抗肿瘤药物。239. 丹参中新型丹参内酯的分离、结构鉴定、全合成及抗乳腺癌活性

Antitumor Agents. 239. Isolation, structure elucidation, total synthesis, and anti-breast cancer activity of neo-tanshinlactone from Salvia miltiorrhiza.

作者信息

Wang Xihong, Bastow Kenneth F, Sun Chang-Ming, Lin Yun-Lian, Yu Hsi-Jung, Don Ming-Jaw, Wu Tian-Shung, Nakamura Seikou, Lee Kuo-Hsiung

机构信息

Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA.

出版信息

J Med Chem. 2004 Nov 4;47(23):5816-9. doi: 10.1021/jm040112r.

DOI:10.1021/jm040112r

PMID:15509181

Abstract

Neo-tanshinlactone (1) was isolated and synthesized for the first time and evaluated in vitro against several human cancer cell lines. Compound 1 showed significant inhibition against two ER+ human breast cancer cell lines and was 10-fold more potent and 20-fold more selective as compared to tamoxifen citrate. Compound 1 also potently inhibited an ER-, HER-2 overexpressing breast cancer cell line. Therefore, this novel compound merits further development as an anti-breast cancer drug candidate.

摘要

新丹参内酯（1）首次被分离和合成，并在体外对多种人类癌细胞系进行了评估。化合物1对两种雌激素受体阳性（ER+）的人类乳腺癌细胞系表现出显著的抑制作用，与柠檬酸他莫昔芬相比，其效力高10倍，选择性高20倍。化合物1还能有效抑制一种雌激素受体阴性（ER-）、人表皮生长因子受体2（HER-2）过表达的乳腺癌细胞系。因此，这种新型化合物作为一种抗乳腺癌药物候选物值得进一步开发。