Collagen proline hydroxylase inhibitor

IC50: N/A

Collagen proline hydroxylase inhibitor is one member of the collagen proline hydroxylase inhibitor family, which are used as antifibroproliferative agents. Proline hydroxylase is a multiple function oxygenase catalyzing specific prolyl residues in the collagen peptide precursor. Proline hydroxylase has been known as one of the critical enzymes in the biosynthesis of collagen and its activity is enhanced in tissues of various pathological fibrosis. Thus, the specific inhibitor of proline hydroxylase could have clinical application in fibrotic diseases treatment.

In vitro: One of collagen proline hydroxylase inhibitors, P-1894B, was found to in vitro inhibit proline hydroxylase and had been proposed as a topical treatment for dermal fibrosis. P-1894B was observed to be with similar activities on one fibroblast line from a patient with infection and two fibroblast lines from normal human skin. 72-hour drug exposure on growing cells showed both time- and dose-dependent inhibition of proliferation. A similar result was also observed in the epithelial cell line NCTC 2544 [1].

In vivo: So far, collagen proline hydroxylase inhibitor has not been applied to animal in vivo study.

Clinical trial: Currently, no clinical study is available.

Reference:
[1] Priestley GC.  Toxicity of the anthraquinone glycoside P-1894B for human skin fibroblasts. Br J Dermatol.1987 Jul;117(1):67-72.