Mufson R A, Simsiman R C, Boutwell R K
Cancer Res. 1977 Mar;37(3):665-9.
To measure the in vivo levels of cyclic adenosine 3':5'-monophosphate (cyclic AMP) in mouse skin, precautions must be taken to avoid artifactual alterations after excision of the skin from the mouse. With such precautions, the level of cyclic AMP in mouse epidermal-dermal preparations was unchanged 1 to 18 hr after application of 12-O-tetradecanoylphorbol-13-acetate (TPA) to mouse skin. The accumulation of cyclic AMP in response to isoproterenol or the naturally occurring catecholamine epinephrine was, however, significantly diminished 9 to 24 hr after application of TPA. No enhanced accumulation of cyclic AMP in response to alpha-adrenergic stimulation accompanied this diminished beta-adrenergic responsiveness. Experiments with pure epidermis confirmed that these observations reflected the effects of TPA on the epidermal cells in the epidermal-dermal preparations. The metabolism of isoproterenol in TPA-treated epidermis was the same as that in control epidermis. Finally, the tumor-promoting activity of various doses of TPA and of other phorbol esters correlated with their ability to diminish the beta-adrenergic responsiveness of the epidermis.
为了测量小鼠皮肤中3':5'-环磷酸腺苷(环磷腺苷)的体内水平,必须采取预防措施,以避免从小鼠身上切除皮肤后出现人为改变。采取这些预防措施后,在将12-O-十四酰佛波醇-13-乙酸酯(TPA)应用于小鼠皮肤后1至18小时,小鼠表皮-真皮制剂中环磷腺苷的水平没有变化。然而,在应用TPA后9至24小时,对异丙肾上腺素或天然存在的儿茶酚胺肾上腺素产生反应的环磷腺苷积累显著减少。β-肾上腺素能反应性降低的同时,并未伴随α-肾上腺素能刺激引起的环磷腺苷积累增强。对纯表皮进行的实验证实,这些观察结果反映了TPA对表皮-真皮制剂中表皮细胞的影响。TPA处理的表皮中异丙肾上腺素的代谢与对照表皮中的相同。最后,不同剂量的TPA和其他佛波酯的促肿瘤活性与其降低表皮β-肾上腺素能反应性的能力相关。