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Capsaicin: A "hot" KDM1A/LSD1 inhibitor from peppers.

Abstract：

:Capsaicinoids are plant secondary metabolites, and capsaicin is the main principal that responsible to the pungency of chili peppers, with widely application as food additive. In our study, capsaicin was characterized as lysine specific demethylase 1A (KDM1A/LSD1) inhibitor with IC50 of 0.6 ± 0.0421 μM in biochemical level, and can bind KDM1A recombinant directly and reversibly. Further cellular study confirmed that capsaicin can bind and inhibit KDM1A in gastric cancer cell line BGC-823 and further inhibit cell invasion and migration by reversing epithelial-mesenchymal transition (EMT). In sum, our findings identified KDM1A as a target of capsaicin and reveals capsaicin as a modifier of histone methylation for the first time, which may provide a new skeleton for further optimization of KDM1A inhibitor.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Jia G,Cang S,Ma P,Song Z

doi

10.1016/j.bioorg.2020.104161

subject

Has Abstract

pub_date

2020-10-01 00:00:00

pages

104161

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31458-9

journal_volume

103

pub_type

杂志文章

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