Coibamide A 是一种 N-甲基稳定的细胞毒性缩酚肽，具有强大的抗增殖活性。Coibamide A 通过 mTOR 独立机制诱导自噬体积累。Coibamide A 诱导细胞凋亡。Coibamide A 抑制VEGFA/VEGFR2表达并抑制胶质母细胞瘤异种移植物中的肿瘤生长。
| 生物活性 | Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A inducesautophagosomeaccumulation via an mTOR-independent mechanism. Coibamide A inducesapoptosis. Coibamide A inhibitsVEGFA/VEGFR2expression and suppresses tumor growth in glioblastoma xenografts[1][2]. |
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体外研究
(In Vitro) | Coibamide A (0.3-1 nM; 3-60 小时) 抑制 MDA-MB-231 乳腺癌细胞的增殖[1]。
Coibamide A (2.3-230 nM; 3 天) 在人 U87-MG 和 SF-295 胶质母细胞瘤细胞中产生浓度和时间依赖性细胞毒性死亡[2]。
Coibamide A (10-300 nM; 72 小时) 以细胞类型特异性的方式诱导 caspase-3/7 的激活和细胞凋亡[2]。
Coibamide A (20 nM; 48 小时) 在抗凋亡的 U87-MG 细胞中诱导自噬体积累[2]。
Cell Proliferation Assay[1] | Cell Line: | MDA-MB-231 breast cancer cells | | Concentration: | 0.3, 1 nM | | Incubation Time: | 3-60 hours | | Result: | Showed a steady concentration-dependent decrease in proliferative activity relative to vehicle-treated cells |
Cell Cytotoxicity Assay[2] | Cell Line: | U87-MG and SF-295 cells | | Concentration: | 2.3 to 230 nM | | Incubation Time: | 3 days | | Result: | Induced concentration-dependent cytotoxicity with EC50values of 28.8 nM and 96.2 nM for U87-MG and SF-295 cells, respectively. |
Apoptosis Analysis[2] | Cell Line: | U87-MG and SF-295 cells | | Concentration: | 10-300 nM | | Incubation Time: | 72 h | | Result: | An 89 kDa band corresponding to the caspase 3-cleaved form of PARP1 was readily detected by 48 h indicative of apoptotic cell death in SF-295 cells, whereas only trace levels of this fragment were observed in late, detaching U87-MG cell lysates |
Cell Autophagy Assay[2] | Cell Line: | U87-MG cell | | Concentration: | 20 nM | | Incubation Time: | 48 h | | Result: | Caused a clear increase in LC3-II expression by 1 h, and this increase in LC3-II expression was generally sustained through 48 h. |
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体内研究
(In Vivo) | Coibamide A (300 μg/kg; 瘤内注射; 前两天, 之后每 48 小时注射一次, 持续 35 天) 抑制胶质母细胞瘤皮下小鼠模型的肿瘤生长[1]。
| Animal Model: | 8-week old female nude athymic mice with U87-MG cells[1] | | Dosage: | 300 μg/kg | | Administration: | Intratumoral injections; for the first two days, and then every 48 h afterward for 35 days | | Result: | Remained stable at 200-300 mm3without significant growth over 4 weeks of treatmen, whereas the tumors of vehicle-treated animals continued to grow at a steady rate consistent with this aggressive cancer cell type |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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