• Journal of Life Science
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• v.33 no.10
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• pp.783-790
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• 2023

Modern people have an increased incidence of metabolic diseases due to changed eating habits, and diabetes is considered the most significant metabolic disease. Given that existing diabetes treatments are accompanied by side effects, the aim of this study was to identify traditional natural products that have anti-diabetic activity. The potential anti-diabetic and antioxidant activities of natural products were examined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay, α-glucosidase assay, and protein tyrosine phosphatase 1B (PTP1B) inhibition assay. Methanol extracts of Ulmus davidiana var. japonica, Acer tegmentosum branches, Nelumbo nucifera seeds, and Carthamus tinctorius seeds were found to have high anti-diabetic activity and further fractionated with solvents using ethyl acetate and butanol. Consequently, the ethyl acetate fraction of C. tinctorius seeds (MG-11-E) with high α-glucosidase and PTP1B inhibitory activity was selected. MG-11-E was subjected to preparative thin layer chromatography, and fraction #6 showed high α-glucosidase and PTP1B inhibitory activity. Fraction #6 was analyzed and fractionated via high performance liquid chromatography with 50% methanol as the mobile phase, and anti-diabetic activity was observed in the sample that eluted after 4 min as a single peak. The α-glucosidase inhibitory activity exhibited by this sample seemed to be greater than the PTP1B inhibitory activity; thus, it was concluded that a greater anti-diabetic therapeutic effect may be achieved by combining this agent with natural products that inhibit PTP1B activity.

• Journal of fish pathology
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• v.36 no.2
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• pp.293-302
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• 2023

This study evaluated the acute toxicity induced by oxolinic acid (OA), neomycin-oxytetracycline combination (NEO-OTC) and florfenicol (FF) administered to guppy (Poecilia reticulata) by comparing standard formulations with commercial preparations (COOaqua curinpotion, COOaqua terafinpotion and COOaqua profenpotion, respectively) for ornamental fish at concentrations of 2-4%. NEO-OTC exhibited the highest acute toxicity in guppy, with no difference observed between the pstandard formulation and commercial preparation (LC₅₀ = 126.08 mg/L and 112.44 mg/L, respectively). OA acute toxicity was assessed in the form of sodium salt, with an LC₅₀ of 504.61 mg/L for the standard formulation and a slightly increased toxicity of 316.11 mg/L for the commercial preparation. In contrast, no mortality was observed during the 96-hour exposure period with the standard formulation in the form of oxolinic acid. The acute toxicity of FF was measured to be above 1,000 mg/L for the standard formulation; however, the commercial preparation significantly increased to 158.53 mg/L. These results indicate that toxicity can significantly increase in commercial formulations, especially those with low levels of active ingredients. This is presumed to be attributed to the organic solvents or solubilizing agents present in the commercial preparations, which may enhance toxicity. Additionally, guppy infected with Aeromonas salmonicida were effectively protected against mortality by administering OA, NEO-OTC and FF at concentrations of 50 mg/L, 100 mg/L and 15 mg/L, respectively, for 2 hours and at half the dose for 24 hours. This result indicates that liquid formulations containing low concentrations of antibiotics may partially increase toxicity, but there is no problem in effectively treating diseases in ornamental fish.

• Nuclear Medicine and Molecular Imaging
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• v.41 no.3
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• pp.241-246
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• 2007

Purpose: $[^{11}C]6-OH-BTA-1$ ([N-methyl-$^{11}C$]2-(4'-methylaminophenyl)-6-hydroxybenzothiazole, 1), a -amyloid imaging agent for the diagnosis of Alzheimer's disease in PET, can be labeled with higher yield by a simple loop method. During the synthesis of $[^{11}C]1$, we found the formation of by-products in various solvents, e.g., methylethylketone (MEK), cyclohexanone (CHO), diethylketone (DEK), and dimethylformamide (DMF). Materials and Methods: In Automated radiosynthesis module, 1 mg of 4-aminophenyl-6-hydroxybenzothiazole (4) in 100 l of each solvent was reacted with $[^{11}C]methyl$ triflate in HPLC loop at room temperature (RT). The reaction mixture was separated by semi-preparative HPLC. Aliquots eluted at 14.4, 16.3 and 17.6 min were collected and analyzed by analytical HPLC and LC/MS spectrometer. Results: The labeling efficiencies of $[^{11}C]1$ were $86.0{\pm}5.5%$, $59.7{\pm}2.4%$, $29.9{\pm}1.8%$, and $7.6{\pm}0.5%$ in MEK, CHO, DEK and DMF, respectively. The LC/MS spectra of three products eluted at 14.4, 16.3 and 17.6 mins showed m/z peaks at 257.3 (M+1), 257.3 (M+1) and 271.3 (M+1), respectively, indicating their structures as 1, 2-(4'-aminophenyl)-6-methoxybenzothiazole (2) and by-product (3), respectively. Ratios of labeling efficiencies for the three products $([^{11}C]1:[^{11}C]2:[^{11}C]3)$ were $86.0{\pm}5.5%:5.0{\pm}3.4%:1.5{\pm}1.3%$ in MEK, $59.7{\pm}2.4%:4.7{\pm}3.2%:1.3{\pm}0.5%$ in CHO, $9.9{\pm}1.8%:2.0{\pm}0.7%:0.3{\pm}0.1%$ in DEK and $7.6{\pm}0.5%:0.0%:0.0%$ in DMF, respectively. Conclusion: The labeling efficiency of $[^{11}C]1$ was the highest when MEK was used as a reaction solvent. As results of mass spectrometry, 1 and 2 were conformed. 3 was presumed.

• The Korean Journal of Nuclear Medicine
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• v.33 no.3
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• pp.298-305
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• 1999

Purpose: N-(3-[$^{18}F$]Fluoropropyl)-$2{\beta}$-carbomethoxy-$3{\beta}$-(4-iodophenyl)nortropane [$^{18}F$]FP-CIT) has been shown to be very useful for imaging the dopamine transporter. However, synthesis of this radiotracer is somewhat troublesome. In this study, we used a new method for the preparation of [$^{18}F$]FP-CIT to increase radiochemical yield and effective specific activity. Materials and Methods: [$^{18}F$]FP-CIT was prepared by N-alkylation of nor-${\beta}$-CIT (2 mg) with 3-bromo-1-[$^{18}F$]fluoropropane in the presence of $Et_3N$ (5-6 drops of $DMF/CH_3CN$, $140^{\circ}C$, 20 min). 3-Bromo-1-[$^{18}F$]fluoropropane was synthesized from $5{\mu}L$ of 3-bromo-1-trifluoromethanesulfonyloxypropane (3-bromopropyl-1-triflate) and $nBu_4N^{18}F$ at $80^{\circ}C$. The final compound was purified by reverse phase HPLC and formulated in 13% ethanol in saline. Results: 3-Bromo-1-[$^{18}F$]fluoropropane was obtained from 3-bromopropyl-1-triflate and $nBu_4N^{18}F$ in 77-80% yield. N-Alkylation of nor-${\beta}$-CIT with 3-bromo-1-[$^{18}F$]fluoropropane was carried out at $140^{\circ}C$ using acetonitrile containing a small volume of DMF as the solvents. The overall yield of [$^{18}F$]FP-CIT was 5-10% (decay-corrected) with a radiochemical purity higher than 99% and effective specific activity higher than the one reported in the literature based on their HPLC data. The final [$^{18}F$]FP-CIT solution had the optimal pH (7.0) and it was pyrogen-free. Conclusion: In this study, 3-bromopropyl-1-triflate was used as the precursor for the [$^{18}F$]fluorination reaction and new conditions were developed for purification of [$^{18}F$]FP-CIT by HPLC. We established this new method for the preparation of [$^{18}F$]FP-CIT, which gave high effective specific activity and relatively good yield.

• Applied Biological Chemistry
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• v.15 no.3
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• pp.213-219
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• 1972

In order to utilize sweet potatoes for the material of Takju, brewing experiments with raw sweet potatoes, sweet potato chips powder and its koji were conducted; and various tests were carried out on effect of the treatments of acid, alkali, polyphenol oxidase inhibitor, oxidizing and reducing agents upon the prevention against coloring of sweet potato chips by steaming, and on peeling effect of sweet potatoes by the alkali and heat treatments. The results obtained were as follows. 1) In the case of brewing with raw sweet potatose, each plot showed low acid and ethanol content, and its finished Takju had an undersirable color and odor. The plots which were mashed after peeling showed higher ethanol contents than the plots mashed without peeling. 2) In the case of brewing with sweet potato chips powder, each plot contained considerably more amount of ethanol than the plots brewed with raw sweet potatoes, white it contained less amount of acid. The ethanol contents of the plots using wheat bran koji were $10.5{\sim}11.4$ per cent 4 days after mashing, and were higher than those of the plots using malts powder. Their finished Takju was inferior in quality because of the lack of acid and being darkened gradually in process of time. 3) The kojies which were made of sweet potato chips powder with Neurospora sitophila or Aspergillus oryzae had good appearance, but the Takju mashes brewed with these contained remarkably less amount of ethanol. 4) Effect of the treatments of acid, alkali, polyphenol oxidase inhibitor and organic solvents such as ether and ethanol upon the prevention against coloring of sweet potato chips was not recognized. Alum and burnt alum were effective a little on the decolorization, and among the oxidizing and reducing agents tested, potassium permanganate was most effective. 5) Darkening of sweet potato chips powder in course of heating after mixing with water was not affected by pectin and amino acids, but by tannin. 6) Sweet potatoes were not peeled easily by friction after soaking in the boiling solution of 3 per cent alkali for 6 minutes and peeled in boiling water for 12 minutes. From the viewpoint of the results above mentioned, it seems to be necessary to study further on the isolation of microorganisms which are able to decompose the coloring substances and yeasts which are adequate for the fermentation of sweet potatoes in order to utilize sweet potatoes for Takju brewing, because brewing with raw sweet potatoes, sweet potato chips powder and its koji was unsuccessful, and effect of the various treatments on the decolorization of sweet potatoes was not recognized.

• Applied Biological Chemistry
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• v.17 no.3
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• pp.149-176
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• 1974

Eight substituted diphenyl ether herbicides and some of their photoproducts were studied in terms of solution phase photolysis under simulated environmental conditions by using a Rayonet photochemical reactor. The test compounds absorbed sufficient light energy at the wavelength of 300 nm to undergo various photoreactions. All the photoproducts were confirmed by means of tlc, glc, ir, ms, and/or nmr spectrometry. The results obtained are summarized as follows: Solution phase photolysis of C-6989: An exceedingly large amount of p-nitrophenol formed strongly indicates the readiness of the ether linkage cleavage of this compound as the main reaction in all solvents used. Photoreduction of nitro to amino group(s) and photooxidation of trifluoromethyl to carboxyl group were recognized as minor reactions. Aqueous photolysis of p-nitrophenol: Quinone(0.28%), hydroquinone (0.66%), and p-aminophenol (0.42%) were confirmed as photoproducts, in addition to a relatively small amount of an unknown compound. The mechanisms of formation of these products were proposed to be the nitro-nitrite rearrangement via $n{\rightarrow}{\pi}^*$ excitation and the photoreduction through hydrogen abstractions by radicals, respectively. Solution phase photolysis of Nitrofen: Photochemical reduction leading to the p-amino derivative was the main reaction in n-hexane. In aqueous solution, the photoreduction of nitro to amino group and hydroxylation predominated over the ether linkage cleavage. Nucleophilic displacement of the nitro group by hydroxide ion and replacement of chlorine substituents by hydroxyl group or, to a lesser extent, hydrogen were also observed as minor reactoins. Solution phase photolysis of MO-338: Photoreduction of the nitro to amino group was marked in the n-hexane solution photolysis. In the aqueous solution, photoreduction of the nitro substituent and hydroxylation were the main reactions with replacement of chlorine substituents by the hydroxyl group and hydrogen, and cleavage of the ether linkage as minor reactions. Photolyses of MC-4379, MC-3761, MC-5127, MC-6063, and MC-7181 in n-hexane and cyclohexane: Photoreduction of the nitro group leading to the corresponding amino derivative and replacement of one of the halogen substituents by hydrogen from the solvent used were the key reactions in each compound. Aqueous photolysis of MC-4379: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, hydroxylation, and replacement of the nitro by hydroxy group were prominent with photoreduction and dechlorination as minor reactions. Aqueous photolysis of MC-3761: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, and photoreduction followed by hydroxylation were the main reactions. Aqueous photolysis of MC-5127: Replacement of carboxyethyl by hydrogen was predominant with ether linkage cleavage, photoreduction, and dechlorination as minor reactions. It was obvious that the decarboxyethylation proceeded more readily than decarboxymethylation occurring in the other compounds. Aqueous photolysis of MC-6063: Cleavage of the ether linkage and photodechlorination were the main reactions. Aqueous photolysis of MC-7181: Replacement of the carboxymethyl group by hydrogen and monodechlorination were the remarkable reactions. Cleavage of the ether linkage and hydroxylation were thought to be the minor reactions. Aqueous photolysis of 3-carboxymethyl-4-nitrophenol: The photo-induced Fries rearrangement common to aromatic esters did not appear to occur in the carboxymethyl group of this type of compound. Conversion of nitro to nitroso group was the main reaction.

• Journal of Preventive Medicine and Public Health
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• v.29 no.4 s.55
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• pp.785-799
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• 1996

We investigated the 1,004 workers who worked in a automobile factory to study the epidemiologic characterists of dermatoses due to cutting oils. Among the workers, 667(66.4%) answered the questionaire. They are belong to 5 departments of the factory-the Engine-Work(258 workers), Gasoline engine Assembly(210), Diesel engine Assembly(96), Power train Work(86), Power train Assembly(17). We measured the oil mist concentration in air of the departments and examined the workers who had dermatologic symptoms. The results were follows; 1) Oil mist concentration ; Of all measured points(52),9 points(17.2%) exeeded $5mg/m^3$- the time-weighed PEL-and one department had a upper confidence limit(95%) higher than $5mg/m^3$. 2) Dermatologists examined 213 workers. 172 of them complained any skin symptoms at that time - itching(32.5%), papule(21.6%), scale(15.7%), vesicle(12.5%) in order. The abnormal skin site found by dermatologist were palm(29.3%), finger & nail(24.6%), forearm(16.2%), back of hand(8.4%) in order. 3) As the result of physical examination, we found that 160 workers had skin diseases. Contact dermatitis was the most common; 69 workers had contact dermatitis alone(43.1%), 11 had contact dermatitis with acne(6.9%), 10 had contact dermatitis with folliculitis(6.3%), 1 had contact dermatitis with acne & folliculitis, and 1 had contact dermatitis with abnormal pigmentation. Others were folliculitis(9 workers, 5.6%), acne(8, 5.0%), folliculitis & acne (2, 1.2%), keratosis(1, 0.6%), abnormal pigmentation (1, 0.6%), and non-specific hand eczema (47, 29.3%). 4) The prevalence of any skin diseases was 34.0 pet 100 in cutting oil users, and 13.3 per 100 in non- users. Especially, the prevalence of contact dermatitis was 23.0 per 100 in cutting oil users and 23.0 per 100 in non-users. 5) We tried patch test(standard serise, oil serise, organic solvents) on 49 patients to differentiate allergic contact dermatitis from irritant contact dermatitis and found 20 were positive. 6) In a multivariate analysis(independant=age, tenure, kinds of cutting oil), the risk of skin diseases was higher in the water-based cutting oil user and both oil user than non-user or neat oil user(odds ratio were 2.16 and 2.78, respectively). And the risk of contact dermatitis was much higher at the same groups(odds ratio were 5.16 and 6.82, respectively).