Acyclovir(Synonyms: 阿昔洛韦; Aciclovir; Acycloguanosine)

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Acyclovir (Synonyms: 阿昔洛韦; Aciclovir; Acycloguanosine) 纯度: 99.34%

Acyclovir (Aciclovir) 是一种鸟嘌呤类似物和一种具有口服活性的抗病毒剂。Acyclovir 具有抗 HSV-1 (IC50 为 0.85 μM),HSV-2 (IC50 为 0.86 μM) 和水痘带状疱疹病毒的活性。Acyclovir 可被病毒胸苷激酶 (TK) 磷酸化,Acyclovir triphosphate 可干扰病毒 DNA 聚合。Acyclovir 可预防急性白血病的诱导疗法中的细菌感染。

Acyclovir(Synonyms: 阿昔洛韦; Aciclovir;  Acycloguanosine)

Acyclovir Chemical Structure

CAS No. : 59277-89-3

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生物活性

Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].

IC50 & Target[1][2]

HSV-1

0.85 μM (IC50)

HSV-2

0.86 μM (IC50)

Bacterial

 

体外研究
(In Vitro)

Acyclovir (3-100 µM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) treatment shows a dose- and time-dependent reduction of cell viability[3].
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment shows a delay/block in S phase and an increase of the sub-G1 peak[3].
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment activates caspase-3 and presences nuclear DNA fragmentation, thereby indicating apoptotic cell death[3].
In HSV-infected cells, HSV thymidine kinase (HSV-TK) specifically phosphorylate Acyclovir to its monophosphate, and this activation confers a high degree of selectivity of the drugs. Thereafter, the monophosphate is further phosphorylated to the diphosphate (Acyclovir -DP) and triphosphate (Acyclovir -TP) by cellular kinases. The triphosphate is the fully activated metabolite that is toxic to the virus[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Jurkat, U937, and K562 leukemia cells
Concentration: 3 µM, 10 µM, 30 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Showed a dose- and time-dependent reduction of cell viability.

Cell Cycle Analysis[3]

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Revealed a dose-dependent accumulation of cells in S phase after 24 and 48 h. Showed a dose-dependent increase of the sub-G1 hypodiploid peak after 72 h.

Apoptosis Analysis[3]

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Induced cell apoptosis.

体内研究
(In Vivo)

Acyclovir (20 mg/kg; oral administration; three times daily; for 10 days; BALB/c mice) treatment in infected mice suppresses the development of skin lesions and results in a dissociation between DTH response and antibody production[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Specific-pathogen-free BALB/c mice (7-week-old) infected with HSV-1[1]
Dosage: 20 mg/kg
Administration: Oral administration; three times daily; for 10 days
Result: Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production.

Clinical Trial

分子量

225.20

Formula

C8H11N5O3

CAS 号

59277-89-3

中文名称

阿昔洛韦;阿昔洛维;开糖环鸟苷;羟乙氧甲鸟嘌呤;无环鸟嘌呤核苷;无环鸟嘌呤;无环鸟苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (222.02 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4405 mL 22.2025 mL 44.4050 mL
5 mM 0.8881 mL 4.4405 mL 8.8810 mL
10 mM 0.4440 mL 2.2202 mL 4.4405 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.10 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.10 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Li Z, et al. Acyclovir treatment of skin lesions results in immune deviation in mice infected cutaneously with herpes simplex virus. Antivir Chem Chemother. 1999 Sep;10(5):251-7.

    [2]. Suzuki M, et al. Synergistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61.

    [3]. Benedetti S, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity. Life Sci. 2018 Dec 15;215:80-85.

    [4]. Hayashi K, et al. The role of a HSV thymidine kinase stimulating substance, scopadulciol, in improving the efficacy of cancer gene therapy. J Gene Med. 2006 Aug;8(8):1056-67.

    [5]. Lönnqvist B, et al. Oral acyclovir as prophylaxis for bacterial infections during induction therapy for acute leukaemia in adults. The Leukemia Group of Middle Sweden. Support Care Cancer. 1993 May;1(3):139-44.

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