Bohemine

Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC₅₀s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC₅₀ of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities^[1][2]. In Vitro: Bohemine (0-30 µM; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 µM results in a short-term arrest of growth and of monoclonal antibody production. The short-term suppression of cell functions is followed by a significant temporary increase of specific growth rate and of specific production rate^[1].
Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 µM) concentration^[1].
T-lymphoblastic cell line CEM is treated by Bohemine, five proteins are found to be downregulated, namely α-enolase, triosephosphate isomerase, initiation factor 5A, and α- and β-subunits of Rho GDP-dissociation inhibitor 1. These proteins play significant roles in glycolysis, proteosynthesis, and in cytoskeleton rearrangement^[1].
Bohemine inhibits growth of human tumor cell lines with an IC₅₀ of 27 µM^[2]. In Vivo: Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows C_max is 72,308 nM, observed clearance is 0.23 L/h and T_1/2 is 1.39 h^[2].