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Ginkgolide B 및 ginkgoflavonoids의 in vitro와 ex vivo 및 임상에서의 항혈전 작용
권광일,이영신 충남대학교 약학대학 의약품개발연구소 1995 藥學論文集 Vol.11 No.-
The effects of ginkgolides(natural mixture of ginkgolides, ginkgolide B, ginkgolide C) and flavonoids(quercetin, kaempferol, myricetin), extracted from Ginkgo biloba, on ADP and PAF-induced platelet aggregation in vitro and ex vivo were investigated. In these experiments, both of ginkgolides and ginkgoflavonoids did not affect the ADP(5μM) induced platelet aggregation in vitro. The IC_50 value on PAF (0.3μM) induced platelet aggregation were 2.52μM (ginkgolide B) and 6.35μM (natural mixture of ginkgolides) and 2.80 μM (mixture of ginkgolide B and quercetin). Oral administration of ginkgolide B(1 and 3 ㎎/㎏) and quercetin (3 and 9 ㎎/㎏) to rabbits inhibited ex vivo PAF induced platelet aggregation in a dose-dependent manner. Ginkomin-F tablets administered to the diabetic patients showed inhibitory activities on the ADP and PAF induced platelet aggregation in a dose and time dependent manner.
Cefamandole nafate 함유 주사제의 지원자에 대한 생물학적 동등성 시험
권광일,이혜숙,지옥표 충남대학교 약학대학 의약품개발연구소 1990 藥學論文集 Vol.6 No.-
The bioequivalence of Mandol and Mancef (cefamondole nafate injection preparation) was investigated for 8 healthy human volunteers. Cefamandole nafate hydrolysis to cefamandole base in the blood and shows antibacterial activity. As the rate of the hydrolysis can be varied according to the buffer used in the preparation, the bioequivalence of cefamandole nafate I.V. was studied. A new HPLC method, the column switching technique, was developed and used for the simultaneous determination of cefamandole and cefamandole nafate in the plasma and in the urine. There were no statistically significant difference in between Mandol and Mancef for the parameters of AUC and Cp 0.25 hr even through the power of the test was not enough.
한국 전통간장 제조시 맥아첨가방법이 간장의 성분과 식미에 미치는 영향
권광일,이종구,이륜경,최종동,유문균,임무혁,김기주,홍영표,안영순,최광수,Kwon, Kwang-Il,Lee, Jong-Gu,Lee, Ryun-Kyung,Choi, Jong-Dong,Ryu, Mun-Kyun,Im, Moo-Hyeog,Kim, Ki-Ju,Hong, Yeong-Pyo,An, Yeong-Sun,Choi, Kwang-Soo 한국응용생명화학회 2003 한국농화학회지 Vol.46 No.3
전통간장의 맛과 품질을 개선하기 위하여 간장제조시 탄수화물과 효소원으로써 맥아의 첨가법에 대하여 연구하였다. 전통메주(대조)와 메주제조시 맥아를 첨가하여 만든 메주 및 간장 담금시 전통메주에 맥아를 첨가하여 각각 간장을 담금한 후 150일간의 숙성기간동안 간장의 성분 변화를 조사하고 숙성간장의 식미검사를 실시하였다. 메주 제조시 맥아를 첨가하여 만든 메주로 담근 간장은 대조구인 전통 콩메주로 담근 간장에 비하여 간장 담금 초기부터 150일간의 숙성을 마칠 때까지 총질소, TCA가용성 질소, 색도, 순추출물 및 젖산함량이 높았으며 맥아첨가량이 더 많은 메주로 만든 간장에서 이들 성분함량이 더 높았다. 그러나 간장 담금 할 때 간장덧에 맥아를 첨가하였을 때는 포도당을 제외하고는 전통메주로 담금한 대조구 간장보다 오히려 성분함량이 낮았다. 식미검사에서도 메주제조시 맥아를 30% 첨가한 간장이 모든 기호도 특성에서 가장 높은 점수를 얻었고 종합적 기호도 점수도 7.56점으로서 전통간장(대조구)보다 5% 수준에서 유의적으로 식미가 우수함을 보여주었다. Methods of adding barley malt as source of carbohydrates and enzymes in the production of kanjang in order to improve it's tastes and qualities were investigated. Soybean meju, soybean-malt meju and soybean meju cummalt was mashed with 20% salt brine in the ratio of 1:3 respectively, matured and analyzed the chemical compositions of the soy sauce mash samples for 150 days of maturing. Organoleptic evaluations for the matured soy sauce samples were done. The higher total nitrogen, TCA soluble nitrogen, O.D. at 500 nm, pure extract and lactic acid content could be observed with the soy sauce mash made of soybean-malt meju than those of contrast one from the beginning of the mashing throughout to the whole maturing period of 150 days. The higher the content of malt in the soybean-malt meju, the higher those content in the mash. But the lower content of those compositions in the soy sauce mash made of soybean meju cum malt than those in the contrast was found. The highest scores in all the sensory characteristics including 7.56 points, which were significantly different from that of contrast soy sauce at 5% level, in overall palatability were obtained by the soy sauce made of soybean-malt meju added with 30% malt in the organoleptic evaluations.
권광일,이선경,유성은,Kwon, Kwang-Il,Lee, Sun-Kyung,Yoo, Sung-Eun The Korean Society of Pharmacology 1991 대한약리학잡지 Vol.27 No.2
${\beta}-$수용체 효능약물 ((-)-NE), 길항약물 $((\pm)-propranolol,\;labetalol)$ 및 PDE 억제약물(imazodan, KR-30045, KR-30075 등)에 대한 ${\beta}-adrenoceptor$ binding 실험을 ${\beta}_1/{\beta}_2$ 비선택적 radioligand인 $(-)-[^3H]-DHA$를 사용하여 실시하였다. Saturation 실험에서 ${\beta}_1$ 및 ${\beta}_2$ 수용체를 모두 갖고 있는 rat 좌심실의 ${\beta}$ 수용체에 대한 $(-)-[^3H]-DHA$의 $K_d$ 값은 $1.5{\pm}0.43\;nM$, $B_{max}$는 $22.0{\pm}0.9\;fmol/mg$ protein이었다. $({\pm})propranolol$, labetalol 및 (-)NE는 단일상으로 $(-)-[^3H]-DHA$의 결합을 억제하였으며 Ki 값은 각각 $17.0{\pm}0.43\;nM$, $57.3{\pm}1.30\;nM$, $1.57{\pm}0.95\;{\mu}M$로 나타났다. 실험에 사용한 모든 PDE 억제약물들은 $(-)-[^3H]-DHA$ 결합을 $10^{-3}\;M$의 고농도에서도 10% 미만으로 억제했다. 실험결과, propraolol, labetalol 및 NE는 ${\beta}_1/{\beta}_2$ 수용체에 대해 비선택적인 약물로 나타났으며, imazodan 및 신합성 PDE 억제약물들은 rat 심근에 있는 ${\beta}-$수용체에 친화성이 거의 없음을 알 수 있었다. ${\beta}-Adrenoceptor$ binding study of ${\beta}-agonist$ ((-)NE), ${\beta}-antagonists$ $(({\pm})\;propranolol,\;labetalol)$ and PDE inhibitors (imazodan, KR-30045, KR-30075 etc.) was performed using $(-)-[^3H]-DHA$, as a $non-{\beta}_1/{\beta}_2$ selective radioligand. In saturation studies, $K_d$ and $B_{max}$ of $(-)-[^3H]-DHA$ to ${\beta}-adrenoceptors$ in rat left ventricle in which both ${\beta}_1$ and ${\beta}_2$ receptors coexist were determined to be $1.5{\pm}0.43\;nM$ and $22.0{\pm}0.9\;fmol/mg$ protein, respectively. $({\pm})Propranolol$, labetalol and (-)NE competed for $(-)-[^3H]-DHA$ binding sites in an essentialy monophasic manner with $Ki=17.0{\pm}0.40\;nM,\;57.3{\pm}1.30\;nM,\;and\;1.57{\pm}0.95\;{\mu}M$, respectively. All of PDE inhibitors inhibited the $(-)-[^3H]-DHA$ binding by only below 10% even at the high concentration of $10^{-3}M$. The present results suggest that propranolol, labetalol and NE are $non-{\beta}_1/{\beta}_2$ selective antagonists and agonist, respectively. Additionally, this study shows that imazodan and new synthesized PDE inhibitors may hardly have the affinities to ${\beta}-adrenoceptors$ in cardiac muscle.