Trichostatin A (TSA) is an antifungal antibiotic derived from Streptomyces that inhibits mammalian histone deacetylase (HDAC). TSA inhibits the eukaryotic cell cycle during the beginning of the growth stage. Trichostatin A (TSA) can be used to alter gene expression by interfering with the removal of acetyl groups from histones (histone deacetylases, HDAC) and therefore altering the ability of DNA transcription factors to access the DNA molecules inside chromatin. It is a member of a larger class of histone deacetylase inhibitors (HDIs or HDACIs) that have a broad spectrum of epigenetic activities. Trichostatin A has also been shown to inhibit both G1- and G2-phases of the mammalian cell cycle and has been tested for use as a potential anticancer agent.
|Cell lines||MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3 cell lines|
|Preparation method||Cell Proliferation Assay.
Stock cultures of breast cancer cell lines MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, CAL 51, and SK-BR-3 (American Type Culture Collection, Rockville, MD) were grown in DMEM containing 10% (v/v) FCS, 2 mM L-glutamine, 100 units/ml penicillin, and 100 mg/ml streptomycin at 37°C in 5% CO2 humidified atmosphere. Cells were counted in a hemocytometer after detachment using 0.25% (w/v) trypsin in Dulbecco’s PBS without Ca21 or Mg21 (DPBS; Sigma-Aldrich) containing 0.02% (w/v) EDTA. Viability was determined by trypan blue exclusion. For each cell line, cells were seeded in 96-well microtiter plates at optimal densities determined in prior experiments to ensure exponential growth for the duration of the assay. After a 24-h preincubation, growth medium was replaced with experimental medium containing TSA at final concentrations ranging from 10-12 M to 10-5 M in log dilutions and 0.1% (v/v) ethanol, or growth medium containing 0.1% (v/v) ethanol as a vehicle control. After 96 h incubation, cell proliferation was estimated using the sulforhodamine B colorimetric assay (11), and the results are expressed as the mean 6 SD for six replicates as a percentage of vehicle control (taken as 100%).
|Concentrations||10-12 M to 10-5 M|
|Incubation time||96 h|
|Animal models||Inbred virgin female (Ludwig/Wistar/ Olac) rats bearing tumors induced with NMU model|
|Dosages||500 µg/kg TSA in50 µl DMSO twice weekly for 4 weeks|
|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 23 mg/mL|
Trichostatin A selectively suppresses the cold-induced transcription of the ZmDREB1 gene in maize.
Hu et al. PLoS One. 2011;6(7):e22132. PMID: 21811564.
Trichostatin A attenuates airway inflammation in mouse asthma model.
Choi et al. Clin Exp Allergy. 2005 Jan;35(1):89-96. PMID: 15649272.
Trichostatin A induces differential cell cycle arrests but does not induce apoptosis in primary cultures of mitogen-stimulated rat hepatocytes.
Papeleu et al. J Hepatol. 2003 Sep;39(3):374-82. PMID: 12927923.
Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo.
Vigushin et al. Clin Cancer Res. 2001 Apr;7(4):971-6. PMID: 11309348.
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