• Archives of Pharmacal Research
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• v.27 no.11
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• pp.1099-1105
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• 2004

The peroxisome proliferator-activated receptors (PPARs) are a primary regulator of lipid metabolism. Potency for activation of PPAR$\gamma$, one of a subfamily of PPARs, particularly mirrors glucose lowering activity. We prepared thiazolidinediones featuring benzoxazole moiety for subtype selective PPAR$\gamma$ activators. 5-[4-[2-(Benzoxazol-2-yl-alkylamino)ethoxy]benzyl]thiazolidine-2,4-diones have been prepared by Mitsunobu reaction of benzoxazolylalkylaminoethanol 8 and hydroxybenzylthiazolidinedione 6 and their activities were evaluated. Most compounds tested were identified as potent PPAR$\gamma$ agonists.

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.147.2-148
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• 2001

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.125.1-125.1
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• 2003

Diabetes is complex in nature but it gets further complicated in associating with number of other diseases like hypertension, ratinal disintegration, renal failure and many others. The latest addition to diabetic-complication is its association with bone degeneration disease:osteoporosis, which is a form of bone loss. In both the types of primary diabetes, the insulin dependent diabetes militus (IDDM) as well in insulin independent diabetes millitus (IIDM) the glucose metabolism is altered. (omitted)

• KSBB Journal
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• v.7 no.4
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• pp.271-277
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• 1992

Rat hepatocytes were isolated by collagenase perfusion method and cultured on the collagen coated dish or on the floating collagen membrane. Using the primary cu1tured hepatocytes, the efficiency of cell attachment and the hepatic functions such as gluconeogenesis, ureogenesis and albumin synthesis were studied. The cell viability was kept above 50% until 5 days and the hepatic functions of ammonia metabolism and albumin synthesis were maintained until 7 days. Floating collagen membrane was found to be more efficient than the collagen coated dish for the maintenance of hepatic function in-vitro.

• Korean Journal of Environmental Agriculture
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• v.13 no.2
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• pp.209-215
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• 1994

Absorption, translocation, and metabolism of the herbicide alachlor in soybean, Chinese cabbage, and barnyard grass seedlings were examined and compared with each other using [phenyl-U-$^{14}C$] alachlor in search of a primary factor contributing to the selectivity of alachlor. When root of each seedling was immersed into the solution containing [$^{14}C$]alachlor, the amount of absorbed radioactivity/mg dry matter of seedling which was suggested to be correlated with the susceptibility of plants to alachlor decreased in the order of soybean ${\gg}$ Chinese cabbage ${\geq}$ barnyard grass and the rate of translocation to shoot was Chinese cabbage ${\geq}$ barnyard grass ${\gg}$ soybean. These orders did not consistently explain the selective phytotoxicity of alachlor. Analyses of extracts by reverse phase chromatography showed that alachlor was detoxified by conjugation with glutathione in all three plants and the rate of glutathione conjugation of soybean, the resistant species to alachlor, was the greatest, while that of barnyard grass, the susceptible, was the lowest among three plants. This result explained well the selective phytotoxicity of alachlor. Both absorption and translocation contribute undoubtedly to the selectivity by influencing the active internal concentration of alachlor. However, neither of them appeared to be a primary factor. It was concluded that the most important primary factor was the rate of glutathione conjugation, which detoxifies alachlor and plays an important role in selectivity.

• YAKHAK HOEJI
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• v.37 no.5
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• pp.499-503
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• 1993

Betaine, a major component of Lycii Fructus, was evaluated for its anti-hepatotoxic activity on carbon tetrachloride-induced hepatotoxicity in primary cultured rat hepatocytes. Betaine was found to attenuate carbon tetrachloride-induced hepatotoxicity both morphologically and biochemically. Typical hepatocyte necrosis due to carbon tetrachloride seemed to be reduced by 50 to 500 $\mu{M}$ of betaine under microscopical observation. The value of glutamic pyruvic transaminase released from the hepatocytes into the medium significantly decreased as betaine concentration increased. Betaine also significantly elevated the reduced activities of some enzymes, cytochrome P-450, 7-ethoxycoumarin-0-deethylase and glutathione-S-transferase, involved in xenobiotic metabolism due to carbon tetrachloride-induced hepatotoxicity. These results demonstrate a possible hepato-protective role of betaine against fatty liver that could be easily induced by carbon tetrachloride.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.11a
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• pp.135-140
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• 1994

Over past decades, numerous in vitro model has been developed to investigate drug metabolism. In the order of complexity we found the isolated perfused liver, hepatocytes in co-culture with epithelial cells, hepatocytes in suspension and in primary culture and subcellular hepatic microsomal fractions. Because they can be easily prepared from both animals (pharmacological and toxicological species) and humans (whole livers as well as biopsies obtained during surgery) hepatocytes in primary culture provide the most powerful model to better elucidate drug behavior at an early stage of preclinical development such as : 1. the characterization of main biotransformation reactions. 2. the identification of phase I and phase II isozymes involved in such reactions 3. the evaluation of interspecies differences allowing the selection of a second toxicological animal species more closely related to man on the basis of metabolic profiles 4. the detection of the inducing and/or inhibitory effects of a drug on metabolic enzymes, the prediction of drug interactions 5. the estimation of inter-individual variability in biotransformation reactions. The use of hepatocytes, and in particular those obstained from humans, at an early stage of drug development allows the obtention of more predictive preclinical data and a better knowledge of drug behavior in humans before the first administration of the drug in healthy volunteers.

• Animal Bioscience
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• v.37 no.2_spc
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• pp.323-336
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• 2024

Molecular hydrogen (H₂) and formate (HCOO^-) are metabolic end products of many primary fermenters in the rumen ecosystem. Both play a vital role in fermentation where they are electron sinks for individual microbes in an anaerobic environment that lacks external electron acceptors. If H₂ and/or formate accumulate within the rumen, the ability of primary fermenters to regenerate electron carriers may be inhibited and microbial metabolism and growth disrupted. Consequently, H₂- and/or formate-consuming microbes such as methanogens and possibly homoacetogens play a key role in maintaining the metabolic efficiency of primary fermenters. There is increasing interest in identifying approaches to manipulate the rumen ecosystem for the benefit of the host and the environment. As H₂ and formate are important mediators of interspecies interactions, an understanding of their production and utilization could be a significant starting point for the development of successful interventions aimed at redirecting electron flow and reducing methane emissions. We conclude by discussing in brief ruminant methane mitigation approaches as a model to help understand the fate of H₂ and formate in the rumen ecosystem.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.3
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• pp.985-989
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• 2012

Objective: To make sure the feasibility with $^{18F}FDG$ PET/CT to guided dynamic intensity-modulated radiation therapy (IMRT) for nasopharyngeal carcinoma patients, by dosimetric verification before treatment. Methods: Chose 11 patients in III~IVA nasopharyngeal carcinoma treated with functional image-guided IMRT and absolute and relative dosimetric verification by Varian 23EX LA, ionization chamber, 2DICA of I'mRT Matrixx and IBA detachable phantom. Drawing outline and making treatment plan were by different imaging techniques (CT and $^{18F}FDG$ PET/CT). The dose distributions of the various regional were realized by SMART. Results: The absolute mean errors of interest area were $2.39%{\pm}0.66$ using 0.6cc ice chamber. Results using DTA method, the average relative dose measurements within our protocol (3%, 3 mm) were 87.64% at 300 MU/min in all filed. Conclusions: Dosimetric verification before IMRT is obligatory and necessary. Ionization chamber and 2DICA of I'mRT Matrixx was the effective dosimetric verification tool for primary focal hyper metabolism in functional image-guided dynamic IMRT for nasopharyngeal carcinoma. Our preliminary evidence indicates that functional image-guided dynamic IMRT is feasible.

• Endocrinology and Metabolism
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• v.33 no.4
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• pp.485-492
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• 2018

Background: Increasing evidence supports interplay between aldosterone and parathyroid hormone (PTH), which may aggravate cardiovascular complications in various heart diseases. Negative structural cardiovascular remodeling by primary aldosteronism (PA) is also suspected to be associated with changes in calcium levels. However, to date, few clinical studies have examined how changes in calcium and PTH levels influence cardiovascular outcomes in PA patients. Therefore, we investigated the impact of altered calcium homeostasis caused by excessive aldosterone on cardiovascular parameters in patients with PA. Methods: Forty-two patients (mean age $48.8{\pm}10.9$ years; 1:1, male:female) whose plasma aldosterone concentration/plasma renin activity ratio was more than 30 were selected among those who had visited Severance Hospital from 2010 to 2014. All patients underwent adrenal venous sampling with complete access to both adrenal veins. Results: The prevalence of unilateral adrenal adenoma (54.8%) was similar to that of bilateral adrenal hyperplasia. Mean serum corrected calcium level was $8.9{\pm}0.3mg/dL$ (range, 8.3 to 9.9). The corrected calcium level had a negative linear correlation with left ventricular end-diastolic diameter (LVEDD, ${\rho}=-0.424$, P=0.031). Moreover, multivariable regression analysis showed that the corrected calcium level was marginally associated with the LVEDD and corrected QT (QTc) interval (${\beta}=-0.366$, P=0.068 and ${\beta}=-0.252$, P=0.070, respectively). Conclusion: Aldosterone-mediated hypercalciuria and subsequent hypocalcemia may be partly involved in the development of cardiac remodeling as well as a prolonged QTc interval, in subjects with PA, thereby triggering deleterious effects on target organs additively.