| CAS |
No.26833-87-4 |
| 中文名称 |
高三尖杉酯碱(10mM in DMSO,无菌） |
| 英文名称 |
Homoharringtonine(10mM in DMSO，Sterile） |
| 分子式 |
C29H39NO9 |
| 分子量 |
545.62 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 运输条件 |
冷冻运输 |
| 靶点 |
Others |
| 通路 |
Others |
| 背景说明 |
Homoharringtonine 是一种具有抗肿瘤特性的生物碱，通过与核糖体 A 位点的相互作用阻止蛋白质合成的初始延伸步骤来抑制蛋白质翻译。 Homoharringtonine 可逆地抑制 IL-6 诱导的 STAT3 Tyrosine 705 磷酸化并降低抗凋亡蛋白的表达。 |
| 生物活性 |
Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.[1] |
| In Vitro |
Homoharringtonine 以剂量和时间依赖性方式抑制 IL-6 诱导的 STAT3 磷酸化。Homoharringtonine (HHT) 抑制细胞生长、细胞活力和集落形成，并通过线粒体途径诱导细胞凋亡。研究了 Homoharringtonine 对人 NSCLC 细胞系的细胞毒性，A549 (野生型 EGFR) 和 NCI-H1975 (H1975，具有 L858R 和 T790M 的突变型 EGFR)，吉非替尼用作对照。MTT 法检测，Homoharringtonine 对 A549 具有中度细胞毒性，IC50 为 3.7 μM，H1975 细胞对 Homoharringtonine 更敏感，IC50 为 0.7 μM。通过 MTT 测定，Homoharringtonine 以时间和剂量依赖性方式抑制 A549 细胞和 H1975 细胞的细胞增殖和生长。通过台盼蓝排斥试验，Homoharringtonine 以剂量和时间依赖的方式快速减少活的 A549 和 H1975 细胞。Homoharringtonine 显著抑制 A549 和 H1975 细胞的克隆形成能力[1]。 |
| In Vivo |
与载体对照或吉非替尼相比，Homoharringtonine (10 mg/kg) 可有效抑制肿瘤生长 (PSTAT3 磷酸化。与载体对照或吉非替尼处理相比，Homoharringtonine 处理组的 STAT3 磷酸化和 MCL1 水平显著降低。同时，与上述结果一致，AKT1/2/3 和 ERK1/2 磷酸化未被 Homoharringtonine 处理抑制。为了进一步检查经过不同处理的异种移植肿瘤样本中的 STAT3 磷酸化，将肿瘤样本冷冻并切成 10 μM 的切片用于荧光免疫组织化学。与媒介物对照或吉非替尼处理相比，Homoharringtonine 处理抑制 STAT3 磷酸化[1]。 |
| 细胞实验 |
Human NSCLC cell lines MCF-10A， A549 and H1975 cells are seeded into 96-well plate and precultured for 24 h， then treated with Homoharringtonine for 24 h or 48 h. Cell cytotoxicity is determined by MTT assay. The absorbance is measured at 570 nm by Varioskan Flash Multimode Reader， and the cell death rate is calculated. Cell viability is estimated by trypan blue dye exclusion assay. The cells which exclude the dye are viable. Place 0.5 mL of a suitable cell suspension (dilute cells in complete medium without serum to 1×106 cells per mL) following adding 0.1 mL of 0.4% trypan blue dye and mixing thoroughly， and then incubate at room temperature for 3 min and load into a hemacytometer to count cells in three separate fields (nonviable， deep blue cells as well as viable， clear cells). The cell viability rate is calculated. After staining with Hoechst 33258 at 10 mg/mL for 10 min， cell death is observed by a fluorescence microscope[1]. |
| 动物实验 |
Mice[1] Equal amounts of female and male nude immunodeficient mice (nu/nu)， 6-8 weeks old， are injected subcutaneously with NSCLC H1975 cells (2.5×106) suspended in 100 μL RPMI-1640 medium into the rightflank of each mouse. Treatments are started when the tumors reached a palpablesize. Mice are randomly divided into three groups (n=10) and treated with Homoharringtonine (10 mg/kg)， Gefitinib (30 mg/kg) or vehicle control for 3 weeks. Vernier caliper measurements of the longest perpendicular tumor diameters are conducted along with the mice treatment to estimate the tumor volume， using the following formula: 4π/3×(width/2)2×(length/2)， representing the 3-dimensional volume of an ellipse tumor tissue. Animals are sacrificed when tumors reached to 2 cm or if the mice appeared moribund to prevent unnecessary morbidity to the mice. At the time of the animals’ death， tumors are excised; cells are separatedand lyzed for western blot using anti-STAT3 antibody， anti-pSTAT3， anti-MCL1 and anti-GAPDH antibodies and immunohistochemistry. |
| 数据来源文献 |
[1]. Cao W， et al. Homoharringtonine induces apoptosis and inhibits STAT3 via IL-6/JAK1/STAT3 signal pathway in Gefitinib-resistant lung cancer cells. Sci Rep. 2015 Jul 13;5:8477 |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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