• Bulletin of the Korean Chemical Society
• /
• 제32권4호
• /
• pp.1146-1152
• /
• 2011

The discovery of 2'-spirocyclopropyl-ribocytidine (J. Med. Chem. 2010, 53, 8150-8160) as a potent inhibitor of RNA synthesis by NS5B ($IC_{50}=7.3{\mu}M$), the RNA polymerase encoded by hepatitis C Virus (HCV), has led to the synthesis and biological evaluation of several carbocyclic versions of 2'-spiropropyl-nucleosides. The cyclopentenol intermediate 7 was successfully constructed via ring-closing metathesis (RCM) from divinyl 6. Spirocyclopropanation of enone 8 was effected by using (2-chloroethyl)-dimethylsulfonium iodide and potassium tert-butoxide to form the desired intermediate 9. The synthesized nucleoside analogues 21-24 were assayed for their ability to inhibit HCV RNA replication in a subgenomic replicon Huh7 cell line. Among them, the cytosine nucleoside analogue 22 exhibited significant anti-HCV activity ($EC_{50}= 8.2{\mu}M$).

• 한국대기환경학회지
• /
• 제32권6호
• /
• pp.603-612
• /
• 2016

The objective of this study was to estimate the emission characteristics for PM, $PM_{10}$, and $PM_{2.5}$ in the various stationary sources. The particulate matters collected in the various stationary sources such as power plants (Coal and B-C oil), incinerators(municipal and industrial waste), and glass furnaces. The PM and $PM_{10}$, PM and $PM_{2.5}$, $PM_{10}$ and $PM_{2.5}$ samples were collected using the cyclone type $PM_{10}$, $PM_{2.5}$ samplers and 30 species(19 inorganic species, 9 ionic species, OC and EC) were analyzed by ICP, IC, and TOR/IMPROVE methods. The mass concentrations of PM, $PM_{10}$, $PM_{2.5}$ from nine stationary sources ranged $0.63{\sim}9.58mg/Sm^3$, $0.26{\sim}7.47mg/Sm^3$ and $0.13{\sim}6.34mg/Sm^3$, respectively. The level of $PM_{10}$, $PM_{2.5}$ portion in PM calculated 0.63~0.99, 0.38~0.94, respectively. In the case of emission trend for species, power plant showed high concentrations for Al, Mg, Na, Si, V and $SO_4{^{2-}}$, respectively. Also, Ca, Fe, K, Si, $Cl^-$, and $K^+$ showed high in incinerator. In the case of glass furnace, Na, Pb, K, Si, $Na^+$ and $SO_4{^{2-}}$ represented high concentrations. Power plant showed higher EC/OC concentrations than other sampling sites. These results suggest the possible role for complement establishment process of emission inventory and emission management for PM.

• 한국미생물·생명공학회지
• /
• 제22권4호
• /
• pp.333-339
• /
• 1994

In order to screen microorganisms producing phospholipase D (PLD) [EC 3.1.4.4], culture broths of about 900 strains of soil bacteria were subjected to examine for the PLD activity. When the hydrolytic activity of PLD (H-activity) in the supernatant was determined, 64 strains produced PLD more than 0.3 unit/ml and all of them were actinomycetes. Among 26 culture broths tested, 6 ones had transphosphatidylation activity (T-activity) of 30~68%. When the strains except one were cultivated on 3 different media at 30$\circ$C for 3 days under aerobic condition, strain # 1090 on medium B (yeast extract 1%, peptone 1%, glucose 1.5%, glycerol 1%, CaCO$_{3}$ 0.4%, and pH 7.2) produced PLD with much higher H- and T-activity, which were 8.3 units/ml and 76.3%, respectively. Subsequently, time course of PLD production of the strain # 1090 during cultivation with aeration of 1 v/v/m and agitation of 400 rpm at 30$\circ$C for 5 days on medium B in jar fermentor was investigated. H-activty of PLD reached almost maximum (about 9 units/ml) after 32 hours and maximal T-activity was found to be about 80%.

• 농약과학회지
• /
• 제4권4호
• /
• pp.72-76
• /
• 2000

아메리카잎굴파리 외부기생봉인 Hemiptarsenus sp.의 각 태별 크기와 온도에 따른 발육기간, 각 충태에 미치는 살충제의 영향을 조사하였다. 난은 길이가 0.5 mm, 폭 0.1 mm인 장타원형이며, 노숙유충, 용, 암컷과 수컷의 길이는 각각 1.9 mm, 2.0 mm, 2.2 mm, 1.8 mm 이었다 난에서 유충까지의 발육기간은 15, 20, 25, $30^{\circ}C$에서 각각 16.9일, 6.8일, 5.9일, 4.5일 이었으며, 용기간은 각각 20.7일, 9.7일, 5.6일, 3.4일로 온도가 증가함에 따라 발육기간은 짧아졌다. 발육영점온도와 유효적산온도는 난에서 유충이 $9.5^{\circ}C$, 91.5일도 용이 $13.1^{\circ}C$, 66.6일도 이었다. Hemiptarsenus sp.에 추천농도로 살충제를 처리하였을 때 비티 수화제, 주론 수화제, 싸이로마진 수화제는 각 충태에 대해 모두 독성이 낮았다. 반면에 피프로닐 액상수화제, 칼탑 수용제, 스피노사드 입상수화제는 유충과 용에는 독성이 낮았으나 성충에는 독성이 매우 강하였다. 아바멕틴은 각 충태에 비교적 독성이 낮았으나 성충의 산란수가 50% 이상 감소되어 성충 산란에 영향을 미치는 것으로 조사되었다.

• 한국미생물·생명공학회지
• /
• 제47권4호
• /
• pp.546-554
• /
• 2019

This study, for the first time, reports the functional expression of lipase B derived from the yeast Candida antarctica (CALB) in Corynebacterium strain using the Escherichia coli plasmid PK18. The CALB gene fragment encoding a 317-amino-acid protein was successfully obtained from the total RNA of C. antarctica. CALB was readily produced in the Corynebacterium strain without the use of induction methods described in previous studies. This demonstrated the extracellular production of CALB in the Corynebacterium strain. CALB produced in the Corynebacterium MB001 strain transformed with pEC-CALB recombinant plasmid exhibited maximum extracellular enzymatic activity and high substrate affinity. The optimal pH and temperature for the hydrolysis of 4-nitrophenyl laurate by CALB were 9.0 and 40℃, respectively. The enzyme was stable at pH 10.7 in the glycine-KOH buffer and functioned as an alkaline lipase. The CALB activity was inhibited in the presence of high concentration of Mg²⁺, which indicated that CALB is not a metalloenzyme. These properties are key for the industrial application of the enzyme.

• Elastomers and Composites
• /
• 제46권4호
• /
• pp.343-351
• /
• 2011

유기나노점토와 인화합물을 함유한 우레탄폼 복합체를 합성하고, 폼 생성속도, 밀도, 몰포로지, 열적특성 분석을 수행하였다. 우레탄폼 복합체는 Cloisite 30B가 박리/분산된 폴리아디페이트디올과 폴리에테르-폴리올(f=4.6), PMDI(f=2.5), D-580(phenyl polyoxyalkenyl phosphate)로부터 제조하였다. 발포제로써 cyclopentane과 증류수가 우레탄폼 복합체의 특성에 미치는 영향을 D-580의 농도 0~2.9 wt%에서 측정하였다. 증류수는 cyclopentane 보다 약 30% 빠르게 폼을 형성시켰다. 증류수로 발포한 우레탄폼 복합체의 밀도는 cyclopentane으로 발포한 경우보다 32~34% 낮았다. 증류수로 발포한 우레탄폼 복합체의 cell은 타원형인 반면에, cyclopentane으로 발포한 복합체는 구형의 형상이며, D-580의 함량이 증가함에 따라 cell 직경이 $158{\mu}m$에서 $100{\mu}m$로 감소하였다. Cyclopentane 으로 발포한 우레탄폼 복합체의 $T_g$는 D-580 함량이 증가함에 따라 $77.6^{\circ}C$에서 $56.1^{\circ}C$로 낮아졌다. 증류수로 발포한 우레탄 복합체의 $T_g$는 D-580 함량이 증가함에 따라 높아졌다. Cyclopentane과 증류수로 발포한 우레탄폼 복합체는 모두 $250^{\circ}C$에서 열분해가 시작하였다. Cyclopentane로 발포한 우레탄폼 복합체는 $500^{\circ}C$ 이상에서 열분해속도가 증가하는 2차 열분해 현상이 측정되었다. D-580에 의한 열안정성의 개선 정도는 cyclopentane으로 발포한 복합체에 비하여 증류수로 발포한 우레탄 복합체에서 더 높게 측정되었다.

• Bulletin of the Korean Chemical Society
• /
• 제35권8호
• /
• pp.2361-2366
• /
• 2014

A new aliphatic acid amide, ZP-amide F (1), and eight known compounds, including bungeanumamide A (2), tumuramide C (3), ZP-amide A (4), ZP-amide B (5), ZP-amide D (6), hyperin (7), quercitrin (8), and (-)-sesamin (9), were isolated from pericarps of Zanthoxylum piperitum. The effects of these compounds on $TNF{\alpha}$-induced NF-${\kappa}B$ activation and transactivational activity of PPARs, including $PPAR{\alpha}$, $PPAR{\beta}({\delta})$ and $PPAR{\gamma}$ subtypes, were evaluated. Compounds 7 and 9 exhibited potent inhibitory effects on $TNF{\alpha}$-induced NF-${\kappa}B$ activation with $IC_{50}$ values of 5.50 and $8.10{\mu}M$, respectively. Aliphatic acid amide compounds 3, 4 and 6 displayed enhanced effects on PPAR transactivational activity with $EC_{50}$ values of 47.12, 19.13 and $12.02{\mu}M$, respectively. Among them, compound 4 demonstrated an increase in $PPAR{\alpha}$ transactivational activity, compound 3 showed a moderate increase on all PPAR subtypes, whereas compound 6 displayed weak PPAR transactivational activity.

• 한국미생물·생명공학회지
• /
• 제26권5호
• /
• pp.420-426
• /
• 1998

Glutamic acid의 분해능이 뛰어난 aminopeptidase를 생산하는 세균을 토양으로부터 분리하였다. 이 균은 형태적 생리적 특성으로부터 Bacillus licheniformis로 동정되었다. 이 균을 최적 배지에 접종하고 37$^{\circ}C$에서 진탕배양한 후 균이 생산한 aminopeptidase를 ammonium sulfate 침전, Phenyl Sepharose CL-4B, Resource Q, Superose 12HR column을 통해 분리하여서 20.6%의 수율로 17.6배 정제된 glutamyl p-nitroanilide을 기질로 했을 때 9.2unit/mg의 순수효소를 얻었다. SDS-PAGE와 Native-PAGE로 부터 이 효소의 분자량이 42,000Da와 22,000Da으로 구성된 헤테로다이커로 약 64,000Da임이 밝혀졌고 효소의 등전점은 5.2로 나타났다. 이 효소의 반응 최적 온도는 55$^{\circ}C$, 반응최적 pH는 8.0이었고, EDTA와 1,10-phenanthroline에 의해서 효소활성이 저해되는 metalloenzyme으로 판명되었다.

• 한국가축번식학회지
• /
• 제21권1호
• /
• pp.71-78
• /
• 1997

본 연구는 체외성숙 직후의 소 미수정란의 활성화 조건을 검토하기 위하여 실시하였다. 체외에서 22~24시간 성숙배양된 소 미수정란을 다양한 활성화 조건으로 처리하였다. 실험 1에서는 성숙직후 난자를 전기자극(1.25kV/cm, 70$\mu$sec$\times$2회), 에탄올(7%, 5분), Ca2+-ionophore(A23187; 10$\mu$M, 5분) 및 cycloheximide(10$\mu\textrm{g}$/ml, 6시간)로 각각 처리하였다. 활성화율은 전기자극, 에탄올 및 A23187 처리시 48.8~54.3%로 비슷하였으나, cycloheximide처리시는 15.9%로 유의적으로(P<0.05) 낮았고, 무처리구인 대조군은 전혀 활성화 되지 않았다. 실험 2에서 체외성숙 미수정란을 전기자극, 에탄올 및 A23187중 2개 또는 3개를 병용처리한 결과, 활성화율은 46.9~63.5%로 나타났다. 실험 3에서는 전기자극, 에탄올 또는 A23187과 cycloheximide를 병용처리한 결과, 대부분의 난자(98.0~100%)가 활성화되었다. 실험 4에서는 실험 3과 같은 조건으로 처리하여 할성화된 난자를 cytochalasin B로 처리하여 2배체배 형성을 유도한 후 체외배양하여 발육율을 검사하였다. 분할율은 79.8~90.4%였으며, 배반포 발육율은 32.1~42.6%로 나타났다. 이러한 결과는 전기자극, 에탄올 또는 A23187과 chcloheximide의 병용처리가 성숙직후 소 미수정란의 활성화에 효과적임을 확증한다.

• Asian Pacific Journal of Cancer Prevention
• /
• 제16권18호
• /
• pp.8227-8233
• /
• 2016

Background: To investigate polymorphisms in heat shock proteins A1B and A1L (HOM) and associated risk of oesophageal carcinoma in Northeast India. Materials and Methods: The study includes oesophageal cancer (ECA) patients attending general outpatient department (OPD) and endoscopic unit of Gauhati Medical College. Patients were diagnosed based on endoscopic and histopathological findings. Genomic DNA was typed for HSPA1B1267 and HSPA1L2437 SNPs using the polymerase chain reaction with restriction fragment length polymorphisms. Results: A total of 78 cases and 100 age-sex matched healthy controls were included in the study with a male: female ratio of 5:3 and a mean age of $61.4{\pm}8.5years$. Clinico-pathological evaluation showed 84% had squamous cell carcinoma and 16% were adenocarcinoma. Dysphagia grades 4 (43.5%) and 5 (37.1%) were observed by endoscopic and hispathological evaluation. The frequency of genomic variation of A1B from wild type A/A to heterozygous A/G and mutant G/G showed a positive association [chi sq=19.9, p=<0.05] and the allelic frequency also showed a significant correlation [chi sq=10.3, with cases vs. controls, OR=0.32, $p{\leq}0.05$]. The genomic variation of A1L from wild T/T to heterozygous T/C and mutant C/C were found positively associated [chi sq=7.02, p<0.05] with development of ECA. While analyzing the allelic frequency, there was no significant association [chi sq=3.19, OR=0.49, p=0.07]. Among all the risk factors, betel quid [OR=9.79, Chi square=35.0, p<0.05], tobacco [OR=2.95, chi square=10.6, p<0.05], smoking [OR=3.23, chi square=10.1, p<0.05] demonstrated significant differences between consumers vs. non consumers regarding EC development. Alcohol did not show any significant association [OR=1.34, chi square=0.69, p=0.4] independently. Conclusions: It can be concluded that the present study provides marked evidence that polymorphisms of HSP70 A1B and HSP70 A1L genes are associated with the development of ECA in a population in Northeast India, A1B having a stronger influence. Betel quid consumption was found to be a highly significant risk factor, followed by smoking and tobacco chewing. Although alcohol was not a potent risk factor independently, alcohol consumption along with tobacco, smoking and betel nut was found to contribute to development of ECA.