摘要 |
PURPOSE: To obtain compounds of kurasoins A and B, having inhibiting activities against farnesyltransferases and useful as an anticancer agent. CONSTITUTION: These kurasoin compounds are expressed by formula I (R is formula II or III). The compounds are obtained by culturing a microorganism, belonging to the genus Paecilomyces and capable of producing kurasoins A and B, e.g. Paecilomyces sp. FO-3684 strain (FERM P-14761) in a culture medium containing a nutrient source under aerobic conditions, extracting the resultant cultured product with an organic solvent (e.g. acetone) and treating the prepared extract by a chromatography. Physicochemical properties of the kurasoin A: property: white powder; molecular weight: 279.1008; molecular formula: C16 H16 O3 ; solubility: soluble in methanol, acetone and ethyl acetate, sparingly soluble in water, chloroform and hexane; color reaction: positive to sulfuric acid and iodine; distinction among acidic, neutral and basic: wealy acidic substance. The kurasoin compounds are capable of inhibiting activities of farnesyltransferases having activating actions on a carcinogenic protein ras p21 protein. |