COH-SR4 activates AMPK and exhibits strong anti-proliferative effects against leukemia, melanoma, breast, and lung cancers. It hinders adipocyte differentiation by activating AMPK. COH-SR4 is a valuable tool for studying obesity and associated metabolic disorders[1].
体内研究
COH-SR4 (5 mg/kg; i.g.; 3x/week; for 6 weeks) decreases body weight and fat mass in high-fat diet (HFD) obese mice without impacting food intake[2].
COH-SR4 enhances glycemic control and improves dyslipidemia in high-fat diet (HFD) obese mice[2].
COH-SR4 reduces adipose tissue hypertrophy and influences circulating adipokine levels in high-fat diet (HFD) obese mice[2].
COH-SR4 inhibits the build-up of hepatic lipids and fatty liver in obese mice on a high-fat diet (HFD)[2].
体外研究
COH-SR4 (1-5 μM; 24 hours) induces a dose-dependent rise in AMPK phosphorylation and its substrate ACC in 3T3-L1 preadipocytes, as well as in cancer cells like HL-60, HeLa, MCF-7[1].
COH-SR4 (3-5 µM; 7 days) effectively inhibits the differentiation of 3T3-L1 adipocytes in a dose-dependent manner[1].
COH-SR4 markedly decreases intracellular lipid accumulation and suppresses the expression of crucial adipogenesis-related transcription factors and lipogenic proteins[1].
COH-SR4 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A549 cells
1, 3, 5, 10 μM
4 h
SR4 activated phosphorylation of AMPK and ACC in LKB1-deficient A549 cells, indicating its AMPK activation is independent of LKB1 and CaMKKβ.
PLoS One. 2013 Dec 20;8(12):e83801
HepG2 cells
1, 3, 5, 10 μM
4 h
SR4 increased phosphorylation of AMPK and ACC in a concentration-dependent manner, similar to the AMPK activator AICAR.
PLoS One. 2013 Dec 20;8(12):e83801
HAVSMC cells
0–200 μM
96 h
To evaluate the effect of SR4 on the survival of HAVSMC cells, results showed SR4 did not cause significant cytotoxicity.
Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
A2058 cells
11 ± 2 μM (IC50)
96 h
To evaluate the effect of SR4 on the survival of A2058 cells, results showed SR4 significantly inhibited cell survival.
Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
Hs600T cells
6 ± 1 μM (IC50)
96 h
To evaluate the effect of SR4 on the survival of Hs600T cells, results showed SR4 significantly inhibited cell survival.
Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
B16-F0 cells
5 ± 1 μM (IC50)
96 h
To evaluate the effect of SR4 on the survival of B16-F0 cells, results showed SR4 significantly inhibited cell survival.
Biochem Pharmacol. 2012 Dec 1;84(11):1419-27
COH-SR4 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
High-fat diet-induced obese mice
Oral
5 mg/kg
Three times a week for 6 weeks
SR4 significantly reduced body weight and fat mass in HFD-induced obese mice, improved glycemic control and insulin sensitivity, lowered plasma lipid levels, prevented hepatic steatosis, and increased AMPK activation in liver and adipose tissues.
PLoS One. 2013 Dec 20;8(12):e83801
C57B mice and Hsd: Athymic nude nu/nu mice
B16-F0 mouse melanoma model and A2058 human melanoma mouse xenograft model
Oral gavage
4 mg/kg
Alternate day administration for 8 weeks
To evaluate the anti-tumor effect of SR4 in vivo, results showed SR4 significantly inhibited tumor burden and was well tolerated.
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