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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Plant flavone Chrysin as an emerging histone deacetylase inhibitor for prosperous epigenetic-based anticancer therapy
Shabir Ahmad Ganai1, Farooq Ahmad Sheikh2, Zahoor Ahmad Baba1
1Division of Basic Sciences and Humanities, Faculty of Agriculture, SKUAST-Kashmir, Wadura, Sopore, Jammu & Kashmir, India.
Abstract:
Aberrations in epigenetic mechanisms provide a fertile platform for tumour initiation and progression. Thus, agents capable of modulating the epigenetic environment of neoplasms will be a valuable addition to the anticancer therapeutics. Flavones are emerging as befitting anticancer agents due to their inherent antioxidant activity and the ability to restrain epi-targets namely histone deacetylases (HDACs). HDACs have broader implications in pathogenesis of various cancers. Chrysin, a flavone possessing the ability to inhibit HDACs could prove as a potential anticancer drug. Thus, in this article we focussed on Chrysin and its distinct antineoplastic effect against bellicose malignancies including lung, colorectal, cervical, gastric, melanoma, hepatocellular carcinoma and breast cancer. The underlying signalling cascades triggered by Chrysin for inducing cytotoxic effect in these cancer models are discussed. Importantly, approaches towards combinatorial treatments by Chrysin and commercial anticancer agents are taken into account. The downstream molecular mechanism aroused by combined therapy for abrogating onerous cancer chemoresistance is delineated as well. Moreover, the nano-combinatorial approach involving co-encapsulation of Chrysin with other herbal and non-herbal agents for clinical excellence is elucidated.
Insights
Chrysin, a natural flavone, shows anticancer potential by inhibiting histone deacetylases (HDACs). This study explores its effects on various cancers and combinatorial strategies for enhanced cancer treatment.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Epigenetic alterations drive cancer development and progression.
- Histone deacetylases (HDACs) are key epigenetic targets in cancer therapy.
- Flavones, like chrysin, exhibit anticancer properties by targeting HDACs.
Purpose of the Study:
- To investigate the antineoplastic effects of chrysin against multiple cancer types.
- To elucidate the signaling pathways involved in chrysin-induced cytotoxicity.
- To explore combinatorial therapies involving chrysin for overcoming cancer chemoresistance.
Main Methods:
- Review of chrysin's mechanism of action as an HDAC inhibitor.
- Analysis of chrysin's efficacy in various cancer models (lung, colorectal, cervical, gastric, melanoma, HCC, breast).
- Discussion of signaling cascades and molecular mechanisms of combined therapies.
Main Results:
- Chrysin demonstrates distinct antineoplastic effects across a spectrum of malignancies.
- Chrysin triggers specific cytotoxic signaling pathways in cancer cells.
- Combinatorial approaches with chrysin show potential in abrogating chemoresistance.
Conclusions:
- Chrysin is a promising anticancer agent targeting HDACs.
- Combined therapies and nano-formulations of chrysin offer enhanced clinical potential.
- Further research into chrysin-based treatments is warranted for diverse cancers.
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