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.^1,2,3,4,5 It is an inhibitor of voltage-gated sodium channel 1.7 (Na_v1.7; IC₅₀= 47.2 µM) and human-ether-a-go-go (hERG), also known as K_v11.1 (IC₅₀ = 43.7 µM).^2,3 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.¹ Peimine (2.5, 5, and 10 µM) inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells.⁴ 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-1β-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.⁵ 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.

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1. Wang, D., Zhu, J., Wang, S., et al. Antitussive, expectorant and anti-inflammatory alkaloids from Bulbus Fritillariae Cirrhosae. Fitoterapia 82(8), 1290-1294 (2011).

2. Xu, J., Zhao, W., Pan, L., et al. Peimine, a main active ingredient of Fritillaria, exhibits anti-inflammatory and pain suppression properties at the cellular level. Fitoterapia 111, 1-6 (2016).

3. Kan, L., Zhao, W., Pan, L., et al. Peimine inhibits hERG potassium channels through the channel inactivation states. Biomed. Pharmacother. 89, 838-844 (2017).

4. Tan, H., Zhang, G., Yang, X., et al. Peimine inhibits the growth and motility of prostate cancer cells and induces apoptosis by disruption of intracellular calcium homeostasis through Ca²⁺ /CaMKII/JNK pathway. J. Cell. Biochem. 121(1), 81-92 (2020).

5. Chen, K., Lv, Z.-T., Zhou, C.-H., et al. Peimine suppresses interleukin‑1β‑induced inflammation via MAPK downregulation in chondrocytes. Int. J. Mol. Med. 43(5), 2241-2251 (2019).