Hyperforin

Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model^{[1][2][3][4][5][6]}. IC50 & Target:TRPC6^[1] In Vitro:Hyperforin has a multi-directional mechanism of action. It blocks conductance of ligand-gated (GABA, NMDA, and AMPA receptors) and voltage-gated channels (Ca²⁺, K⁺, and Na⁺)^[2].
Hyperforin (0.1, 1, 10 μM; 2 h) reduces the expression and secretion of IL-17A in γδ T cell in vitro cultured murine splenic γδ T cells^[3].
Hyperforin (0.1, 1, 10 μM; 2 h) suppresses phosphorylation of MAPK and STAT3 pathways in TNF-α stimulated HaCaT cells^[3].
Hyperforin (IC₅₀=3.7 μmol/L) inhibits the microvascular tube formation and proliferation of HDMEC in a dose-dependent manner without toxic effects^[4].
In Vivo:Hyperforin (5 mg/kg; i.p.; once daily for 7 d) ameliorates Imiquimod (HY-B0180)-induced psoriatic skin lesion in mice, as well as inhibiting inflammatory cell infiltration and inflammatory cytokines release^[3].