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黄酮类化合物作为乳腺癌预防/治疗中潜在的芳香化酶抑制剂

Flavonoids as Prospective Aromatase Inhibitors in Breast Cancer Prevention/ Therapy.

作者信息

Seth Richa, Kushwaha Soni, Luqman Suaib, Meena Abha

机构信息

Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow- 226015, Uttar Pradesh,India.

Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow- 226015, Uttar Pradesh,India | Academy of Scientific and Innovative Research (AcSIR), Ghaziabad-201002, Uttar Pradesh, India.

出版信息

Curr Mol Pharmacol. 2021;14(6):1112-1124. doi: 10.2174/1874467214666210210123709.

DOI:10.2174/1874467214666210210123709
PMID:33568041
Abstract

Flavonoids have been shown to target aromatase, suppressing the transformed cells' proliferation and growth. Such experimental data further promoted the usage of flavonoids as an aromatase inhibitor and helps prevent cancer, specifically breast and lung cancer. Conversely, flavonoids have certain limitations like low absorption, potency, and some side effects in addition to their tremendous advantages. The pharmacokinetics and toxicity of flavonoids are now being addressed by using advanced nanotechnological approaches. This review discusses the comprehensive aromatase signaling pathway in normal and cancer cells. It also draws attention to how do flavonoids modulate aromatase signaling pathways. Also, different flavonoid groups inhibiting aromatase activities are discussed and listed in the Table comprising flavonoids group, cancer type, clinical trials, IC50, and the assay employed. Moreover, nanoparticles-mediated improvement in the pharmacokinetics and toxicity issues of flavonoids in targeting aromatase are also deliberated. In conclusion, flavonoids act as a potential anticancer agent via targeting aromatase. Besides, nanotechnological approaches are useful in addressing the pharmacokinetics and toxicity of flavonoids.

摘要

黄酮类化合物已被证明可作用于芳香化酶,抑制转化细胞的增殖和生长。此类实验数据进一步推动了黄酮类化合物作为芳香化酶抑制剂的应用,并有助于预防癌症,尤其是乳腺癌和肺癌。相反,黄酮类化合物除了具有巨大优势外,还存在一些局限性,如吸收性低、效力有限以及一些副作用。目前正在通过先进的纳米技术方法来解决黄酮类化合物的药代动力学和毒性问题。本综述讨论了正常细胞和癌细胞中全面的芳香化酶信号通路。它还关注黄酮类化合物如何调节芳香化酶信号通路。此外,还讨论了不同抑制芳香化酶活性的黄酮类化合物组,并在表格中列出,包括黄酮类化合物组、癌症类型、临床试验、IC50以及所采用的测定方法。此外,还探讨了纳米颗粒介导的黄酮类化合物在靶向芳香化酶时药代动力学和毒性问题的改善。总之,黄酮类化合物通过靶向芳香化酶发挥潜在的抗癌作用。此外,纳米技术方法有助于解决黄酮类化合物的药代动力学和毒性问题。

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Flavonoids as Prospective Aromatase Inhibitors in Breast Cancer Prevention/ Therapy.黄酮类化合物作为乳腺癌预防/治疗中潜在的芳香化酶抑制剂
Curr Mol Pharmacol. 2021;14(6):1112-1124. doi: 10.2174/1874467214666210210123709.
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Evaluating flavonoids as potential aromatase inhibitors for breast cancer treatment: In vitro studies and in silico predictions.评估黄酮类化合物作为治疗乳腺癌的潜在芳香酶抑制剂:体外研究和计算机预测。
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[Progress in study of the structure, catalytic mechanism and inhibitors of aromatase].[芳香化酶的结构、催化机制及抑制剂的研究进展]
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