title: The plant alkaloid chelerythrine binds to chromatin, alters H3K9Ac and modulates global gene expression.
abstract: 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.
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Amrita
authors: A
authors: Banerjee
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Sulagna
authors: S
authors: Sanyal
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Shreyasi
authors: S
authors: Dutta
authors: b Genome Informatics Research Group , Bionivid Technology Pvt Ltd. , Bangalore 560043 , India.
authors: Payal
authors: P
authors: Chakraborty
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Prajna Paramita
authors: PP
authors: Das
authors: c Division of Molecular Medicine, Centre for Translational Animal Research , Bose Institute , P 1/12, C. I. T. Road, Scheme - VIIM, Kolkata 700054 , India.
authors: Kuladip
authors: K
authors: Jana
authors: b Genome Informatics Research Group , Bionivid Technology Pvt Ltd. , Bangalore 560043 , India.
authors: Madavan
authors: M
authors: Vasudevan
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Chandrima
authors: C
authors: Das
authors: a Biophysics and Structural Genomics Division , Saha Institute of Nuclear Physics , Block - AF Sector-I, Bidhan Nagar, Kolkata 700064 , India.
authors: Dipak
authors: D
authors: Dasgupta
mesh_terms: D000107:Acetylation / Q000187:drug effects; D000970:Antineoplastic Agents / Q000494:pharmacology*; D053119:Benzophenanthridines / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D042002:Chromatin Assembly and Disassembly; D004247:DNA / Q000737:chemistry / Q000378:metabolism; D044127:Epigenesis, Genetic; D022041:Euchromatin / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D006367:HeLa Cells; D006657:Histones / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D007546:Isoquinolines / Q000494:pharmacology; D009707:Nucleosomes / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D011401:Promoter Regions, Genetic; D011499:Protein Processing, Post-Translational
chemical_list: D000970:Antineoplastic Agents; D053119:Benzophenanthridines; D022041:Euchromatin; D006657:Histones; D007546:Isoquinolines; D009707:Nucleosomes; D004247:DNA; C005705:sanguinarine; C016299:chelerythrine
keywords: chelerythrine; cytotoxicity; dual binder; gene expression; histone H3K9 acetylation