• 한국초지조사료학회지
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• 제35권3호
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• pp.238-244
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• 2015

Three growing wethers were used to investigate the differences in nitrogen (N) retention, blood plasma metabolite concentration and energy-yielding nutrient supply to muscle and adipose tissue. The wethers were fed one of three diets: timothy hay with concentrate (THD), Italian ryegrass with concentrate (IRD), and rice straw with concentrate (RSD) for 11 days. The experimental diets were adjusted to the animals to provide 100 g of daily gain. The triglyceride (TG) concentration of blood plasma in arterial and portal veins was higher with THD and IRD than with RSD. Conversely, the available amount of TG in tissues was higher with IRD. The daily amount of glucose and non-esterified fatty acids (NEFA) supplied to muscle tissue and adipose tissue was numerically higher with THD than IRD or RSD. Although N retention did not differ among the diets, it was numerically higher with THD than with IRD or RSD. The results suggest that the difference in the amount of glucose and NEFA delivered to muscle tissue may reflect the N retention in response to forage based diets.

• Asian Pacific Journal of Cancer Prevention
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• 제17권5호
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• pp.2527-2533
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• 2016

Sensitising cancer cells and at the same time desensitizing normal cells is a double task in cancer management. Agents which can combat the debilitating side effects of cancer therapeutics and simultaneously synergize with anticancer agents in specifically targeting cancer cells are needed. Selenium, a proven anticarcinogen, gains due importance in terms of its efficacy to combat the side effects of cancer therapy. This study is a comparative analysis of the chemoprotective effects of selenium compounds, methyl selenol (generated from organic selenomethionine (5mmol/L ; METase 40U/L)) and sodium selenite (inorganic form)($30{\mu}M$) in peripheral blood human lymphocytes exposed to cisplatin and mitomycin. Biochemical alterations occurring in many cells during apoptosis include loss of plasma membrane phospholipid asymmetry, DNA fragmentation, and activation of caspase-3. The present study demonstrated that the selenium metabolite and selenite are efficient in protecting lymphocytes undergoing DNA damage and exerted their activity by reducing caspase 3 expression. Interestingly organic methylselenol (MeSe) was found to offer more protective effects compared to inorganic selenite (SeL), by reducing the induction of apoptosis by the cytotoxic agents. This suggests that MeSe and to a lesser extent selenite might have potential for assessment in clinical trials and could be considered as strong candidates in pharmacogenomics or in the nutriprotective arena.

• 대한의생명과학회지
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• 제29권3호
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• pp.159-167
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• 2023

The prevalence of diabetes continues to increase worldwide, and the problem is also important in Korea, and about 14% of Korean adults have diabetes. Alcohol consumptions are increasing rapidly around the world and are recognized as one of the major problems in the country. Alcohol consumption is an environmental factor previously known to be associated with the risk of developing diabetes. Alcohol consumption can cause problems in the endocrine system and gastrointestinal function, and oxidative stress of acetaldehyde, an ethanol metabolite, can damage beta cells in the pancreas. In the present study, we found the effect of alcohol intake on fasting blood sugar and the difference between men and women in the risk of diabetes according to alcohol intake. In men, the high-drinking group had a higher risk of diabetes than the non-drinking group (OR, 1.41; P=0.058). In women, the Moderate-drinking group had a lower risk of diabetes compared to the non-drinking group (OR, 0.42; P=0.039). The high-drinking group had a higher risk of diabetes than the non-drinking group (OR, 2.97; P=0.034). The group that consumed more than the WHO's daily alcohol intake risk standard tended to have a higher risk of diabetes than the group that did not (OR, 5.48; P=0.001). This study suggest that moderate alcohol consumption reduce the risk of developing diabetes, and high alcohol consumption increase the risk of developing diabetes.

• 한국환경성돌연변이발암원학회지
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• 제22권4호
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• pp.279-288
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• 2002

According to the epidemiological studies in chromium workers, hexavalent chromium is associated with the risk of lung cancer. Cellular oxidative damages by reactive oxygen species produced by hexavalent chromium exposure may play an important role in the carcinogenesis process. We investigated the availabilities of malondialdehyde measurement for the assessments of oxidative damages from chromium exposure with an experimental inhalation study in vivo. Lipid peroxidation, one kind of cellular oxidative damage, was measured in blood plasma of the rats which inhaled the hexavalent chromium mist for 1, 2 and 3 weeks. The concentrations of malondialdehyde (MDA), the metabolite of lipid peroxidation, in all exposed groups were higher than those of controls with dose-dependant manner. The levels of MDA were also correlated with urine chromium levels of the rats. Therefore, MDA as an indicator of lipid peroxidation could be proper biologic marker for the assessment of the oxidative damage from chromium exposure, which might be involved in carcinogenesis.

• Journal of Microbiology and Biotechnology
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• 제16권3호
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• pp.475-479
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• 2006

Gentisyl alcohol isolated from Penicillium sp. has an antioxidative activity, protecting cells from oxidative stresses. From our in vitro angiogenesis assays with bovine aortic endothelial cells (BAECs), gentisyl alcohol was newly identified as a pro-angiogenic small molecule that induces new blood vessel formation of the cells. Gentisyl alcohol stimulated the proliferation of BAECs in a dose-dependent manner. Moreover, it induced in vitro angiogenesis of BAECs such as invasiveness, migration, and tube formation of the endothelial cells. Effects of gentisyl alcohol on invasion and tube formation were also dose-dependent. These results demonstrate that gentisyl alcohol could affect the angiogenic phenotypes of endothelial cells and be developed as a new small molecule with pro-angiogenic activity.

• 약학회지
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• 제31권4호
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• pp.197-203
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• 1987

When pyrazinamide is used in the treatment of tuberculosis, the measurement of pyrazinoic acid which is an intermediate metabolite of pyrazinamide in body is required in order to prevent its associated side-effects, especially that of hyperuricemia. Effects of vitamin B$_6$ on pyrazinoic acid metabolism were studied in this experiment. The activity of hepatic pyrazinoic acid oxidizing enzyme in the presence of pyridoxal was powerfully inhibited, and the pattern was competitive inhibition type. Whereas, its enzyme activity was significantly increased by the treatment of pyridoxal, and the characteristics of the increase may include induction of enzyme proteins. As mice received pyrazinoic acid(300mg/kg) after pyridoxal-pretreatment(40mg/kg) once daily for 4 days, the blood level of pyrazinoic acid and uric acid was decreased significantly.

• 약학회지
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• 제47권5호
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• pp.331-338
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• 2003

A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.81.1-81.1
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• 2003

Buprenorphine(BPN) is used to treat withdrawal syndromes in narcotic addictions. When narcotics are stopped, withdrawal syndromes such as pupil dilation and blood pressure increment are appeared. And BPN is often prescribed concomitantly with antihypertensives. We researched whether combined medicines of BPN and antihypertensives affected on the metabolism of BPN. After BPN was incubated with antihypertensives such as nifedipine, verapamil, captopril and propranolol in rat or human microsomes, amounts of BPN and its metabolite, norbuprenorphine (NBPN), were measured. (omitted)

• 한국임상약학회지
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• 제23권4호
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• pp.322-326
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• 2013

Purpose: Telmisartan, an angiotensin receptor blocker has been known to be a potent blocker of both CYP2J2 and P-glycoprotein (P-gp) in vitro. This study aims to investigate the drug-drug interactions between telmisartan and ebastine, a CYP2J2 and P-gp substrate in rats. Method: Ebastine (10 mg/kg) was orally given in the presence and absence of telmisartan (4 mg/kg, p.o.). Heparinized blood was serially taken and the plasma concentrations of ebastine and its three metabolites (hydroxyebastine, carebastine and desalkylebastine) were determined using LC-MS/MS, and their pharmacokinetic parameters were compared. Results: Peak concentrations ($C_{max}$) and AUC of ebastine were significantly (p<0.05) increased in the presence of telmisartan by 2.1 and 1.9 times, respectively. While $C_{max}$ of hydroxyebastine was significantly increased by 1.9 times, the half-life of hydroxyebasteine was decreased significantly with telmisartan (p<0.05). There was no change in the pharmacokinetic parameters of carebastine, the active metabolite of ebastine, and desalkylebastine was not detected in plasma. The systemic exposure of ebastine was significantly augmented by telmisartan, indicating that telmisartan may enhance the absorption of ebastine by blocking P-gp. Conclusion: Although telmisartan may also partially contribute to inhibit the biotransformation to hydroxyebastine, the inhibitory action seemed to be overridden by the enhancement of absorption, because the generation of hydroxyebastine was not diminished. In spite of such interactions between telmisartan and ebastine, no clinical consequence could be expected due to no significant change of the active metabolite, carebastine.

• 한국환경농학회지
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• 제16권1호
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• pp.25-30
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• 1997

잉어체내에서 $^{14}C-carbofuran$의 흡수, 분포, 대사 및 배설시험을 이해 carbofuran을 40ppb 수준으로 처리하였다. 약제처리 12시간 후에 적출된 잉어의 조직(간, 신장, 창자, 쓸개)과 혈액에서 방사능$(^{14}C)$의 검출율이 가장 높았다. 잉어의 간과 신장에서 carbofuran은 3-ketocarbofuran과 3-hydroxycarbofuran으로 대사되었고 주요 대사산물로는 3-hydroxycarbofuran이었다. 약제처리 후 조직에서 그의 분포율이 가장 높은 시간대의 잉어를 공시수에 분양하여 배설시험을 수행한 결과 carbofuran은 분양 3시간 후에 배설율이 현저히 증가하였고 검출된 대사산물로는 3-ketocarbofuran과 3-hydroxycarbofuran으로 이 시간 동안의 배설시험에서 이들 대사산물의 검출정도는 각각 32.3%와 52.8%였고 미확인 대사산물은 2.6%이었다.