著者
植木 寛 三樹 修一 川嶋 善仁 本屋敷 敏雄 森田 哲生
雑誌
福山大学薬学部研究年報 = Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University
巻号頁・発行日
no.16, 1998

バナデートは、摘出ラット脂肪組織の穎粒画分に存在するチロシンキナーゼ(PTK)、ミエリン塩基性蛋白質キナーゼ(MBPK)、cAMPホスホジエステラーゼ(PDE)の活性を促進した。部分精製PDE活性はPTKやMBPK画分の添加によって増強した。MBPK画分はウエスタンプロット解析によってMAPキナーゼ(MAPK)を含むことが確認された。これからの結果は、バナデートがバナデート感受性PTKによるMBPK、恐らくMAPK、の活性化を介してPDEの活性を増強することを示唆する。
著者
八木 晟
雑誌
福山大学薬学部研究年報 = Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University
巻号頁・発行日
vol.17, pp.26-51, 1999

Since the establishment of Dietary Supplement Health and Education Act as amendments to the Federal Food, Drug and Cosmetic Act, on October, 1994, herbs, vitamins, minerals and amino acids have been widely applied for dietary supplements. Under the situation, I introduced Aloe from chemical and pharmacological stand point(1993) and Aloe vera gel for an alternative medicine(1996) in Annual report of Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University. Present communication deals with efficacy of Aloe extract based on medicinal experiments.
著者
柿木 充史 金尾 義治 田中 哲郎 細川 宣嗣
出版者
福山大学薬学部
雑誌
福山大学薬学部研究年報 = Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University (ISSN:0288724X)
巻号頁・発行日
no.27, pp.42-43, 2009-12-25

Paclitaxel (PTX) is an antitumor agent for the treatment of various human cancers. Cremophor EL and ethanol are used to formulate PTX in commercial injection solutions, because of its poor solubility in water. However, these agents cause severe allergic reaction upon intravenous administration. The aim of this study is to synthesize water-soluble macromolecular prodrugs of PTX for enhancing the therapeutic efficacy. Poly(vinyl alcohol) (PVA, 80 kDa), water-soluble synthetic polymer, was used as a drug carrier which is safe and stable in the body. The 2'-hydroxyl group of PTX was reacted with succinic anhydride and then carboxylic group of the succinyl spacer was coupled to PVA via ethylene diamine spacer, resulting the water-soluble prodrug of poly(vinyl alcohol)-paclitaxel conjugate (PVA-SPTX). The solubility of PTX was greatly enhanced by the conjugation to PVA. The release of PTX from the conjugate was accelerated at the neutral to basic conditions in in vitro release experiment. [125 I]-labeled PVA-SPTX was retained in the blood circulation for several days and was gradually distributed into the tumorous tissue after intravenous injection to the tumor-bearing mice. PVA-SPTX inhibited the growth of sarcoma 180 cells subcutaneously inoculated in mice. It was suggested that the water-solubility of PTX was markedly enhanced by the conjugation to PVA, and PVA-SPTX effectively delivered PTX to the tumorous tissue due to the enhanced permeability and retention (EPR) effect.Paclitaxel (PTX) is an antitumor agent for the treatment of various human cancers. Cremophor EL and ethanol are used to formulate PTX in commercial injection solutions, because of its poor solubility in water. However, these agents cause severe allergic reaction upon intravenous administration. The aim of this study is to synthesize water-soluble macromolecular prodrugs of PTX for enhancing the therapeutic efficacy. Poly(vinyl alcohol) (PVA, 80 kDa), water-soluble synthetic polymer, was used as a drug carrier which is safe and stable in the body. The 2'-hydroxyl group of PTX was reacted with succinic anhydride and then carboxylic group of the succinyl spacer was coupled to PVA via ethylene diamine spacer, resulting the water-soluble prodrug of poly(vinyl alcohol)-paclitaxel conjugate (PVA-SPTX). The solubility of PTX was greatly enhanced by the conjugation to PVA. The release of PTX from the conjugate was accelerated at the neutral to basic conditions in in vitro release experiment. [125 I]-labeled PVA-SPTX was retained in the blood circulation for several days and was gradually distributed into the tumorous tissue after intravenous injection to the tumor-bearing mice. PVA-SPTX inhibited the growth of sarcoma 180 cells subcutaneously inoculated in mice. It was suggested that the water-solubility of PTX was markedly enhanced by the conjugation to PVA, and PVA-SPTX effectively delivered PTX to the tumorous tissue due to the enhanced permeability and retention (EPR) effect.