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从 L. 的叶子中分离得到的草药提取物和酰化黄酮单糖苷的 GABase 和谷氨酰胺酶抑制活性。

GABase and glutaminase inhibitory activities of herbal extracts and acylated flavonol monoglycosides isolated from the leaves of L.

机构信息

Division of Food and Nutrition, Nakamura Gakuen University Junior College, Fukuoka, 814-0198, Japan.

Department of Medical Technology, Kawasaki University of Medical Welfare, Okayama, 701-0193, Japan.

出版信息

Z Naturforsch C J Biosci. 2023 Aug 4;78(9-10):377-381. doi: 10.1515/znc-2023-0047. Print 2023 Sep 26.

Abstract

This study was to compare GABase [a mixture of -aminobutyric acid (GABA) aminotransferase and succinic semialdehyde dehydrogenase] and glutaminase inhibitory activities of 20 herbal extracts and investigate the isolation, structural elucidation and those inhibitory activities of three acylated flavonol monoglycosides from the selected extract of L. (laurel). On the basis of the NMR spectroscopic data and the ESI MS spectra together with the comparison with the literature values, three compounds were identified as kaempferol-3--(4″---coumaroyl)--l-rhamnopyranoside (), kaempferol-3--(3″,4″-di---coumaroyl)--l-rhamnopyranoside () and kaempferol-3--(2″,4″-di---coumaroyl)--l-rhamnopyranoside (), respectively. The IC values of GABase inhibitory activity of and -hydroxybenzaldehyde (HBA) as control were 0.24 mM, 0.14 mM, 0.12 mM and 0.43 mM, respectively. Additionally, the IC values of glutaminase inhibitory activity of and 6-diazo-5-oxo-l-norleucine (DON) as control were 0.34 mM, 0.13 mM, 0.14 mM and 0.33 mM, respectively. The results suggest that the extract from laurel shows the strongest biological activities among 20 herbal extracts and three acylated flavonol monoglycosides may serve as potential lead compounds for the prevention and treatment of neurodegenerative and lifestyle-related diseases by targeting GABase and glutaminase. This is the first report on GABase and glutaminase inhibitory activities of .

摘要

本研究旨在比较 GABase(-氨基丁酸(GABA)转氨酶和琥珀酸半醛脱氢酶的混合物)和 20 种草药提取物的谷氨酰胺酶抑制活性,并研究从选定的月桂属(月桂)提取物中分离、结构鉴定和三种酰化类黄酮单糖苷的这些抑制活性。根据 NMR 波谱数据和 ESI-MS 谱以及与文献值的比较,鉴定出三种化合物分别为山柰酚-3--(4″--咖啡酰基)--l-鼠李吡喃糖苷()、山柰酚-3--(3″,4″-二--咖啡酰基)-l-鼠李吡喃糖苷()和山柰酚-3--(2″,4″-二--咖啡酰基)-l-鼠李吡喃糖苷()。作为对照的 GABase 抑制活性的 IC 值和 -羟基苯甲醛(HBA)分别为 0.24mM、0.14mM、0.12mM 和 0.43mM。此外,作为对照的谷氨酰胺酶抑制活性的 IC 值和 6-重氮-5-氧代-l-正亮氨酸(DON)分别为 0.34mM、0.13mM、0.14mM 和 0.33mM。结果表明,月桂属提取物在 20 种草药提取物中表现出最强的生物活性,三种酰化类黄酮单糖苷可能作为潜在的先导化合物,通过靶向 GABase 和谷氨酰胺酶,用于预防和治疗神经退行性疾病和与生活方式相关的疾病。这是首次报道关于月桂属的 GABase 和谷氨酰胺酶抑制活性。

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