Aciclovir sodium

Acyclovir (Aciclovir) sodium is a potent, orally active antiviral agent. Acyclovir sodium has antiherpetic activity with IC50 values of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir sodium induces cell cycle perturbation and apoptosis. Acyclovir sodium prevents bacterial infections during induction therapy for acute leukaemia[1][2][3][4].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Anti-infection >> HSV

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

HSV-1:0.85 μM (IC50)

HSV-2:0.86 μM (IC50)

Acyclovir (Aciclovir) sodium (3-100 µM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) reduces cell viability in a dose- and time-dependent[1]. Acyclovir (Aciclovir) sodium (10-100 µM; 24-72 hours; Jurkat cells) blocks DNA synthesis, thereby arresting the cell cycle in G2/M and S phases and increasing the sub-G1 hypodiploid peak in a dose-dependent manner[1]. Acyclovir (Aciclovir) sodium (10-100 µM; 24-72 hours; Jurkat cells) induces apoptosis through activates caspase-3 and presences nuclear DNA fragmentation[1]. Cell Viability Assay[1] Cell Line: Jurkat, U937 and K562 leukemia cells Concentration: 3, 10, 30 and 100 µM Incubation Time: 24, 48 and 72 hours Result: Showed a dose- and time-dependent reduction of cell viability. Apoptosis Analysis[1] Cell Line: Jurkat cells Concentration: 10 and 100 µM Incubation Time: 24, 48 and 72 hours Result: Increased of caspase-3 activity and cleavaged the internucleosomal DNA. Cell Cycle Analysis[1] Cell Line: Jurkat cells Concentration: 10 and 100 µM Incubation Time: 24, 48 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.

Acyclovir (Aciclovir) sodium (20 mg/kg; p.o.; three times daily; for 10 d; BALB/c mice) suppresses the development of skin lesions and results in a dissociation between DTH response and antibody production[3] Animal Model: Specific-pathogen-free BALB/c mice (7-week-old) infected with HSV-1[3] 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.

[1]. 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.

[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]. 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.

[4]. 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.

MOLECULAR FORMULA :

C8-H10-N5-O3.Na

MOLECULAR WEIGHT :

247.22

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

107 mg/kg/5D-I

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - child

DOSE/DURATION :

248 mg/kg/80H-I

TOXIC EFFECTS :

Gastrointestinal - nausea or vomiting

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>20 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

1210 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity)

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

650 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>600 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>10 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

999 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity)

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

405 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - ataxia

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

1550 mg/kg/31D-I

TOXIC EFFECTS :

Gastrointestinal - other changes Kidney, Ureter, Bladder - urine volume decreased Related to Chronic Data - death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

300 mg/kg

SEX/DURATION :

female 10 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

300 mg/kg

SEX/DURATION :

female 10 day(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

300 mg/kg

SEX/DURATION :

female 10 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - delayed effects

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

100 mg/kg

SEX/DURATION :

female 10 day(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - endocrine system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

MUTATION DATA

TEST SYSTEM :

Rodent - mouse

DOSE/DURATION :

1995 umol/kg/24H (Intermittent)

REFERENCE :

MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 369,65,1996