• Biomolecules & Therapeutics
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• 제3권4호
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• pp.256-259
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• 1995

Antinociceptive and desensitizing effects of systemically administered capsaicinoids (capsaicin and KR25018) were investigated in guinea pig. Nociceptive sensitivity to chemical stimulus was examined to test sensory function, and the content of substance P-like immunorractivity (SP-LI) in bronchi was determined as a peripheral marker of capsaicin-sensitive primary afferent neurons. Guinea pigs were pretreated s.c. with several doses of capsaicin (1,2.5,5, 10 mg/kg) or KR25018 (1, 2.5, 5, 10 mg/kg) one week prior to the experiments. Frequency of eye wiping was significantly decreased by capsaicin and KR25018 in a pretreatment dosedependent manner. In capsaicin- or KR25018-pretreated guinea pigs, there was a significant loss of SP-LI in bronchial tissue extracts. In summary, a newly synthesized capsaicin analogue H725018 exhibited antinociceptive effect against chemical stimulus in guinea pig, with comparable potency to capsaicin. This desensitizing activity of capsaicin or KR25018 might be related to the loss of SP-LI in peripheral afferent nerves.

• 미생물학회지
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• 제49권4호
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• pp.369-376
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• 2013

인삼 근계(근권, 근면, 근내부)로부터 ginsenoside Rb1 전환효소인 ${\beta}$-glucosidase 생산 균주(BGB)를 분리하였다. 인삼 근계부터 분리된 BGB 28균주의 계통학적 특성을 확인한 결과, 근권에서 Stenotrophomonas 속(3균주), Pseudoxanthomonas 속(1균주), Bacillus 속(1균주)로 확인되었다. 근면로부터 분리된 BGB는 Stenotrophomonas 속(16균주), Streptomyces 속(1균주), Microbacterium 속(1균주)이며, 근내부는 Stenotrophomonas 속(3균주), Lysobacter 속(2균주)를 포함하는 다양한 계통군이 확인 되었다. 특히 인삼 근계로부터 분리된 BGB 균주의 90%가 Stenotrophomonas 계통군에 속하는 특징을 나타내었다. 근권으로부터 분리된 4KR4 균주는 108.17 unit의 ${\beta}$-glucosidase 활성을 나타내었으며, ginsenoside Rb1을 Rd, Rg3 그리고 minor ginsenoside Rh2로 전환되었다. 4KR4 균주는 Stenotrophomonas rhizophila e-$p10^T$ (AJ293463)와 99.65%의 높은 상동성을 나타내었다. 본 연구에서 분리된 ginsenoside 전환세균 4KR4 균주의 계통학적 위치와 표현형적 특징, 균체 지방산조성, 생리 생화학적 특성을 검토한 결과, Stenotrophomonas sp. 4KR4 (=KACC 17635) 균주로 확인되었다.

• 한국토양비료학회지
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• 제50권3호
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• pp.135-149
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• 2017

In order to obtain promising rice growth-promoting microbial strains that can be used as substitutes for chemical fertilizers, 172 bacterial strains were isolated from rice roots grown in Korean and Russian soils. Out of them, the strains KR076, KR083, KR181 and RRj228 showed plant growth-promoting activities on maize seedlings. Bacillus megaterium KR076 and Bacillus sp. KR083 showed both nitrogen-fixing and plant growth-promoting activities, while Rhizobium sp. KR181 and Pseudomonas sp. RRj228 appeared to support only plant growth-promotion, but not $N_2$ fixation. Especially, RRj228 showed high growth promoting activity at low concentrations. Inoculation studies with KR083 and RRj228 revealed a high affinity to the Japonica rice variety such as Junambyeo than the Korean Tongil type variety such as Arumbyeo. Both KR083 and RRj228 strains showed rhizoplane and/or endophytic colonization in Japonica and Tongil types rice when soaked with the bacterial suspension of $1.1{\times}10^5cfu\;ml^{-1}$ for six and twelve hours. However, the total bacterial cell numbers were higher in the roots of Japonica variety than in the Tongil type. In inoculation trials with Daesanbyeo rice variety, the seedlings inoculated with KR181 and RRj228 at the rate of $2.0{\times}10^6cfu\;ml^{-1}$ showed yield increment of 35% and 33% (p < 0.01), respectively, so that they contributed to the replacement of chemical fertilizer at half doses of N, $P_2O_5$, and $K_2O$ in pots. In Junambyeo rice seedlings, the strain RRj228, when inoculated with a cell suspension of $1.8{\times}10^6cfu\;ml^{-1}$, promoted 3.4% higher yield at 70% dose than at a full dose level of N $110kg\;ha^{-1}$ in field. These results suggest that the rhizobacteria KR181 and RRj228 are prospective strains for enhancing rice performance.

• 한국식품과학회지
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• 제44권2호
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• pp.196-201
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• 2012

본 연구에서는 청국장 및 볏짚에서 분리한 미생물중 decarboxylase 배지에서 탈탄산효소 활성이 낮은 균주로 $B.$ $subtilis$ HH12, $B.$ $subtilis$ HR254, $P.$ $barcinonensis$ KR97을 선발하였다. 이들 선발 미생물들의 histidine decarboxylase($hdc$) gene 과 tyrosine decarboxylase($tdc$) gene을 조사한 결과, $hdc$ gene은 HH12, HR254, KR97 균주에서는 검출되지 않았으나, $tdc$ gene은 HH12, HR254, KR110 균주에서 검출되었다. 또한 HPLC를 통해 선발 균주들의 배양상등액 중 amines 생성량을 분석한 결과, HH12, HR254, KR110 균주는 histamine이 검출되지 않았고 tyramine은 HH12, HR254, KR110 균주는 각각 6.09, 3.68, 6.30 mg/L로 검출되었다. 선발한 biogenic amines 저감화 균주들의 BAs 생성량을 decarboxylase 고생산 미생물로 사료되는 $B.$ $subtilis$ MC138 균주와 비교해보면 현저히 낮은 수준으로 나타났다.

• 한국전기전자재료학회:학술대회논문집
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• 한국전기전자재료학회 2009년도 추계학술대회 논문집
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• pp.154-154
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• 2009

본 연구는 고전압 전력기기인 몰드형변압기와 계기용 변성기인 CT, PT 절연특성에 유용한 Epoxy/Nano-Micro Mixture Composites(이하,ENMMC)를 개발하기위해 무엇보다 중요한 것은 Nano입자인 $SiO_2$_10nm입자의 표면을 제어하여 즉, 표면의 소수성을 크게 하여 나노입자의 균질한 분산을 얻은것이 무엇보다 중요하다. 개발된 Epoxy/$SiO_2$_10nm Nanocomposites와 Microcomposites을 기계적 전단응력을 이용하여 균질 혼합을 실시하였다. 이런 조건을 이용한 전기적특성을 측정하기위해 구대구 전극이 완전함침된 평등전계하에서 절연파괴전압을 측정하기 시편을 제조하였다. 마이크로입자의 충진함량을 일정하게 유지하여 나노입자 충진함량비율을 4가지로 변화시켜 절연파괴특성을 연구하였다. 충진함량이 나노입자의 경우 1wt%이하의 값이 상대적으로 우수한 절연파괴특성으로 와이블 플롯을 통하여 알수있었다. 상대적으로 멀티나노콤포지트의 형상파라미터가 큰 결과값을 얻을수 있었다. 그리고 스케일파리미터는 누적확률 밀도함수로서 63.2%에서 대단히 큰 초절연성의 절연소재를 개발할수 있었다.

• Biomolecules & Therapeutics
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• 제12권4호
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• pp.215-220
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• 2004

In an attempt to develop new anti-diabetic agents, a series of aryloxypropanolamine derivatives was synthesized to serve as ${\beta}_3$ adrenoceptor agonists. Among these derivatives, 1-{1-methyl-3-[4-(2-methyl-2H-1,2,3,4-tetrazol-5-yl)phenyl]propylamino}-3-phenoxy-2-propanol (KR60886) possessed a high affinity for the ${\beta}_3$ adrenoceptor (Ki = 28 nM) and moderate affinities for ${\beta}_1$ and ${\beta}_2$ adrenoceptors (Ki = 95 nM and 100 nM, respectively). In addition, KR60886 stimulated cAMP production with an EC$_{50}$ of 0.4 ${\mu}M$, confirming its agonistic activity for the ${\beta}_3$ adrenoceptor. In vivo activities of KR60886 were examined by using a fat-fed/streptozotocin (STZ)-treated rat model and the ob/ob mouse model. Oral administration of KR60886 (10 mg/kg) for 3 days (b.i.d.) to fat-fed/STZ-treated rats significantly lowered plasma glucose levels and reduced plasma free fatty acid concentrations. Similarly, KR60886 treatment (10 mg/kg/day for 7 d) resulted in a reduction of plasma glucose concentrations in ob/ob mice. The present study suggests that KR60886 is a potent ${\beta}_3$ receptor agonist with in vivo anti-diabetic properties.

• Biomolecules & Therapeutics
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• 제13권1호
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• pp.20-25
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• 2005

The present study was performed to evaluate antiarrhythmic effects of KR-32570, a novel inhibitor of sodium hydrogen exchanger subtype-1 (NHE-1), in rat arrhythmia induced by focal ischemia and reperfusion. During ischemia, KR-32570 significantly decreased the number of premature ventricular contraction (PVC) from 152.0 times to 75.5, 52.4 and 20.0 times for 0.1, 0.3 and 1.0 mg/kg, respectively (p<0.05) and the duration of ventricular tachycardia (VT) from 88.1 s to 35.8, 7.7 and 1.3 s, respectively(p<0.05) in anesthetized rats subjected to 10-min coronary occlusion of coronary artery. Similarlt to ischemia-induced arrhythmia, KR-32570 significantly decreased reperfusion-induced arrhythmia including PVC (41.3, 21.5, 11.3 and 6.6 times at vehicle, 0.1, 0.3 and 1.0 mg/kg, respectively, p<0.05) and VT (100.5, 64.2, 25.8 and 25.2 s, respectively, p<0.05), and VF (86.9, 27.5, 6.9 and 0 s, respectively, p<0.05). Moreover, KR-32570 dose-dependently decreased the incidence of mortality occurring after reperfusion (41, 27, 18 and 0% at vehicle, 0.1, 0.3, 1.0 mg/kg, respectively). These results suggest that KR-32570 has a potent antiarrhythmic effect in rat arrhythmia induced by ischemia and reperfusion.

• 한국응용곤충학회지
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• 제10권2호
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• pp.117-120
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• 1971

이화명충의 유충, 번데기, 성충에 $Co^{60}$ gamma ray를 조사하여 웅성불임기술에 관한 자료를 얻기위한 실험결과를 요약하면 다음과 같다. 1) 번데기의 성비는 암컷 2,903에 대해 숫컷은 2,924이었다. 2) 번데기의 $(LD_{50})$은 암컷이 26KR, 숫컷이 26.7KR이었다. 3) 처리한 숫컷성충과 교미한 암컷의 평균 산란수는 고선량일수록 감소하며 난괴수는 증가하였다. 4) 숫컷의 $(SD_{90})$은 23KR이었으며 30KR 이상에서는 거이 불임이 유기되었다. 5) 웅성불임을 유기 시키기 위하여 방사선을 조사시키는 시기는 번데기 시기가(3-6일령) 가장 적합하다고 본다

• BMB Reports
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• 제40권6호
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• pp.952-958
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• 2007

We isolated many genes induced from pepper cDNA microarray data following their infection with the soybean pustule pathogen Xanthomonas axonopodis pv. glycines 8ra. A full-length cDNA clone of the Capsicum annuum ankyrin-repeat domain $C_3H_1$ zinc finger protein (CaKR1) was identified in a chili pepper using the expressed sequence tag (EST) database. The deduced amino acid sequence of CaKR1 showed a significant sequence similarity (46%) to the ankyrin-repeat protein in very diverse family of proteins of Arabidopsis. The gene was induced in response to various biotic and abiotic stresses in the pepper leaves, as well as by an incompatible pathogen, such as salicylic acid (SA) and ethephon. CaKR1 expression was highest in the root and flower, and its expression was induced by treatment with agents such as NaCl and methyl viologen, as well as by cold stresses. These results showed that CaKR1 fusion with soluble, modified green fluorescent protein (smGFP) was localized to the cytosol in Arabidopsis protoplasts, suggesting that CaKR1 might be involved in responses to both biotic and abiotic stresses in pepper plants.

• Biomolecules & Therapeutics
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• 제28권5호
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• pp.482-489
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• 2020

G protein-coupled receptor kinase 5 (GRK5) has been considered as a potential target for the treatment of heart failure as it has been reported to be an important regulator of pathological cardiac hypertrophy. To discover novel scaffolds that selectively inhibit GRK5, we have identified a novel small molecule inhibitor of GRK5, KR-39038 [7-((3-((4-((3-aminopropyl)amino)butyl)amino)propyl)amino)-2-(2-chlorophenyl)-6-fluoroquinazolin-4(3H)-one]. KR-39038 exhibited potent inhibitory activity (IC₅₀ value=0.02 µM) against GRK5 and significantly inhibited angiotensin II-induced cellular hypertrophy and HDAC5 phosphorylation in neonatal cardiomyocytes. In the pressure overload-induced cardiac hypertrophy mouse model, the daily oral administration of KR-39038 (30 mg/kg) for 14 days showed a 43% reduction in the left ventricular weight. Besides, KR-39038 treatment (10 and 30 mg/kg/day, p.o.) showed significant preservation of cardiac function and attenuation of myocardial remodeling in a rat model of chronic heart failure following coronary artery ligation. These results suggest that potent GRK5 inhibitor could effectively attenuate both cardiac hypertrophy and dysfunction in experimental heart failure, and KR-39038 may be useful as an effective GRK5 inhibitor for pharmaceutical applications.