- 著者
- 島田 智哉子 植沢 芳広 Ishii-Nozawa Reiko 石原 真理子 Kagaya Hajime 金本 大成 寺久保 繁美 中島 秀喜 高尾 浩一 杉田 義昭 坂上 宏
- 出版者
- International Institute of Anticancer Research
- 雑誌
- Anticancer Research (ISSN:2507005)
- 巻号頁・発行日
- vol.34, no.10, pp.5405-5412, 2014-10
Background: Fifteen 3-styrylchromones were subjected to quantitative structure?activity relationship (QSAR) analysis based on their cytotoxicity, tumor selectivity and anti-HIV activity, in order to explore their biological activities. Materials and Methods: Cytotoxicity against four human oral squamous cell carcinoma (OSCC) cell lines and three human oral normal cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Tumor-selectivity was evaluated by the ratio of the mean CC50 (50% cytotoxic concentration) against normal human oral cells to that against OSCC cell lines. Anti-HIV activity was evaluated by the ratio of CC50 to EC50 (50% cytoprotective concentration from HIV infection). Physicochemical, structural and quantum-chemical parameters were calculated based on the conformations optimized by the LowModeMD method followed by the density functional theory (DFT) method. Results: All 3-styrylchromone derivatives showed moderate-to-high tumor selectivity. Especially, compounds that have a methoxy group at 6-position of the chromone ring and hydroxyl group at 4'-position of phenyl group in styryl moiety [11] showed the highest tumor-selectivity. On the other hand, their cytotoxicity against normal cells showed good correlation to the descriptors that reflect hydrophobic interaction and molecular shapes. Conclusion: Multivariate statistics with chemical descriptors for the location of substituted group, molecular shape and electrostatic interaction may be useful for designing the most favorable compound with higher tumor selectivity.
1 0 0 0 OA 若年成人の百日咳菌に対する抗体価の検討および検査法の評価
百日咳、麻疹、風疹はワクチン接種により予防可能な感染症である。近年、我が国ではこれらの疾患の成人発症例が増加している。その原因として抗体低下が考えられる。今回、若年成人(医学生)の抗体価を測定した。百日咳抗体価は28.3%(194/686名)が感染防御レベル(10EU/ml以上)を満たしていなかった。麻疹抗体価は55.6%(322/579名)が感染予防の基準(16以上)を満たしていなかった。風疹抗体価は27.5%(159/579名)が感染予防の基準(8以上)を満たしていなかった。感染予防対策のためにも医学生に対するワクチン接種を積極的に推進する必要があると考える。