<i>In Silico</i>
            Approaches for Investigating the Binding Propensity of Apigenin and Luteolin Against Class I HDAC Isoforms

Ganai, Shabir Ahmad; Farooq, Zeenat; Banday, Shahid; Altaf, Mohammad

doi:10.4155/fmc-2018-0020

Cited by 35 publications

(24 citation statements)

References 84 publications

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“…Moreover, the binding inclination of luteolin has also been evaluated against Class I HDACs through a futuristic in silico approach (Ganai, Farooq, Banday, & Altaf, 2018).…”

Section: Conventional Medicinal Uses Of Luteolin and Its Emerging Targetsmentioning

confidence: 99%

“…Maximum inhibitory effect of luteolin has been seen on HDAC2 followed by HDAC3, HDAC9, HDAC8, HDAC10, HDAC5, and HDAC10 (Godoy, Lucas, Bender, Romanick, & Ferguson, 2017). Moreover, the binding inclination of luteolin has also been evaluated against Class I HDACs through a futuristic in silico approach (Ganai, Farooq, Banday, & Altaf, 2018).…”

Section: Introductionmentioning

confidence: 99%

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Anticancer activity of the plant flavonoid luteolin against preclinical models of various cancers and insights on different signalling mechanisms modulated

Ganai

Sheikh

Baba

et al. 2021

Phytotherapy Research

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Various signaling mechanisms contribute significantly to the development of multiple cancers. Small molecules with the potential of influencing a wide variety of molecular targets may prove as broad-spectrum anticancer agents. Flavonoids from plant sources are strongly emerging as promising antineoplastic molecules because of their ability to hamper different cancer-driving signaling pathways. Further, these flavonoids offer an additional benefit due to their congenital antioxidant potential. This paper discusses the anticancer activity of luteolin against a number of cancers including leukemias, prostate cancer, pancreatic cancer, breast cancer, lung cancer, colorectal cancer, melanoma, liver, gastric, and brain cancer. Strong emphasis has been laid on key molecular mechanisms impacted by luteolin for exerting antineoplastic effect. Importantly, certain epigenetic targets like histone deacetylases (HDACs), DNA methylation regulator enzymes that are influenced by this befitting flavone for inducing cytotoxicity in certain preclinical cancer models, have also been made the part of this review. Additionally, the significantly improved therapeutic benefits of luteolin in combination with other therapeutics are comprehensively discussed. The current loopholes in luteolin research are also considered, which may open novel routes for further valuable studies on this promising flavone.

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“…Moreover, the binding inclination of luteolin has also been evaluated against Class I HDACs through a futuristic in silico approach (Ganai, Farooq, Banday, & Altaf, 2018).…”

Section: Conventional Medicinal Uses Of Luteolin and Its Emerging Targetsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Anticancer activity of the plant flavonoid luteolin against preclinical models of various cancers and insights on different signalling mechanisms modulated

Ganai

Sheikh

Baba

et al. 2021

Phytotherapy Research

Self Cite

View full text Add to dashboard Cite

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“…Ganai et al found that luteolin can stably bind to class-I HDAC isomers. Luteolin, as a natural product, may have better anticancer application prospects than synthetic HDACi's which are associated with more side effects (150).…”

Section: Luteolinmentioning

confidence: 99%

Remodeling the Epigenetic Landscape of Cancer—Application Potential of Flavonoids in the Prevention and Treatment of Cancer

et al. 2021

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Epigenetics, including DNA methylation, histone modification, and noncoding RNA regulation, are physiological regulatory changes that affect gene expression without modifying the DNA sequence. Although epigenetic disorders are considered a sign of cell carcinogenesis and malignant events that affect tumor progression and drug resistance, in view of the reversible nature of epigenetic modifications, clinicians believe that associated mechanisms can be a key target for cancer prevention and treatment. In contrast, epidemiological and preclinical studies indicated that the epigenome is constantly reprogrammed by intake of natural organic compounds and the environment, suggesting the possibility of utilizing natural compounds to influence epigenetics in cancer therapy. Flavonoids, although not synthesized in the human body, can be consumed daily and are common in medicinal plants, vegetables, fruits, and tea. Recently, numerous reports provided evidence for the regulation of cancer epigenetics by flavonoids. Considering their origin in natural and food sources, few side effects, and remarkable biological activity, the epigenetic antitumor effects of flavonoids warrant further investigation. In this article, we summarized and analyzed the multi-dimensional epigenetic effects of all 6 subtypes of flavonoids (including flavonols, flavones, isoflavones, flavanones, flavanols, and anthocyanidin) in different cancer types. Additionally, our report also provides new insights and a promising direction for future research and development of flavonoids in tumor prevention and treatment via epigenetic modification, in order to realize their potential as cancer therapeutic agents.

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“…Notably, luteolin was reported to inhibit class I HDAC activity as well as increase lysine acetylation on histone H3 in cardiac myoblasts [ 119 ]. Furthermore, docking studies demonstrated that luteolin binds within the catalytic domain of class I HDACs to inhibit HDAC activity [ 178 ]. Lastly, luteolin was reported to attenuate cardiac dysfunction by regulating Akt and MAPK signaling [ 174 , 179 ].…”

Section: Phytochemicalsmentioning

confidence: 99%

“…With regard to the heart, baicalein [ 183 , 184 , 185 ] and baicalin [ 83 , 84 , 85 , 186 , 187 , 188 , 189 ] have shown efficacy in ischemia-induced and isoproterenol-induced cardiac dysfunction. Similar to other flavonoids, baicalein and baicalin elicit cardio-protection by inhibiting oxidative stress and inflammation as well as attenuating MAPK signaling [ 178 , 179 , 180 , 183 , 185 , 186 , 187 , 188 ]. Baicalein was also reported to inhibit cardiac hypertrophy and fibrosis in mice exposed to aortic constriction [ 190 ].…”

Section: Phytochemicalsmentioning

confidence: 99%

Food Bioactive HDAC Inhibitors in the Epigenetic Regulation of Heart Failure

Evans

Ferguson

2018

Nutrients

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Approximately 5.7 million U.S. adults have been diagnosed with heart failure (HF). More concerning is that one in nine U.S. deaths included HF as a contributing cause. Current HF drugs (e.g., β-blockers, ACEi) target intracellular signaling cascades downstream of cell surface receptors to prevent cardiac pump dysfunction. However, these drugs fail to target other redundant intracellular signaling pathways and, therefore, limit drug efficacy. As such, it has been postulated that compounds designed to target shared downstream mediators of these signaling pathways would be more efficacious for the treatment of HF. Histone deacetylation has been linked as a key pathogenetic element for the development of HF. Lysine residues undergo diverse and reversible post-translational modifications that include acetylation and have historically been studied as epigenetic modifiers of histone tails within chromatin that provide an important mechanism for regulating gene expression. Of recent, bioactive compounds within our diet have been linked to the regulation of gene expression, in part, through regulation of the epi-genome. It has been reported that food bioactives regulate histone acetylation via direct regulation of writer (histone acetyl transferases, HATs) and eraser (histone deacetylases, HDACs) proteins. Therefore, bioactive food compounds offer unique therapeutic strategies as epigenetic modifiers of heart failure. This review will highlight food bio-actives as modifiers of histone deacetylase activity in the heart.

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In Silico Approaches for Investigating the Binding Propensity of Apigenin and Luteolin Against Class I HDAC Isoforms

Abstract: Apigenin and luteolin may serve as substitutes to synthetic inhibitors for effective HDAC based anticancer therapy.

Cited by 35 publications

References 84 publications

Anticancer activity of the plant flavonoid luteolin against preclinical models of various cancers and insights on different signalling mechanisms modulated

Anticancer activity of the plant flavonoid luteolin against preclinical models of various cancers and insights on different signalling mechanisms modulated

Remodeling the Epigenetic Landscape of Cancer—Application Potential of Flavonoids in the Prevention and Treatment of Cancer

Food Bioactive HDAC Inhibitors in the Epigenetic Regulation of Heart Failure

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