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 ofDNApolymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is anantibioticproduced by moldCephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiatesapoptosisinduced by arabinosyl nucleosides in a human promyelocytic leukemia cell line[1][2][3]. |
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[4].
Aphidicolin (0.4 μg/mL; 3 d) arrests cell cycle at G2 phase[5].
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[6].
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[6].
Aphidicolin (10 μM; 0-6 h) inhibits Varicella-zoster virus (VZV) with EC50s of 0.5-0.6 μM, with low cytotoxicity[7].
Cell Cytotoxicity Assay[4] | Cell Line: | NB cell lines: UKF-NB-1/2/3 and IMR-32 | | Concentration: | 0.5 μM, 5μM | | Incubation Time: | 1, 2, 3, 4, 5 days | | Result: | Resulted in cellular enlargement and extension of cellular processes before cell lysis occurred. |
Cell Cycle Analysis[5] | Cell Line: | Normal human diploid cells | | Concentration: | 0.4 μg/mL | | Incubation Time: | 3 days or 7 days | | Result: | Resulted more than 80% of the cells moved through S phase and were accumulated at G2 phase.
Inbihited the growth of the cells completely without causing apparent cell death. |
Western Blot Analysis[6] | Cell Line: | AtT-20 cells pituitary corticotroph tumor cells | | Concentration: | 10 μM | | Incubation Time: | 0 min, 5 min, 30 min, 2 h, 6 h, 24 h | | Result: | Inhibited Akt phosphorylation in AtT-20 cells during 5 min-2 h, in a time-dependent manner.
Increased protein level of p27 during 30 min-6 h, and remarkably increased p53 level at 24 h. |
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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%[8].
| Animal Model: | M5076 sarcoma s.c. model or B16 melanoma i.p. model in murine[8] | | Dosage: | 60 mg/kg, 100 mg/kg, 300 mg/kg | | Administration: | Intraperitoneal injection; once every 3 h; 9 days | | Result: | Inhibited tumor growth significantly. |
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| 来源 | Cephalosporium aphidicola |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(147.72 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 2.9544 mL | 14.7719 mL | 29.5438 mL | | 5 mM | 0.5909 mL | 2.9544 mL | 5.9088 mL | | 10 mM | 0.2954 mL | 1.4772 mL | 2.9544 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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