Effects of (+)-, (-)- and (±)-Indenestrols A and B on Microtubule Polymerization

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概要

• 論文の詳細を見る

• Indenestrol A (IA) is a metabolite of diethylstilbestrol (DES), and indenestrol B (IB) is an analog of IA. IA was simply obtained from E, E-dienestrol in the presence of dilute sulfuric acid, and a mixture of IA and IB was formed by thermal cyclization of E, E-dienestrol. In order to elucidate the effects of optically active IA and IB on microtubule assembly, the IA and IB enantiomers were separated to >99% purity by high-pressure liquid chromatography using a chiral column. The di(4-bromobenzoate) of (-)-IB was analyzed by X-ray crystallography and its absolute structure was determined as C(3)-S. The (+)-, (-)-, and (±)-indenestrols A and B were shown to be inhibitors of microtubule assembly in vitro using microtubule proteins from porcine brain. (±)-IB is more active than (±)-IA, and the order of inhibitory activity of the enantiomers on microtubule assembly was (+)-IB>(+)-IA>(-)-IA>(-)-IB.

• 社団法人日本薬学会の論文
• 1992-03-25

著者

• 佐藤 義朗

  Kyoritsu College Of Pharmacy

• 小田 泰子

  Kyoritsu College of Pharmacy

• 榊原 由美子

  Kyoritsu College of Pharmacy

• 半沢 宏之

  Analytical and Metabolic Research Laboratories, Sankyo Co., Ltd.,

• 畠 忠

  Analytical and Metabolic Research Laboratories, Sankyo Co., Ltd.,

• 半沢 宏之

  Analytical And Metabolic Research Laboratories Sankyo Co. Ltd.

• 畠 忠

  Analytical And Metabolic Research Laboratories Sankyo Co. Ltd.

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