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이마세(Ma Sae Lee),정성현(Sung Hyun Chung),김동현(Dong Hyun Kim),정세영(Se Young Choung),김신규(Sin Kyu Kim) 대한약학회 1990 약학회지 Vol.34 No.5
Irradiation of the berberinephenolbetaine in a stream of argon produced the 8,14-cycloberberines[1]. On treatment with ethylchloroformate C8-N bond cleavage of the compound[1] occurred, accompanied with dehydrochlorination to give 7-ethylcarboxyisoquinoline[3], and the product[3] treated with strong alkali solution to give the 13-oxonorotensane[4] in 64% yield. Irradiation of the compound[4] converted easily to dihydro-8H-dibenzo[a, g] quinolizine-8-one[5]. and then the compound[5] was treated with methyliodide to give the 8-oxo-quinolizinium methiode. The intermediate colume chromatography on IRA-400 afforded the benzo[c, g]azecine-5-one[6] in 63% yield. The result of biological activities for these compounds are also presented.
페놀베타인 유도체합성 및 항암 활성검토: 프로토베르베린에서 C-환의 화학적 변환
우성주,박예진,황순호,홍유화,이마세,김동현,김인종,김신규,U, Seong-Ju,Park, Ye-Jin,Hwang, Sun-Ho,Hong, Yu-Hwa,Lee, Ma-Se,Kim, Dong-Hyeon,Kim, In-Jong,Kim, Sin-Gyu 대한약학회 1996 약학회지 Vol.40 No.5
The 13-hydroxyberbine(1), derived from berberinephenolbetaine, has been derivatized to furnish a variety of compounds such as 13-oxoberbine(2), 13-thioberbine(3), 13-chloroberbi ne(4), 13-(2-methylaziridine)berbine(5) and 13-carbolactoneberbine(6). Antitumor activity of these compounds was tested.
Preparation and Stability Evaluation of Docetaxel-Loaded Oral Liposome
전종란,김현미,이풍석,오의철,이마세 한국약제학회 2010 Journal of Pharmaceutical Investigation Vol.40 No.2
Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.
Formulation and Evaluation of an Alternative Triglyceride-free Propofol Microemulsion
조재평,조진철,이풍석,이마세,오의철 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.9
A new triglyceride-free propofol microemulsion for intravenous injection was formulated using nonionic surfactants, poloxamers and polyethylene glycol 660 hydroxystearate. The aim of this investigation was to evaluate the formulation for storage stability, antimicrobial activity, toxicity and preclinical efficacy. The results were compared to the characteristics obtained for the most commonly used formulation of propofol (Diprivan®). The mean particle diameter of the microemulsion was less than 100 nm so that it could be readily sterilized using a 0.22 μm membrane at room temperature. The microemulsion formulation demonstrated enhanced stability compared to the marketed macroemulsion formulation. In a stress storage condition, it was physicochemically stable for at least 40 months. This new formulation showed higher antimicrobial activity, lower risk of hyperlipidemia and better tolerability than Diprivan®. In preclinical studies, the efficacy and pharmacokinetic profile of the microemulsion were similar to those of Diprivan®. Nevertheless, the administration of the microemulsion caused considerably low histamine release compared to the macroemulsion. Based on these results, the newly developed microemulsion of propofol appeared to have several advantages and, thus, could be an alternative to the fat macroemulsions of propofol.
이주영,류수진,박예진,황순호,이마세,김인종,김동현,김신규 慶熙大學校 1996 論文集 Vol.25 No.-
Sythesis of β-naphthol derivatives and their anti-tumor activity were investigated. Binaphthol 1 obtained from β-naphthol by oxidative C-C bond formation(phenoloxydation) was converted into its derivatives. Treatment of 1 with POCl_3 followed by aziridine introduction gave phosphoryl aziridine 3. Also, diaziridine 5 was obtained from 1 by chlorination and successive aziridine introdution. Typical chemical transformation of 1 to obtain ester-type afforded compound 7 and 8. Compound 5 was the most effective derivative of the tested compounds on their anti-tumor activity.
김신규(Sin Kyu Kim),이형원(Hyung Won Lee),김인종(In Jong Kim),이마세(Ma Se Lee) 대한약학회 1992 약학회지 Vol.36 No.3
Benzo[C]phenanthidine alkaloids were found to exhibit considerably strong antileukemic activies. These alkaloids have been shown to be biosynthesized from the corresponding alkaloids throung an oxidative C6-N bond cleavage followed by recyclization between C6 and C13 position of the protoberberine. Recently we have achieved the biomimetic transformation of protoberberine alkaloid, berberine into benzo[C]phenanthridine alkaloid, chelerythrine.