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(+)-Aphidicolin

四环二萜类抗生素，Aphidicolin 是 DNA 聚合酶 α 和 δ 的抑制剂，通过干扰 DNA 聚合酶的活性来阻止有丝分裂细胞分裂。Aphidicolin 是 Cephalosporium aphidicola 产生的抗生素, 它是细胞脱氧核糖核酸合成的有效抑制剂，并且强烈抑制单纯疱疹病毒的生长。Aphidicolin 通过人早幼粒细胞白血病细胞系中阿拉伯糖基核苷诱导细胞凋亡(apoptosis)。

目录号: PC12988 纯度: ≥98%

CAS No. :38966-21-1

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中文名称

(+)-Aphidicolin

中文别名

8,11伪-Methano-11aH-cyclohepta[a]naphthalene-4,9-dimethanol,tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3R,4R,4aR,6aS,8R,9R,11aS,11bS)-;艾菲地可宁;(+)-阿非迪霉素;8,11伪-Methano-11aH-cyclohepta[a]naphthalene-4,9-dimethanol,tetradecahydro-3,9-dihydroxy-4,11b-...;阿非迪霉素;阿非科林

英文名称

(+)-Aphidicolin

英文别名

(+)-Aphidicolin;(+)-Aphidicolin (NSC234714, BRN4689958, ICI69653 );ALLOPHYCOCYANIN;Aphidicolin;9-dimethanol,tetradecahydro-3,9-11a-methano-11ah-cyclohepta(a)naphthalene-4;APC;Apchidicolin;Aphidicholin;Aphidicolin from Nigrospora sphaerica;aphidocolin;ICI 69653;NSC 234714;NSC234714;MLS000069677;192TJ6PP19;SMR000058538;8,11

Cas No.

38966-21-1

分子式

C₂₀H₃₄O₄

分子量

338.48

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

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 for reference only.

Cell Cytotoxicity Assay

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

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

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.

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.

Animal Model:	M5076 sarcoma s.c. model or B16 melanoma i.p. model in murine
Dosage:	60 mg/kg, 100 mg/kg, 300 mg/kg
Administration:	Intraperitoneal injection; once every 3 h; 9 days
Result:	Inhibited tumor growth significantly.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

结构分类

来源

Cephalosporium aphidicola

参考文献

[1]. Dresler SL, et al. Involvement of DNA polymerase delta in DNA repair synthesis in human fibroblasts at late times after ultraviolet irradiation. Biochemistry. 1988 Aug 23;27(17):6379-83. [Information]

[2]. Bucknall RA, et al. Antiviral effects of aphidicolin, a new antibiotic produced by Cephalosporium aphidicola. Antimicrob Agents Chemother. 1973 Sep;4(3):294-8. [Information]

[3]. Kuwakado K, et al. Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemiacell lines. Biochem Pharmacol. 1993 Dec 3;46(11):1909-16. [Information]

[4]. Cinatl J, et al. Aphidicolin selectively kills neuroblastoma cells 体外研究. Cancer Lett. 1992 Dec 24;67(2-3):199-206. [Information]

[5]. Kageyama K, et al. Aphidicolin inhibits cell proliferation via the p53-GADD45β pathway in AtT-20 cells. Endocr J. 2015;62(7):645-54. [Information]

[6]. Fukuda M, Ohashi M. Aphidicolin inhibits cell growth by accumulation of G2 cells. Cell Biol Int Rep. 1983 Aug;7(8):579-85. [Information]

[7]. Rowe J, et al. Compounds that target host cell proteins prevent varicella-zoster virus replication in culture, ex vivo, and in SCID-Hu mice. Antiviral Res. 2010 Jun;86(3):276-85. [Information]

[8]. ODwyer PJ, et al. Antitumor activity and biochemical effects of aphidicolin glycinate (NSC 303812) alone and in combination with cisplatin in vivo. Cancer Res. 1994 Feb 1;54(3):724-9. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (147.72 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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