Journal
PHYTOCHEMISTRY LETTERS
Volume 49, Issue -, Pages 93-98Publisher
ELSEVIER
DOI: 10.1016/j.phytol.2022.03.011
Keywords
Withanolide; Histone lysine demethylase; LSD1 inhibitor; Withaferin A; Anti-metastasis
Categories
Funding
- National Natural Science Foundation of China [81803695, 82104359]
- Natural Science Fund in Jiangsu Province [BK20180568]
- China Postdoctoral Science Foundation [2021M691647]
- Fundamental Research Funds for the Central Universities [2632021ZD24]
- Open Project of State Key Laboratory of Natural Medicines [SKLNMKF202207]
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The study found that withanolides, especially withaferin A, can act as LSD1 inhibitors and have potential anti-tumor activity by inhibiting cell migration.
Lysine specific demethylase 1 (LSD1), which is overexpressed in several human cancers and acts as a demethylase of histone 3, lysine 4 and lysine 9, has become an attractive therapeutic target for cancer therapy. Based on our previous systematic studies, withanolides are important secondary metabolites mostly from the Solanaceae family of plants, which are crucial agents for cancer treatment. Here, withanolides were characterized as LSD1 inhibitors, especially withaferin A, with an IC50 value of 3.04 mu M. In vitro bioactivity assays and virtual molecular docking indicated that withaferin A could inhibit MDA-MB-231 cell migration by inhibiting intracellular LSD1 activity. These findings provide a new withanolide-based natural molecular skeleton for LSD1 inhibitors with potential antitumor activity.
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