七尾霉素
| 中文名称 | 七尾霉素 |
|---|---|
| 中文同义词 | 那罗星;七尾霉素;化合物 T16269;七尾霉素 A |
| 英文名称 | NANAOMYCIN A |
| 英文同义词 | (1s-e)-10-dioxo;1h-naphtho(2,3-c)pyran-3-aceticacid,3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,;os-3966-a;rosanomycina;Antibiotic OS 3966A, Nanafrocin, 1H-Naphtho[2,3-c]pyran-3-acetic acid,3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-(1S,3R)-;(1S)-3,4,5,10-Tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-1H-naphtho[2,3-c]pyran-3β-acetic acid;(1S,3R)-3,4,5,10-Tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-1H-naphtho[2,3-c]pyran-3-acetic acid;OS-3966-A; ROSANOMYCINA |
| CAS号 | 52934-83-5 |
| 分子式 | C16H14O6 |
| 分子量 | 302.28 |
| EINECS号 | |
| 相关类别 | 霉菌毒素类 |
| Mol文件 | 52934-83-5.mol |
| 结构式 |  |
七尾霉素 性质
| 熔点 | 179°C |
|---|---|
| 沸点 | 363.32°C (rough estimate) |
| 密度 | 1.2514 (rough estimate) |
| 折射率 | 1.4600 (estimate) |
| 储存条件 | −20°C |
| 溶解度 | 不溶于水； DMSO 中≥15.1 mg/mL； ≥31.07 mg/mL，乙醇溶液，超声波 |
| 形态 | 固体 |
| 颜色 | 黄至橙色 |
Nanaomycin A 是第一个选择性 DNMT3B 抑制剂，IC50 为 500 nM。Nanaomycin A 是一种醌类抗生素，可重新激活人类癌细胞中沉默的抑癌基因。Nanaomycin A 抑制人疟原虫恶性疟原虫的体外生长，IC80 值为 33.1 nM。
|
DNMT3B 500 nM (IC 50 ) |
Nanaomycin A (10-10000 nM; 72 hours) has a distinct cytotoxic effect in all three cell lines.
Nanaomycin A (0.5, 5 μM; 72 hours) reveals induction of RASSF1A protein expression in A549 cells.
Nanaomycin A (5 μM; 72 hours) has an 18-fold relative induction.
Nanaomycin A not affects the enzymatic activity of DNMT1.
Cell Cytotoxicity Assay
| Cell Line: | HCT116 (colon), A549 (lung), and HL60 (bone marrow) human tumor cell lines |
| Concentration: | 10, 100, 1000, 10000 nM |
| Incubation Time: | 72 hours |
| Result: | Had a distinct cytotoxic effect in all three cell lines. |
Western Blot Analysis
| Cell Line: | A549 cells |
| Concentration: | 0.5, 5 μM |
| Incubation Time: | 72 hours |
| Result: | Revealed induction of RASSF1A protein expression. |
RT-PCR
| Cell Line: | A549 cells |
| Concentration: | 5 μM |
| Incubation Time: | 72 hours |
| Result: | Had an 18-fold relative induction. |