Telocinobufagin

Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na⁺/K⁺-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models^{[1][2][3][4][5][6][7][8][9]}. In Vitro:Telocinobufagin (0.01-100 μM, 0-96 h) suppresses proliferation and metastasis in human NSCLC cells, osteosarcoma cells, anaplastic thyroid cancer (ATC) cells, 4T1 breast cancer cells and neck squamous cell carcinoma (HNSCC)^{[1][2][6][7][8][9]}.
Telocinobufagin (0.125-5 μM, 24-48 h) induces apoptosis in human NSCLC cells and osteosarcoma cells and HNSCC cells^[1][2][9].
Telocinobufagin (1-5 μM) induces G2/M phase arrest in Cal-27 cells and SCC-25 cells^[9].
Telocinobufagin (0.5 μg/mL) suppresses malignant metastasis of undifferentiated thyroid carcinoma via modulation of the LARP1-mTOR pathway in CAL-62 cells^[6].
Telocinobufagin (0.1-1 μM, 2-48 h) blocks STAT3 and JAK2/STAT3 signaling and inhibits PLK1^[1][2][9]. Telocinobufagin (0.05-0.5 μg/mL, 24 h) reverses the epithelial-mesenchymal transition (EMT) process in breast cancer cells, downregulates the Snail transcription factor, and inhibits the PI3K/Akt/ERK signaling pathway. Telocinobufagin (10-100 nM, 24 h) activates the pro-fibrotic phenotype of renal tubular epithelial cells (HK2 cells) and primary normal human renal mesangial cells (NHMCs), but is ineffective against SYF fibroblasts^[5].
In Vivo:Telocinobufagin (1-2 mg/kg, i.p., every 2 days for 18 days) inhibits tumor growth in a human NSCLC xenograft model in mice^[1].
Telocinobufagin (5-10 mg/kg, i.p., every 2 days for 20 days) significantly suppresses tumor growth and metastasis by inhibiting the JAK2/STAT3 signaling pathway in an osteosarcoma xenograft model in mice^[2].
Telocinobufagin (10-40 μg, s.c., two doses, 14-day interval) enhances a Th1 immune response to control intracellular S. typhimurium infections in mice^[3].
Telocinobufagin (0.062-10 mg/kg, i.p. and p.o, single dose) exhibits potent analgesic effects in various acute pain models in mice, and it does not rely on the opioid system or affect motor function. Its analgesic potency is four times that of morphine^[4].
Telocinobufagin (0.1 mg/kg, i.p., once daily for 4 weeks) promotes renal fibrosis via Na^+/K+-ATPase profibrotic signaling pathways^[5].
Telocinobufagin (10-20 µg/mouse, i.p., 3 times a day for 2 weeks) inhibits breast cancer tumor growth and the epithelial mesenchymal transition in 4T1 cells xenograft model in mice^[7][8].
Telocinobufagin (4-16 mg/kg, i.p., once daily for 30 days) inhibits tumor growth and lung metastasis in HNSCC cells-bearing mice^[9].