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Acyclovir

CAS No. : 59277-89-3

MCE 站：Acyclovir

产品活性：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。

研究领域：Anti-infection  |  Apoptosis

作用靶点：HSV  |  Bacterial  |  Apoptosis  |  Antibiotic

In Vitro: Acyclovir (3-100 ?M; 24-72 hours; Jurkat, U937, and K562 leukemia cells) treatment shows a dose- and time-dependent reduction of cell viability.
Acyclovir (10-100 ?M; 24-72 hours; Jurkat cells) treatment shows a delay/block in S phase and an increase of the sub-G1 peak.
Acyclovir (10-100 ?M; 24-72 hours; Jurkat cells) treatment activates caspase-3 and presences nuclear DNA fragmentation, thereby indicating apoptotic cell death.
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.

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.

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