生物活性

• 描述Protein kinase C (PKC) is a key molecule involved in cell growth, apoptosis, and differentiation. Phorbol 12-Myristate 13-Acetate (PMA) is an activator of certain types of PKC, including group A and group B isoforms^[3]. Stimulation with 1 μM PMA for 3 min resulted in promoted nucleotide exchange activity in 293T cells^[4]. In differentiated Caco-2 cells, pretreatment with 100 nM PMA for 5 min followed by 2h incubation with 10 nM 1,25(OH)₂D₃ resulted in a 2.6-fold increase in hCYP24A1 mRNA level compared to cells treated by 1,25(OH)₂D₃ alone. Incubation with 100 nM PMA for 30 min resulted in the activation of ERK1/2 and p38 kinase in Caco-2 cells, whereas pretreatment with the MEK inhibitor U0126 at 10, 20 or 100 μM completely inhibited ERK1/2 activation by PMA and partially suppressed PMA-induced p38 kinase activation. Cells pre-treated with 10 μM U0126 or 8 μM p38 kinase inhibitor SB202190 showed reduced enhancing effect of PMA on 1,25(OH)₂D₃-induced hCYP24A1 promoter activity^[5]. In both W/W^v genetically mast cell-deficient mice and congenic normal mice, repeated administration of PMA (5 μg, 3 times per week for 6 weeks) to the ear skin remarkably increased the number of dermal mast cells^[6].
• 作用机制PMA is a phorbol ester structurally analogous to diacylglycerol. It activates PKC isoforms by associating with their C1 domains^[7].

• 动物研究
  剂量	Rat: 1.5 mg/kg - 3 mg/kg[3] (intrarectal instillation); 230 μg/kg[4] (i.v.)
  给药途径	Intrarectal instillation, i.v.