The plant alkaloid chelerythrine binds to chromatin, alters H3K9Ac and modulates global gene expression

• Published in: Journal of biomolecular structure & dynamics Vol. 35; no. 7; pp. 1491 - 1499
• Main Authors: Banerjee, Amrita, Sanyal, Sulagna, Dutta, Shreyasi, Chakraborty, Payal, Das, Prajna Paramita, Jana, Kuladip, Vasudevan, Madavan, Das, Chandrima, Dasgupta, Dipak
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 19.05.2017
• Subjects: Acetylation - drug effects; Antineoplastic Agents - pharmacology; Benzophenanthridines - pharmacology; Cell Survival - drug effects; chelerythrine; Chromatin Assembly and Disassembly; cytotoxicity; DNA - chemistry; DNA - metabolism; dual binder; Epigenesis, Genetic; Euchromatin - chemistry; Euchromatin - drug effects; Euchromatin - metabolism; gene expression; HeLa Cells; histone H3K9 acetylation; Histones - genetics; Histones - metabolism; Humans; Isoquinolines - pharmacology; Nucleosomes - chemistry; Nucleosomes - drug effects; Nucleosomes - metabolism; Promoter Regions, Genetic; Protein Processing, Post-Translational; histone H3K9 acetylation; cytotoxicity; gene expression; chelerythrine; dual binder
• ISSN: 0739-1102; 1538-0254
• DOI: 10.1080/07391102.2016.1188154

Chelerythrine (CHL), a plant alkaloid, possesses antimicrobial, anti-inflammatory, and antitumor properties. Although CHL influences several key signal transduction pathways, its ability to interact directly with nucleoprotein complex chromatin, in eukaryotic cells has so far not been looked into. Here we have demonstrated its association with hierarchically assembled chromatin components, viz. long chromatin, chromatosome, nucleosome, chromosomal DNA, and histone H3 and the consequent effect on chromatin structure. CHL was found to repress acetylation at H3K9. It is more target-specific in terms of gene expression alteration and less cytotoxic compared to its structural analog sanguinarine.