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白杨素广谱抗肿瘤的临床前活性:当前趋势与未来展望。

Broad-Spectrum Preclinical Antitumor Activity of Chrysin: Current Trends and Future Perspectives.

机构信息

Department of Anatomical Sciences, School of Medicine, Shiraz University of Medical Sciences, Shiraz 7134814336, Iran.

Cancer Science Institute of Singapore and Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117599, Singapore.

出版信息

Biomolecules. 2020 Sep 27;10(10):1374. doi: 10.3390/biom10101374.

Abstract

Pharmacological profile of phytochemicals has attracted much attention to their use in disease therapy. Since cancer is a major problem for public health with high mortality and morbidity worldwide, experiments have focused on revealing the anti-tumor activity of natural products. Flavonoids comprise a large family of natural products with different categories. Chrysin is a hydroxylated flavonoid belonging to the flavone category. Chrysin has demonstrated great potential in treating different disorders, due to possessing biological and therapeutic activities, such as antioxidant, anti-inflammatory, hepatoprotective, neuroprotective, etc. Over recent years, the anti-tumor activity of chrysin has been investigated, and in the present review, we provide a mechanistic discussion of the inhibitory effect of chrysin on proliferation and invasion of different cancer cells. Molecular pathways, such as Notch1, microRNAs, signal transducer and activator of transcription 3 (STAT3), nuclear factor-kappaB (NF-κB), PI3K/Akt, MAPK, etc., as targets of chrysin are discussed. The efficiency of chrysin in promoting anti-tumor activity of chemotherapeutic agents and suppressing drug resistance is described. Moreover, poor bioavailability, as one of the drawbacks of chrysin, is improved using various nanocarriers, such as micelles, polymeric nanoparticles, etc. This updated review will provide a direction for further studies in evaluating the anti-tumor activity of chrysin.

摘要

植物化学物质的药理学特性引起了人们对其在疾病治疗中的应用的极大关注。由于癌症是全球范围内死亡率和发病率都很高的主要公共卫生问题,因此实验集中于揭示天然产物的抗肿瘤活性。类黄酮是一大类具有不同类别天然产物的家族。白杨素是一种属于黄酮类的羟基化类黄酮。由于具有生物和治疗活性,如抗氧化、抗炎、保肝、神经保护等,白杨素在治疗不同疾病方面具有巨大的潜力。近年来,人们研究了白杨素的抗肿瘤活性,在本综述中,我们提供了对白杨素抑制不同癌细胞增殖和侵袭的机制讨论。讨论了白杨素作为 Notch1、microRNAs、信号转导和转录激活因子 3(STAT3)、核因子-κB(NF-κB)、PI3K/Akt、MAPK 等分子途径的靶点。描述了白杨素在促进化疗药物的抗肿瘤活性和抑制耐药性方面的效率。此外,白杨素的生物利用度低是其缺点之一,通过使用各种纳米载体,如胶束、聚合物纳米粒等,可以提高其生物利用度。本综述将为进一步研究评估白杨素的抗肿瘤活性提供一个方向。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9fd/7600196/a7daebeb955f/biomolecules-10-01374-g001.jpg

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