써 전기화학적 감응 특성을 증가시킨 스크린 프린팅 방식의 Pt-B/C 전극을 제작하였다. 최적화된 소형 크레아티닌 센서를 흐름계 카트리지에 장착하여 미지시료를 측정한 결과 5% 이내의 오차 범위 내에서 우수한 측정 정확성과 재현성을 보임을 확인하였다.

• 대한의생명과학회지
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• 제20권2호
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• pp.70-76
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• 2014

In this study, we investigated the effect of DMSO, a highly dipolar organic liquid, in collagen ($5{\mu}g/ml$)-stimulated platelet aggregation. DMSO inhibited platelet aggregation at 0.5% by inhibiting production of thromboxane $A_2$ ($TXA_2$) which was associated with blocking cyclooxygenase (COX)-1 activity and $TXA_2$ synthase. In addition, DMSO significantly increased the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP) and cyclic guanosine monophosphate (cGMP) from guanosine triphosphate (GTP). On the other hand, DMSO (0.1~0.5% concentration) did not affect the LDH release which indicates the cytotoxicity. Based on these results, DMSO has anti-platelet effect by regulation of several platelet signaling pathways, therefore we suggest that DMSO could be a novel strategy on many thrombotic disorders.

• Journal of Applied Biological Chemistry
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• 제62권4호
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• pp.425-431
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• 2019

Platelet activation is essential for hemostatic process on blood vessel damage. However, excessive platelet activation can cause some cardiovascular diseases including atherosclerosis, thrombosis, and myocardial infarction. Scoparone is commonly encountered in the roots of genus Artemisia or Scopolia, and has been studied for its potential pharmacological properties including immunosuppression and vasorelaxation, but antiplatelet effects of scoparone have not been reported yet. We investigated the effect of scoparone on human platelet activation prompted by an analogue of thromboxane A₂, U46619. As the results, scoparone dose-dependently increased cyclic adenosine monophosphate (cAMP) levels as well as cyclic guanosine monophosphate (cGMP) levels, both being aggregation-inhibiting molecules. In addition, scoparone strongly phosphorylated inositol 1, 4, 5-triphosphate receptor (IP3R) and vasodilator-stimulated phosphoprotein (VASP), substrates of cAMP dependent kinase and cGMP dependent kinase. Phosphorylation of IP₃R by scoparone resulted in inhibition of Ca²⁺ mobilization in calcium channels in a dense tubular system, and phosphorylation of VASP by scoparone led to an inability of fibrinogen being able to bind to αIIb/β3. Finally, scoparone inhibited thrombin-induced fibrin clotting, thereby reducing thrombus formation. Therefore, we suggest that scoparone has a strong antiplatelet effect and is highly probable to prevent platelet-derived vascular disease.

• 한국식품영양과학회지
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• 제9권1호
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• pp.59-73
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• 1980

A detailed procedure was described for the isolation of cratine kinase (ATP-Creatine phosphotransferase, E. C. 2. 7. 3. 2.) from the muscle of the snake Bungarus fasciatus. The original isolation procedure of Kuby et al. for the rabbit muscle enzyme has been modified and extended to include a chromatographic step. The properties of the enzyme have been investigated and kinetic constants for the reverse reactions determined as the followings: 1) A molecular weight of the enzyme was determined by gel filteration on Sephadex G-100 and by electrophoresis on SDS-polyacrylamide was 86,000. 2) Two reactive sulphydryl groups were detected with dithiobis nitrobenzoic acid (DTNB). 3) The nucleotide substrate specificity in the reverse reaction was determined as ADP*2'-dADP＞GDP＞XDP＞UDP with magnesium as the activating metal ion. 4) The order of the metal specificity in the reverse reaction Mg>Mn>$Ca{\sim}Co$ was determined with ADP as substrate. 5) A detailed kinetic analysis was carried out in the reverse direction with $MaADP^-$ as the nucleotide substrate. Initial velocity and product inhibition studies($MaADP^{2-}$ competitive with respect to MgADP- and noncompetitive with respect to $N-phosphorycreatine^{2-}$ ; Creatine competitive with respect to $N-phosphorycreatine^{2-}$ and noncompetitive with respect to Ma $ADP^-)$ indicated that the reaction obeyed a sequential mechanism of the rapid equilibrium random type.

• Journal of Microbiology and Biotechnology
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• 제25권12호
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• pp.2034-2042
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• 2015

A one-pot process of enzymatic synthesis of deoxythymidine-5'-triphosphate (5'-dTTP) employing whole cells of recombinant Escherichia coli coexpressing thymidylate kinase (TMKase) and acetate kinase (ACKase) was developed. Genes tmk and ack from E. coli were cloned and inserted into pET28a(+), and then transduced into E. coli BL21 (DE3) to form recombinant strain pTA in which TMKase and ACKase were simultaneously overexpressed. It was found that the relative residual specific activities of TMKase and ACKase, in pTA pretreated with 20 mM ethylene diamine tetraacetic acid (EDTA) at 25℃ for 30 min, were 94% and 96%, respectively. The yield of 5'-dTTP reached above 94% from 5 mM deoxythymidine 5'-monophosphate (5'-dTMP) and 15 mM acetyl phosphate catalyzed with intact cells of pTA pretreated with EDTA. The process was so effective that only 0.125 mM adenosine-5'-triphosphate was sufficient to deliver the phosphate group from acetyl phosphate to dTMP and dTDP.

• 대한핵의학회지
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• 제32권3호
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• pp.250-258
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• 1998

목적 : ATP는 작용 시간이 빠르고 반감기가 짧은 효과적인 관상동맥 확장제로 알려져 있어 이를 심근관류 SPECT의 부하 약물로 사용 할 때에 부작용의 빈도와 안전성, 그 진단적 가치에 대해 알아 보고자하였다. 대상 및 방법: 관상동맥 질환이 의심되는 319명의 환자를 대상으로 ATP 부하(0.08 mg/kg/ min for 6min) T1-201 심근관류 SPECT를 실시하여 그 부작용을 조사하고 관상동맥 조영술과 비교하였다. 결과: 76.5%의 환자에서 부작용이 발생하였으나 일시적이고 경미하였으며, 모든 환자에서 ATP 주입을 끝낼 수 있었고 aminophylline이 필요했던 환자는 2명이었다. 관상동맥 조영술과 비교한 결과, 예민도 80%, 특이도 90% 였다. 결론: 6분간 0.08mg/kg/min의 ATP 주입 용량을 사용한 본 연구 결과에서 ATP 부하 심근관류 SPECT는 관상동맥 질환의 진단에서 adenosine이나 dipyridamole을 이용했을 때보다 부작용의 발생 빈도 및 부작용의 정도가 낮아 안전하게 사용될 수 있으며 진단 성능도 동등한 것으로 생각된다.

• Biomolecules & Therapeutics
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• 제8권4호
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• pp.338-348
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• 2000

The present study was attempted to determine the effect of 5'-(N'-ethylcarboxamido) adenosine (NECA), which is an potent $A_2$-adenosine receptor agonist, on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. NECA (20 nM) perfused into the adrenal vein for 60 min produced a time-related inhibition in CA secretion evoked by ACh (5.32x10$^{-3}$ M), high $K^{+}$(5.6x10$^{-2}$ M), DMPP (10$^{-4}$ M for 2 min), McN-A-343 (10$^{-4}$ M for 2 min), cyclopiazonic acid (10$^{-5}$ M for 4 min) and Bay-K-8644 (10$^{-5}$ M for 4 min). Also, in the presence of $\beta$,${\gamma}$-methylene adenosine-5'-triphosphate (MATP), which is also known to be a selective $P_{2x}$-purinergic receptor agonist, showed a similar inhibition elf CA release evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid. However, in adrenal glands preloaded with 20$\mu$M NECA for 20 min under the presence of 20$\mu$M 3-isobutyl-1-methyl-xanthine (IBMX), an adenosine receptors antagonist, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were much recovered in comparison to the case of NECA-treatment only. Taken together, these results indicate that NECA causes the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. This inhibitory effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells through the adenosine receptor stimulation. Therefore, it is suggested that the inhibitory mechanism of adenosine receptor stimulation may play a modulatory role in regulating CA secretion.n.n.