• Journal of Pharmaceutical Investigation
• /
• v.31 no.1
• /
• pp.27-35
• /
• 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.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.26 no.4
• /
• pp.743-750
• /
• 1997

Direct measurement of the kinetics of free fatty acid transfer between phospholipid model membrane is technically limited by the rapid nature of the transfer process. Separation of membrane-bound fatty acid by centrifugation has shown that although the equilibrium distribution of free fatty acid is determined by this method, fatty acid transfer occurs too rapidly for accurate kinetic measurements. Recently fluorescence resonance energy transfer(FRET) assay has been developed to examine transfer of fatty acids between membranes. Donor membranes which has fluorescent fatty acid, anthroyloxy fatty acid(AOFA), is mixed with acceptor membranes which has non-interchangeable fluorescent quencher, nitrobenzo-xadiazol(NBD), using stopped flow apparatus. As the fluorescent fatty acids transfer from donor membrane to acceptor membrane, fluorescence intensity would be decreased and the rate and degree of fatty acid transfer can be analyzed. Fatty acid transfer between micelles is more complicated because of bile salt. Therefore in experiments with micelles, fluorescence self quenching assay is used. At high concentrations, a fluorophore tends to quench its own fluorescence causing a reduction in fluorescence intensity. Donor micelles contained self quenching concentrations of fluorophore and acceptor micelles had no fluorophore. Upon mixing of donor and acceptor micelles, the rate of transfer of the fluorophore from the donor to the acceptor was measured by monitoring the release in self quenching when its concentration in donor decreased over time.

• Journal of Pharmaceutical Investigation
• /
• v.39 no.2
• /
• pp.97-106
• /
• 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
• /
• v.3 no.4
• /
• pp.81-84
• /
• 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
• /
• v.30 no.4
• /
• pp.917-923
• /
• 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.

• Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
• /
• 1995.11a
• /
• pp.22-24
• /
• 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.

• Journal of Embryo Transfer
• /
• v.27 no.4
• /
• pp.229-235
• /
• 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.

• Proceedings of the Korean Society of Soil and Groundwater Environment Conference
• /
• 2000.11a
• /
• pp.209-212
• /
• 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.

• Journal of Korean Society of Environmental Engineers
• /
• v.28 no.3
• /
• pp.292-299
• /
• 2006

Batch experiments were performed to evaluate the effects of the electron donor dosage and the initial biomass on the reductive dechlorination of perchloroethene(PCE) with benzoate as an electron donor. When benzoate was added less than the theoretical requirement for dechlorination(electron donor/acceptor ratio=0.5 and 1), the dechlorination efficiency increased from 71% to 94.3% with the increase in benzoate dosage, but the fraction of electron equivalent utilized for dechlorination decreased from 92.7% to 79.6%. Methane production was observed when the hydrogen concentration was higher than the threshold value(10 nM) after PCE and trichloroethene (TCE) were reduced to cis-1,2-dichloroethene(cDCE). When benzoate was added more than the theoretical requirement, the residual hydrogen converted into methane after the completion of dechlorination. The increase in the seeding biomass shortened the lag time for dechlorination, but it did not affect the maximum dechlorination rate as it was mainly governed by the benzoate fermentation rate. When the seeding biomass concentration was high, active dechlorination during the early period increased dechlorination efficiency while decreasing methane production.

• Food Science of Animal Resources
• /
• v.25 no.3
• /
• pp.340-343
• /
• 2005

The objective of this work was to study separation of short peptide (glycine-tyrosine) by using supported liquid membranes (SLMs) containing Aliquat as a cationic carrier, In the present investigation, the influence of pH of donor phase, concentrations of carrier and salt concentrations of acceptor phase on separation flux rate were investigated. Below pH 7.0 the flux rate was not affected by NaCl concentration or carrier concentration. However, the rate was increased significantly above pH 7.0. The rate with Hossain's SLM(H-SLM) containing $20\%$ Aliquat was about 3-fold higher with pH 9.0 at 0.25 M NaCl and 10-fold higher with pH 8.0 at 1.0 M NaCl than that with Duggan's SLM(D-SLM) containing $8\%$ Aliquat respectively. Furthermore, the rate with H-SLM was 10-fold higher at 1.0 M NaCl than the rate with 0.25 M NaCl, In conclusion, it would appear that the rate of separation was facilitated by using high salt concentrations together with high carrier concentrations above pH 7.0.