Aphidicolin 是 DNA 聚合酶 α 和 δ 抑制剂,通过干扰 DNA 聚合酶的活性来阻止细胞有丝分裂。Aphidicolin 是一种来源于 Cephalosporium aphidicola 的抗生素, 能够抑制细胞脱氧核糖核酸合成和单纯疱疹病毒生长。Aphidicolin 具有抗正痘病毒活性,能够增强阿拉伯糖基核苷对细胞凋亡 (apoptosis) 的诱导作用。Aphidicolin 是 DNA 聚合酶 α 和 δ 抑制剂,通过干扰 DNA 聚合酶的活性来阻止细胞有丝分裂。Aphidicolin 是一种来源于 Cephalosporium aphidicola 的抗生素, 能够抑制细胞脱氧核糖核酸合成和单纯疱疹病毒生长。Aphidicolin 具有抗正痘病毒活性,能够增强阿拉伯糖基核苷对细胞凋亡 (apoptosis) 的诱导作用。
生物活性
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
性状
Solid
体外研究(In Vitro)
Aphidicolin (0.5 μM, 5 μM; 0-5 d) selectively kills neuroblastoma cells, but shows moderate cytotoxicity on normal human embryonal cells and HeLa, H9, A549 and Caco-2 cell lines.Aphidicolin (0.4 μg/mL; 3 d) arrests cell cycle at G2 phase.Aphidicolin (100 nM-10 μM; 48 h) inhibits cell proliferation via the p53-GADD45β pathway and (1 μM; 24 h) induces apoptosis in AtT-20 cells.Aphidicolin (10 μM; 0-6 h) decreases the phosphorylation of Akt, (100 nM-10 μM; 24 h) increases the mRNA levels of the stress response gene growth arrest and DNA damage-inducible 45β (GADD45β), a putative downstream target of p53.Aphidicolin (10 μM; 0-6 h) inhibits Varicella-zoster virus (VZV) with EC50s of 0.5-0.6 μM, with low cytotoxicity.Medlife has not independently confirmed the accuracy of these methods. They are fo
体内研究(In Vivo)
Aphidicolin, has been developed with higher solubility agent, namely Aphidicolin glycinate (AG; NSC 303812).Aphidicolin glycinate (100 mg/kg; i.p.; once every 3 h; 9 d) shows anti-tumor activity against the implanted B16 melanoma and M5076 sarcoma in murine, producing maximum increased life spans of 75%.Medlife has not independently confirmed the accuracy of these methods. They are for reference only.dy>