Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay

Dohyun Son; Chung Sub Kim; Kang Ro Lee; Hyun-Ju Park

doi:10.1016/j.bmcl.2016.03.010

Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay

Bioorg Med Chem Lett. 2016 May 1;26(9):2365-9. doi: 10.1016/j.bmcl.2016.03.010. Epub 2016 Mar 4.

Authors

Dohyun Son¹, Chung Sub Kim¹, Kang Ro Lee¹, Hyun-Ju Park²

Affiliations

¹ School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
² School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address: hyunju85@skku.edu.

PMID: 26996372
DOI: 10.1016/j.bmcl.2016.03.010

Abstract

A fluorescence-based cellular assay system was established to identify potential epigenetic modulator ligands. This assay method is to detect the de-repression of an EGFP reporter in cancer cells by the treatment of HDAC (histone deacetylase) or DNMT (DNA methyltransferase) inhibitor. Using this system, we conducted a preliminary screening of in-house natural product library containing extracts and pure compounds, and identified several active compounds. Among them, novel quinic acid derivatives were recognized as excellent HDAC inhibitors by both enzymatic and cell-based HDAC assays.

Keywords: Epigenetic modulator; Fluorescence-based assay; HDAC inhibitor; Quinic acid derivatives.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Fluorescence
Histone Deacetylase Inhibitors / pharmacology*
Humans
Quinic Acid / pharmacology*

Substances

Histone Deacetylase Inhibitors
Quinic Acid