Periplogenin

Periplogenin is an orally active cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis^[1][2][3]. In Vitro:Periplogenin (0.625-10 μg/mL 44 h) inhibits the viability of human HaCaT keratinocytes, with an IC₅₀ of 1.56 μg/mL^[1].
Periplogenin (2 μg/mL, 6-24 h) induces caspase-independent non-apoptotic and non-autophagic cell death in HaCaT cells^[1].
Periplogenin (1-4 μg/mL, 12-48 h) increases ROS production and induces necroptosis in HaCaT cells^[1].
Periplogenin (0.1-20 μg/mL, 24 h) inhibits the proliferation of rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS), with an IC₅₀ of 1.56 μg/mL^[2].
Periplogenin (0.1-5 μg/mL, 24 h) inhibits the migration, invasion and pyroptosis in RA-FLS^[2].
Periplogenin (0.1-5 μg/mL, 24 h) induces G0/G1 phase arrest in RA-FLS^[2].
Periplogenin (0.1-5 μg/mL, 24 h) downregulates NLRP3, Cleaved-Caspase-1, GSDMD-N, IL-1β, and IL-18 expression in RA-FLS^[2].
Periplogenin (0.02-33 μM, 72 h) inhibits the viability of DU145, DLD-1, U-87MG, and MCF-7 cancer cells, with IC₅₀ values of 2.897 μM, 8.712 μM, 3.008 μM, and 20.025 μM respectively^[3].
Periplogenin (0-100 μM) inhibits the enzymatic activity of ATP1A1 in wild-type DU145 cells^[3].
In Vivo:Periplogenin (2 μg per site, topical application, daily for 11 days starting after 8 days of TPA induction) ameliorates TPA-induced and IMQ (HY-B0180)-induced psoriasis-like skin inflammation in Balb/c mice^[1].
Periplogenin (10-20 mg/kg, i.g., once a day) inhibits tumor growth in DU145 wild-type xenograft mice models^[3].