Natural Products Impacting DNA Methyltransferases and Histone Deacetylases.


:Epigenetics refers to heritable changes in gene expression and chromatin structure without change in a DNA sequence. Several epigenetic modifications and respective regulators have been reported. These include DNA methylation, chromatin remodeling, histone post-translational modifications, and non-coding RNAs. Emerging evidence has revealed that epigenetic dysregulations are involved in a wide range of diseases including cancers. Therefore, the reversible nature of epigenetic modifications concerning activation or inhibition of enzymes involved could be promising targets and useful tools for the elucidation of cellular and biological phenomena. In this review, emphasis is laid on natural products that inhibit DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) making them promising candidates for the development of lead structures for anticancer-drugs targeting epigenetic modifications. However, most of the natural products targeting HDAC and/or DNMT lack isoform selectivity, which is important for determining their potential use as therapeutic agents. Nevertheless, the structures presented in this review offer the well-founded basis that screening and chemical modifications of natural products will in future provide not only leads to the identification of more specific inhibitors with fewer side effects, but also important features for the elucidation of HDAC and DNMT function with respect to cancer treatment.


Front Pharmacol


Akone SH,Ntie-Kang F,Stuhldreier F,Ewonkem MB,Noah AM,Mouelle SEM,Müller R




Has Abstract


2020-08-13 00:00:00








  • Dermaseptins, Multifunctional Antimicrobial Peptides: A Review of Their Pharmacology, Effectivity, Mechanism of Action, and Possible Future Directions.

    abstract::Dermaseptins are a group of α-helical shaped polycationic peptides isolated from the Hylid frogs, with antimicrobial effects against bacteria, parasites, protozoa, viruses in vitro. Besides, anti-tumor effects have been demonstrated. However, few animal experiments and no clinical trials have been conducted thus far. ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Bartels EJH,Dekker D,Amiche M

    更新日期:2019-11-26 00:00:00

  • PAI-1 Exacerbates White Adipose Tissue Dysfunction and Metabolic Dysregulation in High Fat Diet-Induced Obesity.

    abstract::Background: Plasminogen activator inhibitor (PAI)-1 levels and activity are known to increase during metabolic syndrome and obesity. In addition, previous studies have implicated PAI-1 in adipose tissue (AT) expansion while also contributing to insulin resistance. As inflammation is also known to occur in AT during ob...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Wang L,Chen L,Liu Z,Liu Y,Luo M,Chen N,Deng X,Luo Y,He J,Zhang L,Hill MA,Li R,Wu J

    更新日期:2018-09-26 00:00:00

  • Eupalinolide J Suppresses the Growth of Triple-Negative Breast Cancer Cells via Targeting STAT3 Signaling Pathway.

    abstract::Persistent activation of STAT3 plays an important role in the development of triple-negative breast cancer (TNBC), and suppression of STAT3 is considered as a novel approach for cancer therapy. In this project, we aimed to examine the anticancer activity and molecular mechanism of eupalinolide J (EJ) in TNBC cells. Th...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Lou C,Chen Y,Zhang J,Yang B,Zhao H

    更新日期:2019-09-19 00:00:00

  • CB1 Cannabinoid Receptor Expression in the Striatum: Association with Corticostriatal Circuits and Developmental Regulation.

    abstract::Corticostriatal circuits mediate various aspects of goal-directed behavior and are critically important for basal ganglia-related disorders. Activity in these circuits is regulated by the endocannabinoid system via stimulation of CB1 cannabinoid receptors. CB1 receptors are highly expressed in projection neurons and s...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Van Waes V,Beverley JA,Siman H,Tseng KY,Steiner H

    更新日期:2012-03-12 00:00:00

  • Activation of CXCL6/CXCR1/2 Axis Promotes the Growth and Metastasis of Osteosarcoma Cells in vitro and in vivo.

    abstract::Osteosarcoma (OS) is a malignant primary bone tumor with high metastatic rate. C-X-C motif chemokine ligand 6 (CXCL6) and its receptor C-X-C motif chemokine receptor 1/2 (CXCR1/2) have been found to participate in the process of carcinogenesis. In this study, we evaluated the role of CXCL6/CXCR1/2 axis in proliferatio...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Liu G,An L,Zhang H,Du P,Sheng Y

    更新日期:2019-03-28 00:00:00

  • Bu-Yin-Qian-Zheng Formula Ameliorates MPP+-Induced Mitochondrial Dysfunction in Parkinson's Disease via Parkin.

    abstract::As a typical traditional Chinese medicine, Bu-Yin-Qian-Zheng Formula (BYQZF) has been shown to have neuroprotective effects in patients with Parkinson's disease (PD), particularly by ameliorating mitochondrial dysfunction and regulating expression of the parkin protein. However, the underlying mechanisms by which BYQZ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Ma HJ,Gai C,Chai Y,Feng WD,Cheng CC,Zhang JK,Zhang YX,Yang LP,Guo ZY,Gao YS,Sun HM

    更新日期:2020-12-18 00:00:00

  • The Early Awareness and Alert System in Sweden: History and Current Status.

    abstract::Introduction: Over the past decades, early awareness and alert (EAA) activities and systems have gained importance and become a key early health technology assessment (HTA) tool. While a pioneer in HTA, Sweden had no national level EAA activities until 2010. We describe the evolution and current status of the Swedish ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Eriksson I,Wettermark B,Persson M,Edström M,Godman B,Lindhé A,Malmström RE,Ramström H,von Euler M,Bergkvist Christensen A

    更新日期:2017-10-05 00:00:00

  • Human Umbilical Cord Blood Cell Transplantation in Neuroregenerative Strategies.

    abstract::At present there is no effective treatment of pathologies associated with the death of neurons and glial cells which take place as a result of physical trauma or ischemic lesions of the nervous system. Thus, researchers have high hopes for a treatment based on the use of stem cells (SC), which are potentially able to ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Galieva LR,Mukhamedshina YO,Arkhipova SS,Rizvanov AA

    更新日期:2017-09-08 00:00:00

  • Icariin Protects Hippocampal Neurons From Endoplasmic Reticulum Stress and NF-κB Mediated Apoptosis in Fetal Rat Hippocampal Neurons and Asthma Rats.

    abstract::Icariin is a main component of the Chinese medicinal plant Epimedium brevicornu Maxim, exhibits potent activity against inflammatory diseases. Our previous data demonstrated the valid bioactivity of icariin on mitigating rodent asthma. Endoplasmic reticulum (ER) stress and nuclear factor-κB (NF-κB) pathway were involv...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Liu J,Liu L,Sun J,Luo Q,Yan C,Zhang H,Liu F,Wei Y,Dong J

    更新日期:2020-01-31 00:00:00

  • Erratum on: Epoxyeicosatrienoic acid analog attenuates angiotensin II hypertension and kidney injury.

    abstract::[This corrects the article on p. 216 in vol. 5, PMID: 25295006.]. ...

    journal_title:Frontiers in pharmacology

    pub_type: 已发布勘误


    authors: Frontiers Production Office.

    更新日期:2014-11-19 00:00:00

  • A New Pharmacophore Model for the Design of Sigma-1 Ligands Validated on a Large Experimental Dataset.

    abstract::The recent publication of the σ1R crystal structure is an important cornerstone for the derivation of more accurate activity prediction models. We report here a comparative study involving a set of more than 25,000 structures from our internal database that had been screened for σ1R affinity. Using the recently publis...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Pascual R,Almansa C,Plata-Salamán C,Vela JM

    更新日期:2019-05-31 00:00:00

  • Acute Effects of 2C-E in Humans: An Observational Study.

    abstract::2,5-Dimethoxy-4-ethylphenethylamine (2C-E) is psychedelic phenylethylamine, with a chemical structure similar to mescaline, used as new psychoactive substance (NPS). It inhibits norepinephrine and serotonin uptake and, more relevant, acts as a partial agonist of the serotonin 2A (5-HT2A), 2B (5-HT2B), and (5-HT2C) rec...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Papaseit E,Olesti E,Pérez-Mañá C,Torrens M,Grifell M,Ventura M,Pozo OJ,de Sousa Fernandes Perna EB,Ramaekers JG,de la Torre R,Farré M

    更新日期:2020-03-18 00:00:00

  • Slow-Release H2S Donor Anethole Dithiolethione Protects Liver From Lipotoxicity by Improving Fatty Acid Metabolism.

    abstract::"Lipotoxicity" induced by free fatty acids (FAs) plays a central role in the pathogenesis of many metabolic diseases, with few treatment options available today. Hydrogen sulfide (H2S), a novel gaseous signaling molecule, has been reported to have a variety of pharmacological properties, but its effect on FAs metaboli...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Zhao C,Yu N,Li W,Cai H,Liu M,Hu Y,Liu Y,Tang M

    更新日期:2020-09-23 00:00:00

  • Ophiopogonin D', a Natural Product From Radix Ophiopogonis, Induces in Vitro and in Vivo RIPK1-Dependent and Caspase-Independent Apoptotic Death in Androgen-Independent Human Prostate Cancer Cells.

    abstract::Objective: The purpose of this study was to evaluate the anticancer effects of Ophiopogonin D' (OPD', a natural product extracted from a traditional Chinese medicine (Radix Ophiopogonis) against androgen-independent prostate cancer cells and to explore the underlying molecular mechanism(s) of action. Methods: The CCK-...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Lu Z,Wang H,Zhu M,Song W,Wang J,Wu C,Kong Y,Guo J,Li N,Liu J,Li Y,Xu H

    更新日期:2018-04-30 00:00:00

  • Periplaneta americana Extracts Accelerate Liver Regeneration via a Complex Network of Pathways.

    abstract::Successful recovery from hepatectomy is partially contingent upon the rate of residual liver regeneration. The traditional Chinese medicines known as Periplaneta americana extracts (PAEs) positively influence wound healing by promoting tissue repair. However, the effect of PAEs on liver regeneration is unknown. We use...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Zou Y,Zhang M,Zeng D,Ruan Y,Shen L,Mu Z,Zou J,Xie C,Yang Z,Qian Z,Xu R,Li S,Kang Q,Zou H,Zhao S,Liu L,Wang K,Wang X,Zhang X

    更新日期:2020-07-31 00:00:00

  • Anti-Inflammatory Effect of a TCM Formula Li-Ru-Kang in Rats With Hyperplasia of Mammary Gland and the Underlying Biological Mechanisms.

    abstract::Li-Ru-Kang (LRK), a formula of eight traditional Chinese medicines (TCM), has been used to treat hyperplasia of mammary gland (HMG) in TCM clinics. However, how LRK works in HMG patients is unclear. To explore the possible mechanisms of LRK against HMG, the network pharmacology was used to screen the potential targets...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Wang Y,Wei S,Gao T,Yang Y,Lu X,Zhou X,Li H,Wang T,Qian L,Zhao Y,Zou W

    更新日期:2018-11-20 00:00:00

  • Actinidia chinensis Planch.: A Review of Chemistry and Pharmacology.

    abstract::Actinidia chinensis Planch. (A. chinensis), commonly known as Chinese kiwifruit, is a China native fruit, which becomes increasingly popular due to attractive economic, nutritional, and health benefits properties. The whole plant including fruits, leaves, vines, and roots of A. chinensis are used mainly as food or add...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: He X,Fang J,Chen X,Zhao Z,Li Y,Meng Y,Huang L

    更新日期:2019-10-30 00:00:00

  • Aspergillus terreus (Trichocomaceae): A Natural, Eco-Friendly Mycoinsecticide for Control of Malaria, Filariasis, Dengue Vectors and Its Toxicity Assessment Against an Aquatic Model Organism Artemia nauplii.

    abstract::Vector-borne diseases like malaria, filariasis, and dengue are transmitted by mosquitoes and they cause global mortality and morbidity due to an increased resistance against commercial insecticides. The present study was aimed to evaluate the neurobehavioral toxicity, knock-down effect, histopathology, ovicidal, adult...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Ragavendran C,Srinivasan R,Kim M,Natarajan D

    更新日期:2018-11-26 00:00:00

  • Semen cassiae Extract Inhibits Contraction of Airway Smooth Muscle.

    abstract::β2-adrenoceptor agonists are commonly used as bronchodilators to treat obstructive lung diseases such as asthma and chronic obstructive pulmonary disease (COPD), however, they induce severe side effects. Therefore, developing new bronchodilators is essential. Herbal plants were extracted and the extracts' effect on ai...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: She YS,Ma LQ,Liu BB,Zhang WJ,Qiu JY,Chen YY,Li MY,Xue L,Luo X,Wang Q,Xu H,Zang DA,Zhao XX,Cao L,Shen J,Peng YB,Zhao P,Yu MF,Chen W,Nie X,Shen C,Chen S,Chen S,Qin G,Dai J,Chen J,Liu QH

    更新日期:2018-12-04 00:00:00

  • Natural Product Ginsenoside 20(S)-25-Methoxyl-Dammarane-3β, 12β, 20-Triol in Cancer Treatment: A Review of the Pharmacological Mechanisms and Pharmacokinetics.

    abstract::Panax ginseng has been used as an herbal medicine for thousands of years. Most of its pharmacological effects are attributed to its constituent ginsenosides, including 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol (20(S)-25-OCH3-PPD), which is one of the protopanaxadiol type ginsenosides. It has been found to exhibit ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Kim D,Park M,Haleem I,Lee Y,Koo J,Na YC,Song G,Lee J

    更新日期:2020-04-22 00:00:00

  • To Inhibit or Enhance? Is There a Benefit to Positive Allosteric Modulation of P2X Receptors?

    abstract::The family of ligand-gated ion channels known as P2X receptors were discovered several decades ago. Since the cloning of the seven P2X receptors (P2X1-P2X7), a huge research effort has elucidated their roles in regulating a range of physiological and pathophysiological processes. Transgenic animals have been influenti...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Stokes L,Bidula S,Bibič L,Allum E

    更新日期:2020-05-12 00:00:00

  • DT-13 Inhibits Proliferation and Metastasis of Human Prostate Cancer Cells Through Blocking PI3K/Akt Pathway.

    abstract::DT-13, a saponin monomer 13 from the dwarf lilyturf tuber, was reported to exhibit anti-inflammatory, hepatoprotective, cardioprotective as well as antitumor activities in a number of tumor cells. Prostate cancer is the second leading cause of cancer death in males, discovery of novel antitumor drug for therapy of pro...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Wang Z,Wang Y,Zhu S,Liu Y,Peng X,Zhang S,Zhang Z,Qiu Y,Jin M,Wang R,Zhong Y,Kong D

    更新日期:2018-12-07 00:00:00

  • Clonal evolution and therapeutic resistance in solid tumors.

    abstract::Tumors frequently arise as a result of an acquired genomic instability and the subsequent evolution of neoplastic populations with variable genomes. A barrier to the study of the somatic genetics of human solid tumors in vivo is the presence of admixtures of non-neoplastic cells with normal genomes in patient samples....

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Barrett MT,Lenkiewicz E,Evers L,Holley T,Ruiz C,Bubendorf L,Sekulic A,Ramanathan RK,Von Hoff DD

    更新日期:2013-01-28 00:00:00

  • ATC-NLSP: Prediction of the Classes of Anatomical Therapeutic Chemicals Using a Network-Based Label Space Partition Method.

    abstract::Anatomical Therapeutic Chemical (ATC) classification system proposed by the World Health Organization is a widely accepted drug classification scheme in both academic and industrial realm. It is a multilabeling system which categorizes drugs into multiple classes according to their therapeutic, pharmacological, and ch...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Wang X,Wang Y,Xu Z,Xiong Y,Wei DQ

    更新日期:2019-09-05 00:00:00

  • Spatiotemporal Mapping Techniques Show Clozapine Impairs Neurogenic and Myogenic Patterns of Activity in the Colon of the Rabbit in a Dose-Dependent Manner.

    abstract::Background: Clozapine, an antipsychotic used in treatment-resistant schizophrenia, has adverse gastrointestinal effects with significant associated morbidity and mortality. However, its effects on defined patterns of colonic contractile activity have not been assessed. Method: We used novel radial and longitudinal spa...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Every-Palmer S,Lentle RG,Reynolds G,Hulls C,Chambers P,Dunn H,Ellis PM

    更新日期:2017-04-24 00:00:00

  • The Pharmacological Potential of Non-ribosomal Peptides from Marine Sponge and Tunicates.

    abstract::Marine biodiversity is recognized by a wide and unique array of fascinating structures. The complex associations of marine microorganisms, especially with sponges, bryozoans, and tunicates, make it extremely difficult to define the biosynthetic source of marine natural products or to deduce their ecological significan...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章,评审


    authors: Agrawal S,Adholeya A,Deshmukh SK

    更新日期:2016-10-25 00:00:00

  • Trends and Development in Enteral Nutrition Application for Ventilator Associated Pneumonia: A Scientometric Research Study (1996-2018).

    abstract::Background: This study aimed to explore the intellectual landscape of the studies investigating the clinical application of enteral nutrition (EN) in patients with ventilator associated pneumonia (VAP), and to identify thematic development trends and research frontiers in this area. Methods: Scientometric research was...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Chen S,Bie R,Lai Y,Shi H,Ung COL,Hu H

    更新日期:2019-03-20 00:00:00

  • Duloxetine, a Balanced Serotonin-Norepinephrine Reuptake Inhibitor, Improves Painful Chemotherapy-Induced Peripheral Neuropathy by Inhibiting Activation of p38 MAPK and NF-κB.

    abstract::Chemotherapy-induced peripheral neuropathy (CIPN) is a severe, toxic side effect that frequently occurs in anticancer treatment and may result in discontinuation of treatment as well as a serious reduction in life quality. The CIPN incidence rate is as high as 85-90%. Unfortunately, there is currently no standard evid...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Meng J,Zhang Q,Yang C,Xiao L,Xue Z,Zhu J

    更新日期:2019-04-09 00:00:00

  • Paracrine Fibroblast Growth Factor 1 Functions as Potent Therapeutic Agent for Intrahepatic Cholestasis by Downregulating Synthesis of Bile Acid.

    abstract::Endocrine fibroblast growth factor (FGF) 19 has been shown to be capable of maintaining bile acid (BA) homeostasis and thus hold promise to be a potential therapeutic agent for cholestasis liver disease. However, whether paracrine FGFs possess this BA regulatory activity remains to be determined. In our study, we iden...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Lin H,Zhou C,Hou Y,Li Q,Qiao G,Wang Y,Huang Z,Niu J

    更新日期:2019-12-20 00:00:00

  • Layered Double Hydroxide Nanomaterials Encapsulating Angelica gigas Nakai Extract for Potential Anticancer Nanomedicine.

    abstract::We prepared hybrids consisting of Angelica gigas Nakai (AGN) root or flower extract and layered double hydroxide (LDH) for potential anticancer nanomedicine, as decursin species (DS) in AGN are known to have anticancer activity. Dimethylsulfoxide solvent was determined hybridization reaction media, as it has affinity ...

    journal_title:Frontiers in pharmacology

    pub_type: 杂志文章


    authors: Kim HJ,Lee GJ,Choi AJ,Kim TH,Kim TI,Oh JM

    更新日期:2018-07-09 00:00:00