31186-13-7
中文名稱
DEHYDROALTENUSIN
英文名稱
dehydroaltenusin
CAS
31186-13-7
分子式
C15H12O6
分子量
288.25
MOL 文件
31186-13-7.mol
31186-13-7 結(jié)構(gòu)式
常見問題列表
生物活性
Dehydroaltenusin 脫氫阿霉素是真核DNA 聚合酶 α (DNA polymerase α) 的小分子選擇性抑制劑，一種由真菌產(chǎn)生的抗生素，其 IC50值為 0.68 μM。 Dehydroaltenusin 對(duì)哺乳動(dòng)物 polα 活性的抑制作用模式對(duì) DNA 模板引物 (Ki=0.23 μM) 是競爭性的，對(duì) 2'-脫氧核糖核苷 5'-三磷酸底物是非競爭性的 (Ki=0.18 μM)。
Dehydroaltenusin 在 S 期阻止癌細(xì)胞周期并觸發(fā)凋亡 apoptosis。
Dehydroaltenusin 在體內(nèi)具有抗人類腺癌腫瘤的抗腫瘤活性。靶點(diǎn)
IC50: 0.68 μM (DNA polymerase α)
體外研究
Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD 50 values varies from 38.0 to 44.4 μM. Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication. Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin.
Cell Proliferation Assay
| Cell Line: | Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells |
| Concentration: | 38.0-44.4 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited cell growth of human cancer cell lines. |
Cell Cycle Analysis
| Cell Line: | HeLa cells |
| Concentration: | 38.0 μM |
| Incubation Time: | 6 hours |
| Result: | Decreased to 45% of the control value after 6 h of incubation [ 3 H]-thymidine. |
Apoptosis Analysis
| Cell Line: | HeLa cells |
| Concentration: | 75.0 μM |
| Incubation Time: | 12-24 hours |
| Result: | Detected DNA ladders after 12 hours of incubation. |
體內(nèi)研究
Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days.
| Animal Model: | Nude mice bearing HeLa solid tumors |
| Dosage: | 20 mg/kg |
| Administration: | Injection; 20 mg/kg; 2-day intervals; 12-39 days |
| Result: | Suppressed tumor growth. |