PDF(Pubmed)
Abstract：
Biflavonoids are dimeric forms of flavonoids that have recently gained importance as an effective new scaffold for drug discovery. In particular, 3\'-8″-biflavones exhibit antiviral and antimicrobial activity and are promising molecules for the treatment of neurodegenerative and metabolic diseases as well as cancer therapies. In the present study, we directly compared 3\'-8″-biflavones (amentoflavone, bilobetin, ginkgetin, isoginkgetin, and sciadopitysin) and their monomeric subunits (apigenin, genkwanin, and acacetin) and evaluated their radical scavenging activity (with DPPH), antifungal activity against mycotoxigenic fungi (Alternaria alternata, Aspergillus flavus, Aspergillus ochraceus, Fusarium graminearum, and Fusarium verticillioides), and inhibitory activity on enzymes (acetylcholinesterase, tyrosinase, α-amylase, and α-glucosidase). All the tested compounds showed weak radical scavenging activity, while antifungal activity strongly depended on the tested concentration and fungal species. Biflavonoids, especially ginkgetin and isoginkgetin, proved to be potent acetylcholinesterase inhibitors, whereas monomeric flavonoids showed higher tyrosinase inhibitory activity than the tested 3\'-8″-biflavones. Amentoflavone proved to be a potent α-amylase and α-glucosidase inhibitor, and in general, 3\'-8″-biflavones showed a stronger inhibitory potential on these enzymes than their monomeric subunits. Thus, we can conclude that 3\'-8″-dimerization enhanced acetylcholinesterase, α-amylase, and α-glucosidase activities, but the activity also depends on the number of hydroxyl and methoxy groups in the structure of the compound.
摘要：
双类黄酮是类黄酮的二聚体形式,其最近作为用于药物发现的有效新支架而变得重要。特别是,3'-8”-双黄酮具有抗病毒和抗微生物活性，是治疗神经退行性疾病和代谢疾病以及癌症治疗的有前途的分子。在本研究中,我们直接比较了3'-8”-双黄酮(胺黄酮，胆红素,银杏,等银杏素,和sciadopitysin）及其单体亚基（芹菜素，Genkwanin,和刺槐素）并评估了它们的自由基清除活性（使用DPPH），抗真菌活性对霉菌毒素真菌（链格孢菌，黄曲霉,曲霉,禾谷镰刀菌,和镰刀菌），和对酶的抑制活性(乙酰胆碱酯酶，酪氨酸酶,α-淀粉酶,和α-葡萄糖苷酶)。所有测试的化合物都显示出弱的自由基清除活性，而抗真菌活性强烈取决于测试的浓度和真菌种类。双类黄酮,尤其是银杏素和等银杏素，被证明是有效的乙酰胆碱酯酶抑制剂，而单体类黄酮显示出比测试的3\'-8″-双黄酮更高的酪氨酸酶抑制活性。被证明是一种有效的α-淀粉酶和α-葡萄糖苷酶抑制剂，总的来说,3'-8”-双黄酮对这些酶的抑制潜力比其单体亚基更强。因此，我们可以得出结论，3'-8″-二聚化增强了乙酰胆碱酯酶，α-淀粉酶,和α-葡萄糖苷酶活性，但是活性还取决于化合物结构中羟基和甲氧基的数量。
