生物活性 | |||
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描述 | (+)-Griseofulvin (Griseofulvin) is a metabolic product of Penicillium spp. It was the first available oral agent for the treatment of dermatophytoses and has now been used for more than forty years. (+)-Griseofulvin can inhibit the fungal cell mitosis and nuclear acid synthesis, probable interfere with the function of microtubules. Griseofulvin has also anti-inflammatory properties and some direct vasodilatory effects when it is used in high doses[3]. Griseofulvin is an orally administered antifungal drug that affects microtubule formation in vitro and interferes with microtubule dynamics in vivo. Griseofulvin affected porcine oocyte in vitro maturation and following embryo development by disturbing microtubule dynamics[4]. The antifungal drug griseofulvin inhibits mitosis strongly in fungal cells and weakly in mammalian cells by affecting mitotic spindle microtubule (MT) function. Griseofulvin also blocks cell-cycle progression at G(2)/M and induces apoptosis in human tumor cell lines. Griseofulvin inhibited cell-cycle progression at prometaphase/anaphase of mitosis in parallel with its ability to inhibit cell proliferation. At its mitotic IC(50) of 20 muM, spindles in blocked cells displayed nearly normal quantities of MTs and MT organization similar to spindles blocked by more powerful MT-targeted drugs[5]. Griseofulvin strongly suppressed the dynamic instability of individual microtubules in live MCF-7 cells by reducing the rate and extent of the growing and shortening phases. At or near half-maximal proliferation inhibitory concentration, griseofulvin dampened the dynamicity of microtubules in MCF-7 cells without significantly disrupting the microtubule network. Griseofulvin-induced mitotic arrest was associated with several mitotic abnormalities like misaligned chromosomes, multipolar spindles, misegregated chromosomes resulting in cells containing fragmented nuclei[6]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.83mL 0.57mL 0.28mL |
14.17mL 2.83mL 1.42mL |
28.35mL 5.67mL 2.83mL |
参考文献 |
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[2]De Carli L, Larizza L. Griseofulvin. Mutat Res. 1988 Mar;195(2):91-126. [3]Develoux M. Griséofulvine [Griseofulvin]. Ann Dermatol Venereol. 2001 Dec;128(12):1317-25. French |