Griseofulvin-d3 is intended for use as an internal standard for the quantification of griseofulvin by GC- or LC-MS. Griseofulvin is a fungal metabolite that has been found in Penicillium and has diverse biological activities.1 It is active against clinical isolates of the dermatophytes T. rubrum, T. tonsurans, and M. canis (MICs = 0.0078-0.0156, 1-4, and 0.5-2 µg/ml, respectively).2 Griseofulvin binds to tubulin (Kd = 300 µM) and reduces the growth rate and shortening rate of isolated bovine brain microtubulin, indicating stabilization of microtubule dynamics, when used at concentrations ranging from 0.5 to 20 µM.3 It induces abnormal microtubule polymerization and cell cycle arrest at the G2/M phase in HT-29 cells when used at a concentration of 20 µM.4 Griseofulvin (30 mg/kg), alone or in combination with nocodazole , reduces tumor growth in a COLO 205 mouse xenograft model. Formulations containing griseofulvin have been used in the treatment of fungal infections.
1.Singh, P., Rathinasamy, K., Mohan, R., et al.Microtubule assembly dynamics: An attractive target for anticancer drugsIUBMB Life60(6)368-375(2008) 2.Brilhante, R.S.N., Correia, E.E.M., Guedes, G.M.M., et al.In vitro activity of azole derivatives and griseofulvin against planktonic and biofilm growth of clinical isolates of dermatophytesMycoses61(7)449-454(2018) 3.Panda, D., Rathinasamy, K., Santra, M.K., et al.Kinetic suppression of microtubule dynamic instability by griseofulvin: Implications for its possible use in the treatment of cancerProc. Natl. Acad. Sci. USA102(28)9878-9883(2005) 4.Ho, Y.-S., Duh, J.-S., Jeng, J.-H., et al.Griseofulvin potentiates antitumorigenesis effects of nocodazole through induction of apoptosis and G2/M cell cycle arrest in human colorectal cancer cellsInt. J. Cancer91(3)393-401(2001)