Vanina V I, Kovalitskaia Iu A, Kolobov A A, Kampe-Nemm E A, Zolotarev Iu A, Iurovskiĭ V V, Lipkin V M, Navolotskaia E V
Bioorg Khim. 2006 Sep-Oct;32(5):477-84. doi: 10.1134/s1068162006050050.
We found that the tritium-labeled synthetic ACTH-like octapeptide leucocorticotropin corresponding to the 81-88 sequence of the precursor of human interleukin-1alpha ([3H]GKVLKKRR) is bound by the ACTH receptor of rat adrenal cortex with a high affinity and specificity (Kd 2.2 +/- 0.1 nM). This peptide was shown to exert no effect on the adenylate cyclase activity of the membranes of rat adrenal cortex in the concentration range from 1 to 1000 nM. Leucocorticotropin administration three times at doses of 10-20 microg/animal did not change the level of hydroxycorticosteroids (11-HOCS) in the rat adrenal glands in the absence of temperature action. At the same time, the peptide abolishes (at a dose of 20 microg/animal, three times) or significantly decreases (at a dose of 10 microg/animal, three times) the dramatic increase in the 11-HOCS content in the adrenal glands occurring in the case of cold or heat shock. Thus, leucocorticotropin normalizes the 11-HOCS level in the rat adrenal cortex during stress. The stress-protective effect of the peptide is mediated through the ACTH receptor.
我们发现，与人白细胞介素-1α前体81-88序列相对应的氚标记合成促肾上腺皮质激素样八肽亮促肾上腺皮质激素（[3H]GKVLKKRR）能以高亲和力和特异性与大鼠肾上腺皮质的促肾上腺皮质激素受体结合（解离常数Kd为2.2±0.1 nM）。在1至1000 nM的浓度范围内，该肽对大鼠肾上腺皮质膜的腺苷酸环化酶活性无影响。在无温度作用时，以10 - 20微克/动物的剂量给大鼠注射三次亮促肾上腺皮质激素，大鼠肾上腺中皮质醇（11-羟基皮质类固醇，11-HOCS）水平未发生变化。与此同时，该肽（以20微克/动物的剂量，注射三次）可消除或（以10微克/动物的剂量，注射三次）显著降低在冷休克或热休克情况下肾上腺中11-HOCS含量的急剧增加。因此，亮促肾上腺皮质激素可使应激期间大鼠肾上腺皮质中的11-HOCS水平恢复正常。该肽的应激保护作用是通过促肾上腺皮质激素受体介导的。
