Griseofulvin-d3

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 (K_d = 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)