Calcipotriol

Calcipotriol is an analogue of vitamin D3. [1]

Calcipotriol is a ligand of VDR-like receptors and is used as a first-line topical agent in the treatment of psoriasis.[1-2] Calcipotriol is much less effective in causing hypercalcemia.[3] The vitamin D receptor is found on the cells of many different tissues including T cells of the immune system. T cells are known to play a role in psoriasis, and the binding of calcipotriol to VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes. Calcipotriol induced apoptosis in eratinocytes isolated from psoriatic plaques at 100 nM for 20 h.[4] Calcipotriol also induced autophagy in both HeLa cells and keratinocytes.[2] Calcipotriol inhibited the proliferation of HL-60 and MCF-7 cells dose-dependently from 1 nM-1000 nM.[5] Calcipotriol is a potent inducer of terminal differentiation in cultured human keratinocytes.[3] Calcipotriol also decreased the mRNA expression/production of human cathelicidin antimicrobial protein (hCAP18) and LL37 peptide by IL-17A/IL-22-stimulated keratinocytes at 40 nM.[6]

References:
1. M. R. Klaber, P. E. Hutchinson, A. Pedvis-Leftick, K. Kragballe, T. L. Reunala, P. C. Van de Kerkhof, M. K. Johnsson, L. Molin, M. S. Corbett and N. Downess, Br J Dermatol 1994, 131, 678-683.
2. R. C. Wang and B. Levine, J Invest Dermatol 2011, 131, 990-993.
3. K. Kragballe and I. L. Wildfang, Arch Dermatol Res 1990, 282, 164-167.
4. R. Tiberio, C. Bozzo, G. Pertusi, F. Graziola, M. Gattoni, P. Griffanti, P. Boggio, E. Colombo and G. Leigheb, Clin Exp Dermatol 2009, 34, e972-974.
5. M. Milczarek, M. Chodynski, B. Filip-Psurska, A. Martowicz, M. Krupa, K. Krajewski, A. Kutner and J. Wietrzyk, Cancers (Basel) 2013, 5, 1355-1378.
6. J. Sakabe, T. Umayahara, M. Hiroike, T. Shimauchi, T. Ito and Y. Tokura, Acta Derm Venereol 2014, 94, 512-516.