| Description | Homoharringtonine (HHT) is a natural alkaloid that inhibits the translation of proteins and is cytotoxic. Homoharringtonine acts on the ribosomes of tumor cells to inhibit the elongation step of protein translation, thereby inhibiting protein synthesis, and has antitumor activity. |
| In vitro | 方法：人肺癌细胞 A549 和 NCI-H1975 用 Homoharringtonine (1-6 µM) 处理 24-48 h，使用 MTT assay 检测细胞活力。结果：Homoharringtonine 对 A549 具有中等的细胞毒性，IC50 为 3.7 µM。H1975 细胞对 Homoharringtonine 更敏感，IC50 为 0.7 µM。[1]方法：黑色素瘤细胞 A375 和 B16F10 用 Homoharringtonine (100 nM) 处理 48 h，使用 Flow cytometry 检测细胞周期和凋亡情况。结果：Homoharringtonine 诱导 A375 和 B16F10 细胞凋亡和 G2/M 细胞周期停滞。[2] |
| In vivo | 方法：为检测体内抗肿瘤活性，将 Homoharringtonine (10 mg/kg) 腹腔注射给携带人肺癌肿瘤 H1975 的 nude immunodeficient 小鼠，每周五次，持续三周。结果：Homoharringtonine 能有效抑制肿瘤生长。Homoharringtonine 治疗组的 STAT3 磷酸化和 MCL1 水平显著降低。[1]方法：为研究体内抗肿瘤活性，将 Homoharringtonine (0.7 mg/kg) 灌胃给药给携带 ccRCC 肿瘤移植物的 NOD/SCID 小鼠，每天两次，持续二十八天。结果：两个肿瘤移植品系 XP26 和 XP144 在 Homoharringtonine 治疗后显示出可观察到的肿瘤生长抑制作用。对于 XP26 肿瘤，与载体处理的小鼠相比，Homoharringtonine 处理的小鼠的肿瘤生长被抑制 63.7%，而 XP144 小鼠的肿瘤增长被抑制 43.0%。[3] |
| Cell experiments | Homoharringtonine (HHT) is dissolved in PBS at a stock solution of 2.5?mM and kept at ?20°C[1]. 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]. |
| Synonyms | Myelostat, Ceflatonin, 高三尖杉酯碱, HHT, Omacetaxine mepesuccinate |
| molecular weight | 545.62 |
| Molecular formula | C29H39NO9 |
| CAS | 26833-87-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | 5% DMSO+95% Saline: 4.55 mg/mL (8.34 mM) DMSO: 50 mg/mL (91.64 mM) Chloroform, Dichloromethane, Ethyl Acetate, Acetone, etc.: Soluble |
| References | 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. 2. Tang JF, et al. Homoharringtonine inhibits melanoma cells proliferation in vitro and vivo by inducing DNA damage, apoptosis, and G2/M cell cycle arrest. Arch Biochem Biophys. 2021 Mar 30;700:108774. 3. Wolff NC, et al. High-throughput simultaneous screen and counterscreen identifies homoharringtonine as synthetic lethal with von Hippel-Lindau loss in renal cell carcinoma. Oncotarget. 2015 Jul 10;6(19):16951-62. |