Synthetic E-guggulsterone derivative GSD-1 inhibits NF-?B signaling and suppresses the metastatic potential of breast cancer cells - 17/06/21
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Abstract |
Guggulsterone (GS) [4,17(20)-pregnadiene-3,16-dione], is the main active phytosterol constituent in guggul, the gum resin of Commiphora wightii (Arnott.) Bhand./Commiphora mukul Engl. tree, and is known for its medicinal effects. In this study, we report that GSD-1, a structurally-related synthetic GS derivative, strongly inhibits NF-κB activation induced by TNF-α. GSD-1 prevented the nuclear translocation of p65 through the blockade of IκBα degradation and p65 phosphorylation, and further inhibited the activation of upstream kinases, including transforming growth factor-β activated kinase 1 (TAK1), IκB kinase (IKK) α, and IKKβ. Furthermore, GSD-1 inhibited the cell-intrinsic activation of NF-κB, and exerted its direct anti-cancer and anti-metastatic effects in both murine and human breast cancer cell lines. This study demonstrated GSD-1 to be an attractive compound to target NF-κB activation that has potential for treating breast cancer growth and metastasis.
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Highlights |
• | GSD-1, a structurally-related synthetic guggulsterone derivative, strongly inhibits NF-κB activation induced by TNF-α. |
• | GSD-1 prevented the nuclear translocation of p65 through the blockade of IκBα degradation and p65 phosphorylation. |
• | GSD-1 inhibited the activation of upstream kinases, TAK1, IKKα, and IKKβ. |
• | GSD-1 inhibited the cell-intrinsic activation of NF-κB and exerted anti-metastatic effects in breast cancer. |
Keywords : Guggulsterone, NF-κB, Breast cancer, Anti-cancer, Inflammatory signal, Metastasis
Plan
Vol 140
Article 111737- août 2021 Retour au numéro
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