Griseofulvin

Catalog No.S4071 Batch:S407101

Technical Data

Formula	C₁₇H₁₇ClO₆
Molecular Weight	352.77	CAS No.	126-07-8
Solubility (25°C)*	In vitro	DMSO	50 mg/mL (141.73 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.

Targets

Microtubules ^[1]

In vitro

Griseofulvin is active against dermatophytes of different species in the genera Microsporum, Trichophyton and Epidermophyton. Other fungi such as Scopulariopsis brevicaulis and Hendersomula toruloidea are insensitive. Griseofulvin has little or no effect against yeasts and bacteria. The minimum inhibitory concentration of Griseofulvin tested in vitro against various dermatophytes ranges between 0.14 and 0.6 μg/mL. Main effect of Griseofulvin on cell mitosis is disorganization of the spindle microtubules. Griseofulvin is also able to induce structural chromosomal aberrations in mammalian cells. ^[1] Griseofulvin inhibits the viability of human colon adenocarcinoma cells COLO 205 and HT 29, hepatoma cells Hep G2 and Hep 3B, leukemia cells HL 60, and normal keratinocytes (#76 KhGH) with IC50s of ~1 and ~5 μM, 5 and 5 μM, 1 μM, and 50 μM, respectively after a 30 hr incubation,. Griseofulvin (20 μM) induces a marked presence of abnormal mitotic spindle formation with mono-, bi-, and tripolar spindles of varying lengths in HT 29 cells, and causes G2/M cell cycle arrest at 24h through elevation of cyclin B1/cdc2 kinase activity and down-regulation of myt-1 protein expression. Griseofulvin is able to induce apoptosis of HT 29 cells via caspase3 activation, Bcl-2 hyperphosphorylation and inhibition of the normal function of Bcl-2 associated with Bax. ^[2]

In vivo

Griseofulvin displays potent anti-infection activity in vivo. The minimum effective dose of Griseofulvin given daily per os is 250 mg/kg (6 days) in mice with a cutaneous infection of Trichophyton quinckeanum and 25 mg/kg (12 days) in guinea pigs with a cutaneous infection of Trichophyton mentagrophytes. ^[1] Griseofulvin (50 mg/kg) is able to suppress COLO 205 tumor xenografts growth. Treatment with Griseofulvin and nocodazole (5 mg/kg) together significantly enhances the efficacy of nocodazole, leading to cessation of tumor growth. ^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Human hepatoma cells HepG2 Concentrations ~50 μM Incubation Time 30 hours Method The cells (5× 10³/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Griseofulvin in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader.
Animal Study:^{^[2]}	Animal Models Human colon adenocarcinoma xenografts COLO 205 Dosages 50 mg/kg Administration i.p. 3 times per week for 6 weeks

Cell Assay:^{^[2]}

Cell lines
Human hepatoma cells HepG2
Concentrations
~50 μM
Incubation Time
30 hours
Method
The cells (5× 10³/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Griseofulvin in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader.

Animal Study:^{^[2]}

Animal Models
Human colon adenocarcinoma xenografts COLO 205
Dosages
50 mg/kg
Administration
i.p. 3 times per week for 6 weeks

References

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