Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2022 Apr 15;27(8):2568.
doi: 10.3390/molecules27082568.

Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates

Abdelhakim Bouyahya  1 , Naoufal El Hachlafi  2 , Tarik Aanniz  3 , Ilhame Bourais  1 , Hamza Mechchate  4 , Taoufiq Benali  5 , Mohammad Ali Shariati  6 , Pavel Burkov  7 , José M Lorenzo  8   9 , Polrat Wilairatana  10 , Mohammad S Mubarak  11 , Nasreddine El Omari  12
Affiliations
Review

Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates

Abdelhakim Bouyahya et al. Molecules. .

Abstract

Cancer is a complex pathology that causes a large number of deaths worldwide. Several risk factors are involved in tumor transformation, including epigenetic factors. These factors are a set of changes that do not affect the DNA sequence, while modifying the gene's expression. Histone modification is an essential mark in maintaining cellular memory and, therefore, loss of this mark can lead to tumor transformation. As these epigenetic changes are reversible, the use of molecules that can restore the functions of the enzymes responsible for the changes is therapeutically necessary. Natural molecules, mainly those isolated from medicinal plants, have demonstrated significant inhibitory properties against enzymes related to histone modifications, particularly histone deacetylases (HDACs). Flavonoids, terpenoids, phenolic acids, and alkaloids exert significant inhibitory effects against HDAC and exhibit promising epi-drug properties. This suggests that epi-drugs against HDAC could prevent and treat various human cancers. Accordingly, the present study aimed to evaluate the pharmacodynamic action of different natural compounds extracted from medicinal plants against the enzymatic activity of HDAC.

Keywords: cancer; epidrugs; epigenetic; histone deacetylases; natural compounds.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The catalytic action of HDAC enzymes on chromatin condensation.
Figure 2
Figure 2
Chemical structures of flavonoids with anticancer activity by targeting HDAC.
Figure 3
Figure 3
Chemical structures of natural HDAC alkaloids in human cancers.
Figure 4
Figure 4
Chemical structures of HDAC natural terpenoids in human cancers.
Figure 5
Figure 5
Chemical structures of different compounds associated with HDAC in human cancers.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Mansoori B., Mohammadi A., Davudian S., Shirjang S., Baradaran B. The Different Mechanisms of Cancer Drug Resistance: A Brief Review. Adv. Pharm. Bull. 2017;7:339–348. doi: 10.15171/apb.2017.041. - DOI - PMC - PubMed
    1. Bouyahya A., El Menyiy N., Oumeslakht L., El Allam A., Balahbib A., Rauf A., Muhammad N., Kuznetsova E., Derkho M., Thiruvengadam M., et al. Preclinical and Clinical Antioxidant Effects of Natural Compounds against Oxidative Stress-Induced Epigenetic Instability in Tumor Cells. Antioxidants. 2021;10:1553. doi: 10.3390/antiox10101553. - DOI - PMC - PubMed
    1. Mann B.S., Johnson J.R., Cohen M.H., Justice R., Pazdur R. FDA Approval Summary: Vorinostat for Treatment of Advanced Primary Cutaneous T-Cell Lymphoma. Oncologist. 2007;12:1247–1252. doi: 10.1634/theoncologist.12-10-1247. - DOI - PubMed
    1. Lee J., Huang S. Cancer Epigenetics: Mechanisms and Crosstalk of a HDAC Inhibitor, Vorinostat. Chemotherapy. 2013;2:14934. doi: 10.4172/2167-7700.1000111. - DOI - PMC - PubMed
    1. Richon V.M. Cancer Biology: Mechanism of Antitumour Action of Vorinostat (Suberoylanilide Hydroxamic Acid), a Novel Histone Deacetylase Inhibitor. Br. J. Cancer. 2006;95:S2–S6. doi: 10.1038/sj.bjc.6603463. - DOI

MeSH terms

Substances