tcsc7096 Apamin

Apamin, an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known to block Ca²⁺-activated K⁺ channels and prevent carbon tetrachloride-induced liver fibrosis.

IC50 & Target: K⁺ channel^[1]

In Vitro: Apamin is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom). It has long been known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels. Apamin inhibits liver fibrosis in a 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-induced mouse model as determined by hematoxylin and eosin staining. Apamin treatment attenuates inflammatory cytokine expression, including IL-6, IFN-γ, TNF-α and IL-1β compared with expression levels in the DDC-fed group^[1]. Apamin is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom). Apamin, a neurotoxin extracted from bee venom, specifically binds to a particular class of Ca²⁺-activated K⁺ channels which are involved in the slow afterhyperpolarization (S-AHP) that follows action potentials in many excitable cell^[2].

In Vivo: To investigate the anti-fibrotic effect of Apamin on ECM deposition in the DDC-fed mice, Liver fibrosis induced by DDC is confirmed by induction of fibrogenic genes, FSP-1, α-smooth muscle actin (α-SMA) and collagen I expression. Expression of α-SMA is strongly expressed in the myofibroblasts and HSCs around the proliferated bile duct in the DDC-fed group and clearly with the Apamin treatment. Moreover, expression of collagen I in the DDC-fed group is significantly increased, especially in the portal tracts^[1].