Apamin

An inhibitor of KCa2.2/SK2 channels

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Background

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity[1].

Apamin (0.5-2 μg/mL; 24 hours; HSC-T6 cells) treatment markedly reduces the expression of α-SMA in the TGF-β1-induced HSC-T6 cells. Apamin treatment abrogats the activation of p-Smad2/3 and Smad4 induced by TGF-β1[1].

Apamin (0.1 mg/kg; intraperitoneal injection; twice a week; for 4 weeks; C57BL/6 male mice) treatment results in decreased liver injury and proinflammatory cytokine levels. Apamin suppresses the deposition of collagen, proliferation of BECs and expression of fibrogenic genes in the 3,5-diethoxycarbonyl-1,4-dihydrocollidine (DDC)-fed mice[1].

参考文献:
[1]. Kim JY, et al. Apamin suppresses biliary fibrosis and activation of hepatic stellate cells. Int J Mol Med. 2017 May;39(5):1188-1194.