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안병준,이유희,김신일 충남대학교 약학대학 의약품개발연구소 1993 藥學論文集 Vol.9 No.-
We have prepared 5 solvent fractions from red ginseng; petroleum ether(GP), diethyl ether (PE), ethyl acetate(GA), n-butanol(GB) and water(GW) fractions, and isolated three polyacetylenes from GP and GE; panaxynol(PN), panaxydol(PD) and panaxytriol(PT). GP, GE and PN potentiated the cytotoxicity of fluorouracil(5-FU) against A549 by 33%, 36% and 29%, respectively. The cytotoxicity of tamoxifen(TMX) against the same was enhanced by GP and PT by 46% and 27%, PN, PD and PT increase the cytotoxicity of mitomycin C by 20%, 18% and 28%, respectively. GP, GE and PD potentiated the cytotoxicity of adriamycin by 27%, 29% and 22%, respectively. GE and PD increased the cytotoxicity of tamoxifen against SK-OV-3 by 25% and 17%. There was evidence that other cytotoxicity-potentiating substances exist in GP and GE.
TPA로 야기된 HL-60 세포의 기질부착 저해작용을 이용한 Protein Kinase C 저해 생약의 탐색
김선희,안종석,김삼용,유관희,안병준 충남대학교 약학대학 의약품개발연구소 1993 藥學論文集 Vol.9 No.-
Thirty-five kinds of herbal drugs, believed to be active for treatment of tumors, were selected as the experimental materials for observing their effects on TPA-induced adherence of HL-60 cell and activity of protein kinase C. They were extracted with ethyl ether(E) and ethyl acetate(EA), methanol(M) in sequence. Among the extracts, Sophorae Flos(EA), Paeoniae Radix(EA), Equisetum hiemale(EA), Phellodendri Cortex(E, EA), Mori Cortex radicis(EA), Ferula assafoetida(E, EA), Sophora subprostrata(EA, M) and Cnidium monnieri(E) inhibited the TPA-in-duced adherence of HL-60 cell more than 50% and Sophorae Flos(E, EA, M), Paeoniae Radix(E, EA, M), Eguisetum hiemale(E), Phellodenri Cortex(E,H), Mori Cortex radicis(M), Ferula assafoetida(M), Sophora subprostrata(EA, M), Cnidium monnieri(M) and Artemisia argyi(M) showed inhibiting effects on the activity of protein kinase C more than 50%. The extracts showing good inhibiting effects on the adherence and enzyme activity were Sophorae Flos(EA), Paeoniae Radix(EA), Phellodendri Cortex(E), Sophora subsprostrate(EA) and Equisetum hiemale(EA).
Acetylshikonine 및 합성 Naphthazarin 유도체의 L1210 및 S-180 암에 대한 항암효과
김현,안병준 忠南大學校 癌共同硏究所 1991 癌共同硏究所 硏究誌 Vol.1 No.1
Acetylshikonine, isolated from the root of Lithospermum erythrorhizon showed a strong cytotoxic activity (ED_(50)=0.10 ug/m/) against L1210 cell and T/C=182% in ICR mice bearing S-180 at a dose of 5 mg/kg. Administrations of 10 mg/kg and 15 mg/kg reduced the T/C values to 60 and 77% respectively. Higher doses reveal toxicity. Seven naphthazarin derivatives synthesized showed good cytotoxic activities against L1210 cell. Especially, naphthazarin and hydronaphthazarin have strong activities (ED_(50)=0.05 ug/m/ for both). Naphthazarin showed a severe toxic effect on ICR mice bearing S-180; no significant toxic effect was observed at a dose of 1 mg/kg or 2 mg/kg, but a severe toxicity (T/C=23%) by administration of 5 mg/kg. Alkylation of C-2 of naphthazarin is necessary for reducing the toxic effect on ICR mice bearing S-180.
2,3-Alkyl Aziridinecarboximidate류의 합성 및 항암효과 평가
정상헌,안병준 忠南大學校 癌共同硏究所 1991 癌共同硏究所 硏究誌 Vol.1 No.1
Seven drivatives of 2,3-alkyl substituted aziridinecarboximidates were prepared from alkyl substituted alkene and cyanamide. Their ED_(50) values against L_(1210) cell in vitro were evaluated as 1.5 to 4 μg/ml.
백경업,안병준 충남대학교 약학대학 의약품개발연구소 1988 藥學論文集 Vol.4 No.-
Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5, 2'-dihydroxy-6,7,8-trimethoxy-6'-geranyloxyflavone 4(8.5 ㎍/㎖), 5,6-dihydroxy-7-gerenyloxyflavone 9(2.3㎍/㎖). 2 has showed the same range of cytotoxicity as the starting material, 5,2'-dihydroxy-6,7,8-trimethoxy-6'-benzyloxyflavone(17.0㎍/㎖). The cytotoxicity of 4 was lower than its starting substance, 5,2',6'-trihydroxy-6,7,8-trimethoxyflavone (4.5㎍/㎖). On geranylating 5,6,7-trihydroxyflavone(baicalein, 15.0㎍/㎖) the cytotoxic activity has been strongly potentiated (2.3㎍/㎖ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone Ⅱ-type flavones, was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.
배기환,민병선,도동선,김남수,양기종,안병준 충남대학교 약학대학 의약품개발연구소 1992 藥學論文集 Vol.8 No.-
For the research of cytotoxic natural products, 50 medicinal plants were extracted with benzene and methanol, separately, and screened against L1210 cells. From the results(Table I), 6 samples showed cytotoxicity both in benzene and methanol extracts of 17 samples in benzene extracts and 3 samples in methanol extracts, respectively. Generally, the cytotoxicity exhibited high frequency (34%) in benzene extract but low frequency in methanol extract(6%), it meant that active cytotoxic components had less polarity. ED_50 values less than 10 ㎍/㎖ were observed in 17 medicinal plants.
배기환,민병선,백흠영,안병준 충남대학교 암연구소 1991 癌共同硏究所 硏究誌 Vol.1 No.1
The extractability and stability of ginkgoflavonolglycosides under presence of several cellulase preparations were investigated. The enzymes used were macerosin, cellulase C and cellulase NC. The content variation of the glycosides was measured with HPLC method, using caffeic acid as an internal standard. The methanol extract of ginkgo leaf, containing the total flavonolglyco-sides of 4.46%, was used for the content comparison. By extraction with the enzymes, each or mixed, the peak levels of all the glycosides began to decrease after 1 or 2 hours. After 24 hour extraction, most of the glycosides were degraded to minor components. The flavonolglycosides in ginkgo leaf were also hydrolysed simply by the water extraction. After 24 hour extraction with water at 40°C, the peak levels of major glycosides were distinctly decreased. Rutin was hydrolysed by enzyme treatment or by ginkgo leaf itself. As a result, it was concluded that the commercially available cellulases and the ginkgo leaf itself contain the activities of β-glycosidase and α-rhamnosi-dase. Kaempferol-3-0-(6' -0-p-coumaroylglucosyl)-rhamnoside and four other ginkgo flavonolglycosides were not hydrolysed under the same condition."
金光洙,李景道,安丙浚 충남대학교 약학대학 의약품개발연구소 1992 藥學論文集 Vol.8 No.-
Five isoflavones were isolated from the root of Caragana microphylla Lam. and the structures have been identified by means of chemical and physical methods. The isoflavones are 7-hydroxy-4'-methoxyisoflavone(formononetin), formononetin-7-O-β-glucoside(ononin), 7-hydroxy-3', 4'-methylenedioxyisoflavone(pseudobaptigenin), 7-O-β-glucuopyranosyloxy-3'-hydroxy-4'-methoxyi-soflavone(calycosin-7-O-β-gluc-oside) and maackiain.