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Griseofulvin is a polyketide synthase-derived fungal metabolite originally isolated from P. griseofulvum with antifungal and anticancer activities.1,2 It inhibits microtubule assembly when used at concentrations ranging from 20 to 200 µM.3 Griseofulvin is active against a variety of dermatophytes (MICs = 0.14-0.42 µg/ml) and reduces the number of infected hair follicles in a guinea pig model of M. canis infection when administered at a dose of 60 mg/kg.4,5 It also reduces viability of a variety of human colorectal cancer cells in vitro and induces abnormal mitotic spindle formation and cell cycle arrest at the G2/M phase in HT-29 cells when used at a concentration of 20 µM.6 Griseofulvin (50 mg/kg) reduces tumor growth in a COLO 205 mouse xenograft model. Formulations containing griseofulvin have been used in the treatment of dermatophyte infections of the skin and nails.
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1. Complexity generation in fungal polyketide biosynthesis: A spirocycle-
2. Griseofulvin, a new oral antibiotic for the treatment of fungous infections of the skin. Can. Med. Assoc. J. 81(3), 173-175 (1959).
3. Inhibition by griseofulvin of microtubule assembly in vitro. FEBS Lett. 67(3), 248-251 (1976).
4. In vitro studies of the antifungal antibiotic griseofulvin. J. Invest. Dermatol. 33, 403-418 (1959).
5. Experimental ringworm in guinea pigs: Oral treatment with griseofulvin. Nature 182(4633), 476-477 (1958).
6. Griseofulvin potentiates antitumorigenesis effects of nocodazole through induction of apoptosis and G2/M cell cycle arrest in human colorectal cancer cells. Int. J. Cancer 91(3), 393-401 (2001).