5,7-二羟基黄酮对意大利青霉的结构-抗真菌活性关系
The structure-antifungal activity relationship of 5,7-dihydroxyflavonoids against Penicillium italicum.
作者信息
Yang Shuzhen, Zhou Jie, Li Dongmei, Shang Chunyu, Peng Litao, Pan Siyi
机构信息
Key Laboratory of Environment Correlative Dietology, Ministry of Education, College of Food Science and Technology, Huazhong Agricultural University, Wuhan 430070, PR China.
Georgetown University Medical Center, Washington, DC, USA.
出版信息
Food Chem. 2017 Jun 1;224:26-31. doi: 10.1016/j.foodchem.2016.12.001. Epub 2016 Dec 9.
To evaluate the structure-activity relationship of 5,7-dihydroxyflavonoids against P. italicum, we tested the antifungal activity of 23 selected 5,7-dihydroxyflavonoids against spore germination of P. italicum, and the effects of hydroxyl group, hydrogenation, methylation and glycosylation on the antifungal activity are explored. C-4'-OH and C-3-OH are active groups for the 5,7-dihydroxyflavonoids against P. italicum. We find that hydrogenation of the C2/C3 bond decreases the antifungal activity of 5,7-dihydroxyflavonoids. Antifungal activity of 5,7-dihydroxyflavonoids against P. italicum was affected by the conjugation site of glycosylation and the class of sugar moiety. The correlation between antifungal activity and the inhibition of respiration of 5,7-dihydroxyflavonoids was further evaluated. We find no significant relationship among the IC50 of 5,7-dihydroxyflavonoids on spore germination and on respiration. Some 5,7-dihydroxyflavonoids even enhance the respiration of P. italicum. This indicate respiration is not the only target for 5,7-dihydroxyflavonoids against P. italicum.
为了评估5,7 - 二羟基黄酮类化合物对意大利青霉的构效关系，我们测试了23种选定的5,7 - 二羟基黄酮类化合物对意大利青霉孢子萌发的抗真菌活性，并探讨了羟基、氢化、甲基化和糖基化对抗真菌活性的影响。C - 4'- OH和C - 3 - OH是5,7 - 二羟基黄酮类化合物对意大利青霉的活性基团。我们发现C2/C3键的氢化会降低5,7 - 二羟基黄酮类化合物的抗真菌活性。5,7 - 二羟基黄酮类化合物对意大利青霉的抗真菌活性受糖基化的共轭位点和糖部分的种类影响。进一步评估了5,7 - 二羟基黄酮类化合物的抗真菌活性与呼吸抑制之间的相关性。我们发现5,7 - 二羟基黄酮类化合物对孢子萌发和呼吸的IC50之间没有显著关系。一些5,7 - 二羟基黄酮类化合物甚至会增强意大利青霉的呼吸作用。这表明呼吸作用不是5,7 - 二羟基黄酮类化合物对抗意大利青霉的唯一靶点。
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