In vitro: HepG2 cells are treated with various concentrations of AICAR (0.1-1.0 mM) for 12, 24, and 48 h, respectively. The expression level of IR-β significantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48 h to 50%, 53%, and 46% of the control, respectively.
In vivo: Fourteen-week-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injected with the AMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg/g per day or saline control (C) for 14 days. At 24 h after the last injection (including a 12-h fast), all mice are killed, and the plantar flexor complex muscle (gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC (159±12 mg) than LC, LA, and OA (176±10, 178±9, and 166±16 mg, respectively) mice, independent of a body weight change. The kidney weight is significantly higher in the untreated group when compared with both the exercise and AICAR (0.5 mg/g body wt) groups. The heart weight is higher in the exercise group than in the other groups, whereas the liver weight is significantly higher in the AICAR-treated group when compared with the exercise and untreated groups.
|Source||Sci Rep (2018). Figure 1. AICAR|
|Method||Cytometric bead array assays|
|Cell Lines||Human peripheral blood mononuclear cells|
|Incubation Time||24 h|
|Results||Inhibition of adenosine kinase-mediated AICAR phosphorylation to ZMP, using the inhibitor ABT-702, left suppression of LPS-induced target genes by AICAR unaltered and even potentiated the effect of low AICAR concentrations, suggesting an AMPK-independent effect.|
|Cell lines||K562 cell lines|
|Preparation method||Acadesine is added to K562 cell lines or primary cells (103 CD34+ cells/mL) growing in semisolid methyl cellulose medium. MethoCult H4100 or H4236 are used for cell lines and primary CD34+ cells respectively. Colonies are detected after 10 days of culture by adding 1 mg/mL of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reagent and are scored by Image J quantification software.|
|Incubation time||10 days|
|Animal models||mouse xenograft model of K562 cells|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Acadesine kills chronic myelogenous leukemia (CML) cells through PKC-dependent induction of autophagic cell death.
Robert G, et al. PLoS One. 2009 Nov 18;4(11):e7889. PMID: 19924252.
AICAR, an activator of AMP-activated protein kinase, down-regulates the insulin receptor expression in HepG2 cells.
Nakamaru K, et al. Biochem Biophys Res Commun. 2005 Mar 11;328(2):449-54. PMID: 15694368.
Acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes.
Campas C, et al. Blood. 2003 May 1;101(9):3674-80. PMID: 12522004.
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