Ciclopirox

Ciclopirox (HOE296b) is a synthetic and orally active antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic. Ciclopirox also has anticancer and anti-inflammatory effect^[1][2][3]. In Vitro:Ciclopirox (10 μM, 18 h) inhibits HUVEC proliferation and angiogenesis^[4].
Ciclopirox (0-10 μM, 20 h) inhibits deoxyhypusine hydroxylation in HUVECs^[4].
Ciclopirox (0-40 μM, 72 h) shows anti-tumor activity in H1299 and 95D cells (decreases cell viability, with IC₅₀s of 11.13 and 4.136 μM respectively), and inhibits cell migration and invasion^[5].
Ciclopirox (0-40 μM, 48 h) arrests both H1299 and 95D cells in G1 phase, decreases Cyclin D1 and CDK4 protein level in H1299 and 95D cells^[5].
Ciclopirox (0-20 μM) induces cell aerobic glycolysis, impairs mitochondrial functions and enhances the generation of ROS in H1299 and 95D cells^[5].
Ciclopirox (0-40 μM, 48 h) activates PERK-dependent ER stress in CRC cells (HCT-8, HCT-8/5-FU, and DLD-1 cells)^[6].
In Vivo:Ciclopirox (20 mg/kg, i.p.) reduces tumor size in mouse H1299 xenograft model, and reduces tumor cell proliferation (Ki67 staining) and increases apoptosis (Cleaved-Caspase 3 and Tunel staining)^[5].
Ciclopirox (25 mg/kg, p.o., daily) also inhibits tumor growth in human breast cancer MDA-MB231 xenografts in mice^[6].