Sirtuin (Sirt) 1 and 2 are members of the NAD+-dependent class III histone deacetylase family that are involved in various cellular events, such as transcriptional silencing, chromatin remodeling, and lifespan duration. Salermide is a potent inhibitor of both Sirt1 and Sirt2. It dose-dependently inhibited human Sirt1 protein with 80% inhibition at 90μM. Salermide shows more efficient inhibitory effect on Sirt2 with 80% inhibition at 25μM. Treatment with 100μM Salermide for 24h induced the decrease of cell numbers in cancer cell lines derived from leukaemia (MOLT4, KG1A, K562), lymphoma (Raji), colon (SW480) and breast (MDA-MB-231) primary malignancies, but not in non-tumorigenic MRC5 cells. The IC50 values of Salermide in MOLT4, MDA-MB-231 and SW480 cancer cells were around 20, 110, and 100 μM, respectively. After 72-h incubation with 100 μM Salermide, only 10% of KG1A cells and 50% of Raji and K562 cells were viable. An increase of cytosolic-activated caspase 3 and a decrease of mitochondrial-cytochrome c were observed in Salermide-treated cells 2h post treatment. Twenty-four-hour incubation of 25 and 100μM Salermide induced slight tubulin acetylation in MOLT4, MDA-MB-231 and SW480 cells. Intraperitoneal injection of 100μM Salermide over 34 days in nude mice showed no apparent toxicity as monitored by diet consumption, body-weight gain, and postural and behavioral changes[2].
Salermide 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Acanthamoeba castellanii trophozoites
100 µM
24 and 48 hours
Inhibited the proliferation of Acanthamoeba castellanii trophozoites
Parasit Vectors. 2020 Jul 22;13(1):368.
H1650
20 µM
24 hours
To evaluate the apoptosis effect of Salermide on H1650 cells, results showed H1650 cells were particularly sensitive to Salermide.
J Cell Mol Med. 2012 Jul;16(7):1618-28.
HCT116 Oxa-R cells
20 µM
24 hours
To evaluate the effect of CAY10602 on oxaliplatin resistance, results showed that CAY10602 enhancement of SIRT1 expression decreased the resistance of HCT116 Oxa-R cells to oxaliplatin.
World J Gastroenterol. 2025 Mar 21;31(11):100785.
HCT116 Oxa-R cells
10 µM
24 hours
To evaluate the effect of Salermide on oxaliplatin resistance, results showed that Salermide inhibition of SIRT1 expression increased the resistance of HCT116 Oxa-R cells to oxaliplatin.
World J Gastroenterol. 2025 Mar 21;31(11):100785.
BxPC-3 cells
5-100 µM
24 hours
To evaluate the effect of Salermide alone or in combination with EF24 on the viability of BxPC-3 cells. Results showed that Salermide alone significantly reduced the viability of BxPC-3 cells with an IC50 value of approximately 40 µM.
EXCLI J. 2016 Apr 4;15:246-55.
H157
50 µM
24, 48 hours
To evaluate the time-dependent apoptosis induced by Salermide, results showed apoptosis started at 24 hrs and peaked at 48 hrs.
J Cell Mol Med. 2012 Jul;16(7):1618-28.
Acanthamoeba castellanii trophozoites
100 µM
24, 48, 72 hours
Inhibited the proliferation of Acanthamoeba castellanii trophozoites
Parasit Vectors. 2020 Jul 22;13(1):368.
Human brain microvascular endothelial cells and astrocytes co-culture model
50 µM
30 min pretreatment
Sirt1 inhibition significantly reduced BBB permeability (increased TEER) and attenuated OGD-induced apoptosis and mitochondrial ROS generation
Redox Biol. 2018 Apr;14:229-236.
SKOV-3 cells
50 µM
48 hours
Comparison of anticancer effects between MHY2256 and salermide in SKOV-3 cells, showing IC50 values of salermide as 36.5-50.9 μM
Int J Biol Sci. 2016 Dec 6;12(12):1555-1567.
MCF-7 cells
50 µM
48 hours
Comparison of anticancer effects between MHY2256 and salermide in MCF-7 cells, showing IC50 values of salermide as 36.5-50.9 μM
Int J Biol Sci. 2016 Dec 6;12(12):1555-1567.
H1792
12.5, 25, 50 µM
48 hours
To evaluate the effect of Salermide on cell growth, results showed Salermide induced growth inhibition in a concentration-dependent manner.
J Cell Mol Med. 2012 Jul;16(7):1618-28.
Ishikawa endometrial cancer cells
0.1–50 µM
48 hours
To compare the cytotoxicity of MHY2256 and Salermide on Ishikawa cells. Results showed that the IC50 value of MHY2256 was approximately 10-fold lower than that of salermide.
Int J Mol Sci. 2018 Sep 13;19(9):2743.
LLCMK2 cells
2 µM
48 hours
Salermide reduced the number of intracellular parasites in vitro infection assays with minimal effects on host cell viability.
Inhibited the encystation of Acanthamoeba castellanii
Parasit Vectors. 2020 Jul 22;13(1):368.
Salermide 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Zebrafish
Dmd mutant zebrafish
Embryo bath
1 μM
From 1 dpf to 4 dpf, changing the treatment solution daily
To evaluate the effect of Salermide in combination with oxamflatin on the skeletal muscle structure of dmd mutant zebrafish. Results showed that the combination significantly ameliorated skeletal muscle degeneration.
Skelet Muscle. 2020 Oct 15;10(1):29
BALB/c nude mice
Subcutaneous xenograft model of HCT116 Oxa-R cells in nude mice
Subcutaneous injection
10 mg/kg
Three times a week until tumor volume reached 1500 mm³
To evaluate the effect of CAY10602 on oxaliplatin resistance, results showed that CAY10602 enhanced the growth-inhibitory effect of oxaliplatin on HCT116 Oxa-R cells.
World J Gastroenterol. 2025 Mar 21;31(11):100785.
BALB/c mice
Chagas disease model
Intraperitoneal injection
100 μM
Daily for 12 days
Salermide partially controlled in vivo infection, reducing parasitemia.
Evaluation of the antitumor effects of salermide in the MCF-7 xenograft model, showing significant inhibition of tumor growth
Int J Biol Sci. 2016 Dec 6;12(12):1555-1567.
Nude mice
Ishikawa endometrial cancer cell xenograft model
Intraperitoneal injection
30 mg/kg
Once per week for 30 days
To evaluate the antitumor effect of Salermide on Ishikawa cell xenograft model. Results showed that salermide significantly inhibited tumor growth.
Int J Mol Sci. 2018 Sep 13;19(9):2743.
Mice
Photothrombotic stroke model
Intracerebroventricular injection
400 μM
Single administration, 1 hour after stroke
To study the effect of Salermide on infarction volume and apoptotic index after stroke. Results showed that Salermide did not significantly alter infarction volume or apoptotic index compared to control samples.
搜索
