莪术二酮，一种从日本厚朴茎皮中提取的倍半萜，可抑制RAS-法尼基蛋白转移酶。

Costunolide, a sesquiterpene from the stem bark of Magnolia sieboldii, inhibits the RAS-farnesyl-proteintransferase.

作者信息

Park S H, Choi S U, Lee C O, Yoo S E, Yoon S K, Kim Y K, Ryu S Y

出版信息

Planta Med. 2001 Jun;67(4):358-9. doi: 10.1055/s-2001-14315.

DOI:10.1055/s-2001-14315

Abstract

Costunolide, a germacrane sesquiterpene lactone isolated from the stem bark of Magnolia sieboldii demonstrated a significant inhibition upon the farnesylation process of human lamin-B by farnesyl-proteintransferase (FPTase), in a dose dependent manner in vitro (IC50 value was calculated as 20 microM). It was also found to exhibit an inhibition upon the proliferation of cultured human tumor cells, i.e., A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon), in vitro.

摘要

莪术二酮是从日本厚朴茎皮中分离得到的一种吉马烷型倍半萜内酯，在体外实验中，它对法尼基蛋白转移酶（FPTase）催化的人核纤层蛋白B的法尼基化过程具有显著的剂量依赖性抑制作用（IC50值计算为20微摩尔）。此外，还发现它在体外对培养的人肿瘤细胞增殖具有抑制作用，这些肿瘤细胞包括A549（非小细胞肺癌）、SK-OV-3（卵巢癌）、SK-MEL-2（黑色素瘤）、XF498（中枢神经系统肿瘤）和HCT-15（结肠癌）。