藤黄酮类化合物对芳香化酶(CYP19)的抑制作用

Angelica Maria Recalde-Gil, L. Klein-Júnior, Juliana Salton, Sérgio A L Bordignon, V. Cechinel-Filho, C. Matté, A. Henriques
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引用次数: 6

摘要

芳香化酶在乳腺癌细胞中的过度表达可能会显著影响其进展和维持。从这个意义上说,抑制芳香化酶是绝经后妇女乳腺癌治疗的关键靶点。虽然一些类黄酮已经证明了抑制芳香酶活性的能力,但生物类黄酮作为芳香酶抑制剂的作用研究很少。本研究以栀子黄酮(1)、黄酮(2)、葡萄糖-2a-7- o -葡萄糖(3)为研究对象,对从栀子黄酮中分离得到的生物黄酮进行了体外实验,以评价其对芳香化酶的调节作用。结果表明,所有类黄酮均能抑制该酶,IC50值在1.35 ~ 7.67 μM之间。这表明,生物类黄酮是开发新的芳香化酶抑制剂的重要支架来源,重点是开发新的抗癌药物。
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Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae)
Abstract Overexpression of aromatase in breast cancer cells may substantially influence its progression and maintenance. In this sense, the inhibition of aromatase is a key target for the treatment of breast cancer in postmenopausal women. Although several flavonoids had already demonstrated the capacity of inhibiting aromatase activity, the role of biflavonoids as aromatase inhibitors is poorly studied. In this work, the biflavonoids isolated from Garcinia gardneriana, morelloflavone (1), Gb-2a (2) and Gb-2a-7-O-glucose (3) were submitted to in vitro assay to evaluate the aromatase modulatory effect. As results, it was demonstrated that all biflavonoids were able to inhibit the enzyme, with IC50 values ranging from 1.35 to 7.67 μM. This demonstrates that biflavonoids are an important source of scaffolds for the development of new aromatase inhibitors, focusing on the development of new anticancer agents.
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