Anthralin

Anthralin is an anthrone inhibitor of keratinocyte proliferation and a modulator of differentiation.¹ It increases apoptosis and inhibits proliferation of normal human keratinocytes (NHKs) when used at a concentration of 2.5 μM. It also decreases the mitochondrial membrane potential, increases cytochrome c release, and induces perinuclear mitochondrial clustering in NHKs when used at a concentration of 5 μM.² Anthralin (0.25 μM) decreases the expression of β-defensin-2 (Item No. 24577) and S100 calcium-binding protein A9 (S100A9) and increases the expression of IL-6 and IL-8 in IL-17A- and IL-22-stimulated NHKs.¹ It also inhibits leukotriene B₄ (LTB₄; Item No. 20110) production, stimulated by the calcium ionophore A23187 (Item No. 11016), from human neutrophils (IC₅₀ = 7 μM).³ Topical anthralin (0.1%) induces hair regrowth in a Dundee experimental bald rat (DEBR) model of alopecia areata.⁴

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1. Holstein, J., Fehrenbacher, B., Brück, J., et al. Anthralin modulates the expression pattern of cytokeratins and antimicrobial peptides by psoriatic keratinocytes. J. Dermatol. Sci. 87(3), 236-245 (2017).

2. McGill, A., Frank, A., Emmett, N., et al. The anti-psoriatic drug anthralin accumulates in keratinocyte mitochondria, dissipates mitochondrial membrane potential, and induces apoptosis through a pathway dependent on respiratory competent mitochondria. The FASEB Journal 19(8), 1012-1014 (2005).

3. Schröder, J.M. Anthralin (1,8-dihydroxyanthrone) is a potent inhibitor of leukotriene production and LTB₄-ω oxidation by human neutrophils. J. Invest. Dermatol. 87(5), 624-629 (1986).

4. Tang, L., Sundberg, J.P., Liu, H., et al. Old wine in new bottles: Reviving old therapies for alopecia areata using rodent models. J. Invest. Dermatol. Symp. Proc. 8(2), 212-216 (2003).