3-Alkylthio-6-allylthiopyridazine 유도체 합성 및 SK-Br3 인간유방암세포와 Hep-G2 인간간암세포에 대한 항암작용

권순경,박명숙,박해선 德成女子大學校 2005 德成女大論文集 Vol.34 No.-

Allylthio group of allicin and other organosulfur compounds which are isolated from garlic is considered as a pharmacophore, a key structure component of the molecule which is due to biological activities. In the foregoing studies various 3-alkoxy-6-allylthiopyridazine derivatives (K-compounds) were synthesized and their biological activities were tested in test animals. They showed good hepatoprotective activities on the carbon tetrachloride-treated mouse and aflatoxin B1-treated rats and chemopreventive activities on hepatocarcinoma cells in rat as expected. Now two pyridazine derivatives whose oxygen atom at 6-position of 3-alkoxy-6-allylthiopyridazine is displayed by sulfur(S) were synthesized and their activities were synthesized and their activities were tested in vitro against SK-Br3 human breast cancer cells and Hep-G2 human liver cancer cells. Thio-K6 and Thio-K16 showed good chemopreventive activities on hepatocarcinoma and breast cancer.

Ethyl 2-Methyl-3-Pyrazinyl-3-oxopropionate의 합성과 케토-엔올 토토머화현상

권순경,박명숙,박해선 德成女子大學校 藥學硏究所 2002 藥學論文誌 Vol.13 No.1

Ethyl 2-methyl-3-pyrazinyl-3-oxopropionate is a key intermediate for the development of new drugs and can be synthesized through Claisen condensation from methyl pyrazine carboxylate and ethyl propionate. Even though in β-diketones esters in general the amount of enol form present at equilibrium is far higher than keto form, this key compound showes that the keto concentration is high. It can be explained because of the electron-releasing effect of α-methyl group.

유기과산화물의 합성방법에 관한 고찰

권순경,박영남,박해선 德成女子大學校 藥學硏究所 2004 藥學論文誌 Vol.15 No.1

Compounds with an oxygen-oxygen single bond, are called peroxides, which undergo homolysis readily by heating or irradiation with light, because the oxygen-oxygen bond is weak. The formed products are radicals, which are short-lived and highly reactive. This property is used as initiator in radical chain reaction such as halogenation and many kinds of polymerization. Peroxides are one of the important oxidants and initiators. In this paper synthetic methods of peroxides and mechanisms are reviewed.

잠재적 COX-2의 억제작용이 있는 1,5-Diarylhtdantoin 유도체의 합성

권순경,박해선 德成女子大學校 藥學硏究所 2004 藥學論文誌 Vol.15 No.1

For the development of new COX-2 inhibitors, 1,5-diarylhydantoins 5a~5c and 1,5-diaryl-2-thiohydantoin 6a~6c were synthesized from commercially available phenylacetic acids through esterification, bromination, C-N bond formation and cyclization. Esters 2a~c were efficiently synthesized from the starting materials la~c by refluxing in absolute methanol for 3 hours with catalytic concentrated sulfuric acid. Bromination of 2a~c was carried out with use of N-bomosuccinimide at rt in dichloromethane. The bromine of 3a~c was substituted with aniline in ethanol or N,N-dimethylformamide to provide 4a~c. Hydantoins and 2-thiohydantoins were synthesized from 4a~c by treatment of potassium isocyanate or potassium thiocyanate in dil-ethanol with triethylamine.

신원방우황청심원의 심혈관계에 관한 약효

조태순,이선미,김낙두,허인회,안형수,권광일,박석기,심상호,신대희,박대규 성균관대학교 약학연구소 1999 成均藥硏論文集 Vol.11 No.-

Abstract-In order to investigate the phamacological properties of New Wonbang Woohwangchungsimwon Pill (NSCH), effects of Wonbang Woohwangchungsimwon Pill (SCH) and NSCH were compared using various experimental models. In rat aorta, NSCH and SCH made the relaxation of blood vessels in maximum contractile response to phenylephrine (10^-6 M) regardless to endothelium containing or denuded rings of the rat aorta. Furthermore, the presence of the inhibitors of NO synthase and guanylate cyclase did not aftect significantly the relaxing effects of NSCH and SCH, NSCH and SCH inhibited the vascular contractions induced by acetylcholine, prostaglandin endoperoxide or peroxide in a dose-dependent manner. In conscious spontaneously hypertensive rats (SHRs). NSCH and SCH decreased significantly heart rate. These, at high doses, had a negative inotropic effect that was a decrease of left ventricular developed pressure and (-dp/dt)/(+dp/dt) in the isolated perfused rat hearts, and also decreased the contractile force and heart rate in the isolated rat right atria. In guinea-pig papillary muscle, these had no effects on parameters of action potential such as action potential amplitude (APA). V_max and resting membrane potential (RMP) at low doses, whereas inhibited the cardiac contractility at high doses. Furthermore, these had a significant inhibitory effects on palpitation of the heart in normotensive rats and SHRs. These results suggest that NSCH and SCH have weak cardiovascular effects, and that there is no significant differences between cardiovascular effects of two preparations.

신원방우황청심원액의 심혈관계에 관한 약효

조태순,이선미,김낙두,허인회,안형수,권광일,박석기,심상호,신대희,박대규 충남대학교 약학대학 의약품개발연구소 1999 藥學論文集 Vol.15 No.-

In order to investigate the pharmacological properties of New Wonbang Woohwangchungsimwon Liquid (NSCL), effects of Wonbang Woohwangchungsimwon Liquid (SCL) and NSCL were compared. In isolated rat aorta, NSCL and SCL showed the relaxation of blood vessels in maximum contractile response to phenylephrine (10^-6M) regardless to intact endothelium or denuded rings of the rat aorta. Furthermore, the presences of the inhibitor of NO synthase and guanylate cyclase did not affect the relaxing effect of NSCL and SCL. NSCL and SCL inhibited the vascular contractions induced by acetylcholine, prostaglandin endoperoxide or peroxide in a dose-dependent manner. In conscious spontaneously hypertensive rats (SHRs), NSCL and SCL significantly decreased heart rate. NSCL and SCL, at high doses, had a negative inotropic effect that was a decrease of left ventricular developed pressure and (-dp/dt)/(+dp/dt) in the isolated perfused rat hearts, and also decreased the contractile force and heart rate in the isolated rat right atria. In excised guinea-pig papillary muscle, NSCL and SCL had no effects on parameters of action potential such as resting membrane potential, action potential amplitude, APD_90 and V_max at low doses, whereas inhibited the cardiac contractility at high doses. These results suggested that NSCL and SCL have weak cardiovascular effects with relaxation of blood vessels and decrease of heart rate, and that this effect is no significant differences between cardiovascular effects of two preparations.

신우황청심원액의 심혈관계에 관한 약효연구

조태순,이선미,김낙두,허인회,안형수,권광일,박석기,심상호,신대희,박대규 충남대학교 약학대학 의약품개발연구소 1997 藥學論文集 Vol.13 No.-

In order to investigate the pharmacological properties of New Woohwangchungsimwon Liquid (NCL), efects of Woohwangchungsimwon Liquid (CL) and NCL were compared. In isolated rat aorta, NCL and CL showed the relaxation of blood vessels in maximum contractile response to phenylephrine (10^6M) without regard to intact endothelium or denuded rings of the rat aorta. Furthemore, the presences of the inhibitor of NO synthase and guanylate cyclase did not affect the relaxation of NCL and CL. NCL and CL inhibited the vascular contractions induced by acetylcholine, prostaglandin endoperoxide or peroxide in a dosedependent manner. In conscious spontaneously hypertensive rats (SHRs), NCL and CL significantly decreased heart rate. NCL and CL, at high doses, had a negative inotropic effect that was a decrease of LVDP and (-dp/dt)/(+dp/dt) in the isolated perfused rat hearts, and also decreased the contractile force and heart rate in the isolated rat right atria. In excised guinea-pig papillary muscle, NCL and CL had no efects on parameters of action potential at low doses, whereas inhibited the cardiac contractility at high doses. These results suggested that NCL and CL have weak cardiovascular effects with relaxation of blood vessels and decrease of heart rate, and that this effect is no significant differences between two preparations.

비소세포 폐암 환자의 이차 치료로서 Gemcitabine과 Vinorelbine 혼합 요법의 효과

장필순,강현모,이정은,권선중,안진영,이연선,정성수,김주옥,김선영 충남대학교 암공동연구소 2006 암공동연구소 업적집 Vol.5 No.

Background : Both gemcitabine and vinorelbine are effective anticancer drugs with mild toxicity on non-small cell lung cancer, and monotherapy of these drugs are effective as a second-line chemotherapy. The aim of this trial was to assess the response and toxicity of a combination of gemcitabine and vinorelbine in patients of previously treated for non-small cell lung cancer. Materials and Methods : 24 patients, initial stage III A/B,IV and previously treated with platinium and taxane based regimens, were enrolled from June 2000 to March 2004. The regimens consisted of vinorelbine 25mg/㎡ followed by an infusion of gemcitabine 1000mg/㎡ on day 1 and day 8 every three weeks. This course was repeated more than twice. Results : Twenty-four patients were analyzed for the response, survival rate, and toxicities. The overall response was 17% with a complete remission rate of 4%. The median time-to progression (TTP) was 3.1 months (95%, CI l-10months), and the survival time was 8.2 months (95%, CI 1-23 months). The grade 3/4 toxicities encountered were neutropenia (12.5%), anemia (0%), thrombocytopenia (0%). Non-hematological 3/4 toxicities were not observed. Conclusion : A combination of gemcitabine and vinorelbine in patients previously treated for non-small cell lung cancer provides a relatively good response rate, and a low toxicity profile. However, further study will be needed to confirm its effectiveness. (Tuberc Respir Dis 2005; 58: 344-351) 배경 : Gemcitabine, paditaxel, docetaxel, vinorelbine, ir-rinotecan 새로운 항종양제의 출현으로 일차 치료의효과가 증대 되고 있고 재발시에도 좋은 신체 활동도를 보이고 있어서 이차 치료의 대상군도 늘어나는 효과를 보이고 있다. 치료의 필요성은 증대 되고 있지만 현재까지 표준 치료가 확립되지 않은 상황에서 Gem-citabine과Vinorelbine모두 독성이 강하지 않아서 혼합 요법이 가능한 장점이 있고 비소세포 폐암에 대한효과도 입증이 되어있어서 본 연구는 반응이 없거나 반응을 보인후에 재발된 진행된 비소세포 폐암에 ge-mdtabine과 vinorelbine 흔합 요법을 시행하여서 치료 반응률과 생존율 그리고 부작용을 평가하였다. 대상 및 방법 :2000년 6월부터 2004년 3월까지 충남대학교병원에내원하여 진행성 비소세포 폐암 IIIA/IIIB, IV로 진단을 받고 일차 항암화학요법치료를 받은 환자중에 초기 치료에 반응이 없거나, 치료에 반응이 있었으나 병이 진행된 환자로 추적 관찰 기간이 6개월 이상인 환자를 대상으로 생존율과 반응률 그리고 독성을 분석하였다. 결과 : 총 치료 반응률은 17%. 반응 유지기간의 중앙값은 3.1개월(1-10개월)이었고 생존기간의 중앙값은 8.2개월 (1-23개월) 그리고 1년 생존율은 35%였다. 항암화학요법에 의한 독성은 3도 이상의 중성구 감소가 12%, 오심과 구토가 12.5% 였다. 결론 : 일차 치료에 반응이 없거나 재발한 비소세포 폐암환자의 이차 치료로 gemcitabine과 vinorelbine 혼합요법은 효과적이라고 생각되며 향후 3상 연구를 통한다른 약제와의 비교 연구가 필요하다고 생각된다.

호소수를 이용한 용존공기부상법(DAF)의 효율에 관한 연구

이선주,권순범 대한상하수도학회 2002 상하수도학회지 Vol.16 No.3

The purpose of testing the efficiency of the DAF process, we operated a pilot plant scaled to about 60㎥/day. We tested a sedimentation basin in comparison to DAF, changed the G values in the coagulation and flocculation process and the removal efficiency of the turbidity. As well, we investigated the efficiency of the DAF process. Variables such as low temperature water, coagulation and flocculation type and remove of algae ability were examined. Testing results showed that DAF is superior than a sedimentation basin in turbidity and UV-254 removal efficiency. A combination of the G values in the flocculation process yields the best results at 70/50 and alum of 83%, PACS is 87% marked removal efficiency. An in line static mixer and back mix coagulation type is better than a back mixed coagulation type in turbidity removal efficiency, and algae was almost removed after 1 hours,

비소세포 폐암 환자의 이차 치료로서 Gemcitabine과 Vinorelbine 혼합 요법의 효과

장필순,강현모,이정은,권선중,안진영,이연선,정성수,김주옥,김선영 충남대학교 암연구소 2006 암연구소 업적집 Vol.5 No.-

Background : Both gemcitabine and vinorelbine are effective anticancer drugs with mild toxicity on non-small cell lung cancer, and monotherapy of these drugs are effective as a second-line chemotherapy. The aim of this trial was to assess the response and toxicity of a combination of gemcitabine and vinorelbine in patients of previously treated for non-small cell lung cancer. Materials and Methods : 24 patients, initial stage III A/B,IV and previously treated with platinium and taxane based regimens, were enrolled from June 2000 to March 2004. The regimens consisted of vinorelbine 25mg/㎡ followed by an infusion of gemcitabine 1000mg/㎡ on day 1 and day 8 every three weeks. This course was repeated more than twice. Results : Twenty-four patients were analyzed for the response, survival rate, and toxicities. The overall response was 17% with a complete remission rate of 4%. The median time-to progression (TTP) was 3.1 months (95%, CI l-10months), and the survival time was 8.2 months (95%, CI 1-23 months). The grade 3/4 toxicities encountered were neutropenia (12.5%), anemia (0%), thrombocytopenia (0%). Non-hematological 3/4 toxicities were not observed. Conclusion : A combination of gemcitabine and vinorelbine in patients previously treated for non-small cell lung cancer provides a relatively good response rate, and a low toxicity profile. However, further study will be needed to confirm its effectiveness. (Tuberc Respir Dis 2005; 58: 344-351)