Peimine

Peimine is an alkaloid that has been found in Fritillaria and has diverse biological activities, including ion channel inhibitory, anti-tussive, anticancer, and anti-inflammatory properties.{53420,56003,56004,56005,56006} It is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50= 47.2 µM) and human-ether-a-go-go (hERG), also known as Kv11.1 (IC50 = 43.7 µM).{56003,56004} It increases the latent period of coughs, decreases the number of coughs, and has expectorant activity in a mouse model of ammonia liquor-induced cough when administered at a dose of 3 mg/kg.{53420} Peimine (2.5, 5, and 10 µM) inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells.{56005} It also induces phosphorylation of calcium/calmodulin-dependent protein kinase II (CaMKII) in, and apoptosis of, PC3 cells and inhibits PC3 cell invasion, migration, and epithelial-to-mesenchymal transition. Peimine (10, 20, or 50 mg/animal) reduces tumor growth in a PC3 mouse xenograft model. It decreases IL-1B-induced nitric oxide (NO) and prostaglandin E2 (PGE2; Item No. 14010) production and reduces inducible NO synthase (iNOS) and COX-2 protein levels in primary mouse articular chondrocytes in vitro.{56006} It also decreases the severity of osteoarthritis-associated histopathological alterations in a mouse model of osteoarthritis when administered at a dose of 20 mg/kg.