Hergenhahn M, Fürstenberger G, Opferkuch H J, Adolf W, Mack H, Hecker E
J Cancer Res Clin Oncol. 1982;104(1-2):31-9. doi: 10.1007/BF00402051.
The kinetics of the irritant response on the mouse ear [erythema measured quantitatively by the irritant dose 50 (ID50)] and its relation to the initiation-promoting activity on the back skin of NMRI mice of some polyfunctional diterpene esters were investigated: (1) A very rapid and transient erythema response is associated with low or absent promoting activity (2) an early and more persistent erythema response in most cases is associated with moderate-to-high promoting activity, and (3) a relatively late onset but persistence up to at least 24 h of the erythema response is associated with high promoting activity. These results may indicate a relationship between the kinetics of the erythema response and the initiation-promoting activity of diterpene esters. The comparatively low promoting activity of esters carrying polyunsaturated acyl functions may indicate the importance of pharmacological parameters such as bioavailability and stability in the biological system, drug-receptor interaction, and "intrinsic activity" of the diterpene esters.
研究了某些多官能二萜酯对小鼠耳部刺激性反应的动力学(通过刺激性剂量50(ID50)定量测量红斑)及其与NMRI小鼠背部皮肤引发促进活性的关系:(1)非常快速且短暂的红斑反应与低促进活性或无促进活性相关;(2)在大多数情况下,早期且更持久的红斑反应与中度至高促进活性相关;(3)红斑反应相对较晚出现但持续至少24小时与高促进活性相关。这些结果可能表明红斑反应动力学与二萜酯的引发促进活性之间存在关系。带有多不饱和酰基官能团的酯的促进活性相对较低,这可能表明诸如生物利用度和在生物系统中的稳定性、药物 - 受体相互作用以及二萜酯的“内在活性”等药理学参数的重要性。