• Journal of Pharmaceutical Investigation
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• 제31권1호
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• pp.27-35
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• 2001

To evaluate the site-specific permeation of aspalatone (acetylsalicylic acid maltol ester, AM) through gastrointestinal tract, the enzymatic degradation and permeation studies were carried out using gastric, duodenal and jejunal mucosae of rabbits. It was found that $15.2{\pm}11.4%$, $11.6{\pm}5.2$ and $0.8{\pm}0.6%$ of the donor dose of AM, salicylmaltol (SM) and aspirin (ASA) permeated through the upper gastric mucosa after 8 hr of permeation, respectively. After 8 hr of AM permeation, SM and ASA were measured to be $15.0{\pm}1.7$ and $2.6{\pm}0.8%$ of the dose in the donor solutions, respectively, and salicylic acid (SA) was not detected even after 6 hr, suggesting a very low gastric damage. For the gastric mucosa, the increase of donor dose from 100 to $1,000\;{\mu}g/ml$ increased the permeation flux dose-dependently (r=0.9905). For the duodenal and jejunal mucosae, however, AM was fully degraded into SM and SA due to the esterase activities within 30 min. AM and ASA were not detected in the receptor solution. This result indicates that AM is not a prodrug of ASA. Addition of potassium fluoride (0.5%) into the donor solution delayed the degradation of AM, but did not allow the permeation through duodenal mucosa even by the inhibition of esterase activity. The addition of $dimethyl-{\beta}-cyclodextrin$ and $2-hydroxypropyl-{\beta}-cyclodextrin$ (5%) into the donor solutions also did not show favorable effects on the permeation of AM through various mucosae. In comparison of permeation rates of AM and ASA through the upper gastric mucosa, the flux of ASA was 4.2 times faster than AM based on the molar concentration. ASA also was fully degraded in the donor solutions faced with duodenal and jejunal mucosae within 2 hr, and was not detected in the receptor solution, suggesting a slower metabolism compared with AM.

• 한국식품영양과학회지
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• 제26권4호
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• pp.743-750
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• 1997

세포막에서의 지방산 이동은 매우 빠르게 일어나므로 방사성 원소를 사용해서는 여러가지 단점이 있고, 정확한 이동속도 측정에도 어려움이 많았다 최근에 개발된 FRET assay는 형광성 물질과 형광성 물질을 상쇄시키는 quencher를 사용한 실험방법 이다. 이는 공명 에너지 이동의 원리를 이용한 것으로 형광광도계, stopped-flow장치를 사용하여 소수성 물질 이동을 직접 컴퓨터 모니터로 측정하는 방법으로 기존방법의 단점을 보완하였다. Donor막에는 형광성 표지를 붙인 지방산이 들어 있고 acceptor막에는 형광을 흡수하는 물질이 들어 있어서 형광성 지방산이 donor에서 acceptor로 이동하면 형광도가 감소하며, 시간에 따른 형광도 감소를 측정하여 지방산 이동속도를 측정하는 방법이다. 형광성 표지를 이용하여 소수성 물질 이동에 사용되는 또 다른 방법은 self-Quenching assay이다. 형광 물질의 농도가 높아지면 서로 형광을 흡수하는 성질을 이용한 방법으로 주로 micelle에서의 물질 이동에 많이 쓰인다. Donor micelle에는 높은 농도의 형광성 지방산이 들어 있고 acceptor micelle에는 형광성 지방산이 들어 있지 않을 때 형광성 지방산이 donor에서 acceptor로 이동하면 형광도가 증가하게 되고 시간에 따른 형광도 증가를 측정하는 방법이다.

• Journal of Pharmaceutical Investigation
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• 제39권2호
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• pp.97-106
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• 2009

Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl-$\beta$-cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be $0.69{\pm}0.41$, $0.87{\pm}0.51$, $0.84{\pm}0.46$, $0.47{\pm}0.17$ and $0.68{\pm}0.32{\mu}g/cm^2/hr$ for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS.

• Rapid Communication in Photoscience
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• 제3권4호
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• pp.81-84
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• 2014

To examine the microenvironmental effect of DNA on the photosensitized reaction, the electron-donor-connecting porphyrin, meso-(9-phenanthryl)-tris(N-methyl-p-pyridinio) porphyrin (Phen-TMPyP), was synthesized. Phen-TMPyP can bind to oligonucleotides with two binding modes, depending on the DNA concentration. The fluorescence lifetime measurement of Phen-TMPyP shows a shorter component than that of the reference porphyrin without the phenanthryl moiety. However, the observed value is much longer than those of previously reported similar types of electron-donor-connecting porphyrins, suggesting that electron-transfer quenching by the phenanthryl moiety is not sufficient. The fluorescence quantum yield of Phen-TMPyP ($5{\mu}M$) decreased with an increase in DNA concentration of up to $5{\mu}M$ base pair (bp), possibly due to self-quenching through an aggregation along the DNA strand, increased with an increase in DNA concentration of more than $5{\mu}M$ bp and reached a plateau. The fluorescence quantum yield of Phen-TMPyP with a sufficient concentration of DNA was larger than that of the reference porphyrin. The singlet oxygen ($^1O_2$) generating activity of Phen-TMPyP was confirmed by the near-infrared emission spectrum measurement. The quantum yield of $^1O_2$ generation was decreased by a relatively small concentration of DNA, possibly due to the aggregation of Phen-TMPyP, and recovered with a sufficient concentration of DNA. The recovered quantum yield was rather smaller than that without DNA, indicating the quenching of $^1O_2$ by DNA. These results show that a DNA strand can stabilize the photoexcited state of a photosensitizer and, in a certain case, suppresses the $^1O_2$ generation.

• Bulletin of the Korean Chemical Society
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• 제30권4호
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• pp.917-923
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• 2009

The maize lipoxgyenase-1 is a non-traditional dual positional specific enzyme and the reaction proceeds via enzyme-initiated catalysis. Bioinformatic analysis indicated that the maize lipoxygenase-1 is structurally more similar to soybean LOX1 than pea LOXN2 in that it has an additional external loop (residues 318-351) in the carboxy-terminal catalytic domain. We analyzed the dependence of product distribution on concentration of linoleic acid and monitored the formation of hydroperoxyoctadecadienoic acid as a function of enzyme concentration. Product distribution was strongly influenced by substrate concentration, such that kinetically-controlled regioisomers were enriched and thermodynamically-controlled regioisomers were depleted at high substrate concentration. Kinetic studies indicated that the formation of hydroperoxyoctadecadienoic acid saturated rapidly in an enzyme concentration-dependent manner, which implied that reactivation by reoxidation of inactive Fe(II) failed to occur. Our results support the previously proposed enzyme-initiated catalytic mechanism of the maize lipoxgyenase-1 and reveals that a substrate molecule serves as a hydrogen atom donor in its enzyme-initiated catalysis.

• 한국전기전자재료학회:학술대회논문집
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• 한국전기전자재료학회 1995년도 추계학술대회 논문집
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• pp.22-24
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• 1995

The electrical conductivity of TiO$_2$doped ZnO was investigated by means of complex impedance measurement and voltage-current source and meaurement unit. The e1ectrical conductivity of TiO$_2$added ZnO was increased with increasing the concentration of TiO$_2$. The calculated relative dielectric constant was decreased with increasing the concentration of TiO$_2$. The increase of electrical conductivity seems to be the effect of TiO$_2$donor doping.

• 한국수정란이식학회지
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• 제27권4호
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• pp.229-235
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• 2012

This research was investigated the relationship, in high-producing Holstein donor cows, between the number of the transferable embryos and the blood serum concentrations of Blood Urea Nitrogen (BUN), glucose and cholesterol, which affect the nutritional state of cows. CIDRs were inserted into the vaginas of twenty two heads of Holstein cows, regardless of estrous cycle. Superovulation was induced using folliclar stimulating hormone (FSH). For artificial insemination, donor cows were injected with $PGF_{2{\alpha}}$ and estrus was checked about 48 hours after the injection. Then they were treated with 4 straws of semen 3 times, with 12-hour intervals. Embryos were collected by a non-surgical method 7 days after the first artificial insemination. The total numbers of ova collected from 3 experimental groups whose blood BUN concentrations were <10 mg/dl, 11~18 mg/dl and ${\geq}19$ mg/dl were 8.9, 12.5 and 19.0, respectively; whereas the numbers of transferable embryos were 5.8 + 1.9, 7.9 + 2.8 and 5.2 + 1.4, respectively. When glucose concentration was <60 mg/dl, the total number of collected ova was 9.9, which was smaller than when the concentration was 60~70 mg/dl or ${\geq}70$ mg/dl. When glucose concentration was 60~70 mg/dl, the number of transferable embryos was 7.1 + 2.4, which was slightly larger than the numbers 6.4 + 2.1 and 6.1 + 1.7 that were obtained when the concentrations were <60 mg/dl and ${\geq}70$ mg/dl, respectively ; however, the differences were not significant (p>0.05). When cholesterol concentrations were <150 mg/dl, 150~200 mg/dl and ${\geq}200$ mg/dl, the total numbers of collected ova were 11.2, 11.3 and 8.6, respectively. Whereas the numbers of transferable embryos were 7.1 + 2.1, 7.3 + 1.9 and 5.6 + 1.3, respectively ; however, the differences were again not significant (p>0.05). The result of this research showed no significant difference in ovum recovery rate and the number of transferable embryos according to major metabolite concentrations in high-producing Holstein donor cows. However, it is considered that the failure of maintaining proper nutritional status would cause the fall in in vivo embryo productivity.

• 한국지하수토양환경학회:학술대회논문집
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• 한국지하수토양환경학회 2000년도 추계학술대회
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• pp.209-212
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• 2000

As a bench-scale study, transformation of nitrate to nitrogen gas under anoxic condition was determined by using autotrophic denitrifiers containing Thiobacillus denitrificans and elemental sulfur as an electron donor. The research objective is to measure the basic kinetic parameters of autotrophic denitrification reaction on the removal efficiency of nitrate. The results showed that nitrate was almost completely transformed to nitrite in the first 4 days of column operation. After 2 days of accumulation of nitrite, its concentration slowly decreased and the compound was detected less than 0.5 mg/L in 14 days. In the experiment, sulfate concentration in the effluent was the 70~90 mg-S/L and the pH was maintained around pH 7.5. When nitrate concentration of bank filtrate in the real field is considered, this sulfate concentration seems to be acceptable. At 17 cm from the bottom of the column, the effluent showed the highest nitrite concentration, and nitrate concentration decreased rapidly to the Point of 33 cm from the bottom. The results suggest that an appropriate thickness of permeable reactive barriers is about 30 cm.

• 대한환경공학회지
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• 제28권3호
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• pp.292-299
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• 2006

전자공여체로 벤조산염을 이용한 perchloroethene(PCE)의 환원성 탈염소화 과정에서 전자공여체의 첨가량 및 초기 미생물 식종량이 탈염소화에 미치는 영향을 평가하기 위하여 회분식 실험을 수행하였다. 벤조산염이 탈염소화를 위한 양론비 이하(전자공여체/수용체 비=0.5와 1)로 첨가된 경우 탈염소화 효율은 벤조산염 첨가량이 증가함에 따라 71%에서 94.3%로 증가하였으나, 탈염소화에 이용된 전자공여체의 분율은 92.7%에서 79.6%로 감소하였다. 메탄생성은 PCE와 trichloroethene(TCE)가 모두 cis-1,2-dichloroethene(cDCE)으로 전환된 후 문턱농도(threshold value, 10 nM) 이상으로 수소농도가 유지되는 동안 진행되었다. 벤조산염이 양론비 이상으로 첨가된 경우 탈염소화 완료 후 잔존하는 수소는 메탄생성량을 증가시켰다. 식종 미생물량의 증가는 지체기를 감소시켰지만 최대 탈염소화 속도는 벤조산염 분해 속도에 의해 결정되어 식종 미생물량에 큰 영향을 받지 않았다. 식종 미생물 농도가 높은 경우 초기 활발한 탈염소화로 인하여 메탄생성량은 감소하고, 탈염소화 효율은 증가하였다.

• 한국축산식품학회지
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• 제25권3호
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• pp.340-343
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• 2005

SLM을 이용한 short peptide의 분리를 목적으로 donor phase의 pH 및 acceptor phase의 염농도, membrane의 carrier 농도 차에 따른 peptide의 이동속도를 확인한 결과는 다음과 같다. 즉, pH 7.0 이하에서는 acceptor phase의 NaCl 농도나 carrier 농도에 상관없이 Gly-Tyr의 이동속도는 거의 영향을 끼치지 않았고, pH 7.0 이상에서는 이동속도가 급격히 증가함을 알 수 있었다. 그리고 Aliquat가 $8\%$ 함유된 D-SLM과 $20\%$ 함유된 H-SLM의 경우 Gly-Tyr의 이동속도는 H-SLM이 D-SLM보다 pH 9.0, 0.25 M NaCl 용액에서는 약 3배, pH 8.0, 1.0 M NaCl용액에서는 10배 정도 빠르게 이동하였다. 또한 H-SLM에서 acceptor phase의 NaCl 농도가 1.0 M 인 경우 0.25 M에 비해 10배 정도 이동속도가 빠른 것으로 나타났다. 따라서, short peptide인 Gly-Tyr의 SLM을 이용한 추출에서 donor phase의 pH 7.0 이상, carrier 농도가 높은 H-SLM 사용, acceptor phase의 염 농도가 높을수록 이동속도가 빠른 것으로 나타났다.