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.

中文翻译：

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从藤黄 (Clusiaceae) 的分支中获得的双黄酮类化合物对芳香酶 (CYP19) 的抑制作用

摘要 乳腺癌细胞中芳香化酶的过度表达可能会显着影响其进展和维持。从这个意义上说，芳香化酶的抑制是治疗绝经后妇女乳腺癌的关键目标。尽管几种黄酮类化合物已经证明具有抑制芳香酶活性的能力，但对双黄酮类化合物作为芳香酶抑制剂的作用的研究却很少。在这项工作中，从藤黄中分离出的双黄酮类化合物、羊肚菌黄酮 (1)、Gb-2a (2) 和 Gb-2a-7-O-葡萄糖 (3) 进行了体外测定，以评估芳香酶的调节作用。结果表明，所有双黄酮类化合物都能够抑制该酶，IC50 值范围为 1.35 至 7.67 μM。