3-TYP is a selective SIRT3 inhibitor with an IC50 value of 16 nM, which is more potent over SIRT1 and SIRT2. 3-TYP significantly attenuates melatonin-induced increases in deacetylated-SOD2 expression and SOD2 activity in HepG2 cells exposed to Cd.
In vivo, 3-TYP significantly decreases SIRT3 activity and increases the acetylation of SOD2 compared with that in the control group, without influencing SIRT3 expression. 3-TYP attenuates the cardioprotective effects of melatonin by decreasing the LVEF and LVFS after 24 hour of reperfusion. 3-TYP also increases the infarct size, serum LDH levels, and apoptotic ratio compared with those in the IR+Mel group.
|Cell lines||HepG2 cells|
|Preparation method||Cells are randomly divided into the following treatment groups: 10 μM Cd; melatonin (1 μM)+10 μM Cd; 3-TYP (50 μM)+10 μM Cd; and 3-TYP (50 μM)+melatonin (1 μM)+10 μM Cd. cells are treated for 12 h. The role of the SIRT3-SOD2 pathway in hepatic cell protection after melatonin pretreatment is investigated.|
|Incubation time||12 h|
|Animal models||Sprague-Dawley rats|
|Formulation||ethanol (70%), propylene glycol (20%), NaHCO3 (10%)|
|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: ≥ 25 mg/mL|
Melatonin ameliorates myocardial ischemia reperfusion injury through SIRT3-dependent regulation of oxidative stress and apoptosis.
Zhai M, et al. J Pineal Res. 2017 Sep;63(2). PMID: 28500761.
Polydatin ameliorates injury to the small intestine induced by hemorrhagic shock via SIRT3 activation-mediated mitochondrial protection.
Zeng Z, et al. Expert Opin Ther Targets. 2016 Jun;20(6):645-52. PMID: 27067422.
SIRT3-SOD2-mROS-dependent autophagy in cadmium-induced hepatotoxicity and salvage by melatonin.
Pi H, et al. Autophagy. 2015;11(7):1037-51. PMID: 26120888.
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