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植物黄酮白杨素作为一种新兴的组蛋白去乙酰化酶抑制剂,用于繁荣的基于表观遗传学的抗癌治疗。

Plant flavone Chrysin as an emerging histone deacetylase inhibitor for prosperous epigenetic-based anticancer therapy.

机构信息

Division of Basic Sciences and Humanities, Faculty of Agriculture, SKUAST-Kashmir, Wadura, Sopore, Jammu & Kashmir, India.

Division of Plant Breeding & Genetics, Faculty of Agriculture, SKUAST-Kashmir, Jammu & Kashmir, India.

出版信息

Phytother Res. 2021 Feb;35(2):823-834. doi: 10.1002/ptr.6869. Epub 2020 Sep 15.

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.

摘要

表观遗传机制的异常为肿瘤的发生和发展提供了一个有利的平台。因此,能够调节肿瘤表观遗传环境的药物将是抗癌治疗的一个有价值的补充。由于黄酮类化合物具有内在的抗氧化活性和抑制表观遗传靶点(即组蛋白去乙酰化酶(HDACs))的能力,它们作为抗癌药物而崭露头角。HDACs 在各种癌症的发病机制中具有更广泛的意义。具有抑制 HDAC 能力的黄酮类化合物白杨素可能成为一种有潜力的抗癌药物。因此,在本文中,我们专注于白杨素及其对包括肺癌、结直肠癌、宫颈癌、胃癌、黑色素瘤、肝癌和乳腺癌在内的恶性肿瘤的独特抗肿瘤作用。讨论了白杨素在这些癌症模型中诱导细胞毒性作用的潜在信号级联。重要的是,考虑了白杨素与商业抗癌药物联合治疗的组合方法。还描述了联合治疗通过下游分子机制来消除恶性癌症化疗耐药性。此外,还阐明了涉及将白杨素与其他草药和非草药药物共同包封的纳米组合方法,以实现临床卓越性。

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