TY - JOUR
T1 - Role for inner ring deiodination preventing transcutaneous passage of thyroxine
AU - Santini, Ferruccio
AU - Vitti, Paolo
AU - Chiovato, Luca
AU - Ceccarini, Giovanni
AU - Macchia, Marco
AU - Montanelli, Lucia
AU - Gatti, Gianluca
AU - Rosellini, Veronica
AU - Mammoli, Claudia
AU - Martino, Enio
AU - Chopra, Inder J.
AU - Safer, Joshua D.
AU - Braverman, Lewis E.
AU - Pinchera, Aldo
PY - 2003/6/1
Y1 - 2003/6/1
N2 - Creams containing thyroid hormone are commonly employed for cosmetic purposes. To verify whether T4 applied to the skin surface can enter the bloodstream either directly or as a metabolite, a cream containing L-T4 [3,5,3′,5′-tetraiodothyronine (T4)] was self-applied by volunteers for 2 wk. No significant variations in urinary iodide, TSH, and serum (total and free) T4 and T3 concentrations were observed at any time relative to pretreatment values, whereas rT3 concentrations increased significantly 6 and 12 h after cream application. The increased rT3 concentration led us to investigate the presence of inner ring type III deiodinase (D3) activity in human skin. Using human surgical discard skin, we found that T4 can be carried across human epidermis in a liposome cream. Substantial inner ring deiodination was suggested by the fact that only 10% of transferred thyroid hormone remained as T4, and T3 was not detected. We then measured D3 activity in a surgical skin specimen. The Km for T3 was 1.74 nmol/liter, and the maximum velocity was 23.5 fmol/μg microsomal protein/h. In conclusion, our study indicates that normal human skin serves as a substantial, but incomplete, barrier to T4 passage. D3 plays an important role in augmenting T4 blockade by inactivating T4 to rT3.
AB - Creams containing thyroid hormone are commonly employed for cosmetic purposes. To verify whether T4 applied to the skin surface can enter the bloodstream either directly or as a metabolite, a cream containing L-T4 [3,5,3′,5′-tetraiodothyronine (T4)] was self-applied by volunteers for 2 wk. No significant variations in urinary iodide, TSH, and serum (total and free) T4 and T3 concentrations were observed at any time relative to pretreatment values, whereas rT3 concentrations increased significantly 6 and 12 h after cream application. The increased rT3 concentration led us to investigate the presence of inner ring type III deiodinase (D3) activity in human skin. Using human surgical discard skin, we found that T4 can be carried across human epidermis in a liposome cream. Substantial inner ring deiodination was suggested by the fact that only 10% of transferred thyroid hormone remained as T4, and T3 was not detected. We then measured D3 activity in a surgical skin specimen. The Km for T3 was 1.74 nmol/liter, and the maximum velocity was 23.5 fmol/μg microsomal protein/h. In conclusion, our study indicates that normal human skin serves as a substantial, but incomplete, barrier to T4 passage. D3 plays an important role in augmenting T4 blockade by inactivating T4 to rT3.
UR - http://www.scopus.com/inward/record.url?scp=0037564003&partnerID=8YFLogxK
U2 - 10.1210/jc.2002-021439
DO - 10.1210/jc.2002-021439
M3 - Article
C2 - 12788895
AN - SCOPUS:0037564003
SN - 0021-972X
VL - 88
SP - 2825
EP - 2830
JO - Journal of Clinical Endocrinology and Metabolism
JF - Journal of Clinical Endocrinology and Metabolism
IS - 6
ER -