摘要

Hypoxia-inducible factor 1 alpha (HIF-1α) is closely related with chemoresistance of solid tumors. The purpose of this study was to investigate the ability of noscapine to inhibit HIF-1α and sensitize ovarian cancer cells to cisplatin (DDP) under hypoxic conditions. Herein, we report that noscapine sensitized cobalt-induced chemoresistant ovarian cancer cells to DDP-induced apoptosis and inhibition of cell proliferation. Noscapine also promoted proteasome-mediated degradation of cobalt-stabilized HIF-1α protein, with subsequent inhibition of HIF-1 transcriptional activity. These data establish noscapine as a small molecule inhibitor of HIF-1α and provide an evidence for its combination with DDP in combating ovarian cancer chemoresistance.

译文

缺氧诱导因子 1 α (HIF-1 α) 与实体瘤化疗耐药密切相关。本研究的目的是探讨在缺氧条件下诺沙平抑制 HIF-1 α 和使卵巢癌细胞对顺铂 (DDP) 敏感的能力。在此,我们报道了诺卡品致敏钴诱导的化疗耐药卵巢癌细胞对 DDP 诱导的凋亡和抑制细胞增殖。Noscapine 还促进蛋白酶体介导的钴稳定 HIF-1 α 蛋白的降解,随后抑制 HIF-1 的转录活性。这些数据确定了诺沙平是 HIF-1 α 的小分子抑制剂,并为其与 DDP 联合治疗卵巢癌化疗耐药性提供了证据。

Noscapine

呼吸 一种异喳琳类生物碱 药物
概述  :  

那可丁是来自罂粟属植物鸦片中的一种异喳琳类生物碱,近几十年一直用作镇咳药,属外周性镇咳剂。其代谢物归属、生物利用度和药物动力学都已得到了较深入的研究。近年来,那可丁及其衍生物的抗肿瘤作用得到了广泛而系统的研究,它们具有抗肿瘤活性高、作用机制独特、不良反应小等特点。体外增殖实验结果表明,不同肿瘤细胞株对那可丁的敏感性不同。 指征和剂量 镇咳作用与可待因相当,并有罂粟碱样的支气管平滑肌松弛作用,无成瘾性。治疗剂量对呼吸中枢无明显抑制作

Noscapine   /'nɔskeipin/ 

释    义   那可丁

例    句   Noscapine has been primarily used as antitussive agent for several decades. 过去几十年中,那可丁一直被用作镇咳药。

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