|Compound||Structure||Enzyme activity||Biological Effects||Reference(s)|
|SIRT1 EC1.5 a = 46.2 μM||
Improves mitochondrial functions and protects against fat diet-induced obesity (DIO). In obese mice leads to increased health-span and lifespan.|
Promising effects and in clinical trials for the treatment of some diseases of aging (metabolic disorders, type 2 diabetes, etc.).
35 SIRT1 EC1.5 = 2.9 μM|
SIRT1 max act.b 447%
36 SIRT1 EC1.5 = 0.16 μM
SIRT1 max act. 781%
37 SIRT1 EC1.5 = 0.36 μM
SIRT1 max act. 296%
All SRT compounds, with different potencies, improve insulin sensitivity in DIO and genetically obese mice (Lepob/ob), lower plasma glucose and increase mitochondrial capacity.|
In Zucker fa/fa rats, improve whole-body glucose homeostasis, insulin sensitivity in adipose tissue, skeletal muscle and liver, and mitochondrial bioenergetics in a SIRT-1 dependent manner.
Very good activities in different age-related disease conditions.
SIRT1 EC1.5 = 1.2 μM|
SIRT1 max act. 890%
|Promising activities in different age-related disease models: obesity and metabolic disorders, inflammatory and autoimmune disorders, cardiovascular disease, hepatic steatosis, neurodegeneration, and cancer.||[99–101]|
SIRT1 EC1.5 = 0.5 μM|
SIRT1 max act. 220%
40 SIRT1 EC1.5 = 0.3 μM|
SIRT1 max act. 253%
41 SIRT1 EC1.5 = 0.4 μM
SIRT1 max act. 820%
EC1.5 < 250 nM|
SIRT1 max act. ≥300%
|Not reported.||[99–101, 103]|
SIRT1 EC1.5 = 0.4 μM|
SIRT1 max act. 1310%
|Promising activities in different age-related disease models: obesity and metabolic disorders, inflammatory and autoimmune disorders, cardiovascular disease, hepatic steatosis, neurodegeneration, and cancer.||[99–101, 104]|
46a (MC2562) (Ar = Ph, R1 = OEt, R2 = benzyl):|
SIRT1 EC1.5 ≈ 1 μM
SIRT2 EC1.5 = 25 μM
SIRT3 EC1.5 ≈ 50 μM
Induce α-tubulin hypoacetylation in U937 cells and reduce the number of senescent cells of 30-40% in human mesenchymal stem cells.|
Increase NO release in HaCat cells, and accelerate tissue renewal in a mouse model of skin repair. In C2C12 myoblasts improve mitochondrial density and functions through activation of the SIRT1/AMPK axis. A water-soluble analog displays antiproliferative effect and increased H4K16 deacetylation in a panel of human cancer cells at 8-35 μM
Increases SIRT3 levels by nearly two-fold @5μM and 10μM in cardiomyocytes after 24h treatment.|
In vitro directly binds to SIRT3 and increases the affinity of SIRT3 for NAD+.
Blocks hypertrofic response of cardiomyocytes in vitro.|
Protects mice from developing cardiac hypertrophy, attenuates pre-established cardiac hypertrophy in mice, reduces ROS production and prevents cardiomyocyte death in a SIRT3-dependent manner.