6-Methoxymellein, a phytoalexin, is a NF-κB inhibitor. 6-Methoxymellein reduces nuclear localization and DNA binding activity of NF-κB p65 and p50 subunits. 6-Methoxymellein decreases mRNA transcription and secretion of IL-6 and IL-8. 6-Methoxymellein reduces the proportion of CD44 + /CD24 − breast cancer cells, decreases expression of c-Myc, Sox-2 and Oct4, inhibits proliferation and migration of breast cancer cells, and reduces mammosphere growth. 6-Methoxymellein inhibits fungal growth of Trichophyton rubrum and Botrytis cinerea, and inhibits Trichophyton rubrum biofilm formation via hyphal disintegration. 6-Methoxymellein can be used for the research of breast cancer, tinea corporis, and carrot post-harvest storage rot [1] [2] [3].
In Vitro, 6-Methoxymellein (0.5-3 mM; 24 h) suppresses proliferation of MDA-MB-231 and MCF-7 human breast cancer cells in a concentration-dependent manner, with significant inhibition starting at 0.8 mM for MDA-MB-231 cells and 0.5 mM for MCF-7 cells after 24-hour incubation[1]. 6-Methoxymellein (0.2-1 mM, 0.5-1 mM; 7-day culture period) inhibits mammosphere formation by MDA-MB-231 and MCF-7 human breast cancer cells, reducing mammosphere size, number, and formation efficiency in a concentration-dependent manner, with maximum inhibition at 1 mM[1]. 6-Methoxymellein (1 mM; 24 h) significantly inhibits migration of MDA-MB-231 and MCF-7 human breast cancer cells[1]. 6-Methoxymellein (0.5-1 mM; 7-day culture period) inhibits colony formation by MDA-MB-231 and MCF-7 human breast cancer cells in a concentration-dependent manner, with maximum inhibition at 1 mM after 7 days of culture[1]. 6-Methoxymellein (1 mM; 24 h) reduces the proportion of CD44+/CD24− breast cancer stem-like cells in MDA-MB-231 cultures from 80.3% to 41.6% after 24-hour incubation[1]. 6-Methoxymellein (1 mM; 48 h) reduces protein expression of the stemness markers c-Myc, Sox-2, and Oct4 in MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (1 mM; 48 h) suppresses nuclear localization of NF-κB p65 and p50 in MDA-MB-231 human breast cancer cell-derived mammospheres after 48-hour incubation, without altering total cellular levels of these subunits[1]. 6-Methoxymellein (1 mM; 1, 2, 3 days post-treatment) inhibits growth of MDA-MB-231 human breast cancer cell-derived mammosphere cells over a 3-day period[1]. 6-Methoxymellein (1 mM) inhibits NF-κB DNA binding activity in nuclear extracts from MDA-MB-231 human breast cancer cell-derived mammospheres[1]. 6-Methoxymellein (1 mM; 48 h) significantly reduces secretion of IL-6 and IL-8 by MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (1 mM; 48 h) significantly reduces mRNA transcription of IL-6 and IL-8 in MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (6.25-200 μg/mL) potently inhibits growth of the Trichophyton rubrum T.R.1085 S isolate, with an MIC of 6.25 μg/mL, and produces increasing inhibition zone diameters with increasing concentrations up to 29 mm at 200 μg/mL[2]. 6-Methoxymellein (1.5625-200 μg/mL) dose-dependently inhibits biofilm formation by the Trichophyton rubrum T.R.1085 S isolate, reaching a maximum inhibition of 68.38% at 200 μg/mL[2]. 6-Methoxymellein (6-MM) (>30 μg/g tissue; 1-2 weeks) accumulated in UV-C treated carrot (Daucus carota L.) slices inhibits growth of Botrytis cinerea and Sclerotinia sclerotiorum at cold storage temperatures (1°C, 4°C), with concentrations above 30 μg/g tissue inhibiting B. cinerea and maximum inhibition at ~60 μg/g, leading to up to 88.5% reduction in fungal growth[3].
References:
[1]. Liu R, et al. 6-Methoxymellein Isolated from Carrot (Daucus carota L.) Targets Breast Cancer Stem Cells by Regulating NF-κB Signaling. Molecules. 2020 Sep 23;25(19):4374.
[2]. Ahmed Hagag, et al. Antibiofilm potential of 6-methoxymellein from geranium-associated Aspergillus caespitosus endophyte against clinical isolates of dermatophytes: Phytochemical, in silico and in vitro investigation. South African Journal of Botany 167 (2024) 448-456.
[3]. J. Mercier, et al. Induction of 6-Methoxymellein and Resistance to Storage Pathogens in Carrot Slices by UV-C. Phytopathology 137, 44-54 (1993).
In Vitro, 6-Methoxymellein (0.5-3 mM; 24 h) suppresses proliferation of MDA-MB-231 and MCF-7 human breast cancer cells in a concentration-dependent manner, with significant inhibition starting at 0.8 mM for MDA-MB-231 cells and 0.5 mM for MCF-7 cells after 24-hour incubation[1]. 6-Methoxymellein (0.2-1 mM, 0.5-1 mM; 7-day culture period) inhibits mammosphere formation by MDA-MB-231 and MCF-7 human breast cancer cells, reducing mammosphere size, number, and formation efficiency in a concentration-dependent manner, with maximum inhibition at 1 mM[1]. 6-Methoxymellein (1 mM; 24 h) significantly inhibits migration of MDA-MB-231 and MCF-7 human breast cancer cells[1]. 6-Methoxymellein (0.5-1 mM; 7-day culture period) inhibits colony formation by MDA-MB-231 and MCF-7 human breast cancer cells in a concentration-dependent manner, with maximum inhibition at 1 mM after 7 days of culture[1]. 6-Methoxymellein (1 mM; 24 h) reduces the proportion of CD44+/CD24− breast cancer stem-like cells in MDA-MB-231 cultures from 80.3% to 41.6% after 24-hour incubation[1]. 6-Methoxymellein (1 mM; 48 h) reduces protein expression of the stemness markers c-Myc, Sox-2, and Oct4 in MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (1 mM; 48 h) suppresses nuclear localization of NF-κB p65 and p50 in MDA-MB-231 human breast cancer cell-derived mammospheres after 48-hour incubation, without altering total cellular levels of these subunits[1]. 6-Methoxymellein (1 mM; 1, 2, 3 days post-treatment) inhibits growth of MDA-MB-231 human breast cancer cell-derived mammosphere cells over a 3-day period[1]. 6-Methoxymellein (1 mM) inhibits NF-κB DNA binding activity in nuclear extracts from MDA-MB-231 human breast cancer cell-derived mammospheres[1]. 6-Methoxymellein (1 mM; 48 h) significantly reduces secretion of IL-6 and IL-8 by MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (1 mM; 48 h) significantly reduces mRNA transcription of IL-6 and IL-8 in MDA-MB-231 human breast cancer cell-derived mammospheres after 2 days of treatment[1]. 6-Methoxymellein (6.25-200 μg/mL) potently inhibits growth of the Trichophyton rubrum T.R.1085 S isolate, with an MIC of 6.25 μg/mL, and produces increasing inhibition zone diameters with increasing concentrations up to 29 mm at 200 μg/mL[2]. 6-Methoxymellein (1.5625-200 μg/mL) dose-dependently inhibits biofilm formation by the Trichophyton rubrum T.R.1085 S isolate, reaching a maximum inhibition of 68.38% at 200 μg/mL[2]. 6-Methoxymellein (6-MM) (>30 μg/g tissue; 1-2 weeks) accumulated in UV-C treated carrot (Daucus carota L.) slices inhibits growth of Botrytis cinerea and Sclerotinia sclerotiorum at cold storage temperatures (1°C, 4°C), with concentrations above 30 μg/g tissue inhibiting B. cinerea and maximum inhibition at ~60 μg/g, leading to up to 88.5% reduction in fungal growth[3].
References:
[1]. Liu R, et al. 6-Methoxymellein Isolated from Carrot (Daucus carota L.) Targets Breast Cancer Stem Cells by Regulating NF-κB Signaling. Molecules. 2020 Sep 23;25(19):4374.
[2]. Ahmed Hagag, et al. Antibiofilm potential of 6-methoxymellein from geranium-associated Aspergillus caespitosus endophyte against clinical isolates of dermatophytes: Phytochemical, in silico and in vitro investigation. South African Journal of Botany 167 (2024) 448-456.
[3]. J. Mercier, et al. Induction of 6-Methoxymellein and Resistance to Storage Pathogens in Carrot Slices by UV-C. Phytopathology 137, 44-54 (1993).