Antitumor activity of phenylahistin in vitro and in vivo
Antitumor activity of phenylahistin in vitro and in vivo
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DOI：
10.1271/bbb.63.1130
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发表时间：
1999-06-01
影响因子：
1.6
通讯作者：
Uno, I
中科院分区：
文献类型：
--
作者：
Kanoh, K;Kohno, S;Uno, I
苯拉组蛋白是一种新的细胞周期抑制剂。由于苯拉组蛋白是由（-）-苯拉组蛋白及其对映异构体组成的比例混合物，因此我们分离了每种对映异构体并评价了它们的体外抗肿瘤活性。（-）-苯组氨酸对8种肿瘤细胞系显示出抗肿瘤活性，IC 50值范围为1.8 × 10（-7）至3.7 × 10（-6），而（+）-苯组氨酸的活性比（-）-苯组氨酸低33-100倍。（-）-苯组氨酸对P388白血病细胞和刘易斯肺癌细胞也有抗肿瘤活性。
Phenylahistin is a new cell cycle inhibitor produced by Aspergillus ustus. Since phenylahistin was produced as a scalemic mixture of (-)-phenylahistin and its enantiomer, we separated each enantiomer and evaluated their antitumor activity in vitro. (-)-Phenylahistin exhibited antitumor activity against 8 tumor cell lines with IC50 values ranging from 1.8 x 10(-7) to 3.7 x 10(-6), while (+)-phenylahistin exhibited 33-100-fold less potent activity than (-)-phenylahistin did. (-)-Phenylahistin also showed antitumor activity against P388 leukemia and Lewis lung carcinoma cells in vivo.