首页|Natural withanolide-based lysine-specific demethylase 1 inhibitors for antitumor metastasis activity

Natural withanolide-based lysine-specific demethylase 1 inhibitors for antitumor metastasis activity

扫码查看
原文链接
  • NSTL
  • Elsevier
? 2022 Phytochemical Society of EuropeLysine 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 μM. 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.

Anti-metastasisHistone lysine demethylaseLSD1 inhibitorWithaferin AWithanolide

Zhang J.、Gu M.、Ren C.、Xu X.、Kong L.、Li Z.、Han C.

展开 >

State Key Laboratory of Natural Medicines Jiangsu Key Laboratory of Bioactive Natural Product Research School of Traditional Chinese Pharmacy China Pharmaceutical University

2022

10.1016/j.phytol.2022.03.011

Phytochemistry Letters

Phytochemistry Letters

SCI
ISSN：1874-3900
年,卷(期)：2022.49
  • 25