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手性(E)-13-羟基-10-氧代-11-十八碳烯酸及其内酯的细胞毒性活性评估

Evaluation of the Cytotoxic Activity of Chiral (E)-13-Hydroxy-10-oxo-11-octadecenoic Acid and Its Lactone.

作者信息

Hayashi Y, Nishikawa Y, Mori H, Matsushita Y, Sugamoto K, Matsui T

机构信息

a Research Laboratories II, Tamanoi Vinegar Co.Ltd.

b Faculty of Engineering, Miyazaki University.

出版信息

Biosci Biotechnol Biochem. 1998;62(9):1771-3. doi: 10.1271/bbb.62.1771.

Abstract

Both the S and R enantiomers of (E)-13-hydroxy-10-oxo-11-octadecenoic acid (1) and (E)-10-oxo-11-octadecen-13-olide (2) had similar IC50 values against P388 mouse leukemia cells; i.e. the stereochemistry of the asymmetric center of 1 and 2 had no influence on the cytotoxic activity. Bioassay results of various compounds related to 1 and 2 suggests that the 10-oxo and lactone moieties of 2 were important for enhancing the cytotoxicity.

摘要

(E)-13-羟基-10-氧代-11-十八碳烯酸(1)和(E)-10-氧代-11-十八碳烯-13-内酯(2)的S和R对映体对P388小鼠白血病细胞具有相似的IC50值;即1和2不对称中心的立体化学对细胞毒性活性没有影响。与1和2相关的各种化合物的生物测定结果表明,2的10-氧代和内酯部分对增强细胞毒性很重要。

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