• Interdisciplinary Bio Central
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• 제2권2호
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• pp.3.1-3.4
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• 2010

In the present research, we assessed the utility of the structural information of drugs for predicting human in vivo intrinsic clearance from in vitro intrinsic clearance data obtained by human hepatic microsome experiment. To compare with the observed intrinsic clearance, human intrinsic clearance values for 51 drugs were estimated by the classical methods using in vivo-in vitro scale-up and by the new methods using the in vitro experimental data and selected molecular descriptors of drugs by the forward selection technique together. The results showed that taking consideration of molecular descriptors into prediction from in vitro experimental data could improve the prediction accuracy. The in vitro experiment is very useful when the data can estimate in vivo data accurately since it can reduce the cost of drug development. Improvement of prediction accuracy in the present approach can enhance the utility of in vitro data.

• Food Science and Biotechnology
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• 제16권5호
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• pp.854-857
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• 2007

In this study, the crude methanol extract of mulberry leaves was fractionated with chloroform, ethyl acetate, n-butanol, and water, successively. The antioxidant activities of the fractions were examined with the 2-deoxyribose oxidation and linoleic acid peroxidation methods. The ethyl acetate fraction showed the strongest antioxidant activity. From it we isolated chlorogenic acid, caffeic acid, quercetin $3-O-{\beta}-D-glucopyranoside$, and kaempferol $3-O-{\beta}-D-glucopyranoside$ with preparatory octadecyl silane-high performance liquid chromatography (ODS-HPLC), and identified the compounds by nuclear magnetic resonance (NMR) and fast atom bombardment mass (FAB-MS) analyses. Overall, quercetin $3-O-{\beta}-D-glucopyranoside$ showed the strongest antioxidant activity by both the 2-deoxyribose oxidation and rat liver microsome peroxidation methods.

• Environmental Analysis Health and Toxicology
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• 제15권1_2호
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• pp.7-12
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• 2000

Scavenging effects on paraquat induced toxicity were investigated by using methanol (MeOH) and ethylacetate (EtoAC) extracts of Lonicera japonica. The results are summerized as follows: 1. To Fe(III)-ADP-NADPH induced microsomal lipid peroixdation, MeOH and EtoAC extracts showed antioxidative activiies and inhibition ratio at 100 $\mu\textrm{g}$/$m\ell$ 44.4% and 73.8% respectively 2. To microsomal NADPH dependent cytochrome p -450 reductase in rat liver, MeOH and EtoAC extracts inhibited the enzyme activiies and inhibition ratio were 26.3% and 44.8% respectively. 3. Administration (30 mg/kg, iv) of paraquat to rats caused the marked elevation of GOT, GPT, LDH, ALP in the serum and lipid peroxides in the microsome as compared to the control group. Serum GTP, LDH, ALP and liver microsomal LPO were reduced significantaly by administration of MeOH extract. (1,000 mg/kg), EtoAC extract (40 mg/kg) and Silymarin (150 mg/kg) as compared to the paraquat group. From the results, MeOH and EtoAc exuacts. of Lonicera japonica showed the useful scavenger and reducer on the paraquat induced hepatotoxicty.

• 한국양식학회지
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• 제16권2호
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• pp.99-103
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• 2003

Olive flounder (Paralichthys olivaceus) was exposed to water-borne phenanthrene for 4 weeks. After the exposure for 2-weeks, hepatic cytochrome P450 contents were significantly elevated. Induction of hepatic ethoxy resorufin-O-deethylase (PROD) activity was significantly increased in flounders treated with 1.0 and 2.0 $\mu$M phenanthrene, compared to untreated group and 0.5 $\mu$M treated group. However, there were no significant changes in pentoxyresorufin-O-deethylase (PROD) activity in hepatic microsome of all the phenanthrene-treated groups, compared to the untreated group. Phenanthrene has the potential to induce cytochrome P450 and EROD enzyme of the olive flounder.

• 약학회지
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• 제34권5호
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• pp.291-295
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• 1990

A modified method was investigated for the determination of benzo(a)pyrene metabolites generated by the rat liver microsomes based on the HPLC technique with radioactive flow detection. By adding $[^3H]-dexamethasone$ to the B(a)P metabolites mixture metabolized by the microsome, the poor yield of solvent extaction of B(a)P metabolites was compensated.

• Archives of Pharmacal Research
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• 제9권1호
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• pp.45-47
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• 1986

Phenylglycine was obtained as the sole metabolite when .alpha.-aminophenylacetonitrile was ted to the culture broth of Aspergillus furmigatus furmigatus. The isolated phenylglycine showed L-configuration with 80% optical purity. Examination of the hydrolysis of the substrate to phenylglycine with cell free extracts, and the supernatant fraction and the particulate fraction both of which were obtained after ultracentrifugation of the cell free extract at 100,000g, indicated that the nitrile group hydrolyzing enzymes, nitrilase existed not only in cytoplasm, but in microsome fractions.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1992년도 제1회 신약개발 연구발표회 초록집
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• pp.41-41
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• 1992

새로이 합성된 1,4-Naphthoquinone(1,4-NQ) 화합물의 세포독성의 확인과 그 작용기전을 규명코져 본 실험을 수행하였다. 분리된 흰쥐 간세포를 1,4-NQ유도체들과 반응 시켰을때 이들 중 YC 001과 YC 008은 독성을 나타냈으나 YC 012는 독성율 나타내지 아니하였다. 세포독성은 세포치사, lactate dehydrogenase 유출 및 산소소비의 억제등으로 확인하였다. 세포 독성의 기전은 mitochondria에서의 전자흐름 차단작용과 microsome에서 redox-cycling 기전에 의한 산소리디칼 생성의 두가지에 대하여 검토하였다. 분리된 mitochondria를 YC 001과 YC 008은 반응 시켰을때 mitochondria의 호흡은 완전히 억제되었다. 그러나 YC 012는 전혀 작용을 나타내지 아니하였다. 이는 간세포에 대한 독성작용과 일치하는 결과이며 따라서 mitochondria에 대한 억제 작용은 이들의 세포독성에 주요한 요인이라고 추측되었다.

• KSBB Journal
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• 제5권3호
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• pp.201-205
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• 1990

The characteristics of steroid acyl transferase were studied in the rat brain with (4-14C)-dehydroepiandrosterone(DHEA). The results could be summarized as followings: The enzyme system responsible for the biosynthesis was localized at the microsome fraction. The optimum pH of this enzyme was 4.6 When DHEA was utilized as substrate, $\Delta$5-pregnenolone was proved to be a competitive inhibitor. However testosterone was a noncompetitive inhibitor. The acylation at 3${\beta}$-hydroxyl group was favored when the hydrophilicity at Cl7 position increased. However, this acylation at C3 was very low when A ring was aromatic. The acylation at Cl7 hydroxyl group reguired an absolute 17${\beta}$-conformation.

• 대한약리학회지
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• 제2권1호
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• pp.31-40
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• 1966

The microsomal fraction is isolated from rabbit heart and skeletal muscle. The fraction is found to contain the $Na^+$-and $K^+$-activated ATPase. The maximal ATPase activity is obtained in $Na^+$ and $K^+$ concentration of 100 mM. Calcium itself stimulates the $Na^+$-and $K^+$-activated portion of ATPase in the presence of $Mg^{++}$. However, calcium does not stimulate ATPase in the absence of $Mg^{++}$.

• 대한예방한의학회지
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• 제1권1호
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• pp.118-125
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• 1997

In oriental medicine, Artemisiae asiatica (AA) has been used as analgesic, antiinflammatory agent, and coagulatory agent. Furthermore, eupatilin, a kind of flavonoids, is known as the active principle component of AA. This study was undertaken to determine the gastric antiulceration of AA and to elucidate its mechanism. AA showed the inhibitory effect on gastric ulceration induced by EtOH/HCl and aspirin. To elucidate its mechanism, the effect of AA on lipidperoxide level in gastric mucosa, microsome lipidperoxidation, iron -dependent lipidperoxidation, and neutrophil activation were examined. It is suggested that the antiperoxidative and antineutrophil activity of AA play important roles as a possible mechanism. These results suggest that AA might have gastric antiulceration activity due to antilipidperoxdative and antineutrophil activity.