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K252a通过上调p21WAF1抑制卵巢癌细胞的增殖。

K252a inhibits proliferation of ovarian cancer cells by upregulating p21WAF1.

作者信息

Takai Noriyuki, Ueda Tami, Nishida Masakazu, Nasu Kaei, Fukuda Junichiro, Miyakawa Isao

机构信息

Department of Obstetrics and Gynecology, Oita University Faculty of Medicine, Hasama-machi, Oita 879-5593, Japan.

出版信息

Oncol Rep. 2005 Jul;14(1):141-3.

PMID:15944781
Abstract

The furanosylated indolocarbazole, K252a, belongs to a family of microbial alkaloids that also includes staurosporine, which is known to inhibit proliferation, stimulate apoptosis and induce cell cycle arrest of cancer cells. To elucidate the involvement of K252a in ovarian cancer, we investigated the effects of K252a on the ovarian cancer cell line, SK-OV-3. SK-OV-3 cells were treated with K252a, and its effect on cell growth, cell cycle, and related measurements was assessed. MTT assays showed that the ovarian cancer cell line SK-OV-3 cells were sensitive to the growth inhibitory effect of K252a. Cell cycle analysis indicated that their exposure to K252a decreased the proportion of cells in the S-phase and increased the proportion of cells in the G0/G1 phase of the cell cycle. This occurred in concert with altered expression of p21WAF1 protein related to the G0/G1 phase of the cell cycle. These results raise the possibility that K252a may prove particularly effective in treatment of ovarian cancer.

摘要

呋喃糖基化吲哚咔唑K252a属于一类微生物生物碱,该类生物碱还包括星形孢菌素,已知星形孢菌素可抑制癌细胞增殖、刺激细胞凋亡并诱导细胞周期停滞。为阐明K252a在卵巢癌中的作用,我们研究了K252a对卵巢癌细胞系SK-OV-3的影响。用K252a处理SK-OV-3细胞,并评估其对细胞生长、细胞周期及相关指标的影响。MTT法显示卵巢癌细胞系SK-OV-3细胞对K252a的生长抑制作用敏感。细胞周期分析表明,用K252a处理后,S期细胞比例降低,G0/G1期细胞比例增加。这与细胞周期G0/G1期相关的p21WAF1蛋白表达改变同时发生。这些结果提示K252a在卵巢癌治疗中可能特别有效。

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Angiostatic effects of K252a, a Trk inhibitor, in murine brain capillary endothelial cells.K252a(一种 Trk 抑制剂)对鼠脑毛细血管内皮细胞的血管生成抑制作用。
Mol Cell Biochem. 2010 Jun;339(1-2):201-13. doi: 10.1007/s11010-010-0386-9. Epub 2010 Feb 11.
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