Phellamurin

Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity[1][2][3].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

Research Areas >> Metabolic Disease

Phellamurin (0-10 μg/mL; 48 hours; U2OS and Saos-2 cells) treatment leads to a repression of cell viability in U2OS and Saos-2 cells in a dose-dependent manner[1]. Phellamurin (0-10 μg/mL; 48 hours; U2OS and Saos-2 cells) treatment concentration-dependently promots the apoptosis of U2OS and Saos-2 cells[1]. Phellamurin (0-10 μg/mL; 48 hours; U2OS and Saos-2 cells) treatment declines the ratios of p-PI3K/PI3K, p-AKT/AKT, and p-mTOR/mTOR in U2OS and Saos-2 cells[1]. Cell Viability Assay[1] Cell Line: U2OS and Saos-2 cells Concentration: 0 μg/mL, 2.5 μg/mL, 5 μg/mL, and 10 μg/mL Incubation Time: 48 hours Result: Suppressed the viability of U2OS and Saos-2 cells in a concentration-dependent manner. Apoptosis Analysis[1] Cell Line: U2OS and Saos-2 cells Concentration: 0 μg/mL, 2.5 μg/mL, 5 μg/mL, and 10 μg/mL Incubation Time: 48 hours Result: Induced apoptosis of U2OS and Saos-2 cells in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: U2OS and Saos-2 cells Concentration: 0 μg/mL and 10 μg/mL Incubation Time: 48 hours Result: Repressed the PI3K/AKT/mTOR pathway in U2OS and Saos-2 cells.

Phellamurin (50 mg/kg/day; intraperitoneal injection; daily; for 21 days; female BALB/c nude mice) treatment represses osteosarcoma tumor growth in vivo. The ratios of p-PI3K/PI3K, p-AKT/AKT, and p-mTOR/mTOR are decreased in xenograft in Phellamurin-treated mice[1]. Animal Model: Athymic female BALB/c nude mice (6 weeks old ) injected with U2OS cells[1] Dosage: 50 mg/kg/day Administration: Intraperitoneal injection; daily; for 21 days Result: Repressed osteosarcoma tumor growth in vivo.

[1]. Hongzhi Zhang, et al. Anti-tumor Efficacy of Phellamurin in Osteosarcoma Cells: Involvement of the PI3K/AKT/mTOR Pathway. Eur J Pharmacol. 2019 Sep 5;858:172477.

[2]. Hung-Yi Chen, et al. Marked Decrease of Cyclosporin Absorption Caused by Phellamurin in Rats. Planta Med. 2002 Feb;68(2):138-41.

[3]. Keiichi Honda, et al. Synergistic or Antagonistic Modulation of Oviposition Response of Two Swallowtail Butterflies, Papilio Maackii and P. Protenor, to Phellodendron Amurense by Its Constitutive Prenylated Flavonoid, Phellamurin. J Chem Ecol. 2011 Jun;37(6):575-81.