Plicamycin binds to the minor groove of DNA at GC-rich sites, resulting in inhibition of RNA synthesis; this agent also inhibits mRNA expression, resulting in a reduction in protein synthesis. In addition, plicamycin may inhibit bone resorption by down regulating transcription of c-src, an oncogene involved in bone metabolism and resorption.
In vivo, the antitumorigenic activity of Plicamycin (0.2 mg/kg/day) is determined in a xenograft model and observed reduction in tumor volume and weight. No significant mouse body weight loss is observed in Plicamycin-treatment groups, indicating that Plicamycin-associated toxicity is minimal. Plicamycin also increases TUNEL-positive cells in tumor xenografts.
|Cell lines||HEp-2 cells and KB cells|
|Preparation method||HEp-2 cells and KB cells are cultured in DMEM 100 U/mL each of Penicillin and Streptomycin and 10% FBS for HEp-2 cells and 5% FBS for KB in a humidified atmosphere containing 5% CO2 at 37°C. Equal numbers of cells are seeded and allowed to attach. At 50-60% confluence, cells are treated with DMSO or indicated concentrations of Plicamycin (50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells). After treatment, 30 µL MTS solution is added to each well and cells are incubated for 2 h at 37°C. MTS solution is analyzed using a microplate reader at 490 nm and 690 nm.|
|Concentrations||50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells|
|Animal models||Female nude mice|
|Dosages||0.2 mg/kg/day, three times per week for 29 days|
|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 14 mg/mL|
Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer.
Choi ES, et al. Sci Rep. 2014 Nov 24;4:7162. PMID: 25418289.
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