• 대한화학회지
• /
• 제45권4호
• /
• pp.312-317
• /
• 2001

7'-Aldehyde-nucleoside 유사체(2a, 2c)을 6-N-benzoyl-2',3'-O-isopropylideneadenosiner과 uridine으로부터 합성하였다. 2와 Wittig reagent인 ethoxycarbonylmethylene을 축합시켜 ethoxycarbonyl group을 갖는 탄소수를 증가시킨 공액 이중 결합을 지닌 nucleosi de 유사체, ethyl-1',5',6',7',8'-pentadeoxy-1'-(adenin-9-yl)-$\beta$-D-ribo-nnona-5'(E).7'(E)-dienofuranuronate(4b), ethyl-1',5',6',7',8'-pentadeoxy-1'-(uracyl-1-yl)-$\beta$-D-ribo-nona-5'(E),7'(E)-dienofuranuronate(4c)을 얻었다. 또한 2와 CBr4, Ph3P을 반응시켜 공액 이중 결합을 지닌 9-[8',8'-dibromo-5',6',7',8'-tetradeoxy-$\beta$-D-ribo-octa-5'(E),7'(E)-diene]nucleosides (6b,6c) 유사체를 각각 합성하였다.

• 대한약리학회지
• /
• 제29권1호
• /
• pp.97-105
• /
• 1993

흰쥐의 지방세포에 존재하는 아데노신 수용체는 $A_{1}$, subclass로 알려져 있다. 따라서 효현제 (Agonist)에 의해 자극되면 adenylyl cyclase가 억제되고 결과적으로 지방분해가 억제된다. 본 연구에서는 당뇨병으로 인하여 생기는 쥐의 지방세포의 $A_{1]$, 아데노신 수용체-adenylyl cyclase 시스템의 변화를 규명하고자 하였다. 흰쥐에 streptozotocin을 투여하여 당뇨병을 유발시킨 후 1주일이 되는 날, 굶기지 않은 쥐에 서 collagenase를 사용하여 지방세포를 분리하였다. 분리한 지방세포에 1 unit/ml adenosine deaminase와 $1\;{\mu}M$ isoproterenol을 가한 후 $37^{\circ}C$에서 1시간 동안 incubation하여 생성되는 glycerol을 측정하였을 때, 당뇨병군에서는 대조군에 비해 $A_{1}$, 아데노신 수용체의 효현제인 $(-)-N^{6}-(R-phenylisopropyl)$ adenosine (PIA)에 의해 지방분해가 약 두배 더 억제되었다. 그 기전을 밝히기 위하여 지방세포막의 $[{^3}H]PIA$ binding을 측정하였는데, 친화력이나 수용체의 수는 당뇨병군과 대조군 사이에 통계적으로 유의한 차이가 없었다 (대조군의 $K_{d}$는 $0.51{\pm}0.09\;nM$이었고 $B_{max}$는 $1.60{\pm}0.12\;pmoles/mg$ protein이었다. 당뇨병군의 $K_{d}$는 $0.54{\pm}0.21\;nM$이었고 $B_{max}$는 $1.72{\pm}10.31\;pmoles/mg$ protein이었다). 그러나 $100\;{\mu}M$ isoproterenol 자극에 의한 adenylyl cyclase activity의 PIA에 의한 억제를 비교하여 보았을 때 당뇨병군에서의 억제는 대조군의 1.9배로 나타났다. 이상의 결과로 보아 당뇨병군의 지방세포에 나타나는 변화, 즉 지방 분해가 PIA와 같은 $A_{1}$, 아데노신 수용체의 효현제에 의해 더욱 억제되는 것은 지방세포막의 수용체 자체의 변화때문이 아니라 수용체 이후의 신호전달 체계의 변화때문인 것으로 생각된다.

• 생약학회지
• /
• 제27권1호
• /
• pp.15-19
• /
• 1996

In the course of phytochemical studies of Chrysanthermi Flos(Chrysanthemum indicum L., Compositae), two compounds were isolated by repeated column chromatography. Compound 1 is identified as adenosine on the basis of spectroscopic means and comparison with an authentic standard. Compound 2 is determined to be a new alkyl alcohol glycoside, 1-octen-3-ol $3-O-{\beta}-D-xylopyranosyl(1{\rightarrow} 6)-{\beta}-D-glucopyranoside$ on the spectroscopic evidence. Compounds 1 and 2 are reported for the first time from this plant.

• Biomolecules & Therapeutics
• /
• 제8권4호
• /
• pp.325-331
• /
• 2000

The present study was designed to assess the role of spinal adenosine $A_2$ receptor in the regulation of cardiovascular functions such as mean arterial pressure (MAP) and heart rate (HR) in male Sprague-Dawley rats. Rats (250~300 g) were anesthetized with urethane and paralyzed with d-tubocurarine and artificially ventilated. blood pressure and HR were continuously monitored via a femoral catheter connected to a pressure transducer and a polygraph. Drugs were administered intrathecally using injection cannula through guide cannula which was inserted inthrathecally at lower thoracic level through a puncture of an atlantooccipital mombrane. Intrathecal injection of an adenosine $A_2$ receptor agonist, 5'-(N-cyclopropyl)-carboxamaidoadenosine (CPCA; 1, 2 and 3 nmol, respectively), produced a dose-dependent decrease in MAP and HR. Pretreatment with $N^{G}$-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor or 10 nmol of MDL-12,330, an adenylate cyclase inhibitor blocked significantly the depressor and bradycardic effect of 2 nmol of CPCA. But, Pretreatment with 3 nmol of bicuculline, gamma-aminobutyric acid A (GAB $A_{A}$) receptor antagonist, or 50 nmol of 5-aminovaleric acid, GAB $A_{B}$ receptor antagonist did not inhibit the depressor and bradycardic effect of 2 nmol of CPCA. These results indicate that adenosine $A_2$ receptor in the spinal cord plays an inhibitory role in the regulation of cardiovascular function and that the depressor and bradycardic action of adonosine $A_2$ receptor are mediated via the synthesis of nitric oxide and the activation of adenylate cyclase in the spinal cord of rats.s.s.s.

• 한국미생물생명공학회:학술대회논문집
• /
• 한국미생물생명공학회 1978년도 춘계학술대회
• /
• pp.97.5-98
• /
• 1978

By the treatment of various mutagens, a number of 5'-guanylic acidproducing from 5'-xanthylic acid were obtained from Brevibacterium ammoniagenes ATCC 6871. The indispensable genetic characters of the mutants were adenine requirement, lack of GMP-reductase and mutation to adenosine resistance from adenosine sensitiveness. Main product of these mutants from 5'-xanthylic acid was 5'-guanylic acid. The substance was isolated in a crystalline form the culture broth of BA 17-2, and identified as 5'-guanylic acid by means of paper chromatography, ultra violet, absorption spectra, and infra red spectrum.

• 한국미생물·생명공학회지
• /
• 제7권3호
• /
• pp.127-133
• /
• 1979

5'-GMP의 직접발효생산균주의 분리목적으로 Breuibacterium ammoniagenes ATCC 6871에 자외선조사 및 NTG, DES 등의 변이제처리를 한 결과 guanine계 핵산관련물질을 직접 배지중에 축적하는 변이주는 분리할 수 없었으며, adenine영양요구주로써 GMP-reductase가 결핍되고 adenosine 및 AMP에 의해 생육저해를 받지 않는 변이주가 XMP-aminase activity가 현저히 높았음을 알았다. 이러한 변이주중 BA-17-2가 XMP-aminase의 activity가 가장 높았으며 또한 전환된 5'-GMP를 GDP나 GTP로 거의 인산화하지 않았으며 그리고 guanosine이나 guanine으로 분해하지 않았다. 생성된 5'-GMP를 anion exchange resin Duolite 102 D를 사용하여 분리하고 ultraviolet 및 Infra-red spectrum을 조사한 결과 5'-GMP로 동정되었다.

• Journal of the Korean Wood Science and Technology
• /
• 제31권4호
• /
• pp.63-70
• /
• 2003

송이(Tricholoma matsutake) 자실체의 메탄올(methanol, MeOH) 추출물로부터 4개의 화합물을 분리하였으며, 기기분석 결과 adenosine (9-𝛽-D-ribofuranosyladenine)을 비롯하여, methyl trans-cinnamate, ergosterol (ergosta-5, 7, 22-triene-3𝛽-ol) 및 ergosta-4, 6, 8 (14), 22-tetraen-3-one으로 각각 동정하였다.

• 생명과학회지
• /
• 제20권3호
• /
• pp.453-456
• /
• 2010

백혈병은 조혈모세포의 비정상적인 증식에 의해 일어나서 질환이고, adenosine deaminase (ADA) 유전자는 백혈병의 약물 작용점으로 중요하다. 이러한 연구의 일환으로 한국인 백혈병 환자 20명의 ADA 유전자의 변이를 조사하기 위해 혈액 genomice DNA를 추출하여 염기서열을 결정하였다. 그 결과 nonsense 변이인 F101F 하나, missense 변이 E260K, D8Y 각각 하나, 그리고 외국에서는 보고되지 않은 것으로 정상인에서 IVS6-52 에 GC가 도입된 것을 확인하였다. 백혈병 환자와 유전자 변이간에 통계학적인 차이점은 없지만 이러한 연구는 앞으로 백혈병의 진단 마크 개발에 도움이 될 것으로 사료된다.

• Korean Journal of Anesthesiology
• /
• 제71권6호
• /
• pp.476-482
• /
• 2018

Background: Several types of receptors are found at neuromuscular presynaptic membranes. Presynaptic inhibitory $A_1$ and facilitatory $A_{2A}$ receptors mediate different modulatory functions on acetylcholine release. This study investigated whether adenosine $A_1$ receptor agonist contributes to the first twitch tension (T1) of train-of-four (TOF) stimulation depression and TOF fade during rocuronium-induced neuromuscular blockade, and sugammadex-induced recovery. Methods: Phrenic nerve-diaphragm tissues were obtained from 30 adult Sprague-Dawley rats. Each tissue specimen was randomly allocated to either control group or 2-chloroadenosine (CADO, $10{\mu}M$) group. One hour of reaction time was allowed before initiating main experimental data collection. Loading and boost doses of rocuronium were sequentially administered until > 95% depression of the T1 was achieved. After confirming that there was no T1 twitch tension response, 15 min of resting time was allowed, after which sugammadex was administered. Recovery profiles (T1, TOF ratio [TOFR], and recovery index) were collected for 1 h and compared between groups. Results: There were statistically significant differences on amount of rocuronium (actually used during experiment), TOFR changes during concentration-response of rocuronium (P = 0.04), and recovery profiles (P < 0.01) of CADO group comparing with the control group. However, at the initial phase of this experiment, dose-response of rocuronium in each group demonstrated no statistically significant differences (P = 0.12). Conclusions: The adenosine $A_1$ receptor agonist (CADO) influenced the TOFR and the recovery profile. After activating adenosine receptor, sugammadex-induced recovery from rocuronium-induced neuromuscular block was delayed.

• Journal of Applied Biological Chemistry
• /
• 제49권4호
• /
• pp.162-164
• /
• 2006

The roots of Codonopsis lanceolata afforded tangshenoside I(1) and $\beta$-adenosine (2) as $\alpha$-glucosidase inhibitors. Their structures were unambiguously determined by 1D and 2D NMR data including HMQC and HMBC experiments. Compounds 1 and 2 exhibited weak $\alpha$-glucosidase inhibitory activities in vitro with $IC_{50}$ of 1.4 and 9.3 mM, respectively.