For the environmental friendly soil management on the cultivation of crops in the greenhouse, organic materials, such as the by product-fertilizer derived from livestock manure, rice straw, mushroom media, rice hulls, wood sawdust, and cocopeat, were used as carbon sources adjusting the ratio of carbon to nitrogen to 10, 20, and 30 based on the inorganic soil N. In each C/N ratio of greenhouse soil, watermelon was cultivated in the greenhouse as crop for experiment for the spring and summer of the year and the experimental results were summarized as follows. The concentration of T-C in the organic materials applied were between $289{\sim}429g\;kg^{-1}$, In the C/N ratio of 10, using watermelon as the crop cultivated during the second half of the year in the greenhouse soil, the $NO_3$-N and EC were reduced by 21 to 37%, and 26 to 33%, respectively, except the by product-fertilizer from livestock manure, compared to the soil $NO_3$-N and EC used in the experiment. After the watermelon was cultivated in soils that C/N ratios were controlled as 10, 20, and 30 with wood sawdust adding as carbon sources in the three soils with the different EC values, EC values of the soils were reduced by 33, 42, and 39%, respectively, compared to the soil EC used in the experiment. The weight of watermelon was 10.1-13.4 kg per one unit, and, of the three soils with different EC values. In the soils with three different EC values controlled at C/N ratio of 20, the weight of watermelon was good. The degree of sugar of watermelon were 11.8 to 12.3 Brix, which means that the difference between the treatments was not significant. In conclusion, the C/N ratio of 20 controlled by the proper supply of organic materials according to the representative EC values shown in the greenhouse soils was optimal condition enough to maintain the soil management for the organic culture with the proper nutrient cycling.
This study was to investigate the effect of apigenin on the bioavailability of paclitaxel after oral and intravenous administration in rats. The effect of apigenin on P-glycoprotein (P-gp), cytochrome P450 (CYP)3A4 activity was evaluated. The pharmacokinetic parameters of paclitaxel were determined in rats after oral (40 mg/kg) or intravenous (5 mg/kg) administration of paclitaxel with apigenin (0.4, 2 and 8 mg/kg) to rats. Apigenin inhibited CYP3A4 activity with 50% inhibition concentration ($IC_{50}$) of 1.8 ${\mu}M$. In addition, apigenin significantly inhibited P-gp activity. Compared to the control group, apigenin significantly increased the area under the plasma concentration-time curve (AUC, p<0.05 by 2 mg/kg, 59.0% higher; p<0.01 by 8 mg/kg, 87% higher) of oral paclitaxel. Apigenin also significantly (p<0.05 by 2 mg/kg, 37.2% higher; p<0.01 by 8 mg/kg, 59.3% higher) increased the peak plasma concentration ($C_{max}$) of oral paclitaxel. Apigenin significantly increased the terminal half-life ($t_{1/2}$, p<0.05 by 8 mg/kg, 34.5%) of oral paclitaxel. Consequently, the absolute bioavailability (A.B.) of paclitaxel was significantly (p<0.05 by 2 mg/kg, p<0.01 by 8 mg/kg) increased by apigenin compared to that in the control group, and the relative bioavailability (R.B.) of oral paclitaxel was increased by 1.14- to 1.87-fold. The pharmacokinetics of intravenous paclitaxel were not affected by the concurrent use of apigenin in contrast to the oral administration of paclitaxel. Accordingly, the enhanced oral bioavailability by apigenin may be mainly due to increased intestinal absorption caused via P-gp inhibition by apigenin rather than to reduced renal and hepatic elimination of paclitaxel. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the gastrointestinal tract via the inhibition of P-gp and reduced first-pass metabolism of paclitaxel via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by apigenin. It appears that the development of oral paclitaxel preparations as a combination therapy is possible, which will be more convenient than the i.v. dosage form.
Lichen planus is a chronic inflammatory mucocutaneous disease that affects multiple sites of the body. Often it involves the oral mucosa, but also involve other sites such as skin, genitals, scalp and nails. There is no clear cause of oral lichen planus (OLP), current data suggest that OLP is a T-cell mediated autoimmune disorder which may have an altered self-peptide triggering apoptosis of oral epithelial cells. Usually OLP appears in middle-aged women which tends to be chronic with periods of exacerbation and remission. There are many theories those causes the OLP such as psychological and environmental factors, genetic tendency, drugs and more. 60-70% of lichen planus is accompanied by oral lesions, and more than half of its cases are not able to defined by their skin. In this study, among all the possibility(possible) theories, we tried to evaluate the influence of emotional stress in exacerbating OLP. There were thirty patients with a clinical or histological diagnosis of OLP and other thirty subjects who did not show any signs of systemic disorders include OLP. They were evaluated by using modified Holmes and Rahe's Social Readjustment Rating Scale (SRRS). As a result, a significantly higher level of stress was found in the OLP patients than the control group. Therefore it could be concluded that psychological stressors play an important role in the exacerbating OLP.
Journal of the Korean Society of Fisheries and Ocean Technology
/
v.39
no.2
/
pp.120-127
/
2003
In Korea, Trachysalambria curvirostris occurs widely along the south and west coasts with a range extending from Kanghwado in the northwest down to Sarangdo in the southeast. Sex ratio showed seasonal variations, with a mean value of 48.6% for the females. T. curvirostris produces one cohort a year, with the ovaries ripening from July to August. Insemination appeared to take place from June to August, as more than half of the females sampled in the study of over 19 mm carapace length were inseminated. The mean gonado somatic index (GSI) reached a maximum between July and August. The smallest mature female found was a 18 mm carapace length (CL). Size at 50% sexual maturity (CL$_(50)$), determined from both mature females and inseminated females was 18.89 mm and 19.91 mm CL, respectively. The life span of females appeared to be 14-15 months according to size frequency distributions, while that of the male was 13-14 months. Population growth was estimated by the modified von Bertalanffy growth function incorporating seasonal variation in growth. Based on the growth parameters (K = 1.40 yr$_(-1)$ and L$L\infty$ = 29.54 mm CL for females, and K = 2.00yr$_(-1)$ and L$L\infty$ = 18.95 mm CL for males) growth curves showed that females grew faster and reached a larger size than males.
Park, Jeong-Chan;Pandya, Darpan N.;Jeon, Hak-Rim;Lee, Sang-Woo;Ahn, Byeong-Cheol;Lee, Jae-Tae;Yoo, Jeong-Soo
Nuclear Medicine and Molecular Imaging
/
v.41
no.4
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pp.326-334
/
2007
Purpose: The estrogen receptor (ER), which is over-expressed in ER-positive breast tumors, has been imaged by positron emission tomography (PET) using $[^{18}F]$ labeled estrogen ligands, especially $[^{18}F]FES$. However, $[^{18}F]$ has relatively short-lived half-life ($t_{1/2}$ =1.8 h) and the labeling yield of radio-fluorination is usually low compared with $^{64}Cu\;(t_{1/2}=12.7\;h)$. 1,4,7,10-tetraazacyclododecane (cyclen) is used to form stable metal complexes with copper, indium, gallium, and gadolinium. With these in mind, we prepared cyclen-based Cu complexes which mimic estradiol in aspect of two hydroxyl groups. Materials and Methods: 1.7-Protected cyclen, 1.7-bis (benzyloxycarbonyl)-cyclen was synthesized according to the reported procedure. After introducing two 4-benzyloxybenzyl groups at 4,10-positions, the benzyloxycarbonyl and benzyl groups were removed at the same time by hydrogenation on Pd/C to give 1,7-bis(4-hydroxybenzyl)-1,4,7,10-tetraazacyclododecane (1). Results: The prepared ligand 1 was fully characterized by $^1H,\;^{13}C$ NMR, and mass spectrometer. The synthesized ligand was reacted with copper chloride and copper perchlorate to give copper complexes $[Cu(1)]^{2+}2(CIO_4^-)\;and\;[Cu(1)Cl]^+Cl^-$ which were confirmed by high-resolution mass (FAB). Conclusion: We successfully synthesized a cyclen derivative of which two phenol groups are located on trans position of N-atoms. And, two Cu(ll) complexes of +2 and +1 overall charge, were prepared as a potential PET tracers for ER imaging.
Yoon, D. H.;Kim, T. H.;Lee, K. H.;Park, E. W.;Lee, H. K.;Cheong, I. C.;Hong, K. C.
Journal of Animal Science and Technology
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v.45
no.1
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pp.13-22
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2003
Growth Hormone (GH) gene is a member of gene family through the evolutionary process from a small common ancestral gene by a series of gene duplications. The role of the GH in growth and performance controls has been extensively studied in human, mice and livestock. Many researchers have considered GH as a strong candidate gene for evaluation of genetic polymorphisms that could be associated with economic traits in cattle. We report here a novel missense mutation within the exon 5 of the bovine Growth Hormone (bGH) gene. We could amplified 522 bp fragments from eight unrelated Hanwoo cattle by PCR, then, subsequently cloned and sequenced. An Msp I RFLP corresponding to a C to T transition was observed at position 2258 nt. From this result, we could predict a missense mutation (Arg to Trp) at codon 166 in a highly conserved region among many mammals. Codominant Mendelian segregation of the two alleles, Msp I (+) and Msp I (-), was observed in two full-sib F2 families (n = 32, African taurine Bos taurus ${\times}$ African zebu Bos indicus) and eight half-sib Hanwoo families. For the availability of genetic marker, we have performed PCR-RFLP with a large number of individual animals from 15 different cattle breeds (European and Asian taurines, and African indicines). Consideration of breed frequencies of Msp I (-) allele in relation to breed type and their geographic origins, shows higher frequencies in humped breeds or Asian cattle breeds than in humpless or European breeds. This result indicates that the missense mutation can be contributed the functional significance such as the signal transduction through the receptor binding, also may be used as a marker for selection of the economic traits in Hanwoo.
Stability-enhanced mutants, H44, 11-94, 5A2-84, and F8, of L-threonine aldolase(L-TA) from Streptomyces coelicolor A3(2)(SCO1085) were isolated by an error-prone PCR followed by a high-throughput screening. Each of these mutant, had a single amino acid substitution: H177Y in the H44 mutant, A169T in the 11-94 mutant, D104N in the 5A2-84 mutant and F18I in the F8 mutant. The residual L-TA activity of the wild-type L-TA after a heat treatment for 20 min at $60^{\circ}C$ was only 10.6%. However, those in the stability-enhanced mutants were 85.7% for the H44 mutant, 58.6% for the F8 mutant, 62.1% for the 5A2-84 mutant, and 67.6% for the 11-94 mutant. Although the half-life of the wild-type L-TA at $63^{\circ}C$ was 1.3 min, those of the mutant L-TAs were longer: 14.6 min for the H44 mutant, 3.7 min for the 11-94 mutant, 5.8 min for the 5A2-84 mutant, and 5.0 min for the F8 mutant. The specific activity did not change in most of the mutants, but it was decreased by 45% in the case of mutant F8. When the aldol condensation of glycine and 3,4-dihydroxybenzaldehyde was studied by using whole cells of Escherichia coli containing the wild-type L-TA gene, L-threo-3,4-dihydroxyphenylserine(L-threo-DOPS) was successfully synthesized with a yield of 2.0 mg/ml after 20 repeated batch reactions for 100 h. However, the L-threo-DOPS synthesizing activity of the enzyme decreased with increased cycles of the batch reactions. Compared with the wild-type L-TA, H44 L-TA kept its L-threo-DOPS synthesizing activity almost constant during the 20 repeated batch reactions for 100 h, yielding 4.0 mg/ml of L-threo-DOPS. This result showed that H44 L-TA is more effective than the wild-type L-TA for the mass production of L-threo-DOPS.
Park, Hyun Sik;Lee, Hong Jin;An, Hyun Ho;Moon, Byung Seok;Lee, Byung Chul;Kim, Sang Eun
Journal of Radiopharmaceuticals and Molecular Probes
/
v.2
no.2
/
pp.123-131
/
2016
Increasing clinical demand for carbon-11 labeled radiopharmaceuticals has triggered technological advances in fields of radiochemistry and automated modules. Even though carbon-11 has a short half-life ($t_{1/2}=20.4min$), the consecutive second production of carbon-11 labeled radiopharmaceutical in one $^{11}C$-synthetic module should be delayed at least over 4 h to avoid the high radiation exposure. We herein aimed to produce two different carbon-11 labeled radiopharmaceuticals ([$^{11}C$]PIB and [$^{11}C$]methionine) by sharing of [$^{11}C$]methylation source in one $^{11}C$-synthetic module. The synthesis of $^{11}C$-labeling reagents ($[^{11}C]CH_3I$ or $[^{11}C]CH_3OTf$) is fully automated using the commercial TRACERlab $FX_{C-pro}$ module and is readily adaptable to $^{11}C$-labeling reactor for [$^{11}C$]PIB as well as another $^{11}C$-labeling apparatus for [$^{11}C$]methionine via the three-way valve. After completing the [$^{11}C$]PIB production, the re-synthesized $[^{11}C]CH_3I$ was passed through the three-way valve connected the polyetheretherketone (PEEK) line and loaded into the C18 Sep-Pak cartridge including the methionine precursor. The labeled product [^${11}C$]methionine was purified by a simple cartridge separation and reformulated into saline. The radiochemical yield of [$^{11}C$]PIB and [$^{11}C$]methionine were $5.3{\pm}0.6%$ and $18.7{\pm}0.8%$ (n.d.c.), respectively, with over 97% of radiochemical purity. The specific activity of [$^{11}C$]PIB was over $110GBq/{\mu}mol$. Total production time of two radiopharmaceuticals needs about 2 h from $1^{st}$ beam irradiation including quality control tests. Final [$^{11}C$]PIB and [$^{11}C$]methionine were satisfied all quality control test standards.
Purpose $^{18}F-THK5351$ is the newly developed PET probe for tau imaging in alzheimer's disease. The purpose of study was to establish the automated production of $^{18}F-THK5351$ on a commercial module. Materials and Methods Two different approaches were evaluated for the synthesis of $^{18}F-THK5351$. The first approach (method I) included the nucleophilic $^{18}F$-fluorination of the tosylate precursor, subsequently followed by pre-HPLC purification of crude reaction mixture with SPE cartridge. In the second approach (method II), the crude reaction mixture was directly introduced to a semi-preparative HPLC without SPE purification. The radiosynthesis of $^{18}F-THK5351$ was performed on a commercial GE $TRACERlab^{TM}$$FX-_{FN}$ module. Quality control of $^{18}F-THK5351$ was carried out to meet the criteria guidelined in USP for PET radiopharmaceuticals. Results The overall radiochemical yield of method I was $23.8{\pm}1.9%$ (n=4) as the decay-corrected yield (end of synthesis, EOS) and the total synthesis time was $75{\pm}3min$. The radiochemical yield of method II was $31.9{\pm}6.7%$ (decay-corrected, n=10) and the total preparation time was $70{\pm}2min$. The radiochemical purity was>98%. Conclusion This study shows that method II provides higher radiochemical yield and shorter production time compared to the pre-SPE purification described in method I. The $^{18}F-THK5351$ synthesis by method II will be ideal for routine clinical application, considering short physical half-life of fluorine-18 ($t_{1/2}=110min$).
Metabolism and phamacokinetics of albendazole have been studied in Korean native cattle after oral administration of 5 mg/kg of albendazole. As ABZ is known to be rapidly biotransformed to many metabolites in most animal species, it is very imperative to establish the analytical conditions for its metabolites. LC/MS methods for ABZSO and ABZS $O_2$met every requirement enough to study the metabolism of pharmacokinetics of albendazole in Korean native cattle. The parent drug (ABZ) was only measured at first two time points of 0.5 h and 1h, whereas two metabolites were consistently formed between 0.5 h to 48-72 h post-treatment. Formation kinetics for ABZSO and ABZS $O_2$were similar. Time to peak concentration (Tmax) of ABZ-SO appeared at 12h post-treatment of ABZ, faster than that of ABZS $O_2$at 24h. Cmax of ABZS $O_2$(1.05$\pm$0.05 ug/ml) was 1.09 times higher than that of ABZSO (0.96$\pm$0.15). Elimination half-life of ABZS $O_2$(4.2 h) was much shorter than ABZS $O_2$(7.0h) (p<0.005). ABZSO was detected until 48h post-administration but ABZS $O_2$was measurable even at 72h post-dosing. AU $C_{0longrightarrow{\infty}}$ of ABZSO was smaller than that of ABZS $O_2$. Regimen of ABZ is advised to take into consideration is metabolite profiles, especially that of ABZSO, an active metabolite.
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