Camptothecin

国际站：Camptothecin

中文名：喜树碱

CAS：7689-03-4

品牌：MedChemExpress (MCE)

存储条件：4°C, protect from light

生物活性：Camptothecin (CPT) 是一种生物碱，是一种 DNA 拓扑异构酶 I (Topo I) 抑制剂，IC₅₀ 为 679 nM^[1]。喜树碱 (CPT) 对结直肠癌、乳腺癌、肺癌和卵巢癌表现出强大的抗肿瘤活性，通过改变 microRNA (miRNA)hypoxia-inducible factor-1α (HIF-1α) 活性> 人类癌细胞中的表达模式^[2][3]。 IC50 和目标：IC50：679 nM（拓扑异构酶 I）

体外：高 TOP1 酶活性 MCF7（Luminal 亚型）和 HCC1419（HER2 亚型）对喜树碱（0.1 μM 至 5 μM；72 小时）处理表现出高敏感性，IC₅₀ 值分别为 0.089 μM 和 0.067 μM ，分别^[4]。喜树碱（0.5 μM；6 和 24 小时）降低去铁胺激活的 VEGF 表达。喜树碱（0.5 μM；8 至 24 小时）强烈阻止去铁胺依赖的 HIF-1a 积累^[2]。

体内：喜树碱（每隔一天 2 毫克/千克）治疗小鼠，已出现大量肺转移。用核因子-kappaB-1 (KINK-1) 激酶抑制剂和喜树碱治疗后，在统计学上显着降低了肺转移灶数量^[5]。

参考文献：[1]. Luzzio MJ, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.[2]. Bertozzi D, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells. Mol Cancer Ther. 2014;13(1):239-248.[3]. Schön M, et al. KINK-1, a novel small-molecule inhibitor of IKKbeta, and the susceptibility of melanoma cells to antitumoral treatment. J Natl Cancer Inst. 2008;100(12):862-875..[4]. Huang Q, et al. Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. Eur J Med Chem. 2013;63:746-757.[5]. Tesauro C, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study. BMC Cancer. 2019;19(1):1158. Published 2019 Nov 29.