SF002-96-1, a new drimane sesquiterpene lactone from an Aspergillus species, inhibits survivin expression.

SF002-96-1, a new drimane sesquiterpene lactone from an Aspergillus species, inhibits survivin expression.
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DOI:
10.3762/bjoc.9.323
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发表时间:
2013
影响因子:
2.7
通讯作者:
Erkel G
Erkel G
中科院分区:
化学4区
文献类型:
--
作者:
Felix S;Sandjo LP;Opatz T;Erkel G

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Survivin是IAP(细胞凋亡抑制剂)基因家族的成员,在几乎所有人类癌症中过表达,并且在功能上参与细胞凋亡的抑制、细胞增殖的调节、转移和对治疗的抗性。由于其在恶性肿瘤中的上调,生存素作为抗癌治疗的新靶点目前吸引了相当大的兴趣。在筛选约200株用于生产存活素启动子活性抑制剂的半知真菌中,从曲霉属物种的发酵物中分离到一种新的补身烷倍半萜内酯SF 002 -96-1。该化合物以剂量依赖性方式抑制瞬时转染的科洛320细胞中的生存素启动子活性,IC 50值为3.42 µM(1.3 µg/mL)。此外,它还降低了生存素的mRNA水平和蛋白合成,并引发细胞凋亡。
Survivin, a member of the IAP (inhibitor of apoptosis) gene family, is overexpressed in virtually all human cancers and is functionally involved in the inhibition of apoptosis, regulation of cell proliferation, metastasis and resistance to therapy. Because of its upregulation in malignancy, survivin has currently attracting considerable interest as a new target for anticancer therapy. In a screening of approximately 200 strains of imperfect fungi for the production of inhibitors of survivin promoter activity, a new drimane sesquiterpene lactone, SF002-96-1, was isolated from fermentations of an Aspergillus species. The compound inhibited survivin promoter activity in transiently transfected Colo 320 cells in a dose dependent manner with IC50 values of 3.42 µM (1.3 µg/mL). Moreover, it also reduced mRNA levels and protein synthesis of survivin and triggered apoptosis.
DOI: 10.1111/j.1349-7006.2002.tb01226.x
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