Section of Endocrinology, Diabetes, and Nutrition, Boston Medical Center, Boston University School of Medicine, Boston, Massachusetts 02118, USA.
Thyroid. 2011 Nov;21(11):1263-8. doi: 10.1089/thy.2011.0105. Epub 2011 Sep 21.
Many tissues express thyroid hormone metabolizing deiodinases that both activate and inactivate thyroid hormones through conversion processes. Many believe that the primary role of thyroid hormone deiodinases is the activation of the prohormone thyroxine (T(4)) to the active hormone triiodothyronine because athyreotic humans can be treated with T(4) alone. In our hands a nonspecific deiodinase inhibitor (iopanoic acid [IOP]) decreased cutaneous cell proliferation in vitro, so we hypothesized that topical IOP would inhibit epidermal proliferation in vivo.
IOP was applied topically to mice. Treatments were applied daily for 1 week. Skin biopsies were either stained for 5-bromo-2-deoxyuridine or flash-frozen to assay for deiodinase activity.
Topical IOP resulted in a dose-dependent increase in epidermal proliferation. Assay revealed significant inactivating type 3 deiodinase (Dio3) activity in the epidermis but little or no activating (Dio1 or Dio2) activity. Dio3 activity was decreased 44%±21% in epidermis from mice treated with low-dose IOP and 80%±4% in epidermis from mice treated with high-dose IOP (p<0.001).
We hypothesize that keratinocytes express Dio3 in vivo to maintain cutaneous health and prevent the skin from becoming hyperproliferative. Our data support the developing recognition that the primary role of thyroid hormone deiodinases in some tissues may be the degradation of thyroid hormone to protect the tissue against thyrotoxicosis.
许多组织表达甲状腺激素代谢脱碘酶,这些酶通过转化过程激活和失活甲状腺激素。许多人认为甲状腺激素脱碘酶的主要作用是将前激素甲状腺素(T4)转化为活性激素三碘甲状腺原氨酸,因为无甲状腺的人可以单独用 T4 治疗。在我们的研究中,一种非特异性脱碘酶抑制剂(碘帕酸[IOP])在体外降低皮肤细胞增殖,因此我们假设局部 IOP 会抑制体内表皮细胞增殖。
IOP 局部应用于小鼠。治疗方法为每天应用一次,持续一周。皮肤活检标本或进行 5-溴-2-脱氧尿苷染色,或进行 flash-frozen 以测定脱碘酶活性。
局部 IOP 导致表皮增殖呈剂量依赖性增加。检测结果显示,表皮中存在显著的失活型 3 型脱碘酶(Dio3)活性,但激活型(Dio1 或 Dio2)活性很小或没有。低剂量 IOP 处理的小鼠表皮中的 Dio3 活性降低了 44%±21%,高剂量 IOP 处理的小鼠表皮中的 Dio3 活性降低了 80%±4%(p<0.001)。
我们假设角质形成细胞在体内表达 Dio3 以维持皮肤健康并防止皮肤过度增殖。我们的数据支持这样一种认识,即在某些组织中,甲状腺激素脱碘酶的主要作用可能是降解甲状腺激素,以保护组织免受甲状腺功能亢进的影响。